WO2007110380A1 - Préparation soulageant les piqûres d'insecte comprenant de l'épinastine - Google Patents

Préparation soulageant les piqûres d'insecte comprenant de l'épinastine Download PDF

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Publication number
WO2007110380A1
WO2007110380A1 PCT/EP2007/052772 EP2007052772W WO2007110380A1 WO 2007110380 A1 WO2007110380 A1 WO 2007110380A1 EP 2007052772 W EP2007052772 W EP 2007052772W WO 2007110380 A1 WO2007110380 A1 WO 2007110380A1
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WO
WIPO (PCT)
Prior art keywords
epinastine
optionally
bite
addition salts
acid addition
Prior art date
Application number
PCT/EP2007/052772
Other languages
English (en)
Inventor
Ursula Fauth
Original Assignee
Boehringer Ingelheim International Gmbh
Boehringer Ingelheim Pharma Gmbh & Co. Kg
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Boehringer Ingelheim International Gmbh, Boehringer Ingelheim Pharma Gmbh & Co. Kg filed Critical Boehringer Ingelheim International Gmbh
Publication of WO2007110380A1 publication Critical patent/WO2007110380A1/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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders

Definitions

  • the invention relates to a method of relieving the discomfort associated with an insect bite comprising topically applying to the area of the bite an effective amount of epinastine, optionally in the form of its racemate, its enantiomers and optionally in the form of the pharmacologically acceptable acid addition salts thereof in an acceptable vehicle.
  • Epinastine chemically known as 3-Amino-9,13b-dihydro-1 H-dibenz-[c,f]imidazol- [1 ,5-a]azepine and its acid addition salts are disclosed for the first time in the German Patent application P 30 08 944.2 which forms the basis for EP 0035749.
  • Chemically epinastine is represented by the following formula, which does not reflect stereochemical properties:
  • Epinastine can be used either as free base or as a pharmaceutically acceptable salt thereof.
  • epinastine is used as hydrochloride.
  • epinastine is used for the free base as well as for pharmaceutically acceptable salts. Methods for its preparations can be taken from EP 0496306 or from WO 01/40229.
  • the present invention relates to a method for ceasing pain associated with an insect bite comprising topically applying to the area of the bite an effective amount of epinastine, optionally in the form of its racemate, its enantiomers and optionally in the form of the pharmacologically acceptable acid addition salts thereof in an acceptable vehicle.
  • the present invention relates to a method for cease of itching associated with an insect bite comprising topically applying to the area of the bite an effective amount of epinastine, optionally in the form of its racemate, its enantiomers and optionally in the form of the pharmacologically acceptable acid addition salts thereof in an acceptable vehicle.
  • the present invention relates to the use of epinastine, optionally in the form of its racemate, its enantiomers and optionally in the form of the pharmacologically acceptable acid addition salts thereof for the preparation of a medicament for topical application to the skin in the area of an insect bite to relieve the discomfort thereof and/or to reduce the swelling associated with an insect bite and or to cease the pain associated with an insect bite and/or to cease the itching associated with an insect bite.
  • epinastine optionally in the form of its racemate, its enantiomers and optionally in the form of the pharmacologically acceptable acid addition salts thereof for the preparation of a medicament for topical application to the skin in the area of an insect bite to relieve the discomfort thereof and/or to reduce the swelling associated with an insect bite and or to cease the pain associated with an insect bite and/or to cease the itching associated with an insect bite.
  • any of the well known suitable components for such type preparations may be physically admixed therewith, generally in the amounts customarily used for such specific embodiments.
  • the instant invention includes the provision of a topical skin preparation adapted to relieve the discomfort associated with insect bites comprising an effective amount of epinastine, optionally in the form of its racemate, its enantiomers and optionally in the form of the pharmacologically acceptable acid addition salts thereof in a suitably acceptable vehicle.
  • Epinastine can optionally be used in form of the free base, in the form of its racemate, its enantiomers and optionally in the form of the pharmacologically acceptable acid addition salts thereof.
  • Suitable acid addition salts include for example those of the acids selected from, succinic acid, hydrobromic acid, acetic acid, fumaric acid, maleic acid, methanesulphonic acid, lactic acid, phosphoric acid, hydrochloric acid, sulphuric acid, tartaric acid and citric acid. Mixtures of the abovementioned acid addition salts may also be used. From the aforementioned acid addition salts the hydrochloride and the hydrobromide, particularily the hydrochloride, are preferred.
  • the amount in equivalent quantity of Epinastine hydrochloride is between 0.005 and 50 mg per 1 g of composition, preferably between 0.1 and 30 mg per 1 g of composition, more preferably between 0.2 and 15 mg per 1 g of composition and even more preferably between 0.3 and 5 mg per g of composition.
  • topically administered solutions are preferably prepared which typically contain 0.005 to 5, preferably 0.01 to 1 , most preferably 0.3 to 0.7 mg/ml of epinastine, optionally in the form of its racemate, its enantiomers and optionally in the form of the pharmacologically acceptable acid addition salts thereof.
  • the pharmaceutically active substance can be dispensed in refrigerants, antioxidants or stabilizing agents, agents adjusting a certain pH-value can be added as well as the viscosity, the osmotic pressure or the salt concentration influencing agents. These methods can also be combined.
  • additives can be added: excipients, bases, binders, disintegrators, lubricants, superplasticizers, plasticizers, antifoaming agents, foaming agents, antistatic agents, desiccant, moisturizing agents, surfactant, solubilizer, buffer agents, resolvents, solubilizing agents, solvents, diluents, stabilizers, emulsifying agents, suspension, suspending agents, dispersing agents, isotonizing agents, aerosol propellant, adsorbents, reducing agents, antioxidant, backing, wetting agents, wet modifier, filler, extender, adhesives, viscous agent, softeners, pH modifiers, antiseptics, preservatives, corrigent, refrigerative agents, flavoring agents, perfume, fragrance, coloring matters, and the like. Any of these additives may be used in the regular compositions methods, and do not impose any limitation to such composition methods.
  • Suitable aqueous solvents are physiologically acceptable aqueous solvents, physiologically acceptable saline solutions being particularly preferred.
  • the pH of the solutions according to the invention should preferably be maintained within the range from 4 to 8, preferably within the range from 4.5 to 7.5, more preferably within the range from 6.5 to 7.2 by means of a suitable buffer system.
  • the preparations may also contain conventional, pharmaceutically acceptable excipients, preservatives, stabilisers and/or penetration promoters.
  • the preferred carrier which may be used in the solutions according to the invention is purified water and preferably a physiological saline solution.
  • the excipients which may be used according to the invention include viscosity agents such as polyvinyl alcohol, povidone, hydroxypropylmethylcellulose, poloxamers, carboxymethylcellulose, carbomers and hydroxyethylcellulose.
  • the preferred preservatives which may be used in the solutions according to the invention may include benzalkonium chloride, chlorobutanol, thimerosal, phenyl mercury acetate and phenyl mercury nitrate.
  • the penetration promoters may be, for example, surfactants, specific organic solvents such as dimethylsulphoxide and other sulphoxides, dimethylacetamide and pyrrolidone, specific amides of heterocyclic amines, glycols such as propyleneglycol, propylene carbonate, oleic acid, alkylamines and derivatives thereof, various cationic, anionic, non-ionogenic and amphoteric surfactants and the like.
  • specific organic solvents such as dimethylsulphoxide and other sulphoxides, dimethylacetamide and pyrrolidone
  • specific amides of heterocyclic amines such as propyleneglycol, propylene carbonate, oleic acid, alkylamines and derivatives thereof
  • various cationic, anionic, non-ionogenic and amphoteric surfactants and the like may be, for example, surfactants, specific organic solvents such as dimethylsulphoxide and other sulphoxides
  • Substances may be added as necessary or as desired in order to adjust the tonicity of the solution.
  • Such substances include salts and especially sodium chloride, potassium chloride, mannitol and glycerol or other suitable physiologically acceptable agents for adjusting tonicity, without restricting the invention to the above.
  • Various buffers and substances may be used to adjust the pH, provided that the preparation obtained is physiologically acceptable. These buffers might include acetate buffer, citrate buffer, phosphate buffer and borate buffer.
  • physiologically acceptable antioxidants which may be used according to the invention include sodium metabisulphite, sodium thiosulphate, acetylcysteine, butylated hydroxyanisole and butylated hydroxytoluene, without restricting the invention to this list.
  • carrier components which may be incorporated in the solutions according to the invention are chelating agents.
  • the preferrred chelating agent is disodium edetate (Na-EDTA), although other chelating agents may also be used instead of or in conjunction with disodium edetate.
  • the propellant used in connection with the aerosol embodiment of the invention may be any non-toxic, liquifiable propellant suitable for use in connection with the dispensing of the material. That is to say, any non-toxic, volatile, organic material which exists as a gas at the temperature of use (and ambient or atmospheric pressure), like carbon dioxide, nitrogen or N 2 O or which exists as a liquid at the same temperature under superatmospheric pressures can be used as the gas- producing agent.
  • C3-C 4 aliphatic hydrocarbons namely liquefied propane, n-butane, and isobutane
  • fluorinated aliphatic hydrocarbons which contain from 1 to 3 carbon atoms and include, by way of example, fluorohydrocarbons (HFC), like HFC 134a (1 ,1 ,2,2-tetrafluorethan) and HFC 227 (1 ,1 ,1 ,2,3,3,3-heptafluorpropan) and mixtures thereof.
  • HFC fluorohydrocarbons
  • the saturated hydrocarbons and halogenated saturated aliphatic hydrocarbons are employed in the subject composition.
  • the following ingredients were processed through a regular method to form a cream of a total weight of 1 kg, added with sodium citrate to adjust at pH 5.

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne l'utilisation d'épinastine pour la préparation d'un médicament destiné à une application topique sur la peau dans la zone d'une piqûre d'insecte pour soulager la gêne provoquée par celle-ci.
PCT/EP2007/052772 2006-03-25 2007-03-22 Préparation soulageant les piqûres d'insecte comprenant de l'épinastine WO2007110380A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP06006193.4 2006-03-25
EP06006193 2006-03-25

Publications (1)

Publication Number Publication Date
WO2007110380A1 true WO2007110380A1 (fr) 2007-10-04

Family

ID=38066584

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2007/052772 WO2007110380A1 (fr) 2006-03-25 2007-03-22 Préparation soulageant les piqûres d'insecte comprenant de l'épinastine

Country Status (1)

Country Link
WO (1) WO2007110380A1 (fr)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1087574A (en) * 1965-02-18 1967-10-18 West Mount Chemicals Ltd Medical appliances
WO1998000168A1 (fr) * 1996-07-02 1998-01-08 Novartis Consumer Health S.A. Composition topique contenant une combinaison de composes antihistaminiques et de composes terpenoides
US5942503A (en) * 1995-11-14 1999-08-24 Boehringer Indelheim Kg Use of Epinastine for the treatment of pain
US20030129209A1 (en) * 2002-01-04 2003-07-10 Hatto Walch Topical application of cetirizine and loratadine
US20040247686A1 (en) * 2003-04-04 2004-12-09 Boehringer Ingelheim International Gmbh Pharmaceutical compositions comprising epinastine for the treatment of skin diseases

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1087574A (en) * 1965-02-18 1967-10-18 West Mount Chemicals Ltd Medical appliances
US5942503A (en) * 1995-11-14 1999-08-24 Boehringer Indelheim Kg Use of Epinastine for the treatment of pain
WO1998000168A1 (fr) * 1996-07-02 1998-01-08 Novartis Consumer Health S.A. Composition topique contenant une combinaison de composes antihistaminiques et de composes terpenoides
US20030129209A1 (en) * 2002-01-04 2003-07-10 Hatto Walch Topical application of cetirizine and loratadine
US20040247686A1 (en) * 2003-04-04 2004-12-09 Boehringer Ingelheim International Gmbh Pharmaceutical compositions comprising epinastine for the treatment of skin diseases

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
FRAUNFELDER, FREDERICK W.: "Epinastine hydrochloride for atopic disease", DRUGS OF TODAY , 40(8), 677-683 CODEN: MDACAP; ISSN: 0025-7656, 2004, XP002436960 *
FURUE, M. ET AL: "Effects of Cetirizine and Epinastine on the skin response to histamine iontophoresis", JOURNAL OF DERMATOLOGICAL SCIENCE , 25(1), 59-63 CODEN: JDSCEI; ISSN: 0923-1811, 2001, XP002436959 *
RENTSCHLER ARZNEIMITTEL GMBH: "Soventol Gel", July 2004, XP002436962 *

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