Classifications

• • 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
  • A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
• • 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
  • A61P27/00—Drugs for disorders of the senses
  • A61P27/02—Ophthalmic agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/74—Biological properties of particular ingredients
  • A61K2800/75—Anti-irritant
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q1/00—Make-up preparations; Body powders; Preparations for removing make-up
  • A61Q1/14—Preparations for removing make-up
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/004—Aftersun preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/005—Preparations for sensitive skin

Definitions

• the present invention relates to a cosmetic, dermatological and / or pharmaceutical composition intended in particular for treating, in humans, certain skin disorders and / or skin diseases, in particular painful and / or pruritic.
• Some of these diseases are currently being treated with local corticosteroids or PUVA therapy.
• Corticosteroids are very effective in calming the symptoms of these diseases, but, unfortunately, they often have very detrimental side effects such as atrophies, especially mycotic or bacterial infections.
• PUVA therapy is the local irradiation of diseased skin with UVA rays, after absorption of a photosensitizing substance. This technique has the serious disadvantages of photoaging, which can most often lead to skin cancer.
• this treatment is not ambulatory, forcing patients to go regularly to a specialized center for the duration of treatment, which is very restrictive and limits their professional activity and leisure.
• the subject of the present invention is precisely a topical composition making it possible to effectively treat these skin diseases, while remedying these drawbacks.
• dysesthetic sensations is meant more or less painful sensations felt in a skin area such as tingling, tingling, itching or itching, burning, heating, discomfort, tightness, etc.
• sensitive skin was not allergic skin.
• allergic skin is skin that reacts to an external agent called an allergen, which triggers an allergic reaction. It is an immunological process which occurs only in the presence of an allergen and which only affects sensitized subjects.
• the essential characteristic of sensitive skin is, according to the applicant, on the contrary, a mechanism of response to external factors, which can affect any individual, even if so-called sensitive skin individuals react more quickly than others. This mechanism is not immunological.
• sensitive skin can be divided into two main clinical forms, irritable and / or reactive skin, and intolerant skin.
• Irritable and / or reactive skin is skin that reacts with pruritus, that is, itching or tingling, to various factors such as the environment, emotions, food, wind, friction, razor, soap, surfactants, hard water with a high concentration of limestone, temperature variations or wool.
• these signs are associated with dry skin, with or without sores, or with skin that presents with erythema.
• Intolerant skin is skin that reacts with feelings of heating, tightness, tingling and / or redness, to various factors such as the environment, emotions, food. In general, these signs are associated with hyperseborrheic or acneic skin, with or without sores, and erythema.
• “Sensitive” scalps have a more unequivocal clinical semiology: the sensations of pruritus and / or tingling and / or overheating are essentially triggered by local factors such as friction, soap, surfactants, hard water with a high concentration of limestone. , shampoos or lotions. These sensations are also sometimes triggered by factors such as the environment, emotions and / or food. Erythema and hyperseborrhea of the scalp and dandruff are frequently associated with the above signs.
• the sensitive skin results in itchy sensations and / or dysesthetic sensations. (heating, tingling) linked in particular to sweat, friction, wool, surfactants, hard water with a high lime concentration and / or temperature variations.
• the applicant has also developed a test. In fact, he surprisingly found that there was a link between people with sensitive skin and those who reacted to a topical application of capsaicin.
• This capsaicin test consists of applying to approximately 4 cm ⁇ of skin 0.05 ml of a cream containing 0.075% capsaicin and of noting the appearance of subjective signs caused by this application, such as tingling, burning and itching. . In subjects with sensitive skin, these signs appear between 3 and 20 minutes after application and are followed by the appearance of an erythema which begins at the periphery of the application area.
• Capsaicin causes a release of neuropeptides, and in particular of the 5 tachykinins which come from nerve endings of the epidermis and the dermis.
• the dysesthetic manifestations which are caused by the release and / or the synthesis and or the fixation of its neuropeptides are said to be "neurogenic”.
• the applicant has now discovered that by acting on the skin and ocular receptors sensitive to capsaicin, it was possible to obtain a preventive and / or curative effect for skin and / or mucous and / or ophthalmological diseases linked to the release and / or synthesis and / or fixation of neuropeptides such as shingles, eczema, sensitive skin and eyes, pruritus and pruritic diseases, herpes, atopic or contact dermatitis, 5 lichens, prurigos, erythema in particular solar , insect bites, rosacea, conjunctivitis, uveitis, skin or eye pain, irritation.
• neuropeptides such as shingles, eczema, sensitive skin and eyes, pruritus and pruritic diseases, herpes, atopic or contact dermatitis, 5 lichens, prurigos, erythema in particular solar , insect bites, rosacea, conjunctivitis,
• capsazepine In sensitive eyes, in humans, the applicant has considered using capsazepine. He has surprisingly found that the incorporation of capsazepine in a composition for topical application makes it possible to avoid irritation, dysaesthetic sensations, pruritus and skin disorders mentioned above.
• the present invention therefore relates to a topical composition containing, in a topically and physiologically acceptable medium, capsazepine and at least one active agent with irritant side effect.
• capsazepine in or for the manufacture of a topical composition containing a cosmetically and / or dermatologically acceptable medium, of capsazepine to prevent and / or fight against skin pain, in particular of neurogenic origin. , and more particularly pains in shingles and in particular post-zoster pain, "ghostly" pains after amputation of the limb, pains due to burns and in general skin pains due to aggression of the skin ( insect bite, sunburn, jellyfish sting, etc.).
• the present invention also relates to the use of capsazepine, in or for the manufacture of a composition for topical application to prevent and / or fight against skin and / or eye irritations, erythemas, pruritus, feelings of overheating and / or dysesthesia of the skin, eyes or mucous membranes, in particular of the human being.
• capsazepine in or for the manufacture of a composition for topical application to prevent and / or fight against symptoms linked to shingles, eczema, sensitive skin or eyes, diseases pruritic, pruritus, herpes, atopic or contact dermatitis, lichens, prurigos, insect bites, rosacea, conjunctivitis, uveitis, especially of humans.
• the present invention also relates to the use of capsazepine as an anti-irritant agent in or for the manufacture of a topical composition.
• the clinical signs of sensitive skin according to the applicant are essentially subjective: tingling, tingling, pruritus, tightness, overheating, and they are sometimes associated with erythema. These signs are due to specific non-specific factors.
• a cosmetically, dermatologically or physiologically acceptable medium is, according to the invention, a medium compatible with the skin, including the scalp, nails, mucous membranes, eyes and hair.
• the composition of the invention can therefore be applied to the whole face, the neck, the hair and the nails, or any other cutaneous zone of the body.
• Capsazepine is an organic molecule with the following formula
• capsazepine is preferably used in an amount ranging from 0.000001 to 5% by weight relative to the total weight of the composition, and in particular in an amount ranging from 0.0001 to 0, 5% by weight relative to the total weight of the composition.
• compositions according to the invention can be in all dosage forms normally used for topical application, in particular aqueous, hydroalcoholic or oily solutions or dispersions of the lotion or serum type, emulsions of liquid or semi-liquid consistency of the milk type, obtained by dispersing a fatty phase in an aqueous phase (O / W) or vice versa (W / O), or suspensions or emulsions of soft consistency of the aqueous, anhydrous cream, ointment or gel type, or even microgranules, or vesicular dispersions of ionic and / or nonionic type.
• These compositions are prepared according to the usual methods.
• compositions constitute in particular cleansing, protective, treatment or care creams for the face, for the hands, for the feet, for large anatomical folds or for the body (for example day creams, night creams, make-up removing creams, foundation creams, after-sun creams), fluid foundations, makeup-removing products (milks), protective or care body milks, after-sun milks or lotions, lotions, gels or skin care foams, such as cleansing lotions, artificial tanning lotions, bath compositions, deodorant compositions containing a bactericidal agent, aftershave gels or lotions, depilatory creams, counter compositions insect bites, pain relieving compositions.
• compositions according to the invention may also consist of solid preparations constituting soaps or cleaning bars.
• They can also be used for the hair in the form of aqueous, alcoholic or hydroalcoholic solutions, or in the form of creams, gels, emulsions, foams or also in the form of aerosol compositions also containing a propellant under pressure.
• Capsazepine can therefore be incorporated into various compositions for hair care and treatments, and in particular shampoos, conditioning lotions. folds, treating lotions, styling creams or gels, dye compositions (in particular oxidation dyes) possibly in the form of coloring shampoos, restructuring hair lotions, perm compositions (in particular compositions for the first stage of a perm), hair loss lotions or gels, etc.
• the compositions of the invention may be in the form of eye drops, ointment or eye wash solution.
• the compositions may consist of care or protection creams for sensitive eyes, milks or lotions for cleaning or removing make-up from sensitive eyes, eye makeup products such as pencils, mascaras, eyeliners. , eyeshadows.
• compositions of the invention can also be for oral use, for example a toothpaste.
• the compositions may contain adjuvants and additives customary for compositions for buccal use and in particular surfactants, thickening agents, humectants, polishing agents such as silica, various active ingredients such as fluorides, in particular particularly sodium fluoride, and optionally sweetening agents such as sodium saccharinate.
• compositions according to the invention are those conventionally used in the fields considered.
• the proportion of 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 oils, emulsifiers and coemulsifiers used in the composition in the form of an emulsion are chosen from those conventionally used in the cosmetic field.
• the emulsifier and the co-emulsifier are present in the composition in a proportion ranging from 0.3% to 30% by weight, and preferably from 0.5 to 30% by weight. weight relative to the total weight of the composition.
• the emulsion may, in addition, contain lipid vesicles.
• the composition of the invention may also contain adjuvants customary in the field under consideration, such as hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active agents, preservatives, antioxidants, solvents, perfumes, fillers, filters and dyes, odor absorbers, pigments.
• adjuvants customary in the field under consideration, such as hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active agents, preservatives, antioxidants, solvents, perfumes, fillers, filters and dyes, odor absorbers, pigments.
• 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.
• These adjuvants depending on their nature, can be introduced into the fatty phase, into the aqueous phase and / or into the lipid spherules.
• emulsifiers which can be used in the invention, there may be mentioned for example glycerol stearate, polysorbate 60 and the mixture of PEG-6 / PEG-32 / Glycoi
• Tefose ⁇ 63 Stearate sold under the name Tefose ⁇ 63 by the company Gattefosse.
• solvents which can be used in the invention mention may be made of lower alcohols, in particular ethanol and isopropanol.
• hydrophilic gelling agents mention may be made of carboxyvinyl polymers (carbomers), acrylic copolymers such as acrylate / alkylacrylate copolymers, polyacrylamides, polysaccharides such as hydroxypropylcellulose, natural gums and clays, and, as lipophilic gelling agents , we can cite modified clays such as bentones, metal salts of fatty acids such as aluminum stearates, hydrophobic silica, polyethylenes and ethylcellulose.
• carboxyvinyl polymers carboxyvinyl polymers
• acrylic copolymers such as acrylate / alkylacrylate copolymers
• polyacrylamides polysaccharides
• polysaccharides such as hydroxypropylcellulose
• natural gums and clays natural gums and clays
• lipophilic gelling agents we can cite modified clays such as bentones, metal salts of fatty acids such as aluminum stearates, hydrophobic silica, poly
• hydrophilic active agents proteins or protein hydrolysates, amino acids, polyols, urea, allantoin, sugars and sugar derivatives, hydrophilic vitamins and plant and bacterial extracts can be used.
• retinol and its derivatives
• tocopherol vitamin E
• essential fatty acids ceramides
• essential oils can be used.
• agents modulating differentiation and / or proliferation and / or skin pigmentation such as retinoic acid and its isomers, retinol and its esters, vitamin D and its derivatives, estrogens such as estradiol, kojic acid or hydroquinone;
• Antibacterials such as clindamycin phosphate, erythromycin or antibiotics of the tetracycline class;
• - antifungals in particular compounds belonging to the class of imidazoles such as econazole, ketoconazole or miconazole or their salts, polyene compounds, such as amphotericin B, compounds of the allylamine family, such as terbinafine, or octopirox;
• - steroidal anti-inflammatory agents such as hydrocortisone, betamethasone valerate or clobetasol propionate, or non-steroidal anti-inflammatory agents such as ibuprofen and its salts, diclofenac and its salts, acetylsalicylic acid, acetaminophen or glycyrrhetinic acid;
• - anesthetic agents such as lidocaine hydrochloride and its derivatives
• - antipruritic agents such as thenaldine, trimeprazine or cyproheptadine
• - keratolytic agents such as alpha- and beta-hydroxy-carboxylic or beta-ketocarboxylic acids, their salts, amides or esters and more particularly hydroxy acids such as glycolic acid, lactic acid, salicylic acid, l citric acid and generally fruit acids, and n-octanoyl-5-salicylic acid;
• - anti-free radical agents such as alpha-tocopherol or its esters, superoxide dismutases, certain metal chelating agents or ascorbic acid and its esters;
• anti-dandruff agents such as octopirox or zinc pyrithione
• - anti-acne drugs such as retinoic acid or benzoyl peroxide.
• capsazepine is associated with active ingredients with an irritant side effect commonly used in the cosmetic or dermatological field.
• the presence of capsazepine in a composition containing an active ingredient having an irritant effect makes it possible to greatly attenuate, or even to eliminate this irritant effect.
• the active ingredients with an irritant side effect are chosen from ⁇ -hydroxy acids, ⁇ -hydroxy acids, ⁇ -keto acids, ⁇ -keto acids, retinoids, anthraiines, anthranoids, peroxides, minoxidil, lithium, antimetabolites, vitamin D and its derivatives, aluminum salts, surfactants, reducing agents, oxidizing agents, strong bases (ammonia, monoethanolamine), strong acids.
• the present invention further relates to a cosmetic or dermatological treatment process, characterized in that a composition as described above containing, on the skin, the eyes, the hair, and / or the mucous membranes, is applied. capsazepine in a cosmetically acceptable medium.
• the treatment method of the invention can be implemented in particular by applying the hygienic or cosmetic compositions as defined above, according to the usual technique for using these compositions. For example: application of creams, gels, serums, lotions, cleansing milks or after-sun compositions on the skin or on dry hair, application of a hair lotion on wet hair, shampoos, or further application of toothpaste on the gums.
• Example 2 Face care cream (oil-in-water emulsioni
• Polysorbate 60 (Tween 60 sold by the company HERE) 1, 00
• Example 6 Pain Qel, in particular for pain associated with shingles
• Polysorbate 60 (Tween 60 sold by ICI) 1.00
• EXAMPLE 8 Care Cream for Sensitive Skins against Solar Erythema (Oil-in-Water Emulsion) or for Treating Symptoms Related to Shingles
• Polysorbate 60 (Tween 60 sold by ICI) 1.00 Stearic acid 1.40

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• Health & Medical Sciences (AREA)
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• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Dermatology (AREA)
• Pharmacology & Pharmacy (AREA)
• Chemical & Material Sciences (AREA)
• Epidemiology (AREA)
• Medicinal Chemistry (AREA)
• Bioinformatics & Cheminformatics (AREA)
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• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Engineering & Computer Science (AREA)
• Birds (AREA)
• Organic Chemistry (AREA)
• Ophthalmology & Optometry (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Cosmetics (AREA)
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• 1995
  • 1995-11-06 FR FR9513096A patent/FR2740682B1/fr not_active Expired - Fee Related
• 1996
  • 1996-10-11 US US09/068,237 patent/US6048855A/en not_active Expired - Fee Related
  • 1996-10-11 EP EP96934898A patent/EP0859616A1/fr not_active Withdrawn
  • 1996-10-11 JP JP9517904A patent/JPH11501941A/ja active Pending
  • 1996-10-11 WO PCT/FR1996/001592 patent/WO1997017077A1/fr not_active Application Discontinuation
  • 1996-10-11 CA CA002234797A patent/CA2234797A1/fr not_active Abandoned
• 1998
  • 1998-05-05 NO NO982032A patent/NO982032L/no not_active Application Discontinuation
• 1999
  • 1999-12-09 US US09/457,667 patent/US6262050B1/en not_active Expired - Fee Related

Non-Patent Citations (1)

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