WO2016055701A1 - Dermatological composition for the prevention and treatment of haemorrhoids - Google Patents

Dermatological composition for the prevention and treatment of haemorrhoids Download PDF

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Publication number
WO2016055701A1
WO2016055701A1 PCT/FR2015/000191 FR2015000191W WO2016055701A1 WO 2016055701 A1 WO2016055701 A1 WO 2016055701A1 FR 2015000191 W FR2015000191 W FR 2015000191W WO 2016055701 A1 WO2016055701 A1 WO 2016055701A1
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Prior art keywords
weight
composition according
agents
potassium salt
composition
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PCT/FR2015/000191
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French (fr)
Inventor
Laurent Apert
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Laboratoires Urgo
Vivatech
Hcp Healthcare Asia Pte. Ltd
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Publication of WO2016055701A1 publication Critical patent/WO2016055701A1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7016Disaccharides, e.g. lactose, lactulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/702Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Definitions

  • the present invention relates to a novel topical dermatological composition, especially useful for preventing and / or treating hemorrhoids comprising, in a physiologically acceptable carrier, at least one effective amount of synthetic polysulfated oligosaccharide potassium salt having 1 to 4 'daring.
  • Sucrose octasulfate salts have long been known for use in all kinds of cosmetic, dermatological or medical applications. Thus, among all these uses, it is described through documents of Pierre Fabre Dermo-Cosmetic companies, or Urgo Laboratories, various salts of sucrose octasulfate for their benefits through healing actions, post-burn tissue remodeling actions or induced by aging, actions on stretch marks or pathological scars.
  • EP 0 391 905 discloses a topical composition based on aluminum salt sucrose octasulfate useful for the prevention and treatment of hemorrhoids in addition to its healing action.
  • Hemorrhoids are often wrongly considered as a variety of varicose veins whose only location seems different. Indeed, many physiopathological hypotheses have been rejected, especially that of the anal "varix" in favor of mechanical and circulatory designs.
  • the disease would be caused by the progressive alteration of the musculo-ligamentous structures (Parks ligament) maintaining in good position the pads of Thomson (cellulo-fibroelastic reinforcements of the submucous connective tissue ensuring complete obturation of light from the anal canal and containing hemorrhoids). This explains the possibility of hemorrhoidal procidence.
  • arterio-venous shunts the cavernous structure that is the Thomson pads, we also speak of arteriovenous anastomosis at this level
  • arteriovenous shunts would be the cause of an excessive arterial blood flow exceeding the drainage capacities of the hemorrhoidal tissue, thus causing congestion and haemorrhage of glowing blood.
  • These vascular abnormalities could lead to venous dystrophy with formation of thrombosis and alteration of the supporting tissue, thus contributing to the gradual exteriorization of hemorrhoids.
  • the synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of risk suggests better results than the aluminum salt of sucrose octasulfate on the prevention and treatment of hemorrhoids.
  • the object of the invention resides in a topical dermatological composition for its use in the prevention and treatment of hemorrhoids, comprising, in a physiologically acceptable support, at least one effective amount of synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of dare.
  • the potassium salt of sucrose octasulfate demonstrates advantageous effects according to any one of the two hypotheses generating hemorrhoids chosen.
  • the potassium salt of sucrose octasulfate has a positive strengthening effect of the longitudinal muscularis of the rectum forming the ligament of Parks.
  • the potassium salt of sucrose octasulfate also has positive effects on the prevention of the opening of arteriovenous shunts (preferentially at the level of Thomson pads), thus making it possible to better channel the excessive blood pressure exerted. at the hemorrhoidal veins.
  • hemorhoid any permanent externalization of veins of any size whatsoever, including hemorrhoids, located at the external rectum or at the lumen of the anal canal or the rectal bulb.
  • prevent and / or treat means any action on the symptoms of hemorrhoids, that is to say, any therapeutic action on the longitudinal muscularis of the rectum forming the ligament of Parks and / or the opening of shunts arteriovenous.
  • skin composition is intended to mean a composition for topical application comprising a dermatologically acceptable medium, that is to say one which has a pleasant color, odor and feel and which does not generate dermal substances. unacceptable discomfort (tingling, tightness, redness), likely to divert consumers from the use of this composition.
  • effective amount is meant in the sense of the present invention an amount sufficient to achieve the expected effect.
  • physiologically acceptable carrier means a non-toxic support and may be applied to at least one keratin material of human beings.
  • composition according to the invention comprises at least one synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of oste, and preferably 1 or 2 units of osteos, generally linked together by glycosidic linkage alpha or beta. In other words, it is mono, di, tri or tetrasaccharides, and preferably mono or dissacharides.
  • ose units of these polysaccharides there is no particular limitation on the nature of the ose units of these polysaccharides. Preferably, it will be pentoses or hexoses.
  • a monosaccharide mention may be made of glucose, galactose or mannose.
  • a disaccharide mention may be made of maltose, lactose, sucrose or trehalose.
  • a trisaccharide mention may be made of melezitose.
  • tetrasaccharide mention may be made of stachyose.
  • the oligosaccharide is a disaccharide, and more preferably sucrose.
  • polysulfated oligosaccharide is understood to mean an oligosaccharide of which at least two, and preferably all, hydroxyl groups of each monosaccharide have been substituted with a sulphate group.
  • the potassium salt of sucrose octasulfate which is a synthetic polymer formed from 2 units of osteosaccharide, generally bonded to one another by an alpha or beta glycosidic bond, is preferably used.
  • the latter in the context of the present invention, may be in the form of a micronized powder or in solubilized form.
  • the synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of risk can be introduced into the compositions according to the invention, preferably alone but also in admixture with other synthetic polysulfated oligosaccharide salts having 1 to 4 units of risk, such as sucralfate and / or with another active substance, preferably an active substance healing and / or restructuring of the skin, such as for example hyaluronic acid.
  • these synthetic polysulfated oligosaccharide salts formed from 1 to 4 units of oste, and their derivatives have a potentiating action of that of the polysulphated oligosaccharide potassium salt, preferably that of the salt.
  • sucrose octasulfate that is to say which have a positive base action on hemorrhoids but which have especially a synergistic effect of the action of polysulfated oligosaccharide potassium salt on said hemorrhoids.
  • alkali metal salts such as sodium, calcium, magnesium, silver salts, aluminum salts, zinc salts; or the amino acid salts.
  • alkali metal salts such as sodium, calcium, magnesium, silver salts, aluminum salts, zinc salts
  • amino acid salts Even more privileged, are used: - salt of calcium, zinc and magnesium;
  • sucralfate the aluminum salt of sucrose octasulfate, more generally called sucralfate.
  • the composition comprises at least one synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of osteoside in a content of between 0.1 and 50% by weight, relative to total weight of the composition.
  • the composition comprises at least one amount of synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of oste so that the quantity released on the hemorrhoid is between 0.001 g / 1 and 50 g / l, and more preferably between 0.01 and 10 g / l.
  • composition according to the invention may comprise one (or more) other active substance (s).
  • the active ingredients are chosen from anti-bacterials, antiseptics, antifungals, anti-inflammatories, active agents promoting healing and / or restructuring of the skin, antipruritic agents, UV filters, soothing agents, moisturizing active agents, depigmenting agents, keratolytic agents, anti-virals, pain relievers, anesthetics, vitamins, polysulfated sunless oligosaccharides formed from 1 to 4 units of oste or their salt, as described above, except potassium salt sucrose octasulfate, and mixtures thereof.
  • the assets are chosen from:
  • anti-bacterials such as polymyxin B, penicillins (amoxycillin), clavulanic acid, tetracyclines, minocycline, chlorotetracycline, aminoglycosides, amikacin, gentamicin, neomycin, silver and its salts (Sulfadiazine argentic), probiotics;
  • antiseptics such as sodium mercurothiolate, eosin, chlorhexidine, phenylmercury borate, hydrogen peroxide, Dakin liquor, triclosan, biguanide, hexamidine, thymol, Lugol, Povidone iodine, Merbromin, Benzalkonium and Benzethonium Chloride, ethanol, isopropanol, silver salts; anti fungal agents such as polyenes, Nystatin, Amphotericin B,
  • anti-inflammatories such as glucocorticoids, nonsteroidal anti-inflammatory drugs, aspirin, ibuprofen, ketoprofen, flurbiprofen, diclofenac, aceclofenac, ketorolac, eloxicam, piroxicam, tenoxicam, Naproxen, Indomethacin, Naproxcinod, Nimesulide, Celecoxib, Etoricoxib, Parecoxib, Rofecoxib, Valdecoxib, Phenylbutazone, Niflumic acid, Mefenamic acid;
  • nonsteroidal anti-inflammatory drugs such aspirin, ibuprofen, ketoprofen, flurbiprofen, diclofenac, aceclofenac, ketorolac, eloxicam, piroxicam, tenoxicam, Naproxen, Indomethacin, Naproxcinod, Nimesulide, Celecoxib, Etoricoxib, Parecoxi
  • the active agents promoting healing and / or restructuring of the skin such as retinol, water-soluble vitamins such as vitamin A or its derivatives, vitamin E or its derivatives, N-acetyl-hydroxyproline, extracts of CentellaAsiatica and dill, papain, silicones, essential oils of thyme, niaouli, rosemary and sage, hyaluronic acid, Pallantoin, Hema'tite (Gattefossé), Vitamin C, TEGO Pep 4-17 (Evonik), Toniskin (Silab), Collageneer (Expanscience), Timecode (Seppic), Gatuline skin repair (Gattefossé), Panthenol, PhytoCellTec Alp Rose (MibelleBiochemistry), Serilesine: Lipotec, Heterosides of Talapetraka (Beyer), Stoechiol (Codif), macarose (Sensient ), Dermaveil (IchimaruPharcos),
  • depigmenting agents such as kojic acid (KojicAcid SL ® - Quimasso (Sino Lion)), Arbutin (Olevatin ® - Quimasso (Sino Lion)), the mixture of palmitoylpropyl of sodium and of white water lily extract ( Sepicalm ® - Seppic), undecylenoyl phenylalanine (Sepiwhite ® - Seppic), licorice extract obtained by fermentation of Aspergillus and ethoxydiglycol (GatulineWhitening ® - Gattefossé), octadecenedioic acid (ODA White ® - Sederma), l alpha-arbutin (alpha-arbutin ®, SACI-CFPA (Pentapharm)), aqueous sheets Uva Ursi extract Arctophylos (Melfade-J ® - SACI-CFPA (Pentapharm)), the complex mixture of plant
  • Antipruriginous agents such as hydrocotisone, enoxolone, diphenyhydramine, antihistamines with local anti H1 application;
  • UV filters such as Parsol MCX, Parsol 1789;
  • Soothing agents such as chamomile, bisabolol, xanthalene, glycyrrhenic acid, tanactin (CPN), Calmiskin (Silab); - Moisturizing active ingredients such as xpermoist (Lipotec), hyaluronic acid, urea, fatty acids, glycerine, waxes, Exossine (Unipex);
  • keratolytic agents such as salicylic acid, zinc salicylate, ascorbic acid, alpha hydroxylated acids (glycolic acid, lactic acid, malic acid, citric acid, tartaric acid), extracts of silver maple, Griottier, tamarind urea, topical retinoid Keratoline ® (Sederma), proteases obtained by fermentation of Bacillus Subtilis, the Linked-Papain ® product (SACI-CFPA), papain (proteolytic enzyme derived from papaya fruit);
  • Vitamins such as retinol (vitamin A) and its derivatives, tocopherol (vitamin E) and its derivatives.
  • Veinotonics such as anthrocyanosides, citroflavonoids and flavonoids in general, diosmin, rutosides, troxerutin, or extracts of ruscus.
  • Analgesics such as morphine, buprenorphine, nalbuphine, sufentanil, remifentanil, fentanyl, alfentanil, codeine, hydromorphone, dextropropoxyphene, tramadol, nefopam, paracetamol or acetaminophen, ibuprofen, or nonsteroidal anti-inflammatory drugs (NSAIDs), including aspirin.
  • NSAIDs nonsteroidal anti-inflammatory drugs
  • the composition according to the invention comprises at least one effective amount of another active substance that promotes healing and / or restructuring of the skin, preferably hyaluronic acid.
  • the composition according to the invention comprises at least one effective amount of another active substance chosen from analgesics and / or venotonic agents.
  • active agents according to the invention may be combined with active agents intended in particular for the prevention and / or treatment of cutaneous affections.
  • compositions according to the invention may be in any galenical form normally used by those skilled in the art.
  • compositions When the compositions are intended for topical administration, they may be in the form of solutions (aqueous, hydroalcoholic or oily), dispersions (lotion or serum type), emulsions of liquid or semi-liquid consistency (milk type). , from suspensions or emulsions (cream type), aqueous or lipophilic gel, microemulsions, microcapsules, microparticles, or vesicular dispersions of ionic and / or nonionic type. They may also be in the form of nonabsorbent interface dressings or compression band impregnated with said composition or comprising the potassium salt of sucrose octasulfate and / or any other associated active within the same fibers constituting said textile product.
  • compositions are prepared according to the usual methods.
  • compositions according to the invention may also consist of solid preparations such as soaps or breads. cleaning.
  • the amount of potassium salt sucrose octasulfate used in the galenic formulation according to the invention is adapted according to the desired kinetics as well as specific constraints related to its nature, solubility, heat resistance, etc. Water and water soluble solvents
  • the composition of the invention may also comprise water, and in particular a thermal and / or mineral water.
  • composition according to the invention may also comprise one or more water-miscible solvents, such as lower alcohols, in particular ethanol and isopropanol, propylene glycol.
  • water-miscible solvents such as lower alcohols, in particular ethanol and isopropanol, propylene glycol.
  • composition according to the invention may also comprise a fatty phase.
  • the proportion of the fatty phase can range from 5 to 80% by weight, and preferably from 5 to 50% by weight, relative to the total weight of the composition.
  • the fatty phase may represent more than 90% of the total weight of the composition.
  • oils used in the composition according to the invention are chosen from those conventionally used in the cosmetic and / or dermatological field.
  • fats usable in the invention include, in addition to unsaturated fatty acids, mineral oils such as hydrogenated polyisobutene and petrolatum oil, vegetable oils such as a liquid fraction of shea butter, sunflower oil, almond and apricot oil, animal oils such as perhydrosqualene, synthetic oils including purcellin oil, isopropyl myristate and ethylhexyl palmitate, and fluorinated oils such as for example perfluoropolyethers.
  • mineral oils such as hydrogenated polyisobutene and petrolatum oil
  • vegetable oils such as a liquid fraction of shea butter, sunflower oil, almond and apricot oil
  • animal oils such as perhydrosqualene
  • synthetic oils including purcellin oil, isopropyl myristate and ethylhexyl palmitate
  • fluorinated oils such as for example perfluoro
  • fatty alcohols such as, for example, stearic acid and waxes, especially paraffin, carnauba and beeswax.
  • silicone compounds such as silicone oils and, for example, cyclomethicones and dimethicones, waxes, resins and silicone gums.
  • composition according to the invention when it is in the form of an emulsion, may also comprise one or more emulsifiers and / or co-emulsifiers.
  • the emulsifiers and co-emulsifiers used in the composition are chosen from those conventionally used in the cosmetic and / or dermatological field.
  • the total content of emulsifiers and co-emulsifiers may especially range from 0.3 to 30% by weight, and preferably from 0.5 to 20% by weight, relative to the total weight of the composition.
  • composition according to the invention may also comprise gelling agents.
  • hydrophilic gelling agents As hydrophilic gelling agents, mention may be made of carboxylic polymers such as carbomers, acrylic copolymers such as copolymers of acrylates / alkyl acrylates, polyacrylamides and especially the mixture of polyacrylamide, C13-14-Isoparaffin and Laureth-7 sold under the name Sepigel 305® by the company SEPPIC, polysaccharides such as cellulose derivatives such as hydroxyalkylcelluloses and in particular hydroxypropylcellulose and hydroxyethylcellulose, natural gums such as guar, carob, xanthan gum and clays.
  • carboxylic polymers such as carbomers, acrylic copolymers such as copolymers of acrylates / alkyl acrylates, polyacrylamides and especially the mixture of polyacrylamide, C13-14-Isoparaffin and Laureth-7 sold under the name Sepigel 305® by the company SEPPIC
  • polysaccharides such as cellulose derivatives such as hydroxy
  • lipophilic gelling agents mention may be made of modified clays such as bentones, metal salts of fatty acids such as aluminum stearates and hydrophobic silica, or else ethylcellulose and polyethylene.
  • the cosmetic and / or dermatological composition of the invention may also contain adjuvants which are customary in the cosmetic, pharmaceutical and / or dermatological field, such as preservatives, antioxidants, solvents, perfumes, fillers, odor absorbers and dyestuffs. These adjuvants, depending on their nature, can be introduced into the fatty phase and / or into the aqueous phase of the composition.
  • compositions are those conventionally used in the field under consideration, and for example from 0.01 to 20% of the total weight of the composition.
  • the composition is in the form of a film, preferably a water-soluble polymeric film film type filmogel®.
  • film is meant according to the present invention, a solid and thin film.
  • end is meant a solid having a thickness of at most 1000 ⁇
  • This film is prehensible, that is to say, it is generally of adequate size to be easily manipulated by the user. It can have a shape of square, rectangle, disk or any other form.
  • a film generally has a thickness of 10 ⁇ to 1000 ⁇ , preferably from 20 to 500 ⁇ and better still from 50 to 300 ⁇ .
  • water-soluble film in the sense of the present invention, a film that dissolves in water. It is a film consisting of one or more water-soluble or water-dispersible polymers, that is to say polymers having a solubility in water measured at 25 ° C. of at least 0.1 g / Obtaining a macroscopically isotropic and transparent solution, colored or not). This solubility is preferably greater than or equal to 1 g / L.
  • the film according to the invention is preferably an "anhydrous film", that is to say a film comprising a water content of less than 15% by weight, preferably less than 10% by weight and more preferably less than 5% by weight. % by weight, based on the total weight of the film. More preferably, the film according to the invention is free of water.
  • the polymers that can be used to form these films can be of synthetic or natural origin, and, where appropriate, modified by chemical reactions. They can be film-forming or non-film-forming. They are advantageously film-forming.
  • composition in the form of a film comprises in particular at least one film-forming polymer.
  • “Film-forming polymer” means a polymer capable of forming, by itself or in the presence of an auxiliary film-forming agent, a continuous film, and preferably a film whose cohesion and mechanical properties are such that said film may be isolated from a support.
  • These polymers are cataloged under the heading "Film Formers” in the cosmetic dictionary “International Cosmetic Ingredient Dictionary and Handbook” (see for example pages 2903-2906 of the ninth edition - 2002).
  • the film-forming polymers may be chosen for example from: vinyl polymers such as polyvinyl acetate, polyvinylpyrrolidones, copolymers of methyl vinyl ether and maleic anhydride, copolymer of vinyl acetate and crotonic acid, copolymers of vinylpyrrolidone and polyvinylpyrrolidone; vinyl acetate, copolymers of vinylpyrrolidone and caprolactam, polyvinyl alcohols.
  • the vinyl polymer is polyvinyl acetate (PVA), which is especially prepared by radical polymerization of the vinyl acetate monomer and then hydrolyzed.
  • polyvinyl acetate such as that sold under the name CELVOL 540 PV ALCOHOL by the company Celanese Chemicals
  • cellulosic cellulosic derivatives such as hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, methylcellulose, ethylhydroxyethylcellulose, carboxymethylcellulose, and the quatemized derivatives of cellulose.
  • the cellulose derivatives are chosen from hydroxypropylcellulose (HPC) and hydroxypropylmethylcellulose (HPMC). These polymers are soluble in water as well as in organic solvents. This makes it possible to increase the solubility field of the films containing them.
  • the choice of the molecular weight of these cellulosic polymers must be done judiciously to increase the dissolution of the films.
  • the HPCs used in a preferred manner are those sold by the company Hercules under the name KlucelO MF whose molecular weight is 850,000 (viscosity 4000-6500 mPa at 2% in water) - KlucelO EF whose molecular weight is 80,000 (viscosity 300-600 mPa at 10% in water).
  • the HPMC preferably used is hydroxypropyl methylcellulose of viscosity 40-60 cps (40-60 mPa) at 2% in water at 20 ° C, sold by Sigma-Aldrich.
  • starches and their derivatives starches and their derivatives; polymers of natural origin, optionally modified, such as pullulan, pectin, mannan, galactomannans, glucomannans and their derivatives, gum arabic, guar gum, xanthan gum, karaya gum, alginates, carrageenans, ulvans and other algal colloids, hyaluronic acid and its derivatives, shellac, sandaraque gum, dammars, elemis, copals, deoxyribonucleic acid, mucopolysaccharides such as hyaluronic acid, chondroitin sulfate; polymers derived from chitin or chitosan, anionic, cationic, amphoteric or nonionic;
  • protein polymers such as wheat or soy proteins
  • keratin and its derivatives for example keratin hydrolysates and keratin sulfones, casein, albumin, collagen, glutelin, glucagon, gluten, zein, gelatins and their derivatives;
  • acrylic phosphorylcholine copolymers such as poly-2- (methacryloyloxyethyl) phosphorylcholine sold under the name Lipidure HM by the company NOF Corporation (INCI name: Polyphosphorylcholine glycol acrylate);
  • the film-forming polymer is chosen from vinyl polymers, cellulose derivatives and mixtures thereof.
  • the film-forming polymer is chosen from polyvinyl acetate, hydroxypropylcellulose, hydroxypropylmethylcellulose, and mixtures thereof, polyurethanes, nitrocellulose, and carbomers.
  • the composition according to the invention comprises one or more film-forming polymer (s) in a content ranging from 10 to 95% by weight, preferably from 20 to 70% by weight, and more preferably from 30 to 60% by weight. % by weight, based on the total film ratio.
  • composition according to the invention may comprise at least one organic solvent which may be chosen from:
  • ketones such as methyl ethyl ketone, methyl isobutyl ketone, diisobutyl ketone, isophorone, cyclohexanone, acetone;
  • alcohols that are liquid at room temperature such as ethanol, isopropanol, diacetone alcohol, 2-butoxyethanol, cyclohexanol, n-propanol, n-butanol;
  • propylene glycol ethers which are liquid at room temperature such as propylene glycol monomethyl ether, propylene glycol monomethyl ether acetate, dipropylene glycol mono-butyl ether;
  • glycols such as ethylene glycol, propylene glycol, pentylene glycol, glycerol
  • cyclic ethers such as ⁇ -butyrolactone
  • short-chain esters having from 3 to 8 carbon atoms in total
  • esters such as ethyl acetate, butyl acetate, methyl acetate, propyl acetate, isopropyl acetate isopentyl acetate, methoxypropyl acetate, butyl lactate;
  • ethers such as diethyl ether, dimethyl ether or dichlorodiethyl ether; alkanes which are liquid at ambient temperature, such as decane, heptane, dodecane or cyclohexane;
  • alkyl sulphoxides such as dimethyl sulphoxide
  • aldehydes that are liquid at room temperature, such as benzaldehyde or acetaldehyde;
  • carbonates such as propylene carbonate and dimethyl carbonate
  • acetals such as methylal
  • the organic solvent is volatile.
  • volatile organic solvent is meant an organic solvent capable of evaporating on contact with the skin in less than one hour, at room temperature and atmospheric pressure.
  • the volatile organic solvent is liquid at ambient temperature, in particular having a non-zero vapor pressure at ambient temperature and atmospheric pressure, in particular it has a vapor pressure ranging from 0.13 Pa to 40 000 Pa (10 -3 300 mm Hg), and preferably ranging from 1.3 Pa to 8000 Pa (0.01 to 60 mm Hg).
  • the organic solvent is chosen from alcohols which are liquid at room temperature, such as ethanol, isopropanol, diacetone alcohol, 2-butoxyethanol and cyclohexanol, and mixtures thereof, and preferably ethanol and / or short chain esters (having 3 to 8 carbon atoms in total) such as ethyl acetate, butyl acetate, methyl acetate, propyl acetate, acetate isopropyl, isopentyl acetate, methoxypropyl acetate, butyl lactate.
  • the organic solvent used in the compositions according to the invention is chosen from ethanol, ethyl acetate or a mixture of these.
  • the organic solvent may represent from 60 to 95% by weight, preferably from 65 to 85% by weight, and preferably from 65 to 80% by weight, relative to the total weight of the composition.
  • composition according to the invention when it is in the form of a film, comprises, in addition to the polymeric polymer, at least one polysaccharide thickening agent.
  • the polysaccharide thickening agents used in the film according to the invention may be chosen from polysaccharides with gelling power. "Gelling power" defines the fact that at a concentration greater than or equal to 0.5
  • the viscosity of the solutions thus obtained is greater than or equal to 0.01 Pa.s at a shear rate equal to 1, the measurements being carried out at 25 ° C. using a RheoStress rheometer R5150 of Haake in cone-plane configuration, the measurements of the measuring cone being as follows: diameter: 60 mm and angle: 2 °.
  • the polysaccharide thickening agents may be chosen in particular from gum arabic, ghatti gum, karaya gum, locust bean gum, guar gum, tamarind gum, xanthan gum, gellan, pectins, tragacanth, agar, alginates, carrageenan, furcelleran, konjac and cellulose derivatives, and mixtures thereof.
  • the polysaccharide thickening agents are chosen from carrageenans which are linear polysaccharides extracted from certain red algae of the family Rhodophyceae. They consist of residues 1,3-1,3 and ⁇ -1,4 galactoses alternately, many galactose residues can be sulfated.
  • carrageenans There are three types of carrageenans, called kappacarraghenan, Iota-carrageenan and Lambda-carrageenan. This family of polysaccharides is described for example in Chapter 3 of the book “Food Gels” edited by Peter HARRIS, Elsevier 1989. It is possible in particular to use the carrageenan sold under the name SATIAGUM UTC 10 by the company Degussa.
  • the amount of thickening agent (s) in the composition according to the invention may range, for example, from 0.5 to 40% by weight, in particular from 1 to 20% by weight, and more particularly from 5 to 10% by weight. % by weight relative to its total weight.
  • composition in the form of a film may incorporate, in combination with the polymer as defined above, at least one oxyalkylenated polydimethylsiloxane derivative.
  • such a derivative has the advantage of significantly increasing the dissolution kinetics of the water-soluble film incorporating it.
  • PDMS oxyalkylenated polydimethylsiloxanes
  • water-soluble or water-dispersible means PDMS having a solubility in water measured at 25 ° C at least equal to 0.1 g L (obtaining a macroscopically isotropic solution and transparent, colored or not). This solubility is preferably greater than or equal to 1 g / l.
  • These PDMSs are preferably chosen from water-soluble silicones containing at least one terminal or pendant monovalent polyoxyalkylene group and which, introduced at 0.05% by weight in an aqueous solution, are capable of reducing the surface tension of the water to a minimum. value less than 35 mN / m, and preferably less than 30 mN / m.
  • Such oxyalkylenated PDMS are for example sold by the company OSI under the trade names Silwet, Silwet 1614, and Tegowet.
  • the composition according to the invention is in the form of a water-soluble anhydrous film comprising (i) at least one synthetic polysulfated oligosaccharide, (ii) at least one water-soluble or water-dispersible film-forming polymer and (iii) at least one oxyalkylenated polydimethylsiloxane derivative.
  • composition according to the invention in particular when it is in the form of a film, may further comprise one or more plasticizers chosen for example from castor oil, or polyols such as glycerin, sorbitol, mono- and / or di-saccharides, dipropylene glycol, butylene glycol, pentylene glycol, polyethylene glycols such as PEG-400.
  • plasticizers chosen for example from castor oil, or polyols such as glycerin, sorbitol, mono- and / or di-saccharides, dipropylene glycol, butylene glycol, pentylene glycol, polyethylene glycols such as PEG-400.
  • the amount of plasticizer (s) may range, for example, from 1 to 40% by weight and better still from 2 to 15% by weight relative to the total weight of the composition.
  • compositions according to the invention are provided.
  • composition according to the invention is in the form of an oil-in-water emulsion, preferably in cream form, comprising:
  • composition according to the invention is in the form of an oil-in-water emulsion, preferably in cream form, comprising:
  • sucrose octasulfate KSOS
  • sucrose octasulfate aluminum salt sucrose octasulfate aluminum salt (sucralfate)
  • composition according to the invention is in the form of an oil-in-water emulsion, preferably in cream form, comprising:
  • sucrose octasulfate KSOS
  • sucrose octasulfate aluminum salt sucralfate
  • composition according to the invention is in the form of an oil-in-water emulsion, preferably in cream form, comprising:
  • sucrose octasulfate KSOS
  • sucrose octasulfate aluminum salt sucralfate
  • composition according to the invention is in the form of a water-based filmogel composition
  • a water-based filmogel composition comprising:
  • composition according to the invention is in the form of a solvent-based filmogel composition
  • a solvent-based filmogel composition comprising:
  • plasticizer preferably castor oil
  • compositions or combinations defined above are implemented in a formulation intended for topical use.
  • the invention relates to a topical composition for therapeutically treating hemorrhoids in a subject having a predisposition to the development of said hemorrhoids comprising, in a physiologically acceptable carrier, at least one effective amount of at least one potassium salt of sucrose synthetic octasulfate.
  • the subject of the invention is the use of an effective amount of potassium salt of sucrose octasulfate in combination with an effective amount of at least one other active substance as defined above, for the manufacture of a dermatological composition for treating and / or preventing hemorrhoids.
  • a formulation in the form of a cream (oil-in-water emulsion) comprising a potassium salt of sucrose octasulfate according to the invention having the following composition was prepared:
  • Emulsifying wax 2,000 Emulsifying wax 2,000
  • Silicone oil (Decamethyl- 4,000
  • Emollient Ester (myristyl lactate) 5,000
  • the thickener was dispersed in the water. Glycerin, propylene glycol, KSOS and preservative were added and homogenized. It was heated to 70-75 ° C. When the mixture reached 70-75 ° C, the water content was adjusted and then neutralized with 10% sodium hydroxide and the temperature was reduced to 70-75 ° C.
  • the oil-in-water surfactant, the emulsifying wax, the stearic acid, the iodecyl isononanoate, the silicone oil (decamethylcyclopentasiloxane), the emollient ester (myristyl lactate) were mixed together. ) and heated to 70-75 ° C.
  • a formulation in cream form comprising an aluminum salt and a potassium salt of sucrose octasulfate according to the invention having the following composition: Constituents%
  • Emulsifying wax 2,000 Emulsifying wax 2,000
  • Silicone oil (Decamethyl- 4,000
  • Emollient Ester (myristyl lactate) 5,000
  • the thickener was dispersed in the water. Glycerin, propylene glycol, KSOS, sucralfate and preservative were added and homogenized. It was heated to 70-75 ° C. When the mixture reaches 70-75 ° C, the water content is adjusted then neutralized with 10% sodium hydroxide and the temperature is brought to 70-75 ° C.
  • the oil-in-water surfactant, the emulsifying wax, the stearic acid, the iodecyl isononanoate, the silicone oil (decamethylcyclopentasiloxane), the emollient ester (myristyl lactate) were mixed together. ) and heated to 70-75 ° C.
  • the silicone surfactant was added and heated again for 5 minutes. Finally, the heating was stopped and allowed to cool to room temperature, maintaining sufficient agitation depending on the viscosity of the mixture.
  • the mixture takes an inhomogeneous appearance towards 35 ° C, but the cream then becomes smooth and shiny.
  • Example 3 A solvent-based filmogel formulation was prepared comprising a synthetic polysulfated oligosaccharide according to the invention having the following composition:
  • KSOS octasulfate
  • a water-based filmogel formulation comprising a synthetic polysulfated oligosaccharide according to the invention having the following composition
  • the thickener was dispersed in water with vigorous stirring, then sorbitol and dextran were added by heating at 40 ° C to obtain better solubility.
  • KSOS, parabens and phenoxyethanol were added and allowed to stir to homogenize. It was then allowed to cool to room temperature by stopping the heating, adjusting the water loss if necessary. Finally, it was neutralized with sodium hydroxide and allowed to stir for 10 minutes before stopping the stirring.

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Abstract

The invention relates to a novel topical dermatological composition, especially used in the prevention and/or treatment of haemorrhoids, comprising, in a physiologically acceptable carrier, at least one effective quantity of potassium salt of a synthetic polysulfated oligosaccharide having between 1 and 4 monosaccharide units.

Description

COMPOSITION DERMATOLOGIQUE POUR LA PREVENTION ET LE  DERMATOLOGICAL COMPOSITION FOR PREVENTION AND
TRAITEMENT DES HEMORROÏDES  TREATMENT OF HEMORROIDS
La présente invention a trait à une nouvelle composition dermatologique topique, notamment utile pour prévenir et/ou traiter les hémorroïdes comprenant, dans un support physiologiquement acceptable, au moins une quantité efficace de sel de potassium d'oligosaccharide polysulfaté synthétique ayant 1 à 4 unités d'osés. The present invention relates to a novel topical dermatological composition, especially useful for preventing and / or treating hemorrhoids comprising, in a physiologically acceptable carrier, at least one effective amount of synthetic polysulfated oligosaccharide potassium salt having 1 to 4 'daring.
Les sels de sucrose octasulfate sont connus depuis longtemps désormais pour être utilisés dans toutes sortes d'applications cosmétiques, dermatologiques ou encore médicales. Ainsi, parmi toutes ces utilisations, il est décrit au travers de documents des sociétés Pierre Fabre Dermo-Cosmétique, ou bien des Laboratoires Urgo, divers sels de sucrose octasulfate pour leurs bénéfices au travers d'actions cicatrisantes, d'actions de remodelage tissulaire postbrûlure ou induit par le vieillissement, d'actions sur les vergetures ou encore sur les cicatrices pathologiques. Le document EP 0 391 905 décrit une composition topique à base de sel d'aluminium de sucrose octasulfate utile pour la prévention et le traitement des hémorroïdes en plus de son action cicatrisante. Sucrose octasulfate salts have long been known for use in all kinds of cosmetic, dermatological or medical applications. Thus, among all these uses, it is described through documents of Pierre Fabre Dermo-Cosmetic companies, or Urgo Laboratories, various salts of sucrose octasulfate for their benefits through healing actions, post-burn tissue remodeling actions or induced by aging, actions on stretch marks or pathological scars. EP 0 391 905 discloses a topical composition based on aluminum salt sucrose octasulfate useful for the prevention and treatment of hemorrhoids in addition to its healing action.
Les hémorroïdes sont souvent considérées à tort, comme une variété de varices dont seule la localisation semble différente. En effet, de nombreuses hypothèses physiopathologiques ont été rejetées, notamment celle de la « varice » anale au profit de conceptions mécaniques et circulatoires. Dans une première théorie, la maladie serait provoquée par l'altération progressive des structures musculo-ligamenteuses (ligament de Parks) maintenant en bonne position les coussinets de Thomson (renforcements cellulo-fibro- élastiques du tissu conjonctif sous muqueux assurant l'obturation complète de la lumière du canal anal et contenant les hémorroïdes). Ceci explique la possibilité d'une procidence hémorroïdaire. Dans l'autre théorie, l'ouverture de shunts arterio-veineux (structure caverneuse que sont les coussinets de Thomson, on parle également d'anastomose artério- veineuse à ce niveau) serait à l'origine d'un afflux sanguin artériel excessif dépassant les capacités de drainage du tissu hémorroïdaire, occasionnant ainsi congestion et hémorragie de sang rutilant. Ces anomalies vasculaires pourraient entraîner une dystrophie veineuse avec formation de thromboses et altération du tissu de soutien, contribuant ainsi à l'extériorisation progressive des hémorroïdes. Enfin, une hypertonie sphinctérienne est souvent présente ; elle aggrave les signes fonctionnels en diminuant le retour veineux ce qui accentue les hémorragies [Faculté de Médecine de Marseille - DCEM 2 - Module n°12 « Hepato-Gastro- Entérologie »]. Hemorrhoids are often wrongly considered as a variety of varicose veins whose only location seems different. Indeed, many physiopathological hypotheses have been rejected, especially that of the anal "varix" in favor of mechanical and circulatory designs. In a first theory, the disease would be caused by the progressive alteration of the musculo-ligamentous structures (Parks ligament) maintaining in good position the pads of Thomson (cellulo-fibroelastic reinforcements of the submucous connective tissue ensuring complete obturation of light from the anal canal and containing hemorrhoids). This explains the possibility of hemorrhoidal procidence. In the other theory, the opening of arterio-venous shunts (the cavernous structure that is the Thomson pads, we also speak of arteriovenous anastomosis at this level) would be the cause of an excessive arterial blood flow exceeding the drainage capacities of the hemorrhoidal tissue, thus causing congestion and haemorrhage of glowing blood. These vascular abnormalities could lead to venous dystrophy with formation of thrombosis and alteration of the supporting tissue, thus contributing to the gradual exteriorization of hemorrhoids. Finally, sphincter hypertonia is often present; she aggravates the functional signs by decreasing the venous return which accentuates the haemorrhages [Faculty of Medicine of Marseilles - DCEM 2 - Module n ° 12 "Hepato-gastroenterology"].
De façon tout à fait surprenante, le sel de potassium d'oligosaccharide polysulfaté synthétique ayant 1 à 4 unités d'osés laisse entrevoir des résultats de meilleure facture que le sel d'aluminium de sucrose octasulfate sur la prévention et le traitement des hémorroïdes. Quite surprisingly, the synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of risk suggests better results than the aluminum salt of sucrose octasulfate on the prevention and treatment of hemorrhoids.
Ainsi l'objet de l'invention réside dans une composition dermatologique topique pour son utilisation dans la prévention et le traitement des hémorroïdes, comprenant, dans un support physiologiquement acceptable, au moins une quantité efficace de sel de potassium d'oligosaccharide polysulfaté synthétique ayant 1 à 4 unités d'osés. Thus, the object of the invention resides in a topical dermatological composition for its use in the prevention and treatment of hemorrhoids, comprising, in a physiologically acceptable support, at least one effective amount of synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of dare.
De façon préférée, le sel de potassium de sucrose octasulfate démontre des effets avantageux selon l'une quelconque des deux hypothèses génératrices d'hémorroïdes choisie. En effet, selon la première théorie évoquée, le sel de potassium de sucrose octasulfate présente un effet positif de renforcement de la musculeuse longitudinale du rectum formant le ligament de Parks. Selon la seconde hypothèse, le sel de potassium de sucrose octasulfate démontre également des effets positifs sur la prévention de l'ouverture de shunts artério- veineux (préférentiellement au niveau des coussinets de Thomson), permettant ainsi de mieux canaliser la trop forte pression sanguine exercée au niveau des veines hémorroïdaires. Preferably, the potassium salt of sucrose octasulfate demonstrates advantageous effects according to any one of the two hypotheses generating hemorrhoids chosen. Indeed, according to the first theory mentioned, the potassium salt of sucrose octasulfate has a positive strengthening effect of the longitudinal muscularis of the rectum forming the ligament of Parks. According to the second hypothesis, the potassium salt of sucrose octasulfate also has positive effects on the prevention of the opening of arteriovenous shunts (preferentially at the level of Thomson pads), thus making it possible to better channel the excessive blood pressure exerted. at the hemorrhoidal veins.
Par « hémorroïde», on entend toute extériorisation permanente des veines de quelconque calibre que ce soit, notamment hémorroïdaires, situées au niveau externe du rectum ou au niveau du lumen du canal anal ou de l'ampoule rectale. By "hemorrhoid" is meant any permanent externalization of veins of any size whatsoever, including hemorrhoids, located at the external rectum or at the lumen of the anal canal or the rectal bulb.
Par « prévenir et/ou traiter », on entend toute action au niveau des symptômes des hémorroïdes, c'est-à-dire toute action thérapeutique sur la musculeuse longitudinale du rectum formant le ligament de Parks et/ou sur l'ouverture de shunts artério- veineux. On entend par "composition dermatologique" au sens de la présente demande, une composition pour application topique, comportant un milieu dermatologiquement acceptable, c'est-à-dire qui présente une couleur, une odeur et un toucher agréables et qui ne génère pas d'inconforts inacceptables (picotements, tiraillements, rougeurs), susceptibles de détourner les consommateurs de l'utilisation de cette composition. Par "quantité efficace", on entend au sens de la présente invention une quantité suffisante pour obtenir l'effet attendu. By "prevent and / or treat" means any action on the symptoms of hemorrhoids, that is to say, any therapeutic action on the longitudinal muscularis of the rectum forming the ligament of Parks and / or the opening of shunts arteriovenous. For the purposes of the present application, the term "dermatological composition" is intended to mean a composition for topical application comprising a dermatologically acceptable medium, that is to say one which has a pleasant color, odor and feel and which does not generate dermal substances. unacceptable discomfort (tingling, tightness, redness), likely to divert consumers from the use of this composition. By "effective amount" is meant in the sense of the present invention an amount sufficient to achieve the expected effect.
Par "support physiologiquement acceptable", on désigne un support non toxique et susceptible d'être appliqué sur au moins une matière kératinique d'êtres humains. By "physiologically acceptable carrier" means a non-toxic support and may be applied to at least one keratin material of human beings.
Oligosaccharide polysulfaté synthétique Synthetic polysulfated oligosaccharide
La composition selon l'invention comprend au moins sel de potassium d'oligosaccharide polysulfaté synthétique ayant 1 à 4 unités d'osés, et de préférence de 1 ou 2 unités d'osés, généralement liées entre elles par liaison glycosidique alpha ou bêta. En d'autres termes, il s'agit de mono, di, tri ou tétrasaccharides, et de préférence de mono ou dissacharides. The composition according to the invention comprises at least one synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of oste, and preferably 1 or 2 units of osteos, generally linked together by glycosidic linkage alpha or beta. In other words, it is mono, di, tri or tetrasaccharides, and preferably mono or dissacharides.
Il n'y a pas de limitation particulière concernant la nature des unités oses de ces polysaccharides. De préférence, il s'agira de pentoses ou d'hexoses. A titre d'exemple de monosaccharide, on peut citer le glucose, le galactose ou le mannose. A titre d'exemple de disaccharide, on peut citer le maltose, le lactose, le sucrose ou le tréhalose. A titre d'exemple de trisaccharide, on peut citer le mélézitose. A titre d'exemple de tétrasaccharide, on peut citer le stachyose. There is no particular limitation on the nature of the ose units of these polysaccharides. Preferably, it will be pentoses or hexoses. As an example of a monosaccharide, mention may be made of glucose, galactose or mannose. As an example of a disaccharide, mention may be made of maltose, lactose, sucrose or trehalose. As an example of a trisaccharide, mention may be made of melezitose. As an example of a tetrasaccharide, mention may be made of stachyose.
De préférence, l'oligosaccharide est un disaccharide, et de préférence encore le sucrose. Preferably, the oligosaccharide is a disaccharide, and more preferably sucrose.
On entend par "oligosaccharide polysulfaté" au sens de la présente demande un oligosaccharide dont au moins deux, et de préférence tous les groupes hydroxyles de chaque ose ont été substitués par un groupe sulfate. For the purposes of the present application, the term "polysulfated oligosaccharide" is understood to mean an oligosaccharide of which at least two, and preferably all, hydroxyl groups of each monosaccharide have been substituted with a sulphate group.
De préférence au sens de la présente invention, est utilisé le sel de potassium de sucrose octasulfate qui est un polymère synthétique formé de 2 unités d'osés, généralement liées entre elles par liaison glycosidique alpha ou bêta. Ce dernier, dans le cadre de la présente invention, peut se présenter sous forme de poudre micronisée ou sous forme solubilisée. For the purposes of the present invention, the potassium salt of sucrose octasulfate, which is a synthetic polymer formed from 2 units of osteosaccharide, generally bonded to one another by an alpha or beta glycosidic bond, is preferably used. The latter, in the context of the present invention, may be in the form of a micronized powder or in solubilized form.
Selon un mode de réalisation particulier de l'invention, le sel de potassium d'oligosaccharide polysulfaté synthétique ayant 1 à 4 unités d'osés peut être introduit dans les compositions selon l'invention, de préférence seul mais aussi en mélange avec d'autres sels d'oligosaccharide polysulfaté synthétique ayant 1 à 4 unités d'osés, tel que le sucralfate et/ou avec une autre substance active, de préférence une substance active cicatrisante et/ou restructurante de la peau, tel que par exemple l'acide hyaluronique. Dans le cadre de la présente invention, ces sels d'oligosaccharides polysulfatés synthétiques formés de 1 à 4 unités d'osés, et leurs dérivés, ont une action potentialisatrice de celle du sel de potassium d'oligosaccharide polysulfaté, de préférence de celle du sel de sucrose octasulfate, c'est-à-dire qui possèdent une action de base positive sur les hémorroïdes mais qui présentent surtout un effet synergique de l'action du sel de potassium d'oligosaccharide polysulfaté sur lesdites hémorroïdes. Parmi ces sels d'oligosaccharides polysulfatés synthétiques formés de 1 à 4 unités d'osés, peuvent être utilisés de façon générale, les sels de métal alcalin tels que les sels de sodium, de calcium, de magnésium, les sels d'argent, les sels d'aluminium, les sels de zinc; ou encore les sels d'acide aminé. De manière encore plus privilégiée, sont utilisés : - le sel de calcium, de zinc et de magnésium; According to one particular embodiment of the invention, the synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of risk can be introduced into the compositions according to the invention, preferably alone but also in admixture with other synthetic polysulfated oligosaccharide salts having 1 to 4 units of risk, such as sucralfate and / or with another active substance, preferably an active substance healing and / or restructuring of the skin, such as for example hyaluronic acid. In the context of the present invention, these synthetic polysulfated oligosaccharide salts formed from 1 to 4 units of oste, and their derivatives, have a potentiating action of that of the polysulphated oligosaccharide potassium salt, preferably that of the salt. sucrose octasulfate, that is to say which have a positive base action on hemorrhoids but which have especially a synergistic effect of the action of polysulfated oligosaccharide potassium salt on said hemorrhoids. Among these synthetic polysulphated oligosaccharide salts formed from 1 to 4 units of risk, alkali metal salts such as sodium, calcium, magnesium, silver salts, aluminum salts, zinc salts; or the amino acid salts. Even more privileged, are used: - salt of calcium, zinc and magnesium;
- le sel d'argent du sucrose octasulfate ; the silver salt of sucrose octasulfate;
- le sel d'aluminium de sucrose octasulfate, plus généralement appelé sucralfate. - the aluminum salt of sucrose octasulfate, more generally called sucralfate.
Selon un mode particulier de réalisation de l'invention, la composition comprend au moins un sel de potassium d'oligosaccharide polysulfaté synthétique ayant 1 à 4 unités d'osés en une teneur comprise entre 0,1 et 50% en poids, par rapport au poids total de la composition. According to one particular embodiment of the invention, the composition comprises at least one synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of osteoside in a content of between 0.1 and 50% by weight, relative to total weight of the composition.
Selon un mode particulier de réalisation de l'invention, la composition comprend au moins une quantité de sel de potassium d'oligosaccharide polysulfaté synthétique ayant 1 à 4 unités d'osés de telle sorte que la quantité relarguée sur l'hémorroïde est comprise entre 0,001 g/1 et 50 g/1, et de préférence encore entre 0,01 et 10 g/1. According to one particular embodiment of the invention, the composition comprises at least one amount of synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of oste so that the quantity released on the hemorrhoid is between 0.001 g / 1 and 50 g / l, and more preferably between 0.01 and 10 g / l.
Substance active Outre le sel de potassium d'oligosaccharide polysulfaté synthétique ayant 1 à 4 unités d'osés, la composition selon l'invention peut comprendre une (ou plusieurs) autre(s) substance(s) active(s). Active substance In addition to the synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of risk, the composition according to the invention may comprise one (or more) other active substance (s).
De manière générale, les actifs sont choisis parmi les anti-bactériens, les antiseptiques, les antifongiques, les anti-inflammatoires, les actifs favorisant la cicatrisation et/ou la restructuration de la peau, les antiprurigineux, les filtres UV, les agents apaisants, les actifs hydratants, les agents dépigmentants, les agents kératolytiques, les anti-viraux, les antidouleurs, les anesthésiques, les vitamines, les oligosaccharides polysulfatés sunthétiques formés de 1 à 4 unités d'osés ou leur sel, tels que décrits supra, à l'exception du sel de potassium de sucrose octasulfate, et leurs mélanges. In general, the active ingredients are chosen from anti-bacterials, antiseptics, antifungals, anti-inflammatories, active agents promoting healing and / or restructuring of the skin, antipruritic agents, UV filters, soothing agents, moisturizing active agents, depigmenting agents, keratolytic agents, anti-virals, pain relievers, anesthetics, vitamins, polysulfated sunless oligosaccharides formed from 1 to 4 units of oste or their salt, as described above, except potassium salt sucrose octasulfate, and mixtures thereof.
De manière générale, les actifs sont choisis parmi : In general, the assets are chosen from:
- les anti-bactériens tels que le Polymyxine B, les pénicillines (Amoxycilline), l'acide clavulanique, les tétracyclines, la Minocycline, la chlorotétracycline, les aminoglycosides, l'Amikacine, la Gentamicine, la Néomycine, l'argent et ses sels (Sulfadiazine argentique), les probiotiques ; anti-bacterials such as polymyxin B, penicillins (amoxycillin), clavulanic acid, tetracyclines, minocycline, chlorotetracycline, aminoglycosides, amikacin, gentamicin, neomycin, silver and its salts (Sulfadiazine argentic), probiotics;
- les antiseptiques tels que le mercurothiolate de sodium, l'éosine, la chlorhexidine, le borate de phénylmercure, l'eau oxygénée, la liqueur de Dakin, le triclosan, le biguanide, l'hexamidine, le thymol, le Lugol, la Povidone iodée, le Merbromine, le Chlorure de Benzalkonium et de Benzethonium, l'éthanol, l'isopropanol, les sels d'argent ; - les anti fongiques tels que les polyènes, le Nystatin, l'Amphotéricine B, laantiseptics such as sodium mercurothiolate, eosin, chlorhexidine, phenylmercury borate, hydrogen peroxide, Dakin liquor, triclosan, biguanide, hexamidine, thymol, Lugol, Povidone iodine, Merbromin, Benzalkonium and Benzethonium Chloride, ethanol, isopropanol, silver salts; anti fungal agents such as polyenes, Nystatin, Amphotericin B,
Natamycine, les imidazolés (Miconazole, Ketoconazole, Clotrimazole, Éconazole, Bifonazole, Butoconazole, Fenticonazole, Isoconazole, Oxiconazole, Sertaconazole, Sulconazole, Thiabendazole, Tioconazole), les triazolés (Fluconazole, Itraconazole, Ravuconazole, Posaconazole, Voriconazole), les allylamines, la Terbinafme, l'Amorolfine, la Naftifine, la Buténafine ; Natamycin, imidazoles (Miconazole, Ketoconazole, Clotrimazole, Ecconazole, Bifonazole, Butoconazole, Fenticonazole, Isoconazole, Oxiconazole, Sertaconazole, Sulconazole, Thiabendazole, Tioconazole), triazoles (Fluconazole, Itraconazole, Ravuconazole, Posaconazole, Voriconazole), allylamines, Terbinafme, Amorolfine, Naftifine, Butenafine;
- la Flucytosine (antimétabolite), la Griséofulvine, la Caspofungine, la Micafungine, l'arginine ; Flucytosine (antimetabolite), Griseofulvin, Caspofungin, Micafungin, Arginine;
- les anti-inflammatoires tels que les Glucocorticoïdes, les anti-inflammatoires non stéroïdiens, l'Aspirine, l'Ibuprofène, le Kétoprofène, le Flurbiprofène, le Diclofénac, l'Acéclofénac, le Kétorolac, le éloxicam, le Piroxicam, le Ténoxicam, le Naproxène, l'Indométacine, le Naproxcinod, le Nimésulide, le Célécoxib, l'Etoricoxib, le Parécoxib, le Rofécoxib, le Valdécoxib, la Phénylbutazone, l'acide niflumique, l'acide méfénamique ; anti-inflammatories such as glucocorticoids, nonsteroidal anti-inflammatory drugs, aspirin, ibuprofen, ketoprofen, flurbiprofen, diclofenac, aceclofenac, ketorolac, eloxicam, piroxicam, tenoxicam, Naproxen, Indomethacin, Naproxcinod, Nimesulide, Celecoxib, Etoricoxib, Parecoxib, Rofecoxib, Valdecoxib, Phenylbutazone, Niflumic acid, Mefenamic acid;
- les actifs favorisant la cicatrisation et/ou la restructuration de la peau tels que le Rétinol, les vitamines hydrosolubles telles que la Vitamine A ou ses dérivés, la Vitamine E ou ses dérivés, la N-acétyl-hydroxyproline, les extraits de CentellaAsiatica et d'aneth la papaïne, les silicones, les huiles essentielles de thym, de niaouli, de romarin et de sauge, l'acide hyaluronique, Pallantoïne, Hema'tîte (Gattefossé), Vitamine C, TEGO Pep 4-17 (Evonik), Toniskin (Silab), Collageneer (Expanscience), Timecode (Seppic), Gatuline skin repair (Gattefossé), Panthenol, PhytoCellTec Alp Rose (MibelleBiochemistry), Serilesine : Lipotec, Heterosides de Talapetraka (Beyer), Stoechiol (Codif), macarose (Sensient), Dermaveil (IchimaruPharcos), Phycosaccaride AI (Codif), la metformine ; the active agents promoting healing and / or restructuring of the skin, such as retinol, water-soluble vitamins such as vitamin A or its derivatives, vitamin E or its derivatives, N-acetyl-hydroxyproline, extracts of CentellaAsiatica and dill, papain, silicones, essential oils of thyme, niaouli, rosemary and sage, hyaluronic acid, Pallantoin, Hema'tite (Gattefossé), Vitamin C, TEGO Pep 4-17 (Evonik), Toniskin (Silab), Collageneer (Expanscience), Timecode (Seppic), Gatuline skin repair (Gattefossé), Panthenol, PhytoCellTec Alp Rose (MibelleBiochemistry), Serilesine: Lipotec, Heterosides of Talapetraka (Beyer), Stoechiol (Codif), macarose (Sensient ), Dermaveil (IchimaruPharcos), Phycosaccaride AI (Codif), metformin;
- les agents dépigmentants tels que l'acide kojique (KojicAcid SL® - Quimasso (Sino Lion)), l'Arbutine (Olevatin® - Quimasso (Sino Lion)), le mélange de palmitoylpropyl de sodium et d'extrait de nénuphar blanc (Sepicalm® - Seppic), l'undécylénoyl phénylalanine (Sepiwhite® - Seppic), l'extrait de réglisse obtenue par fermentation d'Aspergillus et éthoxydiglycol (GatulineWhitening® - Gattefossé), l'acide octadécènedioïque (ODA White® - Sederma), l'alpha-arbutin (Alpha-arbutin®, SACI-CFPA (Pentapharm)), l'extrait aqueux de feuilles Arctophylos Uva Ursi (Melfade-J® - SACI-CFPA (Pentapharm)), le mélange de plante complexe Gigawhite® (SACI-CFPA (Alpaflor)), la diacétylboldine (Lumiskin® - Sederma), l'extrait de mandarine du Japon (Melaslow® - Sederma), le mélange d'extrait de citron enrichi en acide citrique et d'extrait de concombre (Uninontan®U-34 - Unipex), le mélange d'extrait de Rumex occidentalis et de vitamine C (Tyrostat® 11 - Unipex), des oligopeptides (Mélanostatine 5® - Unipex), le dipalmitatekojique (KAD-15® - Quimasso (Sino Lion)), le complexe d'origine naturelle Vegewhite® de LCW, des extraits de germe de blé (Clariskin® II - Silab), l'éthyldiaminetriacétate (EDTA); depigmenting agents such as kojic acid (KojicAcid SL ® - Quimasso (Sino Lion)), Arbutin (Olevatin ® - Quimasso (Sino Lion)), the mixture of palmitoylpropyl of sodium and of white water lily extract ( Sepicalm ® - Seppic), undecylenoyl phenylalanine (Sepiwhite ® - Seppic), licorice extract obtained by fermentation of Aspergillus and ethoxydiglycol (GatulineWhitening ® - Gattefossé), octadecenedioic acid (ODA White ® - Sederma), l alpha-arbutin (alpha-arbutin ®, SACI-CFPA (Pentapharm)), aqueous sheets Uva Ursi extract Arctophylos (Melfade-J ® - SACI-CFPA (Pentapharm)), the complex mixture of plant Gigawhite ® (SACI -CFPA (Alpaflor)), diacetylboldine (Lumiskin ® - Sederma), mandarin extract from Japan (Melaslow ® - Sederma), lemon extract mixture enriched with citric acid and cucumber extract (Uninontan ® U-34 - Unipex), the mixture of Rumex occidentalis extract and vitamin C (Tyrostat ® 11 - Unipex), oligopeptides (Melanostatin 5 ® - Unipex), dipalmitate kojic (KAD-15 ® - Quimasso (Sino Lion)), LCW Vegewhite ® natural origin complex, wheat germ extracts (Clariskin ® II - Silab), l ethyldiaminetriacetate (EDTA);
- Les antiprurigineux tels que l'hydrocotisone, l'enoxolone,la diphenyhydramine, les antihistaminiques à application locale anti Hl ; - Antipruriginous agents such as hydrocotisone, enoxolone, diphenyhydramine, antihistamines with local anti H1 application;
- Des filtres UV tels que Parsol MCX, Parsol 1789 ; UV filters such as Parsol MCX, Parsol 1789;
- Des agents apaisants tels que la camomille, le bisabolol, le xanthalène, l'acide glycyrrhébénique, la tanactine (CPN), la Calmiskin (Silab) ; - Des actifs hydratants tels que le xpermoist (Lipotec), l'acide hyaluronique, l'urée, les acides gras, la glycérine, les cires, Exossine (Unipex) ; Soothing agents such as chamomile, bisabolol, xanthalene, glycyrrhenic acid, tanactin (CPN), Calmiskin (Silab); - Moisturizing active ingredients such as xpermoist (Lipotec), hyaluronic acid, urea, fatty acids, glycerine, waxes, Exossine (Unipex);
- les agents kératolytiques tels que l'acide salicylique, le salicylate de zinc, l'acide ascorbique, les acides alpha hydroxylés (acide glycolique, lactique, malique, citrique, tartrique), les extraits d'Erable argenté, de Griottier, de Tamarinier, l'urée, le rétinoïde topique Kératoline® (Sederma), les protéases obtenues par fermentation de Bacillus Subtilis, le produit Linked-Papain® (SACI-CFPA), la papaïne (enzyme protéolytique issue du fruit de papaye) ; keratolytic agents such as salicylic acid, zinc salicylate, ascorbic acid, alpha hydroxylated acids (glycolic acid, lactic acid, malic acid, citric acid, tartaric acid), extracts of silver maple, Griottier, tamarind urea, topical retinoid Keratoline ® (Sederma), proteases obtained by fermentation of Bacillus Subtilis, the Linked-Papain ® product (SACI-CFPA), papain (proteolytic enzyme derived from papaya fruit);
- Les vitamines telles que le rétinol (vitamine A) et ses dérivés, le tocophérol (vitamine E) et ses dérivés. - Les veinotoniques tels que les anthrocyanosides, les citroflavonoïdes et les flavonoïdes en général, la diosmine, les rutosides, la troxérutine, ou encore les extraits de ruscus. - Vitamins such as retinol (vitamin A) and its derivatives, tocopherol (vitamin E) and its derivatives. - Veinotonics such as anthrocyanosides, citroflavonoids and flavonoids in general, diosmin, rutosides, troxerutin, or extracts of ruscus.
- Les analgésiques tels que la morphine, la buprénorphine, la nalbuphine , le sufentanil, le rémifentanil, le fentanyl, l'alfentanil, la codéine, l'hydromorphone, le dextropropoxyphène, le tramadol, le néfopam, le paracétamol ou acétaminophène, l'ibuprophène, ou encore les anti- inflammatoires non stéroïdiens (AINS), parmi lesquels l'aspirine. - Analgesics such as morphine, buprenorphine, nalbuphine, sufentanil, remifentanil, fentanyl, alfentanil, codeine, hydromorphone, dextropropoxyphene, tramadol, nefopam, paracetamol or acetaminophen, ibuprofen, or nonsteroidal anti-inflammatory drugs (NSAIDs), including aspirin.
Selon un mode préféré de réalisation, la composition selon l'invention comprend au moins une quantité efficace d'une autre substance active favorisant la cicatrisation et/ou la restructuration de la peau, de préférence l'acide hyaluronique. According to a preferred embodiment, the composition according to the invention comprises at least one effective amount of another active substance that promotes healing and / or restructuring of the skin, preferably hyaluronic acid.
Selon un autre mode préféré de réalisation, la composition selon l'invention comprend au moins une quantité efficace d'une autre substance active choisie parmi les analgésiques et/ou les veinotoniques. According to another preferred embodiment, the composition according to the invention comprises at least one effective amount of another active substance chosen from analgesics and / or venotonic agents.
On peut, en outre, associer les actifs selon l'invention, à des agents actifs destinés notamment à la prévention et/ou au traitement des affections cutanées. In addition, the active agents according to the invention may be combined with active agents intended in particular for the prevention and / or treatment of cutaneous affections.
Galénique Les compositions selon l'invention peuvent se présenter sous toutes les formes galéniques normalement utilisées par l'homme du métier. Galenic The compositions according to the invention may be in any galenical form normally used by those skilled in the art.
Lorsque les compositions sont destinées à une administration topique, elles peuvent se présenter sous la forme de solutions (aqueuses, hydroalcooliques ou huileuses), de dispersions (type lotion ou sérum), d'émulsions de consistance liquide ou semi-liquide (type lait), de suspensions ou émulsions (type crème), de gel aqueux ou lipophile, de microémulsions, de microcapsules, de microparticules, ou de dispersions vésiculaires de type ionique et/ou non ionique. Elles peuvent également se présenter sous la forme de pansements interfaces non absorbants ou encore de bande de contention imprégnée de ladite composition ou comprenant le sel de potassium de sucrose octasulfate et/ou tout autre actif associé au sein même des fibres constituant ledit produit textile. When the compositions are intended for topical administration, they may be in the form of solutions (aqueous, hydroalcoholic or oily), dispersions (lotion or serum type), emulsions of liquid or semi-liquid consistency (milk type). , from suspensions or emulsions (cream type), aqueous or lipophilic gel, microemulsions, microcapsules, microparticles, or vesicular dispersions of ionic and / or nonionic type. They may also be in the form of nonabsorbent interface dressings or compression band impregnated with said composition or comprising the potassium salt of sucrose octasulfate and / or any other associated active within the same fibers constituting said textile product.
Ces compositions sont préparées selon les méthodes usuelles. These compositions are prepared according to the usual methods.
Elles peuvent notamment se présenter sous la forme de crèmes de traitement ou de soin pour le visage, pour les grands plis anatomiques ou pour le corps, Les compositions selon l'invention peuvent également consister en des préparations solides telles que des savons ou des pains de nettoyage. They may in particular be in the form of creams for treatment or care for the face, for large anatomical folds or for the body. The compositions according to the invention may also consist of solid preparations such as soaps or breads. cleaning.
Bien entendu, la quantité de sel de potassium de sucrose octasulfate utilisée dans la formulation galénique selon l'invention est adaptée en fonction de la cinétique recherchée ainsi que des contraintes spécifiques liées à sa nature, solubilité, résistance à la chaleur, etc. Eau et solvants hydrosolubles Of course, the amount of potassium salt sucrose octasulfate used in the galenic formulation according to the invention is adapted according to the desired kinetics as well as specific constraints related to its nature, solubility, heat resistance, etc. Water and water soluble solvents
Selon un mode préféré de réalisation, la composition de l'invention peut également comprendre de l'eau, et notamment une eau thermale et/ou minérale. According to a preferred embodiment, the composition of the invention may also comprise water, and in particular a thermal and / or mineral water.
La composition selon l'invention peut également comprendre un ou plusieurs solvants miscibles à l'eau, tels que les alcools inférieurs, notamment l'éthanol et l'isopropanol, le propylène glycol. The composition according to the invention may also comprise one or more water-miscible solvents, such as lower alcohols, in particular ethanol and isopropanol, propylene glycol.
Phase grasse Fatty phase
La composition selon l'invention peut également comprendre une phase grasse. The composition according to the invention may also comprise a fatty phase.
Lorsque la composition de l'invention se présente sous la forme d'une émulsion, la proportion de la phase grasse peut aller de 5 à 80 % en poids, et de préférence de 5 à 50 % en poids, par rapport au poids total de la composition. Lorsque la composition de l'invention est une solution ou un gel huileux, la phase grasse peut représenter plus de 90 % du poids total de la composition. When the composition of the invention is in the form of an emulsion, the proportion of the fatty phase can range from 5 to 80% by weight, and preferably from 5 to 50% by weight, relative to the total weight of the composition. When the composition of the invention is a solution or an oily gel, the fatty phase may represent more than 90% of the total weight of the composition.
Les huiles utilisées dans la composition selon l'invention sont choisies parmi celles classiquement utilisées dans le domaine cosmétique et/ou dermatologique. Comme matières grasses utilisables dans l'invention, on peut citer, outre les acides gras insaturés, les huiles minérales comme par exemple le polyisobutène hydrogéné et l'huile de vaseline, les huiles végétales comme par exemple une fraction liquide du beurre de karité, l'huile de tournesol, d'amande et d'abricot, les huiles animales comme par exemple le perhydrosqualène, les huiles de synthèse notamment l'huile de purcellin, le myristate d'isopropyle et le palmitate d'éthylhexyle, et les huiles fluorées comme par exemple les perfiuoropolyéthers. The oils used in the composition according to the invention are chosen from those conventionally used in the cosmetic and / or dermatological field. As fats usable in the invention include, in addition to unsaturated fatty acids, mineral oils such as hydrogenated polyisobutene and petrolatum oil, vegetable oils such as a liquid fraction of shea butter, sunflower oil, almond and apricot oil, animal oils such as perhydrosqualene, synthetic oils including purcellin oil, isopropyl myristate and ethylhexyl palmitate, and fluorinated oils such as for example perfluoropolyethers.
On peut aussi utiliser des alcools gras, des acides gras comme par exemple l'acide stéarique et des cires notamment de paraffine, carnauba et la cire d'abeille. It is also possible to use fatty alcohols, fatty acids such as, for example, stearic acid and waxes, especially paraffin, carnauba and beeswax.
On peut aussi utiliser des composés siliconés comme les huiles siliconées et par exemple les cyclométhicones et diméthicones, les cires, les résines et les gommes siliconées. It is also possible to use silicone compounds such as silicone oils and, for example, cyclomethicones and dimethicones, waxes, resins and silicone gums.
Emulsionnants emulsifiers
La composition selon l'invention, lorsqu'elle se présente sous forme d'émulsion, peut également comprendre un ou plusieurs émulsionnants et/ou co-émulsionnants. The composition according to the invention, when it is in the form of an emulsion, may also comprise one or more emulsifiers and / or co-emulsifiers.
Les émulsionnants et les co-émulsionnants utilisés dans la composition sont choisis parmi ceux classiquement utilisés dans le domaine cosmétique et/ou dermatologique. The emulsifiers and co-emulsifiers used in the composition are chosen from those conventionally used in the cosmetic and / or dermatological field.
Comme émulsionnant utilisable dans l'invention, on peut citer par exemple le stéarate de glycérol, le polysorbate 60, le mélange alcool cétylstéarylique/alcool cétylstéaryliqueoxyéthyléné à 33 moles d'oxyde d'éthylène vendu sous la dénomination Sinnowax AO® par la société HENKEL, le mélange de PEG-6/PEG-32/Glycol Stéarate vendu sous la dénomination de Tefose® 63 par société GATTEFOSSE, le PPG-3 myristyl éther, les émulsionnants siliconés tels que le cétyldiméthicone copolyol et le mono- ou tristéarate de sorbitane, le stéarate de PEG-40, le monostéarate de sorbitane oxyéthyléné (20OE). La teneur totale en émulsionnants et co-émulsionnants peut notamment aller de 0,3 à 30 % en poids, et de préférence de 0,5 à 20 % en poids, par rapport au poids total de la composition. As emulsifier that can be used in the invention, mention may be made, for example, of glycerol stearate, polysorbate 60, cetylstearyl alcohol / cetylstearyloxyethylene mixture with 33 moles of ethylene oxide sold under the name Sinnowax AO® by HENKEL, the mixture of PEG-6 / PEG-32 / glycol stearate sold under the name Tefose® 63 by Gattefosse, PPG-3 myristyl ether, silicone emulsifiers such as cetyldimethicone copolyol and sorbitan mono- or tristearate, PEG-40 stearate, oxyethylenated sorbitan monostearate (20OE). The total content of emulsifiers and co-emulsifiers may especially range from 0.3 to 30% by weight, and preferably from 0.5 to 20% by weight, relative to the total weight of the composition.
Gélifiants La composition selon l'invention peut également comprendre des agents gélifiants. Gelling agents The composition according to the invention may also comprise gelling agents.
Comme gélifiants hydrophiles, on peut citer les polymères carboxyliques tels que les carbomers, les copolymères acryliques tels que les copolymères d'acrylates/alkylacrylates, les polyacrylamides et notamment le mélange de polyacrylamide, C13-14-Isoparaffine et Laureth-7 vendu sous le nom de Sepigel 305® par la société SEPPIC, les polysaccharides comme les dérivés cellulosiques tels que les hydroxyalkylcelluloses et en particulier, les hydroxypropylcellulose et hydroxyéthylcellulose, les gommes naturelles telles que le guar, la caroube, la gomme de xanthane et les argiles. As hydrophilic gelling agents, mention may be made of carboxylic polymers such as carbomers, acrylic copolymers such as copolymers of acrylates / alkyl acrylates, polyacrylamides and especially the mixture of polyacrylamide, C13-14-Isoparaffin and Laureth-7 sold under the name Sepigel 305® by the company SEPPIC, polysaccharides such as cellulose derivatives such as hydroxyalkylcelluloses and in particular hydroxypropylcellulose and hydroxyethylcellulose, natural gums such as guar, carob, xanthan gum and clays.
Comme gélifiants lipophiles, on peut citer les argiles modifiées comme les bentones, les sels métalliques d'acides gras comme les stéarates d'aluminium et la silice hydrophobe, ou encore l'éthylcellulose et le polyéthylène. As lipophilic gelling agents, mention may be made of modified clays such as bentones, metal salts of fatty acids such as aluminum stearates and hydrophobic silica, or else ethylcellulose and polyethylene.
Adjuvants admixtures
La composition cosmétique et/ou dermatologique de l'invention peut contenir également des adjuvants habituels dans le domaine cosmétique, pharmaceutique et/ou dermatologique, tels que les conservateurs, les antioxydants, les solvants, les parfums, les charges, les absorbeurs d'odeur et les matières colorantes. Ces adjuvants, selon leur nature, peuvent être introduits dans la phase grasse et/ou dans la phase aqueuse de la composition. The cosmetic and / or dermatological composition of the invention may also contain adjuvants which are customary in the cosmetic, pharmaceutical and / or dermatological field, such as preservatives, antioxidants, solvents, perfumes, fillers, odor absorbers and dyestuffs. These adjuvants, depending on their nature, can be introduced into the fatty phase and / or into the aqueous phase of the composition.
Les quantités de ces différents adjuvants sont celles classiquement utilisées dans le domaine considéré, et par exemple de 0,01 à 20 % du poids total de la composition. The amounts of these various adjuvants are those conventionally used in the field under consideration, and for example from 0.01 to 20% of the total weight of the composition.
Film Selon un mode préféré de réalisation de l'invention, la composition se présente sous la forme d'un film, de préférence un film polymérique hydrosoluble de type filmogel®. Film According to a preferred embodiment of the invention, the composition is in the form of a film, preferably a water-soluble polymeric film film type filmogel®.
Par "film", on entend selon la présente invention, un film solide et fin. On entend par "fin", un solide ayant une épaisseur d'au maximum 1000 μιη By "film" is meant according to the present invention, a solid and thin film. By "end" is meant a solid having a thickness of at most 1000 μιη
Ce film est préhensible, c'est-à-dire qu'il a généralement une dimension adéquate pour pouvoir être facilement manipulé par l'utilisateur. Il peut avoir une forme de carré, de rectangle, de disque ou toute autre forme. Un film a généralement une épaisseur de 10 μιη à 1000 μιη, de préférence de 20 à 500 μηι et mieux de 50 à 300 μη . This film is prehensible, that is to say, it is generally of adequate size to be easily manipulated by the user. It can have a shape of square, rectangle, disk or any other form. A film generally has a thickness of 10 μιη to 1000 μιη, preferably from 20 to 500 μηι and better still from 50 to 300 μη.
On entend par "film hydrosoluble" au sens de la présente invention, un film qui se dissout dans l'eau. Il s'agit d'un film constitué d'un ou de plusieurs polymères hydrosolubles ou hydrodispersibles, c'est-à-dire des polymères ayant une solubilité dans l'eau mesurée à 25°C au moins égale à 0,1 g/L (obtention d'une solution macroscopiquement isotrope et transparente, colorée ou non). Cette solubilité est de préférence supérieure ou égale à 1 g/L. The term "water-soluble film" in the sense of the present invention, a film that dissolves in water. It is a film consisting of one or more water-soluble or water-dispersible polymers, that is to say polymers having a solubility in water measured at 25 ° C. of at least 0.1 g / Obtaining a macroscopically isotropic and transparent solution, colored or not). This solubility is preferably greater than or equal to 1 g / L.
Le film selon l'invention est de préférence un "film anhydre", c'est-à-dire un film comprenant une teneur en eau inférieure à 15 % en poids, de préférence inférieure à 10 % en poids et plus préférentiellement inférieure à 5 % en poids, par rapport au poids total du film. De préférence encore, film selon l'invention est exempt d'eau. Les polymères pouvant être utilisés pour constituer ces films peuvent être d'origine synthétique ou naturelle, et, le cas échéant, modifiés par réactions chimiques. Ils peuvent être filmogènes ou non filmogènes. Ils sont avantageusement filmogènes. The film according to the invention is preferably an "anhydrous film", that is to say a film comprising a water content of less than 15% by weight, preferably less than 10% by weight and more preferably less than 5% by weight. % by weight, based on the total weight of the film. More preferably, the film according to the invention is free of water. The polymers that can be used to form these films can be of synthetic or natural origin, and, where appropriate, modified by chemical reactions. They can be film-forming or non-film-forming. They are advantageously film-forming.
Ces polymères doivent être physiologiquement acceptables c'est-à-dire compatible avec la peau, les muqueuses, les cheveux et le cuir chevelu. La composition sous forme de film comprend notamment au moins un polymère filmogène. These polymers must be physiologically acceptable, that is to say compatible with the skin, the mucous membranes, the hair and the scalp. The composition in the form of a film comprises in particular at least one film-forming polymer.
Par "polymère filmogène", on entend un polymère apte à former à lui seul ou en présence d'un agent auxiliaire de filmification, un film continu, et de préférence un film dont la cohésion et les propriétés mécaniques sont telles que ledit film peut être isolé d'un support. Ces polymères sont catalogués sous la rubrique "Film Formers" dans le dictionnaire cosmétique "International Cosmetic Ingrédient Dictionary and Handbook" (Voir par exemple pages 2903 à 2906 de la neuvième édition - 2002). "Film-forming polymer" means a polymer capable of forming, by itself or in the presence of an auxiliary film-forming agent, a continuous film, and preferably a film whose cohesion and mechanical properties are such that said film may be isolated from a support. These polymers are cataloged under the heading "Film Formers" in the cosmetic dictionary "International Cosmetic Ingredient Dictionary and Handbook" (see for example pages 2903-2906 of the ninth edition - 2002).
Les polymères filmogènes peuvent être choisis par exemple parmi : - les polymères vinyliques tels que l'acétate de polyvinyle, les polyvinylpyrrolidones, les copolymères du méthylvinyléther et de l'anhydride maléique, le copolymère de l'acétate de vinyle et de l'acide crotonique, les copolymères de la vinylpyrrolidone et de l'acétate de vinyle, les copolymères de la vinylpyrrolidone et du caprolactame, les alcools polyvinyliques. De manière préférée, le polymère vinylique est l'acétate de polyvinyle (PVA), qui est notamment préparé par polymérisation radicalaire du monomère acétate de vinyle puis hydrolyse. On peut utiliser notamment l'acétate de polyvinyle hydrolysé à 88 %, tel que celui vendu sous la dénomination CELVOL 540 PV ALCOHOL par la société Celanese Chemicals ; - les dérivés cellulosiques fïlmogènes, comme l'hydroxyéthylcellulose, l'hydroxypropylcellulose, l'hydroxypropylméthylcellulose, la méthylcellulose, l'éthylhydroxyéthylcellulose, la carboxyméthylcellulose, et les dérivés quatemisés de la cellulose. De manière préférée, les dérivés cellulosiques sont choisis parmi l'hydroxypropylcellulose (HPC) et l'hydroxypropylméthylcellulose (HPMC). Ces polymères sont solubles dans l'eau ainsi que dans des solvants organiques. Ceci permet d'accroître le champ de solubilité des films les contenant. Le choix du poids moléculaire de ces polymères cellulosiques doit être fait de manière judicieuse pour augmenter la dissolution des films.Les HPC utilisés de façon préférée sont ceux commercialisées par la société Hercules sous la dénomination - KlucelO MF dont le poids moléculaire est 850 000 (viscosité 4000-6500 mPa à 2 % dans l'eau) - KlucelO EF dont le poids moléculaire est 80 000 (viscosité 300-600 mPa à 10 % dans l'eau). L'HPMC utilisée de façon préférée est l'hydroxypropylméthylcellulose de viscosité 40-60 cps (40-60 mPa.) à 2 % dans l'eau à 20 °C, commercialisée par la société Sigma-Aldrich. The film-forming polymers may be chosen for example from: vinyl polymers such as polyvinyl acetate, polyvinylpyrrolidones, copolymers of methyl vinyl ether and maleic anhydride, copolymer of vinyl acetate and crotonic acid, copolymers of vinylpyrrolidone and polyvinylpyrrolidone; vinyl acetate, copolymers of vinylpyrrolidone and caprolactam, polyvinyl alcohols. Preferably, the vinyl polymer is polyvinyl acetate (PVA), which is especially prepared by radical polymerization of the vinyl acetate monomer and then hydrolyzed. In particular, it is possible to use 88% hydrolyzed polyvinyl acetate, such as that sold under the name CELVOL 540 PV ALCOHOL by the company Celanese Chemicals; cellulosic cellulosic derivatives, such as hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, methylcellulose, ethylhydroxyethylcellulose, carboxymethylcellulose, and the quatemized derivatives of cellulose. Preferably, the cellulose derivatives are chosen from hydroxypropylcellulose (HPC) and hydroxypropylmethylcellulose (HPMC). These polymers are soluble in water as well as in organic solvents. This makes it possible to increase the solubility field of the films containing them. The choice of the molecular weight of these cellulosic polymers must be done judiciously to increase the dissolution of the films. The HPCs used in a preferred manner are those sold by the company Hercules under the name KlucelO MF whose molecular weight is 850,000 (viscosity 4000-6500 mPa at 2% in water) - KlucelO EF whose molecular weight is 80,000 (viscosity 300-600 mPa at 10% in water). The HPMC preferably used is hydroxypropyl methylcellulose of viscosity 40-60 cps (40-60 mPa) at 2% in water at 20 ° C, sold by Sigma-Aldrich.
- les amidons et leurs dérivés ; - les polymères d'origine naturelle, éventuellement modifiés, tels que le pullulane, la pectine, la mannane, les galactomannanes, les glucomannanes et leurs dérivés, la gomme arabique, la gomme de guar, la gomme de xanthane, la gomme de karaya, les alginates, les carraghénanes, les ulvanes et autres colloïdes algaux, l'acide hyaluronique et ses dérivés, la gomme laque, la gomme sandaraque, les dammars, l'élémis, les copals, l'acide désoxyribonucléique, les mucopolysaccharides tels que l'acide hyaluronique, le sulfate de chondroïtine ; - les polymères dérivant de la chitine ou du chitosane, anioniques, cationiques, amphotères ou non ioniques ; starches and their derivatives; polymers of natural origin, optionally modified, such as pullulan, pectin, mannan, galactomannans, glucomannans and their derivatives, gum arabic, guar gum, xanthan gum, karaya gum, alginates, carrageenans, ulvans and other algal colloids, hyaluronic acid and its derivatives, shellac, sandaraque gum, dammars, elemis, copals, deoxyribonucleic acid, mucopolysaccharides such as hyaluronic acid, chondroitin sulfate; polymers derived from chitin or chitosan, anionic, cationic, amphoteric or nonionic;
- les polymères protéiques, tels que les protéines de blé ou de soja ; la kératine et ses dérivés, par exemple les hydrolysats de kératine et les kératines sulfoniques, la caséine, l'albumine, le collagène, la gluteline, le glucagon, le gluten, la zéine, les gélatines et leurs dérivés ; protein polymers, such as wheat or soy proteins; keratin and its derivatives, for example keratin hydrolysates and keratin sulfones, casein, albumin, collagen, glutelin, glucagon, gluten, zein, gelatins and their derivatives;
- les copolymères acryliques de phosphoryle choline, tels que le poly-2- (methacryloyloxyethyl) phosphorylcholine commercialisé sous la dénomination Lipidure HM par la société NOF Corporation (nom INCI : Polyphosphorylcholine glycol acrylate) ; acrylic phosphorylcholine copolymers, such as poly-2- (methacryloyloxyethyl) phosphorylcholine sold under the name Lipidure HM by the company NOF Corporation (INCI name: Polyphosphorylcholine glycol acrylate);
- les complexes anion-cation de type gomme arabique / gélatine ou gomme arabique /chitosane, ou collagène / GlycosAminoGlycane ; et les mélanges de ces polymères. anion-cation complexes of gum arabic / gelatin or gum arabic / chitosan or collagen / glycosaminoglycane type; and mixtures of these polymers.
Selon un mode préféré de réalisation de l'invention, le polymère filmogène est choisi parmi les polymères vinyliques, les dérivés cellulosiques et leurs mélanges. According to a preferred embodiment of the invention, the film-forming polymer is chosen from vinyl polymers, cellulose derivatives and mixtures thereof.
De manière préférée, le polymère filmogène est choisi parmi l'acétate de polyvinyle, l'hydroxypropylcellulose, l'hydroxypropylméthylcellulose, et leurs mélanges, les polyurethanes, les nitrocelluloses, et les carbomers. Preferably, the film-forming polymer is chosen from polyvinyl acetate, hydroxypropylcellulose, hydroxypropylmethylcellulose, and mixtures thereof, polyurethanes, nitrocellulose, and carbomers.
En particulier, la composition selon l'invention comprend un ou plusieurs polymère(s) filmogène(s) en une teneur allant de 10 à 95 % en poids, de préférence de 20 à 70 % en poids, et plus préférentiellement de 30 à 60% en poids, par rapport total du film. In particular, the composition according to the invention comprises one or more film-forming polymer (s) in a content ranging from 10 to 95% by weight, preferably from 20 to 70% by weight, and more preferably from 30 to 60% by weight. % by weight, based on the total film ratio.
Lorsqu'elle se présente sous forme de film anhydre, la composition selon l'invention peut comprendre au moins un solvant organique qui peut être choisi parmi : When it is in the form of an anhydrous film, the composition according to the invention may comprise at least one organic solvent which may be chosen from:
- les cétones telles que la méthyléthylcétone, la méthylisobutylcétone, la diisobutylcétone, l'isophorone, la cyclohexanone, l'acétone; ketones such as methyl ethyl ketone, methyl isobutyl ketone, diisobutyl ketone, isophorone, cyclohexanone, acetone;
-les alcools liquides à température ambiante tels que l'éthanol, l'isopropanol, le diacétone alcool, le 2-butoxyéthanol, le cyclohexanol, le n-propanol, le n-butanol ; les éthers de propylène glycol liquides à température ambiante tels que le monométhyléther de propylène glycol, l'acétate de monométhyl éther de propylène glycol, le mono n-butyl éther de dipropylène glycol ; alcohols that are liquid at room temperature, such as ethanol, isopropanol, diacetone alcohol, 2-butoxyethanol, cyclohexanol, n-propanol, n-butanol; propylene glycol ethers which are liquid at room temperature, such as propylene glycol monomethyl ether, propylene glycol monomethyl ether acetate, dipropylene glycol mono-butyl ether;
- les glycols tels que l'éthylène glycol, le propylène glycol, le pentylène glycol, le glycérol  glycols such as ethylene glycol, propylene glycol, pentylene glycol, glycerol
- les éthers cycliques tels que la γ-butyrolactone ;  cyclic ethers such as γ-butyrolactone;
- les esters à chaîne courte (ayant de 3 à 8 atomes de carbone au total) tels l'acétate d'éthyle, l'acétate de butyle, l'acétate de méthyle, l'acétate de propyle, l'acétate d'isopropyle, l'acétate d'isopentyle, l'acétate de méthoxypropyle, le lactate de butyle ;  short-chain esters (having from 3 to 8 carbon atoms in total) such as ethyl acetate, butyl acetate, methyl acetate, propyl acetate, isopropyl acetate isopentyl acetate, methoxypropyl acetate, butyl lactate;
- les éthers tels que le diéthyléther, le diméthyléther ou le dichlorodiéthyléther ; -les alcanes liquides à température ambiante tels que le décane, l'heptane, le dodécane, le cyclohexane ;  ethers such as diethyl ether, dimethyl ether or dichlorodiethyl ether; alkanes which are liquid at ambient temperature, such as decane, heptane, dodecane or cyclohexane;
- les alkyl sulfoxides tels que le diméthylsulfoxide ;  alkyl sulphoxides such as dimethyl sulphoxide;
- les aldéhydes liquides à température ambiante tels que le benzaldéhyde, l'acétaldéhyde;  aldehydes that are liquid at room temperature, such as benzaldehyde or acetaldehyde;
- le 3-éthoxypropionate d'éthyle ;  ethyl 3-ethoxypropionate;
- les carbonates tels que le carbonate de propylène, le carbonate de diméthyle, carbonates, such as propylene carbonate and dimethyl carbonate,
- les acétals tels que le méthylal ; acetals such as methylal;
et leurs mélanges. and their mixtures.
Selon un mode préféré de réalisation, le solvant organique est volatil. Par " solvant organique volatil", on entend un solvant organique susceptible de s'évaporer au contact de la peau en moins d'une heure, à température ambiante et pression atmosphérique. Le solvant organique volatil est liquide à température ambiante, présente notamment une pression de vapeur non nulle à température ambiante et pression atmosphérique, en particulier il présente une pression de vapeur allant de 0,13 Pa à 40 000 Pa (10<-3> à 300 mm de Hg), et de préférence allant de 1,3 Pa à 8000 Pa (0,01 à 60 mm de Hg). According to a preferred embodiment, the organic solvent is volatile. By "volatile organic solvent" is meant an organic solvent capable of evaporating on contact with the skin in less than one hour, at room temperature and atmospheric pressure. The volatile organic solvent is liquid at ambient temperature, in particular having a non-zero vapor pressure at ambient temperature and atmospheric pressure, in particular it has a vapor pressure ranging from 0.13 Pa to 40 000 Pa (10 -3 300 mm Hg), and preferably ranging from 1.3 Pa to 8000 Pa (0.01 to 60 mm Hg).
Selon un mode particulièrement préféré de réalisation, le solvant organique est choisi parmi les alcools liquides à température ambiante tels que l'éthanol, l'isopropanol, le diacétone alcool, le 2-butoxyéthanol, le cyclohexanol et leurs mélanges, et de préférence l'éthanol et/ou les esters à chaîne courte (ayant de 3 à 8 atomes de carbone au total) tels l'acétate d'éthyle, l'acétate de butyle, l'acétate de méthyle, l'acétate de propyle, l'acétate d'isopropyle, l'acétate d'isopentyle, l'acétate de méthoxypropyle, le lactate de butyle. Selon un mode plus préféré de réalisation, le solvant organique utilisé dans les compositions selon l'invention est choisi parmi l'éthanol, l'acétate d'éthyle ou un mélange de ceux-ci. According to a particularly preferred embodiment, the organic solvent is chosen from alcohols which are liquid at room temperature, such as ethanol, isopropanol, diacetone alcohol, 2-butoxyethanol and cyclohexanol, and mixtures thereof, and preferably ethanol and / or short chain esters (having 3 to 8 carbon atoms in total) such as ethyl acetate, butyl acetate, methyl acetate, propyl acetate, acetate isopropyl, isopentyl acetate, methoxypropyl acetate, butyl lactate. According to a more preferred embodiment, the organic solvent used in the compositions according to the invention is chosen from ethanol, ethyl acetate or a mixture of these.
Le solvant organique peut représenter de 60 à 95% en poids, de préférence de 65 à 85% en poids, et de préférence de 65 à 80% en poids, par rapport au poids total de la composition. The organic solvent may represent from 60 to 95% by weight, preferably from 65 to 85% by weight, and preferably from 65 to 80% by weight, relative to the total weight of the composition.
On peut également utiliser dans la composition de l'invention, un polymère qui soit à la fois un polymère fîlmogène et un polymère épaississant, choisi par exemple parmi les dérivés cellulosiques et les polymères d'origine naturelle qui peuvent être à la fois filmogènes et épaississants. Selon un mode de réalisation particulier, la composition selon l'invention, lorsqu'elle se présente sous la forme d'un film, comprend, outre le polymère fîlmogène, au moins un agent épaississant polysaccharidique. It is also possible to use in the composition of the invention a polymer which is both a film-forming polymer and a thickening polymer, chosen, for example, from cellulose derivatives and polymers of natural origin which can be both film-forming and thickening agents. . According to one particular embodiment, the composition according to the invention, when it is in the form of a film, comprises, in addition to the polymeric polymer, at least one polysaccharide thickening agent.
Les agents épaississants polysaccharidiques utilisés dans le film selon l'invention peuvent être choisis parmi les polysaccharides à pouvoir gélifiant. On définit par "pouvoir gélifiant" le fait qu'à une concentration supérieure ou égale à 0,5The polysaccharide thickening agents used in the film according to the invention may be chosen from polysaccharides with gelling power. "Gelling power" defines the fact that at a concentration greater than or equal to 0.5
% en poids dans l'eau, la viscosité des solutions ainsi obtenues est supérieure ou égale à 0,01 Pa.s pour un taux de cisaillement égale à 1 les mesures étant réalisées à 25 °C à l'aide d'un rhéomètre RheoStress R5150 de Haake en configuration cône - plan, les mensurations du cône de mesure étant les suivantes : diamètre : 60 mm et angle : 2°. Les agents épaississants polysaccharidiques peuvent être choisis notamment parmi la gomme arabique, la gomme de ghatti, la gomme de karaya, la gomme de caroube, la gomme de guar, la gomme de tamarin, la gomme de xanthane, la gellane, les pectines, le tragacanth, l'agar, les alginates, le carrageenan, le furcelleran, le konjac et les dérivés de cellulose, et leurs mélanges. Selon un mode préféré de réalisation de l'invention, les agents épaississants polysaccharidiques sont choisis parmi les carraghénanes qui sont des polysaccharides linéaires extraits de certaines algues rouges de la famille des Rhodophycée. Ils sont constitués de résidus 1,3-1,3 et a- 1,4 galactoses en alternance, de nombreux résidus galactoses pouvant être sulfatés. Il existe trois types de carraghénanes, appelés Kappacarraghénane, Iota-carraghénane et Lambda-carraghénane. Cette famille de polysaccharides est décrite par exemple dans le chapitre 3 du livre " Food Gels " édité par Peter HARRIS, Elsevier 1989. On peut en particulier utiliser le carraghénane vendu sous la dénomination SATIAGUM UTC 10 par la société Degussa. % by weight in water, the viscosity of the solutions thus obtained is greater than or equal to 0.01 Pa.s at a shear rate equal to 1, the measurements being carried out at 25 ° C. using a RheoStress rheometer R5150 of Haake in cone-plane configuration, the measurements of the measuring cone being as follows: diameter: 60 mm and angle: 2 °. The polysaccharide thickening agents may be chosen in particular from gum arabic, ghatti gum, karaya gum, locust bean gum, guar gum, tamarind gum, xanthan gum, gellan, pectins, tragacanth, agar, alginates, carrageenan, furcelleran, konjac and cellulose derivatives, and mixtures thereof. According to a preferred embodiment of the invention, the polysaccharide thickening agents are chosen from carrageenans which are linear polysaccharides extracted from certain red algae of the family Rhodophyceae. They consist of residues 1,3-1,3 and α-1,4 galactoses alternately, many galactose residues can be sulfated. There are three types of carrageenans, called kappacarraghenan, Iota-carrageenan and Lambda-carrageenan. This family of polysaccharides is described for example in Chapter 3 of the book "Food Gels" edited by Peter HARRIS, Elsevier 1989. It is possible in particular to use the carrageenan sold under the name SATIAGUM UTC 10 by the company Degussa.
La quantité d'agent(s) épaississant(s) dans la composition selon l'invention peut aller par exemple de 0,5 à 40 % en poids, en particulier de 1 à 20 % en poids, et plus particulièrement de 5 à 10 % en poids par rapport à son poids total. The amount of thickening agent (s) in the composition according to the invention may range, for example, from 0.5 to 40% by weight, in particular from 1 to 20% by weight, and more particularly from 5 to 10% by weight. % by weight relative to its total weight.
En outre, selon un mode de réalisation avantageux, la composition se présentant sous la forme d'un film peut incorporer, en association avec le polymère tel que défini ci-dessus, au moins un dérivé polydiméthylsiloxane oxyalkyléné. In addition, according to an advantageous embodiment, the composition in the form of a film may incorporate, in combination with the polymer as defined above, at least one oxyalkylenated polydimethylsiloxane derivative.
Comme décrit dans le document FR0653343 un tel dérivé a pour intérêt d'accroître significativement la cinétique de dissolution du film hydrosoluble l'incorporant. As described in document FR0653343, such a derivative has the advantage of significantly increasing the dissolution kinetics of the water-soluble film incorporating it.
Les polydiméthylsiloxanes (PDMS) oxyalkylénés utilisés selon l'invention sont hydrosolubles ou hydrodispersibles. The oxyalkylenated polydimethylsiloxanes (PDMS) used according to the invention are water-soluble or water-dispersible.
On entend par " hydrosolubles ou hydrodispersibles " des PDMS ayant une solubilité dans l'eau mesurée à 25 °C au moins égale à 0,1 g L (obtention d'une solution macroscopiquement isotrope et transparente, colorée ou non). Cette solubilité est de préférence supérieure ou égale à 1 g/1. Ces PDMS sont choisis de préférence parmi les silicones hydrosolubles comportant au moins un groupement polyoxyalkyléné monovalent terminal ou pendant, et qui, introduits à 0,05 % en poids dans une solution aqueuse, sont susceptibles de réduire la tension superficielle de l'eau à une valeur inférieure à 35 mN/m, et de préférence inférieure à 30 mN/m. De tels PDMS oxyalkylénés sont par exemple vendus par la société OSI sous les dénominations commerciales Silwet, Silwet 1614, et Tegowet. The term "water-soluble or water-dispersible" means PDMS having a solubility in water measured at 25 ° C at least equal to 0.1 g L (obtaining a macroscopically isotropic solution and transparent, colored or not). This solubility is preferably greater than or equal to 1 g / l. These PDMSs are preferably chosen from water-soluble silicones containing at least one terminal or pendant monovalent polyoxyalkylene group and which, introduced at 0.05% by weight in an aqueous solution, are capable of reducing the surface tension of the water to a minimum. value less than 35 mN / m, and preferably less than 30 mN / m. Such oxyalkylenated PDMS are for example sold by the company OSI under the trade names Silwet, Silwet 1614, and Tegowet.
Selon un mode particulièrement préféré de réalisation, la composition selon l'invention se présente sous la forme d'un film anhydre hydrosoluble comportant (i) au moins un oligosaccharide polysulfaté synthétique, (ii) au moins un polymère filmogène hydrosoluble ou hydrodispersible et (iii) au moins un dérivé polydiméthylsiloxane oxyalkyléné. According to a particularly preferred embodiment, the composition according to the invention is in the form of a water-soluble anhydrous film comprising (i) at least one synthetic polysulfated oligosaccharide, (ii) at least one water-soluble or water-dispersible film-forming polymer and (iii) at least one oxyalkylenated polydimethylsiloxane derivative.
La composition selon l'invention, notamment lorsqu'elle se présente sous la forme d'un film, peut comprendre en outre un ou plusieurs plastifiants choisis par exemple parmi l'huile de ricin, ou les polyols tels que la glycérine, le sorbitol, les mono- et/ou di-saccharides, le dipropylène glycol, le butylène glycol, le pentylène glycol, les polyéthylènes glycols tels que le PEG-400. The composition according to the invention, in particular when it is in the form of a film, may further comprise one or more plasticizers chosen for example from castor oil, or polyols such as glycerin, sorbitol, mono- and / or di-saccharides, dipropylene glycol, butylene glycol, pentylene glycol, polyethylene glycols such as PEG-400.
La quantité de plastifiant(s) peut aller par exemple de 1 à 40 % en poids et mieux de 2 à 15 % en poids par rapport au poids total de la composition. The amount of plasticizer (s) may range, for example, from 1 to 40% by weight and better still from 2 to 15% by weight relative to the total weight of the composition.
Compositions selon l'invention Compositions according to the invention
Selon un mode préféré de réalisation, la composition selon l'invention se présente sous la forme d'une émulsion huile-dans-eau, de préférence sous forme de crème, comprenant : According to a preferred embodiment, the composition according to the invention is in the form of an oil-in-water emulsion, preferably in cream form, comprising:
- 0,1 à 5% de sel de potassium du sucrose octasulfate KSOS 0.1 to 5% potassium salt of sucrose octasulfate KSOS
- 40 à 60% en poids d'eau, 40 to 60% by weight of water,
- 20 à 40% en poids d'au moins une huile, 20 to 40% by weight of at least one oil,
- 1 à 10% en poids d'au moins un tensioactif, 1 to 10% by weight of at least one surfactant,
- 0 à 10% en poids d'au moins une cire, 0 to 10% by weight of at least one wax,
- 0 à 20% en poids d'une autre substance active, 0 to 20% by weight of another active substance,
- 0 à 2% en poids de conservateurs, 0 to 2% by weight of preservatives,
- 0 à 5% en poids d'épaississants. 0 to 5% by weight of thickeners.
Selon un autre mode de réalisation, la composition selon l'invention se présente sous la forme d'une émulsion huile-dans-eau, de préférence sous forme de crème, comprenant : According to another embodiment, the composition according to the invention is in the form of an oil-in-water emulsion, preferably in cream form, comprising:
- 0,1 à 5% de sel de potassium de sucrose octasulfate (= KSOS) 0.1 to 5% potassium salt of sucrose octasulfate (= KSOS)
- 0.1 à 5% de sel d'aluminium de sucrose octasulfate (sucralfate) 0.1 to 5% sucrose octasulfate aluminum salt (sucralfate)
- 40 à 60% en poids d'eau, 40 to 60% by weight of water,
- 20 à 40% en poids d'au moins une huile, 20 to 40% by weight of at least one oil,
- 1 à 10% en poids d'au moins un tensioactif, - 0 à 10% en poids d'au moins une cire, 1 to 10% by weight of at least one surfactant, 0 to 10% by weight of at least one wax,
- 0 à 20% en poids d'une autre substance active, 0 to 20% by weight of another active substance,
- 0 à 2% en poids de conservateurs, 0 to 2% by weight of preservatives,
- 0 à 5% en poids d'épaississants. 0 to 5% by weight of thickeners.
Selon un autre mode de réalisation, la composition selon l'invention se présente sous la forme d'une émulsion huile-dans-eau, de préférence sous forme de crème, comprenant : According to another embodiment, the composition according to the invention is in the form of an oil-in-water emulsion, preferably in cream form, comprising:
- 0,1 à 5% de sel de potassium de sucrose octasulfate (= KSOS) 0.1 to 5% potassium salt of sucrose octasulfate (= KSOS)
- 0.1 à 5% de sel d'aluminium de sucrose octasulfate (= sucralfate) 0.1 to 5% sucrose octasulfate aluminum salt (= sucralfate)
- 0.1 à 5% d'acide hyaluronique 0.1 to 5% hyaluronic acid
- 40 à 60% en poids d'eau, 40 to 60% by weight of water,
- 20 à 40% en poids d'au moins une huile, 20 to 40% by weight of at least one oil,
- 1 à 10% en poids d'au moins un tensioactif, 1 to 10% by weight of at least one surfactant,
- 0 à 10% en poids d'au moins une cire, 0 to 10% by weight of at least one wax,
- 0 à 20% en poids d'une autre substance active, 0 to 20% by weight of another active substance,
- 0 à 2% en poids de conservateurs, 0 to 2% by weight of preservatives,
- 0 à 5% en poids d'épaississants. 0 to 5% by weight of thickeners.
Selon un autre mode de réalisation, la composition selon l'invention se présente sous la forme d'une émulsion huile-dans-eau, de préférence sous forme de crème, comprenant : According to another embodiment, the composition according to the invention is in the form of an oil-in-water emulsion, preferably in cream form, comprising:
- 0,1 à 5% de sel de potassium de sucrose octasulfate (= KSOS) 0.1 to 5% potassium salt of sucrose octasulfate (= KSOS)
- 0.1 à 5% de sel d'aluminium de sucrose octasulfate (= sucralfate) 0.1 to 5% sucrose octasulfate aluminum salt (= sucralfate)
- 0.1 à 5% d'extrait de ruscus - 0.1 to 5% ruscus extract
- 40 à 60%) en poids d'eau, 40 to 60% by weight of water,
- 20 à 40% en poids d'au moins une huile, 20 to 40% by weight of at least one oil,
- 1 à 10% en poids d'au moins un tensioactif, 1 to 10% by weight of at least one surfactant,
- 0 à 10%) en poids d'au moins une cire, 0 to 10% by weight of at least one wax,
- 0 à 20%> en poids d'une autre substance active, - 0 à 2% en poids de conservateurs, 0 to 20% by weight of another active substance, 0 to 2% by weight of preservatives,
- 0 à 5% en poids d'épaississants. 0 to 5% by weight of thickeners.
Selon un autre mode préféré de réalisation, la composition selon l'invention se présente sous la forme d'une composition filmogel à base aqueuse comprenant : According to another preferred embodiment, the composition according to the invention is in the form of a water-based filmogel composition comprising:
- 0,1 à 5% de sel de potassium du sucrose octasulfate KSOS 0.1 to 5% potassium salt of sucrose octasulfate KSOS
- 70 à 99% en poids d'eau, 70 to 99% by weight of water,
- 0 à 10% en poids d'une autre substance active, 0 to 10% by weight of another active substance,
- 0 à 2% en poids de conservateurs, 0 to 2% by weight of preservatives,
- 0 à 5% en poids d'épaississants. 0 to 5% by weight of thickeners.
Selon un encore autre mode préféré de réalisation, la composition selon l'invention se présente sous la forme d'une composition filmogel à base solvant comprenant : According to yet another preferred embodiment, the composition according to the invention is in the form of a solvent-based filmogel composition comprising:
- 0,01 à 5% de sel de potassium du sucrose octasulfate KSOS - 15 à 50% en poids d'éthanol, - 0.01 to 5% of potassium salt of sucrose octasulfate KSOS - 15 to 50% by weight of ethanol,
- 40 à 60% d'acétate d'éthyle, 40 to 60% of ethyl acetate,
- 5 à 20% en poids de polymère filmogène de type nitrocellulose, 5 to 20% by weight of film-forming polymer of the nitrocellulose type,
- 5 à 20% de plastifiant, de préférence l'huile de ricin, 5 to 20% of plasticizer, preferably castor oil,
- 0 à 2% en poids de conservateurs, 0 to 2% by weight of preservatives,
- 0 à 5% en poids d'épaississants. 0 to 5% by weight of thickeners.
Utilisation des compositions de l'invention Use of the compositions of the invention
L'utilisation conforme à l'invention peut être telle que les compositions ou associations définies ci-dessus sont mises en œuvre dans une formulation destinée à un usage topique. The use according to the invention may be such that the compositions or combinations defined above are implemented in a formulation intended for topical use.
En particulier, l'invention a pour objet une composition topique pour traiter thérapeutiquement les hémorroïdes chez un sujet présentant une prédisposition au développement desdites hémorroïdes comprenant, dans un support physiologiquement acceptable, au moins une quantité efficace d'au moins un sel de potassium de sucrose octasulfate synthétique. Selon un autre mode de réalisation, l'invention a pour objet l'utilisation d'une quantité efficace de sel de potassium de sucrose octasulfate en association avec une quantité efficace d'au moins une autre substance active telle que définie supra, pour la fabrication d'une composition dermatologique destinée à traiter et/ou prévenir les hémorroïdes. In particular, the invention relates to a topical composition for therapeutically treating hemorrhoids in a subject having a predisposition to the development of said hemorrhoids comprising, in a physiologically acceptable carrier, at least one effective amount of at least one potassium salt of sucrose synthetic octasulfate. According to another embodiment, the subject of the invention is the use of an effective amount of potassium salt of sucrose octasulfate in combination with an effective amount of at least one other active substance as defined above, for the manufacture of a dermatological composition for treating and / or preventing hemorrhoids.
Les exemples ci-après sont présentés à titre illustratif et non limitatif du domaine de l'invention. The following examples are presented by way of illustration and not limitation of the field of the invention.
EXEMPLES Exemple 1 EXAMPLES Example 1
On a préparé une formulation sous forme de crème (émulsion huile-dans-eau) comprenant un sel de potassium de sucrose octasulfate selon l'invention ayant la composition suivante : A formulation in the form of a cream (oil-in-water emulsion) comprising a potassium salt of sucrose octasulfate according to the invention having the following composition was prepared:
Constituants % Constituents%
Tensioactif huile-dans-eau 5,000 Oil-in-water surfactant 5,000
Cire émulsionnante 2,000 Emulsifying wax 2,000
Acide stéarique 1,000 Stearic acid 1,000
Isononanoate d'isodécyle 6,000 Isodecyl isononanoate 6,000
Huile de silicone (Décaméthyl- 4,000 Silicone oil (Decamethyl- 4,000
Cyclopentasiloxane)  cyclopentasiloxane)
Ester émollient (myristyl lactate) 5,000 Emollient Ester (myristyl lactate) 5,000
Eau déminéralisée 62,100 Demineralized water 62,100
Epaississant 0,300 Thickener 0.300
Glycérine 5,000 Propylène glycol 5,000 Glycerin 5,000 Propylene glycol 5,000
Sel de potassium du sucrose octasulfate (= 0,500 Potassium salt of sucrose octasulfate (= 0.500
KSOS)  KSOS)
Conservateur 1,500 Conservative 1,500
NaOH 10% 0,600 NaOH 10% 0.600
Surfactant siliconé 2,000 Silicone Surfactant 2,000
On a dispersé l'épaississant dans l'eau. On a ajouté la glycérine, le propylène glycol, le KSOS et le conservateur et on a homogénéisé. On a chauffé à 70-75°C. Lorsque le mélange atteint 70-75°C, on a ajusté le taux d'eau puis neutralisé avec la soude à 10%> et on a ramené la température à 70-75°C. The thickener was dispersed in the water. Glycerin, propylene glycol, KSOS and preservative were added and homogenized. It was heated to 70-75 ° C. When the mixture reached 70-75 ° C, the water content was adjusted and then neutralized with 10% sodium hydroxide and the temperature was reduced to 70-75 ° C.
Dans un même temps, on a mélangé le tensioactif huile-dans-eau, la cire émulsionnante, l'acide stéarique, l'isononanoate d'iodécyle, l'huile de silicone (Décaméthyl- Cyclopentasiloxane), l'ester émollient (myristyl lactate) et on a chauffé à 70-75°C. At the same time, the oil-in-water surfactant, the emulsifying wax, the stearic acid, the iodecyl isononanoate, the silicone oil (decamethylcyclopentasiloxane), the emollient ester (myristyl lactate) were mixed together. ) and heated to 70-75 ° C.
Lorsque les 2 mélanges on atteint 70-75°C, on a ajouté le second dans le premier sous vive agitation et on a laissé agiter à chaud pendant 10 minutes. When the two mixtures reached 70-75 ° C, the second was added in the first with vigorous stirring and allowed to stir for 10 minutes.
Puis on a ajouté le surfactant siliconé et on a laissé de nouveau sous agitation à chaud pendant 5 minutes. Then the silicone surfactant was added and heated again for 5 minutes.
Enfin, on a arrêté le chauffage et laissé refroidir à température ambiante, en maintenant une agitation suffisante en fonction de la viscosité du mélange. Le mélange prend un aspect non homogène vers 35°C, mais la crème devient ensuite lisse et brillante. Finally, the heating was stopped and allowed to cool to room temperature, maintaining sufficient agitation depending on the viscosity of the mixture. The mixture takes an inhomogeneous appearance towards 35 ° C, but the cream then becomes smooth and shiny.
Exemple 2 Example 2
On a préparé une formulation sous forme de crème (émulsion huile-dans-eau) comprenant un sel d'aluminium et un sel de potassium de sucrose octasulfate selon l'invention ayant la composition suivante : Constituants % A formulation in cream form (oil-in-water emulsion) comprising an aluminum salt and a potassium salt of sucrose octasulfate according to the invention having the following composition: Constituents%
Tensioactif huile-dans-eau 5,000 Oil-in-water surfactant 5,000
Cire émulsionnante 2,000 Emulsifying wax 2,000
Acide stéarique 1,000 Stearic acid 1,000
Isononanoate d'isodécyle 6,000 Isodecyl isononanoate 6,000
Huile de silicone (Décaméthyl- 4,000 Silicone oil (Decamethyl- 4,000
Cyclopentasiloxane)  cyclopentasiloxane)
Ester émollient (myristyl lactate) 5,000 Emollient Ester (myristyl lactate) 5,000
Eau déminéralisée 61,600 Demineralized water 61,600
Epaississant 0,300 Thickener 0.300
Glycérine 5,000 Glycerin 5,000
Propylène glycol 5,000 Propylene glycol 5,000
Sel de potassium du sucrose octasulfate (= 0,500 Potassium salt of sucrose octasulfate (= 0.500
KSOS)  KSOS)
Sel d'aluminium de sucrose octasulfate (= 0.500 Sucrose octasulfate aluminum salt (= 0.500
sucralfate)  sucralfate)
Conservateur 1 ,500 Conservative 1, 500
NaOH 10% 0,600 NaOH 10% 0.600
Surfactant siliconé 2,000 Silicone Surfactant 2,000
On a dispersé l'épaississant dans l'eau. On a ajouté la glycérine, le propylène glycol, le KSOS, le sucralfate et le conservateur et on a homogénéisé. On a chauffé à 70-75°C. Lorsque le mélange atteint 70-75°C, on a ajusté le taux d'eau puis neutralisé avec la soude à 10% et on a ramené la température à 70-75°C. The thickener was dispersed in the water. Glycerin, propylene glycol, KSOS, sucralfate and preservative were added and homogenized. It was heated to 70-75 ° C. When the mixture reaches 70-75 ° C, the water content is adjusted then neutralized with 10% sodium hydroxide and the temperature is brought to 70-75 ° C.
Dans un même temps, on a mélangé le tensioactif huile-dans-eau, la cire émulsionnante, l'acide stéarique, l'isononanoate d'iodécyle, l'huile de silicone (Décaméthyl- Cyclopentasiloxane), l'ester émollient (myristyl lactate) et on a chauffé à 70-75°C. At the same time, the oil-in-water surfactant, the emulsifying wax, the stearic acid, the iodecyl isononanoate, the silicone oil (decamethylcyclopentasiloxane), the emollient ester (myristyl lactate) were mixed together. ) and heated to 70-75 ° C.
Lorsque les 2 mélanges on atteint 70-75°C, on a ajouté le second dans le premier sous vive agitation et on a laissé agiter à chaud pendant 10 minutes. When the two mixtures reached 70-75 ° C, the second was added in the first with vigorous stirring and allowed to stir for 10 minutes.
Puis on a ajouté le surfactant siliconé et on a laissé de nouveau sous agitation à chaud pendant 5 minutes. Enfin, on a arrêté le chauffage et laissé refroidir à température ambiante, en maintenant une agitation suffisante en fonction de la viscosité du mélange. Le mélange prend un aspect non homogène vers 35°C, mais la crème devient ensuite lisse et brillante. Then the silicone surfactant was added and heated again for 5 minutes. Finally, the heating was stopped and allowed to cool to room temperature, maintaining sufficient agitation depending on the viscosity of the mixture. The mixture takes an inhomogeneous appearance towards 35 ° C, but the cream then becomes smooth and shiny.
Exemple 3 On a préparé une formulation de type filmogel à base solvant comprenant un oligosaccharide polysulfaté synthétique selon l'invention ayant la composition suivante : Example 3 A solvent-based filmogel formulation was prepared comprising a synthetic polysulfated oligosaccharide according to the invention having the following composition:
Constituants % Constituents%
Nitrocellulose 12,800 Nitrocellulose 12,800
Huile de ricin 11,000 Castor oil 11,000
Ethanol absolu 24.90 Ethanol absolute 24.90
Acétate d'éthyle 49.70 Ethyl acetate 49.70
Filtres UV 1,500 UV filters 1,500
Sel de potassium du sucrose Potassium salt of sucrose
0,100  0,100
octasulfate (= KSOS) On a dilué la nitrocellulose dans un mélange acétate d'éthyle éthanol absolu. On a ensuite ajouté l'huile de ricin, les filtres UV et le KSOS jusqu'à dissolution pour obtenir une composition de type filmogel. octasulfate (= KSOS) The nitrocellulose was diluted in ethyl acetate absolute ethanol. Castor oil, UV filters and KSOS were then added until dissolution to obtain a filmogel composition.
Exemple 4 Example 4
On a préparé une formulation de type filmogel à base aqueuse comprenant un oligosaccharide polysulfaté synthétique selon l'invention ayant la composition suivante A water-based filmogel formulation was prepared comprising a synthetic polysulfated oligosaccharide according to the invention having the following composition
Figure imgf000025_0001
On a dispersé l'épaississant dans l'eau sous vive agitation, puis on a ajouté le sorbitol et le dextran en chauffant à 40°C pour obtenir une meilleure solubilité. On a ajouté le KSOS, les parabens et le phénoxyéthanol et laissé agiter pour homogénéiser. On a ensuite laissé refroidir jusqu'à température ambiante en arrêtant le chauffage, en ajustant si besoin la perte en eau. Enfin, on a neutralisé avec la soude et laisser agiter 10 minutes avant l'arrêt de l'agitation.
Figure imgf000025_0001
The thickener was dispersed in water with vigorous stirring, then sorbitol and dextran were added by heating at 40 ° C to obtain better solubility. KSOS, parabens and phenoxyethanol were added and allowed to stir to homogenize. It was then allowed to cool to room temperature by stopping the heating, adjusting the water loss if necessary. Finally, it was neutralized with sodium hydroxide and allowed to stir for 10 minutes before stopping the stirring.

Claims

REVENDICATIONS
1. Composition dermatologique topique comprenant dans un support physiologiquement acceptable, au moins une quantité efficace de sel de potassium d'oligosacchande polysulfaté synthétique ayant 1 à 4 unités d'osés, pour son utilisation dans la prévention et le traitement des hémorroïdes. A topical dermatological composition comprising in a physiologically acceptable carrier at least one effective amount of synthetic polysulfated oligosaccharide potassium salt having 1 to 4 units of oste for use in the prevention and treatment of hemorrhoids.
2. Composition selon la revendication 1, caractérisée en ce que le sel de potassium d'oligosacchande polysulfaté synthétique ayant 1 à 4 unités d'osés est le sel de potassium de sucrose octasulfate.  2. Composition according to claim 1, characterized in that the potassium salt of synthetic polysulfated oligosaccharide having 1 to 4 units of dares is the potassium salt of sucrose octasulfate.
3. Composition selon l'une quelconque des revendications précédentes, caractérisée en ce que ledit sel de potassium d'oligosacchande polysulfaté synthétique ayant 1 à 4 unités d'osés est présent en une teneur comprise entre 0,1 et 50% en poids, par rapport au poids total de la composition.  3. Composition according to any one of the preceding claims, characterized in that said potassium polysulfated oligosaccharide potassium salt having 1 to 4 units of risk is present in a content of between 0.1 and 50% by weight, relative to the total weight of the composition.
4. Composition selon l'une quelconque des revendications précédentes, caractérisée en ce qu'elle comprend une (ou plusieurs) autre(s) substance(s) active(s) choisies parmi les anti-bactériens, les antiseptiques, les antifongiques, les anti-inflammatoires, les actifs favorisant la cicatrisation et/ou la restructuration de la peau, les antiprurigineux, les filtres UV, les agents apaisants, les actifs hydratants, les agents dépigmentants, les agents kératolytiques, les anti-viraux, les anti-douleurs, les anesthésiques, les vitamines, les analgésiques, les veinotoniques, les oligosaccharides polysulfatés ayant 1 à 4 unités d'osés, leurs sels et/ou dérivés, et leurs mélanges.  4. Composition according to any one of the preceding claims, characterized in that it comprises one (or more) other active substance (s) selected from anti-bacterials, antiseptics, antifungals, anti-inflammatory agents, active agents promoting healing and / or restructuring of the skin, antipruritic agents, UV filters, soothing agents, moisturizing agents, depigmenting agents, keratolytic agents, anti-virals, anti-pain agents , anesthetics, vitamins, analgesics, veinotonics, polysulfated oligosaccharides having 1 to 4 units of oste, their salts and / or derivatives, and mixtures thereof.
5. Composition selon la revendication précédente, caractérisée en ce que la substance active est choisie parmi l'acide hyaluronique et/ou le sucralfate.  5. Composition according to the preceding claim, characterized in that the active substance is chosen from hyaluronic acid and / or sucralfate.
6. Composition selon la revendication 4, caractérisée en ce que la substance active est choisie parmi les analgésiques et/ou les veinotoniques.  6. Composition according to claim 4, characterized in that the active substance is selected from analgesics and / or venotonic.
7. Composition selon l'une quelconque des revendications précédentes, caractérisée en ce qu'elle se présente sous la forme de solutions (aqueuses, hydroalcooliques ou huileuses), de dispersions (type lotion ou sérum), d'émulsions de consistance liquide ou semi-liquide (type lait), de suspensions ou émulsions (type crème), de gel aqueux ou lipophile, de microémulsions, de microcapsules, de microparticules, de dispersions vésiculaires de type ionique et/ou non ionique, de pansements interfaces non absorbants, ou encore d'article de contention imprégné. 7. Composition according to any one of the preceding claims, characterized in that it is in the form of solutions (aqueous, hydroalcoholic or oily), dispersions (lotion or serum type), emulsions of liquid or semi consistency liquid (milk type), suspensions or emulsions (cream type), aqueous or lipophilic gel, microemulsions, microcapsules, microparticles, vesicular dispersions of ionic and / or nonionic type, non-absorbent interface dressings, or still of impregnated compression article.
8. Composition selon l'une quelconque des revendications précédentes, caractérisée en ce qu'elle se présente sous la forme d'une émulsion huile-dans-eau, de préférence sous forme de crème, comprenant : 8. Composition according to any one of the preceding claims, characterized in that it is in the form of an oil-in-water emulsion, preferably in cream form, comprising:
0,1 à 5% de sel de potassium de sucrose octasulfate KSOS, 0.1 to 5% potassium salt of sucrose octasulfate KSOS,
40 à 60% en poids d'eau,  40 to 60% by weight of water,
20 à 40% en poids d' au moins une huile,  20 to 40% by weight of at least one oil,
1 à 10% en poids d'au moins un tensioactif,  1 to 10% by weight of at least one surfactant,
0 à 10% en poids d'au moins une cire,  0 to 10% by weight of at least one wax,
0 à 20% en poids d'une autre substance active,  0 to 20% by weight of another active substance,
0 à 2% en poids de conservateurs,  0 to 2% by weight of preservatives,
0 à 5% en poids d'épaississants.  0 to 5% by weight of thickeners.
9. Composition selon l'une quelconque des revendications 1 à 9, pour traiter les hémorroïdes chez un sujet présentant une prédisposition au développement des hémorroïdes.  9. Composition according to any one of claims 1 to 9, for treating hemorrhoids in a subject with a predisposition to the development of hemorrhoids.
10. Composition selon l'une quelconque des revendications 1 à 9, pour son utilisation dans le renforcement de la musculeuse longitudinale du rectum formant le ligament de Parks et/ou dans la prévention de l'ouverture de shunts artério-veineux, préférentiellement au niveau des coussinets de Thomson.  10. Composition according to any one of claims 1 to 9, for its use in strengthening the longitudinal muscularis of the rectum forming the ligament Parks and / or in the prevention of the opening of arteriovenous shunts, preferably at the level of Thomson pads.
PCT/FR2015/000191 2014-10-09 2015-10-01 Dermatological composition for the prevention and treatment of haemorrhoids WO2016055701A1 (en)

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