WO2021235424A1 - Composition pour cavité buccale - Google Patents

Composition pour cavité buccale Download PDF

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Publication number
WO2021235424A1
WO2021235424A1 PCT/JP2021/018741 JP2021018741W WO2021235424A1 WO 2021235424 A1 WO2021235424 A1 WO 2021235424A1 JP 2021018741 W JP2021018741 W JP 2021018741W WO 2021235424 A1 WO2021235424 A1 WO 2021235424A1
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WIPO (PCT)
Prior art keywords
component
acid
oral composition
mass
salts
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PCT/JP2021/018741
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English (en)
Japanese (ja)
Inventor
康平 石井
亜紀子 二階堂
将登 平泉
純一 天川
Original Assignee
ライオン株式会社
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Priority to CN202180032501.6A priority Critical patent/CN115484923B/zh
Priority to JP2022524484A priority patent/JPWO2021235424A1/ja
Publication of WO2021235424A1 publication Critical patent/WO2021235424A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
    • A61K31/6615—Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/42—Phosphorus; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/24—Phosphorous; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/362—Polycarboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55—Phosphorus compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom

Definitions

  • the present invention relates to an oral composition.
  • Condensed phosphate is known to have an effect of suppressing stain adhesion to teeth, but it has a problem of strong irritation to the oral mucosa, and the problem is particularly remarkable in liquid preparations such as mouthwashes. rice field.
  • Patent Document 1 discloses the use of a specific fragrance component for alleviating irritation of pyrophosphate and polyphosphate.
  • Patent Document 2 proposes a formulation containing hydroxyalkyl cellulose to suppress irritation by viscosity, masking of irritation by a fragrance component, and the like.
  • Patent Document 1 cannot obtain a sufficient effect with the oral composition, especially the liquid preparation, and the irritation remains strong especially with the preparation not rinsed with water such as a mouthwash and a mouth spray. There was also a problem in terms of sustainability of stimulus relief. Further, the technique of Patent Document 2 has problems such as a decrease in palatability and the inability to mask for a long time.
  • An object of the present invention is to provide an oral composition capable of reducing the irritating sensation in a stimulating component such as a stain adhesion inhibitory component to teeth and exhibiting the original effect of the stimulating component.
  • the present invention provides the following [1] to [11].
  • Component (A) One or more selected from condensed phosphoric acid, phytic acid, and salts thereof
  • component (A) is at least one selected from pyrophosphoric acid, tripolyphosphoric acid, hexametaphosphoric acid, ultraphosphoric acid, phytic acid, and salts thereof.
  • [7] The oral composition according to [5] or [6], wherein the amount of the component (C) is 0.05 to 3% by mass.
  • the stimulant-relieving agent according to [9] wherein the stimulant component is at least one selected from condensed phosphoric acid, phytic acid, and salts thereof.
  • a capable oral composition is provided.
  • each component is a value based on the amount of each component charged when preparing the composition.
  • the oral composition of the present invention contains the components (A) and (B), and may further contain the component (C).
  • the components (A) to (C) will be described.
  • the component (A) is one or more selected from condensed phosphoric acid, phytic acid, and salts thereof. Depending on the component (A), the oral composition can exert a stain adhesion suppressing effect.
  • Examples of the condensed phosphoric acid include linear polyphosphoric acids such as pyrophosphate, tripolyphosphate and tetrapolyphosphate; cyclic polyphosphates such as trimetaphosphate, tetramethaphosphate and hexametaphosphate; and network-like polyphosphates such as ultraphosphoric acid. Examples thereof include polyphosphate, as the linear polyphosphate, pyrophosphate and tripolyphosphate are preferable, and as the cyclic polyphosphate, hexametaphosphate is preferable. As the condensed phosphoric acid, linear polyphosphoric acid is preferable.
  • Condensed phosphate and phytic acid may be in the form of salts, and the salts include, for example, alkali metal salts (eg, sodium salt, potassium salt), alkaline earth metal salts (eg, calcium salt, magnesium salt), copper salt, zinc.
  • Inorganic base salts such as salts, aluminum salts and ammonium salts; organic base salts such as triethylammonium salt, triethanolammonium salt, pyridinium salt and diisopropylammonium salt are mentioned, preferably alkali metal salt and alkaline earth metal salt. , More preferably a sodium salt, a potassium salt, a calcium salt, and even more preferably a sodium salt or a potassium salt.
  • the component (A) preferably contains one or more selected from linear polyphosphoric acid and phytic acid, and may contain one or more selected from pyrophosphate, a sodium salt of tripolyphosphoric acid, and phytic acid. More preferred.
  • the component (A) may be one selected from condensed phosphoric acid, phytic acid, and salts thereof, or may be a combination of two or more.
  • the combination of two or more two or more selected from polyphosphoric acid and a salt thereof are preferable, and it is preferable that the combination contains one or more linear polyphosphoric acid and a salt thereof.
  • Such combinations include a combination of one or more selected from linear polyphosphoric acid and salts thereof and one or more selected from cyclic polyphosphoric acid, reticulated polyphosphoric acid and salts thereof; and linear. Examples thereof include two or more combinations selected from polyphosphoric acid and salts thereof.
  • Condensed phosphoric acid, phytic acid, and salts thereof as the component (A) may be blended in the oral composition as a mixture with phosphoric acid or phosphate other than these.
  • the amount of the component (A) is usually 0.05% by mass or more, preferably 0.1% by mass or more, based on the total amount of the oral composition. As a result, a better effect of suppressing stain adhesion can be exhibited.
  • the upper limit is usually 2% by mass or less, preferably 1% by mass or less. Thereby, the expression of irritation to the oral mucosa of the oral composition can be suppressed, and the deterioration of flavor expression and appearance stability can be suppressed. Therefore, the amount of the component (A) is usually 0.05 to 2% by mass, preferably 0.1 to 1% by mass.
  • the component (B) is (N- (2- (2-pyridinyl) ethyl) -2-isopropyl-5-methylcyclohexanecarboxamide).
  • the amount of the component (B) is not particularly limited, but is usually 0.00001% by mass or more, preferably 0.0001% by mass or more, based on the total amount of the oral composition. Thereby, the irritation sensation of the oral composition can be suppressed and the suppressing effect can be continuously obtained.
  • the upper limit is usually 0.01% by mass or less, preferably 0.005% by mass or less. As a result, the expression of a strong stimulating sensation can be suppressed, and the decrease in flavor expression can be suppressed. Therefore, the amount of the component (B) is usually 0.00001 to 0.01% by mass, preferably 0.0001 to 0.005% by mass.
  • the ratio (A / B) of the amount of the component (A) to the amount of the component (B) is usually 20 or more, preferably 50 or more, and more preferably 80 or more.
  • the upper limit is usually 30,000 or less, preferably 20,000 or less, and more preferably 10,000 or less.
  • the component (C) is one or more selected from organic acids having 3 to 6 carbon atoms and salts thereof. By containing the component (C), the oral composition can exhibit a better effect of suppressing stain adhesion.
  • Examples of the organic acid having 3 to 6 carbon atoms include monocarboxylic acid, dicarboxylic acid, tricarboxylic acid and oxycarboxylic acid, and apple acid, tartaric acid, citric acid, lactic acid, succinic acid and fumaric acid are preferable.
  • Examples of the salt include inorganic base salts such as alkali metal salts (eg, sodium salt, potassium salt), alkaline earth metal salts (eg, calcium salt, magnesium salt), ammonium salts; triethylammonium salt, triethanolammonium salt, etc.
  • organic base salts such as pyridinium salt and diisopropylammonium salt, preferably alkali metal salt and alkaline earth metal salt, more preferably sodium salt, potassium salt and calcium salt, and further preferably sodium salt or It is a potassium salt.
  • the amount of the component (C) is usually 0.05% by mass or more, preferably 0.1% by mass or more, based on the total amount of the oral composition. Thereby, the effect of suppressing stain adhesion can be further improved.
  • the upper limit is usually 3.0% by mass or less, preferably 1.5% by mass or less. If it exceeds 3.0% by mass, the appearance stability and the flavor development may be deteriorated. Therefore, the amount of the component (C) is usually 0.05 to 3% by mass, preferably 0.1 to 1.5% by mass.
  • the dosage form of the oral composition is not particularly limited, and examples thereof include solids, pastes, and liquids, of which liquids are preferable.
  • an oral composition having a liquid dosage form is referred to as a liquid oral composition.
  • the liquid oral composition can be prepared as a liquid preparation such as a mouthwash (eg, a mouthwash, a mouthwash), a liquid toothpaste, and a mouthwash, and may be a concentrated type if necessary.
  • the oral composition may be a pharmaceutical product, a quasi-drug, a cosmetic product, or a food product.
  • the oral composition of the present invention may contain any components other than the above-mentioned components, if necessary.
  • the optional component can be appropriately selected depending on the intended use and dosage form of the oral composition.
  • optional ingredients include surfactants, wetting agents, pH regulators, preservatives, sweeteners, fragrances, active ingredients, and solvents.
  • examples of the components other than the optional components exemplified above include a binder and an abrasive.
  • the content of the optional component is not particularly limited, and can be set to an amount used in a normal oral composition as long as the effect of the present invention is not impaired.
  • surfactant examples include anionic surfactants, nonionic surfactants, cationic surfactants and amphoteric surfactants, and it is preferable to include at least one of anionic surfactants and nonionic surfactants.
  • anionic surfactants When the oral composition contains an anionic surfactant, the effect of suppressing stain adhesion can be further improved.
  • nonionic surfactant When the oral composition contains a nonionic surfactant, the solubilizing effect of the oil-soluble component can be obtained.
  • anionic surfactant examples include alkyl sulfates, N-acylamino acid salts, ⁇ -olefin sulfonates, N-acylsulfonates, N-acyltaurine salts, sulfates of glycerin fatty acid esters, and alkyls. Sulfates and N-acyltaurine salts are preferred.
  • alkyl sulfate examples include an alkyl sulfate having 12 to 14 carbon atoms (eg, an alkali metal salt of lauryl sulfate, myristyl sulfate).
  • N-acylamino acid salt examples include acylglutamates having a saturated or unsaturated hydrocarbon group (eg, having 8 to 18 carbon atoms, preferably 12 to 16; either linear or branched). Examples thereof include acyl amino acid salts such as acyl sarcosine salts.
  • acyl taurine salt an N-acylmethyl taurine salt having a saturated or unsaturated hydrocarbon group (for example, having 8 to 18 carbon atoms, preferably 12 to 16; it may be either a straight chain or a branched chain) is used. Can be mentioned.
  • ⁇ -olefin sulfonate examples include ⁇ -olefin sulfonate having 10 to 16 carbon atoms such as tetradecene sulfonate.
  • alkali metal salts such as sodium salt and potassium salt are preferable.
  • the amount of the anionic surfactant is usually 0.01% by mass or more with respect to the total amount of the oral composition. As a result, a better effect of suppressing stain adhesion can be exhibited.
  • the upper limit is usually 3% by mass or less, preferably 0.5% by mass or less, and more preferably 0.3% by mass or less. Thereby, the expression of a strong stimulus can be suppressed. Therefore, the amount of the anionic surfactant is usually 0.01 to 3% by mass, preferably 0.01 to 0.5% by mass, and preferably 0.01 to 0.3% by mass.
  • nonionic surfactant examples include polyoxyethylene fatty acid esters such as polyoxyethylene hydrogenated castor oil, polyoxyethylene glycerin fatty acid ester, and polyoxyethylene sorbitan fatty acid ester; and polyoxyethylene higher alcohols such as polyoxyethylene alkyl ether.
  • examples include ether; sugar alcohol fatty acid ester; sorbitan fatty acid ester; polyglycerin fatty acid ester; polyoxyethylene sorbitan fatty acid ester.
  • the average number of moles of ethylene oxide added to the polyoxyethylene hydrogenated castor oil is usually 20 to 150 mol, preferably 20 to 130 mol, and more preferably 40 to 110 mol.
  • the amount of the nonionic surfactant is usually 0.1% by mass or more, preferably 0.3% by mass or more, based on the total amount of the oral composition.
  • the upper limit is usually 1% by mass or less, preferably 0.8% by mass or less. Within these ranges, a better solubilizing effect of the oil-soluble component can be obtained. Therefore, the amount of the nonionic surfactant is preferably 0.1 to 1% by mass, preferably 0.3 to 0.8% by mass.
  • Examples of the cationic surfactant include quaternary ammonium compounds such as alkylammonium compounds and alkylbenzylammonium compounds.
  • Examples of the amphoteric tenside include an alkylamide betaine type amphoteric tenside; an acetate betaine type amphoteric tenside such as alkyldimethylaminoacetic acid betaine and fatty acid amidepropyldimethylaminoacetic acid betaine; N-fatty acid acyl-N-carboxymethyl-. Examples thereof include imidazoline-type amphoteric tenside agents such as N-hydroxyethylethylenediamine salt.
  • wetting agent When the oral composition contains a wetting agent, the feeling of use can be further improved.
  • the wetting agent include sugar alcohols such as sorbitol, erythritol, maltitol, lactitol, and xylitol; and polyhydric alcohols such as glycerin, propylene glycol, ethylene glycol, and polyethylene glycol.
  • the polyhydric alcohol is preferably glycerin or propylene glycol, and the sugar alcohol is preferably sorbitol or xylitol.
  • the amount of the wetting agent is usually 3% by mass or more, preferably 5% by mass or more, based on the total amount of the oral composition.
  • the upper limit is usually 40% by mass or less, preferably 30% by mass or less, and more preferably 15% by mass or less. Within these ranges, a better effect of improving usability can be obtained. Therefore, the amount of the wetting agent is usually 3 to 40% by mass, preferably 3 to 30% by mass, and more preferably 5 to 15% by mass.
  • the pH stability of the pharmaceutical product can be ensured.
  • the components (A) and (C) of the present invention also act as a pH adjuster in the composition, but any other pH adjuster can be further used if necessary.
  • the optional pH adjuster include phthalic acid, orthophosphoric acid, acetic acid, carbonic acid, ribonucleic acid, salts thereof (preferably potassium salt, sodium salt, ammonium salt as well as component (A)).
  • Examples thereof include sodium hydroxide and hydrochloric acid, preferably orthophosphoric acid or a salt thereof, and more preferably sodium dihydrogen phosphate, sodium monohydrogen phosphate, potassium dihydrogen phosphate, potassium monohydrogen phosphate.
  • the amount thereof can be such that the pH at 25 ° C. can be adjusted to 5.5 to 8.5, preferably 6 to 8.
  • citric acid or a salt thereof it is preferable to use citric acid or a salt thereof, and it is also preferable to use orthophosphate in combination.
  • the pH can be measured at 25 ° C. after 3 minutes using a pH meter (model number HM-25R) manufactured by DKK-TOA Corporation immediately after preparing the oral composition.
  • Preservative When the oral composition contains an antiseptic, the antiseptic power of the preparation can be ensured.
  • the preservative include paraoxybenzoic acid esters such as methyl paraoxybenzoate and ethyl paraoxybenzoate; sodium benzoate; alkyldiaminoethylglycine hydrochloride; potassium sorbate.
  • the feeling of use can be further improved.
  • the sweetener include sugar alcohols such as xylitol, maltitol, erythritol, and sorbitol; and saccharin, aspartame, sucralose, acesulfame potassium, stevia, neohesperidin hydrocalcone, glycyrrhizin, perilartin, p-methoxycinnamic aldehyde, and thaumatin.
  • High sweetness sweeteners such as.
  • the oral composition contains a fragrance
  • the feeling of use can be improved and the initial irritation after use can be suppressed.
  • the fragrance include menthol and fragrances containing carboxylics, but any fragrance used in the oral composition may be used, and the fragrance is not particularly limited.
  • the content of menthol and carvone in the fragrance containing menthol and carvone is preferably 10 to 80% by mass.
  • Essential oils containing these, such as peppermint oil, Japanese peppermint oil, and sparemint oil, can also be used.
  • the amount of the fragrance is usually 0.00001% by mass or more with respect to the total amount of the oral composition, and the upper limit is usually 3% by mass or less, but is not particularly limited.
  • Active ingredients include, for example, anti-inflammatory agents such as tranexamic acid, epsilon-aminocaproic acid; enzymes such as dextranase, amylases, proteases, mutanase, lysoteam, lytecenzyme; sodium fluoride, sodium monofluorophosphate, fluoride.
  • anti-inflammatory agents such as tranexamic acid, epsilon-aminocaproic acid
  • enzymes such as dextranase, amylases, proteases, mutanase, lysoteam, lytecenzyme
  • sodium fluoride sodium monofluorophosphate, fluoride.
  • Fluorine-containing compounds such as stannous tin; aluminum chlorhydroxyalantin, allantin such as allantin or derivatives thereof; vitamin Cs such as ascorbic acid; plant extracts such as thyme, ginger, chow, and hamamelis; strontium chloride, potassium nitrate, aluminum lactate Antihypersensitivity inhibitors such as azulene, lysozyme chloride, dihydrocholesterol, glycyrrhetin salts, glycyrrhetinic acids, hydrocholesterol, chlorophyll, sodium copper chlorophyllin, copper gluconate, caropeptide, water-soluble inorganic phosphate compounds, polyethylene glycol, polyvinylpyrrolidone, lauroyl.
  • Examples thereof include sodium sarcosin, an anti-dental stone agent, and an anti-plaque agent, but any active ingredient used in an oral composition may be used, and the present invention is not particularly limited.
  • the content of the active ingredient can be appropriately set according to a conventional method.
  • the oral composition If the oral composition is in liquid form, it usually contains a solvent.
  • the solvent include water (eg, purified water) and alcohol (eg, lower monohydric alcohol such as ethanol), which are usually water, and alcohol can be blended as needed, but the dosage form is Any solvent may be used as long as it is used in a liquid oral composition, and is not particularly limited.
  • ethanol When ethanol is added as a solvent, the amount thereof is usually 30% by mass or less, preferably 20% by mass or less, based on the total amount of the oral composition, but it may not be added. Within this range, it is possible to improve the feeling of suppressing bad breath during use.
  • any suitable organic binder conventionally known, for example, a polysaccharide, a cellulosic binder (for example, carboxymethyl cellulose (CMC), hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, methyl cellulose, cation) Celluloseized cellulose, etc.), other polysaccharide thickeners (eg, xanthan gum, guagum, gellan gum, tragant gum, karaya gum, arabiya gum, locust bean gum, carrageenan, sodium alginate), synthetic water-soluble polymers (eg, sodium polyacrylate, etc.) Examples thereof include carboxyvinyl polymer, polyvinylpyrrolidone, polyvinyl alcohol, propylene glycol alginate). Further, an inorganic binder such as thickening silica and aluminum silicate can be contained. The content of the binder when blended is usually 0.01 to 10% by mass with
  • the abrasive may be either an inorganic abrasive or an organic abrasive.
  • the inorganic polishing agent include abrasive silica such as precipitate silica, aluminosilicate, zirconosilicate, crystalline zirconium silicate, and titanium-binding silica; calcium dibasic phosphate / dihydrate salt or anhydrous product, calcium primary phosphate.
  • Calcium phosphate compounds such as tertiary calcium phosphate, calcium pyrophosphate; calcium carbonate abrasives such as calcium carbonate; calcium hydroxides other than carbonate / phosphate such as calcium hydroxide and calcium sulfate; aluminum oxide, aluminum hydroxide, Aluminum-based materials such as alumina; Silica-based materials such as silicic acid anhydride, zeolite, and zirconium silicate; Magnesium-based materials such as magnesium carbonate and tertiary magnesium phosphate; Apatite-based materials such as hydroxyapatite, fluoroapatite, and calcium-deficient apatite.
  • Titanium-based materials such as titanium dioxide, mica titanium, and titanium oxide; minerals such as bentonite can be mentioned.
  • examples of the organic abrasive include polymethylmethacrylate and synthetic resin-based abrasives. Of these, silica-based abrasives are preferable.
  • the content of the abrasive when blended is usually 70% by mass or less, preferably 50% by mass or less, and more preferably 8 to 50% by mass with respect to the total amount of the oral composition.
  • the method of using the oral composition of the present invention is not particularly specified.
  • a method of rinsing the mouth for several tens of seconds with an appropriate amount in the mouth can be mentioned. You can also brush your teeth after washing your mouth.
  • the oral composition is useful in the use of a stain adhesion improving agent because it can suppress stain adhesion by applying the oral composition to teeth.
  • the applicable person is not particularly limited. For example, there are subjects who want to improve the adhesion of stains caused by foods and drinks such as black tea, green tea, and coffee, and subjects who do not have these symptoms but want to prevent them.
  • the oral composition of the present invention can be produced by mixing the above-mentioned components.
  • the order in which the components are mixed is not particularly limited, but it is preferable to mix them so that they are uniform.
  • the above-mentioned component (B) (N- (2- (2-pyridinyl) ethyl) -2-isopropyl-5-methylcyclohexanecarboxamide) is useful as an irritant-relieving agent for the stimulating component contained in the oral composition.
  • the stimulating component include one or more selected from the above-mentioned condensed phosphoric acid, phytic acid, and salts thereof, which are the components (A), and stimulating components having a structure similar to these. It is not particularly limited as long as it is a component that can be contained in the oral composition and causes irritation at the time of use.
  • the amount of the stimulant-relieving agent used may be any amount as long as the irritation caused by the stimulating component in the oral composition is suppressed, and may be an amount exemplified as the amount of the above-mentioned component (B).
  • the oral composition may be an oral composition containing a stimulating component, and when the stimulating component is the component (A), the oral composition contains the amount exemplified as the amount of the above-mentioned component (A).
  • the composition is preferred.
  • the dosage form of the oral composition and optional components that may be contained as needed are not particularly limited.
  • composition containing irritating ingredients Since the above-mentioned component (B) (N- (2- (2-pyridinyl) ethyl) -2-isopropyl-5-methylcyclohexanecarboxamide) is useful as a stimulant-relieving agent, it stimulates as a stimulant-relieving component. Together with the ingredients, it can be an essential ingredient in the oral composition.
  • the stimulant component may be an amount exemplified in the description of the stimulant relieving agent.
  • % means “mass%” unless otherwise specified.
  • the blending amount of each component shown in the following table is a value converted into a pure content (AI).
  • the amount of water (balance) includes the amount of water brought in by each component. It was
  • a mouthwash was prepared by uniformly mixing each component according to the composition shown in Tables 2 to 5 (unit of content of each component in the table: mass%). Specifically, POE-cured castor oil is added to ethanol and stirred, and then an oil layer in which fragrance is dissolved is prepared. An oil layer is added to the water layer in which other components are dissolved in purified water, and the three-one motor (BL1200) , HEIDO) was used to uniformly dissolve the mouthwash to prepare a mouthwash. The pH (25 ° C.) of the prepared mouthwash was 6.5 to 8.0.
  • ⁇ Evaluation method> (1. Stain adhesion suppressing effect)
  • HAP hydroxyapatite pellets
  • Stain adhesion suppression rate is 90% or more and 100% or less ++: Stain adhesion suppression rate is 70% or more and less than 90% +: Stain adhesion suppression rate is 50% or more and less than 70% ⁇ : Stain Adhesion suppression rate is 30% or more and less than 50%-: Stain adhesion suppression rate is less than 30%
  • Criteria for sustainability of lack of irritation ++: Average score 3.5 points or more and 4.0 points or less +: Average score 3.0 points or more and less than 3.5 points ⁇ : Average score 2.0 points or more 3. Less than 0 points-: Average score less than 2.0 points
  • Average score is 3.5 points or more and 4.0 points or less +: Average score is 3.0 points or more and less than 3.5 points ⁇ : Average score is 2.0 points or more 3. Less than 0 points-: Average score is 1.0 points or more and less than 2.0 points
  • the prepared preparation was filled in a container having a capacity of 80 mL, allowed to stand for 1 month under a temperature condition of ⁇ 5 ° C., and the appearance and properties were judged by visual evaluation.
  • Comparative Examples 1 to 4 which do not contain any of the components A and B, there are problems that there is no effect of suppressing stain adhesion, there is a feeling of irritation, or even if there is some lack of feeling of irritation, it does not last.
  • Examples 1 to 20 containing the components A and B good results were obtained in all of the evaluations of the effect of suppressing stain adhesion, the lack of irritation, and the persistence of the lack of irritation, and further, the expression of flavor and the preparation were obtained. The result was also good in terms of appearance stability. This indicates that the oral composition of the present invention can suppress the adhesion of stains on the teeth, suppress the irritation sensation, and maintain the suppressing effect.
  • Table 6 shows a prescription example of a dentifrice as a prescription example.

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Abstract

La présente invention aborde le problème de la fourniture d'une composition pour cavité buccale, ladite composition permettant de réduire la sensation de stimulation d'un élément stimulant tel qu'un élément destiné à supprimer l'adhérence des taches aux dents, tout en permettant à l'élément stimulant de présenter l'effet d'origine souhaité. La présente invention concerne : une composition pour cavité buccale, ladite composition contenant un composant (A) qui est composé d'une ou plusieurs substances choisies parmi un acide phosphorique condensé, un acide phytique et des sels de ces acides, et un composant (B) qui est le (N-(2-(2-pyridinyl)éthyl)-2-isopropyl-5-méthylcyclohexane carboxamide) ; un agent relaxant de stimulation pour un élément stimulant d'une composition pour cavité buccale, ledit agent relaxant de stimulation contenant du (N-(2-(2-pyridinyl)éthyl)-2-isopropyl-5-méthylcyclohexane carboxamide) ; et une composition pour cavité buccale, ladite composition contenant un élément stimulant et du (N-(2-(2-pyridinyl)éthyl)-2-isopropyl-5-méthylcyclohexane carboxamide).
PCT/JP2021/018741 2020-05-18 2021-05-18 Composition pour cavité buccale WO2021235424A1 (fr)

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006182705A (ja) * 2004-12-28 2006-07-13 Lion Corp 歯牙貼付用製品及び口腔ケア物質の供給方法
JP2007527388A (ja) * 2003-07-11 2007-09-27 キャドバリー・アダムズ・ユーエスエイ・エルエルシー ステイン除去複合体を含むチューインガム組成物および菓子組成物、ならびにそれらの製造方法および使用方法
WO2007145287A1 (fr) * 2006-06-16 2007-12-21 Mandom Corporation Détachant oral et composition orale
WO2018221621A1 (fr) * 2017-05-31 2018-12-06 ライオン株式会社 Composition pour utilisation dans la cavité buccale
JP2019182752A (ja) * 2018-04-03 2019-10-24 花王株式会社 液体口腔用組成物

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007527388A (ja) * 2003-07-11 2007-09-27 キャドバリー・アダムズ・ユーエスエイ・エルエルシー ステイン除去複合体を含むチューインガム組成物および菓子組成物、ならびにそれらの製造方法および使用方法
JP2006182705A (ja) * 2004-12-28 2006-07-13 Lion Corp 歯牙貼付用製品及び口腔ケア物質の供給方法
WO2007145287A1 (fr) * 2006-06-16 2007-12-21 Mandom Corporation Détachant oral et composition orale
WO2018221621A1 (fr) * 2017-05-31 2018-12-06 ライオン株式会社 Composition pour utilisation dans la cavité buccale
JP2019182752A (ja) * 2018-04-03 2019-10-24 花王株式会社 液体口腔用組成物

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