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
  • A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
  • A61K8/4953—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom containing pyrimidine ring derivatives, e.g. minoxidil
• • 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
  • A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
• • 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
  • A61K8/49—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
  • A61K8/4913—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid
• • 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
  • A61K8/4913—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid
  • A61K8/492—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid having condensed rings, e.g. indol
• • 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
• • 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
  • A61K2800/70—Biological properties of the composition as a whole

Definitions

• the present invention relates to the use of a 5-hydroxytryptamine antagonist, also called serotonin, specific for the 5HT 2 receptor or a 5-hydroxytryptamine agonist specific for the human 5HT 1D receptor in or for the preparation of '' a cosmetic or dermatological composition, for treating sensitive skin, including the scalp, the contours of the eyes and the mucous membranes, of human beings. It also relates to the cosmetic or dermatological composition obtained.
• a 5-hydroxytryptamine antagonist also called serotonin
• sensitive skin was assimilated to allergic skin. Due to the fact that little was known about the characteristics of sensitive skin, it was until now very difficult to treat them, and they were treated indirectly, for example by limiting in the cosmetic composition the use of products with an irritant nature such as surfactants, preservatives, perfumes and certain active ingredients.
• the Applicant has carried out numerous clinical tests and has been able to determine the symptoms associated with sensitive skin. These symptoms are in particular subjective signs, which are essentially dysaesthetic sensations. “Dysesthetic sensations” is understood to mean more or less painful sensations felt in a skin area such as tingling, tingling, itching or itching, heating, discomfort, tightness, etc.
• allergic skin is skin that reacts to an external agent, an allergen, which triggers an allergic reaction. It is an immunological process which only occurs when an allergen is present 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 concern any individual, even if so-called sensitive skin individuals react to it faster than the others. This mechanism is not immunological.
• the Applicant has now found that 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 lime, variations temperature or wool. In general, these signs are associated with dry skin or skin 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 acne-prone skin 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, permanent conditioning products. 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 capsaicin test consists of applying 0.05 ml of a cream containing 0.075% capsaicin to approximately 4 cm2 of skin and noting the appearance of signs. subjective effects 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 tachykinins which come from sensitive nerve endings of the epidermis and dermis.
• the Applicant has found that the pathophysiological pattern common to all the states of sensitive skin is linked to a great ability to release tachykinins and more particularly of substance P in the skin.
• the dysesthetic manifestations which are caused by the release of neuropeptides are said to be "neurogenic".
• This substance P is a polypeptide developed and released by sensitive nerve endings. It induces in particular, a degranulation of mast cells resulting in particular in the release of serotonin as well as a cascade of biochemical events leading to an inflammatory reaction.
• the Applicant has now discovered that one of the characteristics of sensitive skin is linked to the release of serotonin and / or to the action of this serotonin on the release and / or on certain functional aspects of the activity of substance P and therefore, the use of a serotonin antagonist specific for the 5HT 2 receptor and / or a serotonin agonist specific for the human 5HT 1D receptor made it possible to obtain a preventive and / or curative effect for sensitive skin. Indeed, by decreasing the release and / or the synthesis of serotonin by serotoninic fibers (5HT 1D agonist) and / or by decreasing the binding of serotonin (5HT 2 antagonist), the release and / or the activity of substance P released are greatly diminished.
• serotonin antagonists specific for the 5HT 2 receptor or serotonin agonists specific for the 5HT 1D receptor or a combination of these antagonists and these agonists to treat sensitive skin. It has in fact surprisingly found that the incorporation of a serotonin antagonist specific for the 5HT 2 receptor or a serotonin agonist specific for the 5HT 1D receptor in a cosmetic or dermatological composition makes it possible to avoid irritation. and / or dysesthetic sensations and / or itching of the skin.
• a subject of the present invention is therefore the use of at least one serotonin antagonist specific for the 5HT 2 receptor and / or at least one serotonin agonist specific for the 5HT 1D human receptor in a cosmetic composition or for the preparation of a dermatological composition, containing a physiologically acceptable medium, for treating sensitive skin.
• Another subject of the present invention is the use of at least one serotonin antagonist specific for the 5HT 2 receptor and / or at least one serotonin agonist specific for the human 5HT 1D receptor in a cosmetic composition or for the preparation a dermatological composition containing a physiologically acceptable medium for preventing and / or combating skin irritations and / or scabs and / or feelings of heating and / or dysesthesia and / or pruritus of the skin.
• the invention relates to the use of at least one antagonist of the serotonin specific "5HT 2 receptor and / or of at least one agonist of serotonin specific human 5-HT 1D receptor in a composition cosmetic or for the preparation of a dermatological composition containing a physiologically acceptable medium for treating the skin symptoms linked to the release and / or the synthesis and / or the fixation of serotonin on the 5HT 2 receptor and / or the 5HT 1D human receptor .
• a physiologically acceptable medium is a cosmetically or dermatologically acceptable medium, which is compatible with the skin, mucous membranes, nails and hair.
• the composition containing the serotonin antagonist and / or agonist can be applied to the face, neck, hair and nails, or any other cutaneous area of the body.
• a substance to be recognized as a 5HT 2 receptor-specific serotonin antagonist or a human 5HT 1D receptor-specific serotonin agonist it must inhibit the release and / or fixation and / or synthesis of serotonin in the dermis and / or the epidermis. In particular, it meets at least one of the following characteristics:
• the ultimate goal of these reactions is to decrease the release and / or activity of neuropeptides, and in particular of substance P, released by the sensitive skin fibers.
• serotonin was isolated as the vasoconstrictor principle of the blood where it is stored in red blood cells. In addition, it is found in plasma in combined form with in particular creatinine or sulfuric acid. Serotonin is also found in the central nervous system where it plays a role as a neurotransmitter. On the other hand, no one until today had established a link between serotonin and sensitive skin.
• one or more serotonin antagonists specific for the 5HT 2 receptor can be used, one or more serotonin agonists specific for the 5HT 1D receptor or a combination of one or more of these antagonists with one or more of these agonists.
• the serotonin antagonist specific for the 5HT 2 receptor which can be used in the invention can in particular be chosen from ketanserin, cinanserin, cyproheptadine, LY 53 857, methysergide, ritanserin, ICI 169-369, risperidone, pirenperone, pipamperone, trazodone, LY 281067 and their mixtures.
• the specific agonist serotonin 5HT 1D receptor used in the invention can be selected from sumatriptan sold especially under the brand Imigram ® by Glaxo company, MK / 462, naratriptan and mixtures thereof. Preferably, sumatriptan is used. Until now, this compound was mainly used to treat migraine (see in particular the document Elsevier Science BV Ail rts. Reserv. Mathew NT.; Sanin LC Advances in migraine drug therapy).
• the serotonin antagonist specific for the 5HT 2 receptor and / or the serotonin agonist specific for the 5HT 1D receptor are preferably used in an amount ranging from 0.000001 to 5% of the total weight of the composition, and in particular in an amount ranging from 0.0001 to 1%.
• composition according to the invention may be in any dosage form normally used for topical application to the skin, in particular in the form of a solution or dispersion of the lotion or serum type, of emulsion 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 a suspension or emulsion of soft consistency of the aqueous or anhydrous cream or gel type, of microgranules, nanoparticles, microemulsion , nanocapsules or dispersions of vesicles of ionic and / or nonionic type.
• These compositions are prepared according to the usual methods. It can also be used for hair in the form of an aqueous, alcoholic or hydroalcoholic solution, cream, gel, emulsion, foam or also in the form of aerosol compositions containing a propellant under pressure.
• the amounts of the various constituents of the composition according to the invention are those conventionally used in the fields considered.
• the composition of the invention constitutes in particular a cream for cleaning, protecting, treating or caring for the face, for the hands, for the feet, for large anatomical folds or for the body, (for example day cream, night cream, make-up remover cream, foundation cream, sunscreen cream), a fluid foundation, a cleansing milk, a body milk for protection or care, an anti-sun milk, a lotion, a gel or a skin care foam, such as cleansing lotion, sunscreen lotion, artificial tanning lotion, bath composition, deodorant composition containing bactericidal agent, after shave gel or lotion, cream depilatory, a composition against insect bites, a pain-relieving composition.
• a cream for cleaning, protecting, treating or caring for the face, for the hands, for the feet, for large anatomical folds or for the body for example day cream, night cream, make-up remover cream, foundation cream, sunscreen cream
• a fluid foundation for protection or care
• an anti-sun milk a lotion, a gel or a skin care foam
• composition according to the invention can also consist of a solid preparation constituting a soap or a cleaning bar.
• the 5HT 2 receptor-specific serotonin antagonist or the 5HT 1D receptor-specific serotonin agonist can also be incorporated into any type of composition for hair care, and in particular in a shampoo, a styling lotion, a treatment lotion , a styling cream or gel, a dye composition (in particular oxidation dye) optionally in the form of a coloring shampoo, a restructuring hair lotion, a perm composition (especially a composition for the first time of a perm), fall protection lotion or gel, etc.
• the composition of the invention can also be for oral use, for example in the form of toothpaste.
• the composition may contain adjuvants and additives customary for a composition for buccal use and in particular surfactants, thickeners or humectants, polishing agents such as silica, or various active ingredients such as fluorides, in particular fluoride sodium, and possibly sweetening agents such as sodium saccharinate.
• adjuvants and additives customary for a composition for buccal use and in particular surfactants, thickeners or humectants, polishing agents such as silica, or various active ingredients such as fluorides, in particular fluoride sodium, and possibly sweetening agents such as sodium saccharinate.
• 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 oils, emulsifiers and coemulsifiers then used are chosen from those conventionally used in the field under consideration.
• the emulsifier and the coemulsifier 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 relative to the total weight of the composition.
• the emulsion may, in addition, contain lipid vesicles.
• the composition of the invention can 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 coloring matters.
• 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 coloring matters.
• the amounts of these various " adjuvants are those conventionally used in the field under consideration, and for example from 0.01% to 10% of the total weight of the composition.
• These adjuvants depending on their nature, can be introduced into the fatty phase, in the aqueous phase and / or in the lipid spherules.
• emulsifiers used in the invention there may be mentioned for example glycerol stearate, polysorbate 60 and the PEG-6 / PEG-32 / glycol 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 / alkyl acrylate copolymers, polyacrylamides, polysaccharides such as hydroxypropylcellulose, natural gums and clays, and, 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.
• hydrophilic active agents it is possible to use proteins or protein hydrolysates, amino acids, polyols, urea, allantoin, sugars and sugar derivatives, vitamins and hydroxy acids.
• retinol and its derivatives
• tocopherol vitamin E
• essential fatty acids ceramides
• essential oils ceramides
• active agents there may be mentioned as an example: - 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,
• - 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
• - antiviral agents such as acyclovir
• - 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 in general fruit acids, and C 2 -C 22 alkylated derivatives of salicylic acid such as n-octanoyl-5-salicylic acid;
• - anti-free radical agents such as alpha-tocopherol or its esters, superoxide dismutases, certain metal chelators or ascorbic acid and its esters;
• - antiseborrheics such as progesterone
• - anti-dandruff agents such as octopirox or zinc pyrithione
• - anti-acne drugs such as retinoic acid or benzoyl peroxide.
• sensitive skin is skin that reacts to external factors such as surfactants, perfumes, soaps and to all types of irritants, that is to say all types of products causing tingling. , itching, tingling, pruritus, discomfort, overheating, burning, redness, when these products come into contact with the skin.
• the serotonin antagonist (s) specific for the 5HT 2 receptor or the serotonin agonist (s) specific for the 5HT 1D receptor are associated with active agents having an irritant side effect, commonly used in the fields considered.
• active agents having an irritant side effect commonly used in the fields considered.
• This serotonin antagonist or agonist in a composition of the invention containing an active ingredient with an irritant effect makes it possible to strongly attenuate, or even to eliminate this irritant effect, the sufficient amount of this antagonist or agonist of serotonin to strongly attenuate, even to remove, this irritating effect being within the reach of the skilled person.
• the subject of the invention is also a cosmetic or dermatological composition containing a physiologically acceptable medium and at least one active agent with an irritant side effect, characterized in that it contains, in addition, at least one serotonin antagonist specific for the 5HT receptor 2 and / or at least one serotonin agonist specific for the 5HT 1D receptor.
• the active ingredients with an irritant side effect are chosen from ⁇ -hydroxy acids (fruit acid), ⁇ -hydroxy acids such as salicylic acid and its alkylated derivatives, ⁇ -keto acids, ⁇ - keto acids, retinoids, anthralins, anthranoids, peroxides, lithium salts, antimetabolites, vitamin D and its derivatives.
• the present invention also relates to a cosmetic or dermatological treatment process for sensitive skin and / or sensitive scalps, characterized in that it is applied to the skin and / or hair of human beings, a composition as described above containing at least one serotonin antagonist specific for the 5HT 2 receptor or at least one serotonin agonist specific for the 5HT 1D receptor in a cosmetically or dermatologically acceptable medium.
• This treatment process can be implemented in particular by applying the composition defined above, according to the usual technique of use of this type of composition. For example: application to the skin or mucous membranes of cream, gel, serum, lotion, cleansing milk, anti-sun composition or on dry or wet hair, shampoos or after shampoos, or even application to toothpaste gums.
• Polysorbate 60 (Tween 60 sold by the company ICI) 1, 00
• Polysorbate 60 (Tween 60 sold by the company ICI) 1, 00
• Polysorbate 60 (Tween 60 sold by the company ICI) 1, 00

Landscapes

• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Birds (AREA)
• Epidemiology (AREA)
• Dermatology (AREA)
• Cosmetics (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Applications Claiming Priority (3)

Publications (1)

Family

ID=9502657

Family Applications (1)

Country Status (4)

Families Citing this family (6)

Family Cites Families (7)

• 1997
  • 1997-01-16 FR FR9700412A patent/FR2758263B1/fr not_active Expired - Fee Related
• 1998
  • 1998-01-14 JP JP53331398A patent/JP2001511782A/ja not_active Ceased
  • 1998-01-14 WO PCT/FR1998/000062 patent/WO1998031335A2/fr not_active Ceased
  • 1998-01-14 EP EP98902077A patent/EP1014928A2/de not_active Withdrawn

Non-Patent Citations (1)

Also Published As

Similar Documents

Legal Events