WO2008038807A1 - Composition dermatologique à usage externe - Google Patents

Composition dermatologique à usage externe Download PDF

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Publication number
WO2008038807A1
WO2008038807A1 PCT/JP2007/069111 JP2007069111W WO2008038807A1 WO 2008038807 A1 WO2008038807 A1 WO 2008038807A1 JP 2007069111 W JP2007069111 W JP 2007069111W WO 2008038807 A1 WO2008038807 A1 WO 2008038807A1
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WO
WIPO (PCT)
Prior art keywords
skin
bht
external
composition
present
Prior art date
Application number
PCT/JP2007/069111
Other languages
English (en)
Japanese (ja)
Inventor
Shigeki Sawamura
Original Assignee
Kobayashi Pharmaceutical Co., Ltd.
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 Kobayashi Pharmaceutical Co., Ltd. filed Critical Kobayashi Pharmaceutical Co., Ltd.
Publication of WO2008038807A1 publication Critical patent/WO2008038807A1/fr

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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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A61K8/347—Phenols
    • 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
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05—Phenols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/28—Rubbing or scrubbing compositions; Peeling or abrasive compositions; Containing exfoliants
    • 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
    • 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
    • A61Q19/005—Preparations for sensitive skin

Definitions

  • the present invention relates to a composition for external use on skin having an itching suppression effect, a massage effect and the like.
  • the power of performing massage or the like to obtain a beauty or relaxation effect For example, the power of performing massage or the like to obtain a beauty or relaxation effect.
  • water-insoluble particles are blended as a scrub agent in order to exert a massage effect by physical stimulation.
  • scrubbing agents hard scrubbing agents such as polyethylene beads, talmi shell grains, and crystalline cellulose are widely used. Although hard scrubs are excellent in removing dirt on the skin and in massaging the skin, there are cases in which unpleasant skin irritation or foreign body sensation is felt during use.
  • itch is defined as “a sensation that causes the skin to break! /, And! /”, And is generally an unpleasant sensation.
  • Symptoms associated with “itch” include various forms such as atopic dermatitis, urticaria, insect bites, dry skin, and hypersensitive skin.
  • antihistamines, local anesthetics, moisturizing Agents are used. However, since they penetrate into the inner surface of the skin and involve a scientific approach, it takes time to take effect.
  • Patent Document 1 discloses an external preparation for skin containing natural oils and fats and antioxidants.
  • butylhydroxytoluene is generally added in an amount of about 0.0 ;! to 1% as a preservative, stabilizer, antioxidant and the like.
  • these external preparations have also been unable to effectively suppress the skin rather than those intended to irritate the skin.
  • Patent Document 1 JP 2000-159678 Disclosure of the invention
  • the main object of the present invention is to provide an external preparation for skin that gives skin irritation by application and exhibits a comfortable massage effect.
  • Another object of the present invention is to provide an external composition for skin, which can replace itching caused by insects and hypersensitivity skin with irritation, and can effectively suppress itching. Is.
  • BHT ptylhydroxytonolene
  • the present invention provides the following external composition for skin.
  • Item 1 A composition for external use on skin, characterized by containing solid-state butylhydroxytoluene (hereinafter referred to as BHT).
  • BHT solid-state butylhydroxytoluene
  • Item 2 The external composition for skin according to Item 1, wherein the particle size of BHT is 1000 m or less.
  • Item 4 The composition for external application to skin according to any one of Items 1 to 3, wherein the BHT content is 10 to 40% by weight.
  • Item 5 The external composition for skin according to any one of Items 1 to 4, further comprising a water-soluble polymer.
  • the invention's effect [0009]
  • the external composition for skin according to the present invention is applied directly to the skin, and the BHT in a solid state physically stimulates the skin, so that an appropriate massage stimulus can be given to the skin.
  • the composition for external use of the skin of the present invention when applied to an affected area having itching, it can be replaced with a feeling of irritation in a short time by physical stimulation of BHT in a solid state, and the itching is effectively suppressed. can do.
  • composition for external use of the skin of the present invention is characterized mainly by containing BHT in a solid state.
  • BHT BHT
  • the antipruritic agent of this invention contains BHT as an essential component.
  • Ptylhydroxytoluene is a compound having a white crystal shape, and both 1S, also called dibutylhydroxytoluene, refer to the same compound ([(CH 3) C] C H (CH 2) OH).
  • BHT traditionally makeup
  • antioxidants and stabilizers for foods, pharmaceuticals, foods and the like.
  • BHT commercially available ones can be used.
  • butyl hydroxytoluene (Sanei Chemical Co., Ltd.), dibutylhydroxytoluene (Eastman Chemica Norre Japan Co., Ltd., Ueno Pharmaceutical Co., Ltd.) API Corporation, Sumitomo Chemical Co., Ltd., Nagase Sangyo Co., Ltd., JGC Universal Co., Ltd., Mitsubishi Wel Pharma Co., Ltd.).
  • the particle size of BHT used in the present invention is about lOOOO ⁇ m or less, preferably about 1000 to 50 to 111, more preferably about 1000 to; about 100 to m, more preferably about 1000 to; About 180 in.
  • BHT having each particle diameter can be obtained by pulverizing BHT with a mortar or the like and then applying it to a sieve having each diameter.
  • Preferred combinations include, for example, (a) 501-; about 1000 m A combination of BHT with a particle size of and ⁇ having a particle size of about 350 to 500 ⁇ m; (b) BHT with a particle size of less than 350 [Im and a particle size of about 350 to 500 ⁇ m A combination of BHT having
  • the blending ratio of BHT having each particle size is appropriately set as long as the substitution effect on the irritating feeling of itchiness can be exhibited.
  • BHT having a particle size of about 501 to 1000 m is set to 0.
  • the amount of BHT in the external composition for skin of the present invention is about 10 to 40% by weight, preferably about 15 to 35% by weight, more preferably about 20 to 30% by weight. With such a blending amount, the massage effect and the antipruritic effect due to skin irritation can be exhibited more significantly while maintaining the stability as a preparation.
  • the composition for external use of the present invention preferably contains alcohol in addition to the BHT.
  • alcohol By blending alcohol, solid-state BHT can be dispersed favorably, and the skin can be uniformly and moderately stimulated.
  • the alcohol used in the present invention is not particularly limited as long as it is commonly used in the fields of cosmetics and pharmaceuticals. For example, methanol, ethanol, propanol, isopropanol, butanol, isobutanol and the like are used.
  • Lower alcohol having 1 to 6 carbon atoms, preferably 1 to 3 carbon atoms; propylene glycol, dipropylene glycol, glycerin, 1,3-butylene glycol, butylene glycol, concentrated glycerin, polyethylene glycol, maltitol, mannitol, sorbitol, etc.
  • Examples include polyhydric alcohols. these May be used alone or in combination of two or more.
  • the lower alcohol may be anhydrous or hydrated. In the present invention, it is preferable to use (hydrous) ethanol, absolute ethanol, or isopropanol!
  • the blending amount of alcohol in the composition for external use of the present invention is about 0 to 45% by weight, preferably about 4 to 40% by weight, more preferably about 4 to 35% by weight.
  • the blending ratio of BHT and alcohol in the external composition for skin of the present invention is such that when BHT is 1 part by weight, alcohol is about 3 parts by weight or less, preferably about 2 parts by weight or less, and more preferably about 1 part by weight or less. With such a blending ratio, the solid state of BHT can be maintained and an appropriate stimulus can be given to the skin.
  • the external composition for skin of the present invention may contain water, a water-soluble polymer, or the like, if necessary.
  • Conventionally known water-soluble polymers can be used, for example, carboxyvininole polymer, polyvinyl alcohol, polyvinyl methyl ether, polyvinylinoxychetyl cellulose, pullulan, agar, gelatin, alginic acid and its salts, carrageen Examples include naan and gums. These may be used alone or in combination of two or more.
  • the amount of water in the external composition for skin of the present invention is about 25 to 89.5% by weight, preferably about 27 to 80.2% by weight, more preferably about 28 to 75% by weight;
  • the amount of the conductive polymer to be combined is about 0.5 to 5% by weight, preferably about 0.8 to 4% by weight, and more preferably about 1 to 3% by weight.
  • Typical formulation examples of the present invention 10 to 40 weight BHT 0/0, the Anorekonore 0-45 wt%, a water-soluble polymer 0.5 to 5% by weight, water 25-89.
  • a composition for external use containing 5% by weight is exemplified.
  • the composition for external use of the skin of the present invention includes various components generally used in cosmetics, quasi-drugs, pharmaceuticals, aqueous components, oil-based components, moisturizing components, moisturizing components, and so on.
  • Forms, thickeners, preservatives, antioxidants, pH adjusters, carriers, fragrances, colorants, drugs and the like can be prepared in various dosage forms alone or in combination of two or more.
  • the composition for external use of the skin of the present invention includes a known local anesthetic and antibacterial agent within the range not impairing the effects of the present invention.
  • local anesthetics such as lidocaine, dibu force in, dibu force in hydrochloride, diphenhydramine, ethyl aminobenzoate, desitthecin; chlorpheniramine maleate, diphenhydramine, diphenhydramine hydrochloride, glycyrrhetinic acid, glycyrrhizin
  • Anti-inflammatory agents such as dipotassium phosphate, monoammonium glycyrrhizinate, allantoin, methyl salicylate; 1-menthol nole, dl-menthol nole, camphor, dl-strengthen, lactic acid menthylate, etc .
  • Moisturizers such as urea, salicylic acid, sodium hyaluronate
  • Bactericides such as isopropylmethyl phenol, quaternary ammonium salts (benzalkonium chloride, benzethonium chloride, etc.), chlorhexidine hydrochlor
  • Examples of the dosage form of the external composition for skin of the present invention include force S that can be prepared into a conventionally known dosage form according to the method of use and application, such as an ointment, lotion, gel, aerosol, and the like. It is done.
  • the external composition for skin of the present invention contains an appropriate amount of a base for obtaining a desired dosage form.
  • a base for example, but not limited to, paraffin, petrolatum, squalane, norafin, white wax, plastibase, polyethylene glycolenore, macrogonole, lauromacronore, silicone oil, silicone, polysorbate, polyoxyethylene hydrogenated castor oil, Oil bases such as olive oil, cottonseed oil, soybean oil, coconut oil; higher alcohols such as cetanol and stearyl alcohol; fatty acid esters (such as isopropyl myristate and sorbitan fatty acid ester), higher fatty acid salt emulsifiers, highly refined egg yolk lecithin , Soybean lecithin, refined soybean lecithin, white beeswax, propylene carbonate, egg yolk phospholipid, egg yolk oil, coconut oil fatty acid, sodium lauryl sulfate, other ionic and nonionic surfactants
  • the composition for external use of the present invention can be prepared by mixing and preparing the above components according to a conventionally known method. Conditions such as temperature in preparation, order of addition of each component, mixing time, etc. should be set as appropriate based on the common general technical knowledge according to the physical or scientific properties of each component, concentration, instrument stress, etc. Is not particularly limited.
  • the external preparation for skin of the present invention comprises For example, it can be prepared by dissolving components soluble in water and alcohol, mixing them and stirring them uniformly, and finally adding BHT.
  • composition for external use of the skin of the present invention can be applied as an antipruritic agent, athlete's foot drug or the like to a place where itching occurs.
  • the application target is not particularly limited as long as it is used for this purpose, but for example, when used as an antipruritic agent, it can be applied to symptom accompanied by itching, insect bite, dry skin, hypersensitive skin, etc. .
  • itch refers to "a feeling that causes the idea of wanting to break through the skin” as described above.
  • an appropriate amount of the external composition for skin of the present invention may be spread over the itchy part of the skin.
  • the solid BHT can physically irritate the itchy part of the skin, replace the itching with a feeling of irritation, and suppress the itching without further rebating.
  • “replacing itching with a sense of irritation” refers to making the skin sensation in a short-term (instantaneous) state of feeling an irritation (feeling itchy) other than “itching”.
  • the skin irritation by the external preparation for skin of the present invention is an appropriate stimulation without damaging the skin, and thus can be used for promoting blood circulation at the application site. Therefore, the external preparation for skin of the present invention can also be used as a massage agent, an external anti-inflammatory analgesic or the like.
  • the obtained external composition for skin was stored at room temperature (about 25 ° C) for 1 week, and its properties were visually confirmed to evaluate the stability. Specifically, dispersibility (presence / absence of particle settling and agglomeration (aggregation of particles)), shape retention (presence / absence of obvious changes compared to initial properties such as viscosity reduction), and particles are solid It was confirmed whether the properties were maintained (softening / dissolution). When there was no change in any of these properties, it was marked as ⁇ , and when any one of the changes was confirmed, it was marked as X.
  • composition for external use with a stability evaluation result of “ ⁇ ” was applied to the affected area of 10 subjects complaining of itching caused by insect bites, etc., and it was easy to apply (one point when it was difficult to apply) 5 points when easy to apply), replacement of itching with irritation (1 point when not replaced with irritation, 5 points when replaced with irritation) and anti-itching effect (when itching does not stop) 1 point and 5 points when itching stops) were evaluated in 5 stages each.
  • composition for external application on skin was applied to the skin of 10 healthy subjects, and with regard to comfortable physical irritation (1 point when not felt, 5 points when felt) Evaluation was performed.
  • Table 1 shows the evaluation results.
  • CVP represents carboxybulle polymer and PG represents propylene glycol.
  • composition for external use with skin containing particles other than BHT (Comparative Examples;! -32) was also evaluated in the same manner. The results are shown in Table 2-1 and Table 2-2 below.
  • CVP represents a carboxybule polymer
  • PG represents propylene glycol
  • Comparative Examples 9 to 13, 16, 25 to 29, and 32 are compositions for external use in skin that contain conventionally known particles. These external preparations for skin were relatively stable and good, but all of them had a replacement effect on the irritating feeling of itchiness and a pleasant stimulating action. In the preparations in which BHT was dissolved, it was not possible to obtain a sensation of itchiness or a pleasant irritation (data not shown).
  • the composition for external use of the skin of the present invention has an excellent anti-itching effect as well as a temporary anti-itching effect of replacing itching with a stimulating feeling. That is, the external composition for skin of the present invention has an immediate and long-lasting itch suppression effect.
  • CVP carboxybutyl polymer
  • PG propylene glycol
  • HPC hydroxypropyl cellulose
  • DPG dipropylene glycol
  • 1,3-BG 1,3-butylene glycol

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Birds (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dispersion Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Cosmetics (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une composition dermatologique à usage externe capable de produire une sensation physique de stimulation sur la peau, et de remplacer le prurit causé en particulier par des piqûres d'insectes ou une hypersensibilité de la peau par une sensation de stimulation, de façon à supprimer efficacement le prurit. Cette composition dermatologique à usage externe est caractérisée en ce qu'elle contient du butylhydroxytoluène sous forme solide.
PCT/JP2007/069111 2006-09-29 2007-09-28 Composition dermatologique à usage externe WO2008038807A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2006270076A JP5063072B2 (ja) 2006-09-29 2006-09-29 皮膚外用組成物
JP2006-270076 2006-09-29

Publications (1)

Publication Number Publication Date
WO2008038807A1 true WO2008038807A1 (fr) 2008-04-03

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PCT/JP2007/069111 WO2008038807A1 (fr) 2006-09-29 2007-09-28 Composition dermatologique à usage externe

Country Status (2)

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JP (1) JP5063072B2 (fr)
WO (1) WO2008038807A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2493955A (en) * 2011-08-25 2013-02-27 Hds Ltd Methods and compositions for reducing allergic reactions to fragranced products and perfumes
WO2021204568A1 (fr) 2020-04-07 2021-10-14 Universität Basel Composition topique pour le traitement du prurit

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07126158A (ja) * 1993-10-27 1995-05-16 Taisho Pharmaceut Co Ltd クロタミトン配合外用剤
JPH07173078A (ja) * 1993-12-21 1995-07-11 Taisho Pharmaceut Co Ltd 鎮痒剤組成物
JPH1036883A (ja) * 1996-07-16 1998-02-10 Asahi Chem Ind Co Ltd 皮膚および頭髪洗浄剤組成物
JPH10330217A (ja) * 1997-05-29 1998-12-15 Kose Corp 美白用皮膚外用剤
JPH11106307A (ja) * 1997-09-30 1999-04-20 Pola Chem Ind Inc 亜硫酸塩含有石鹸
WO2004078157A2 (fr) * 2003-03-04 2004-09-16 The Procter & Gamble Company Regulation de la croissance des poils chez les mammiferes
JP2004256805A (ja) * 2003-02-07 2004-09-16 Kao Corp 枠練り石鹸組成物
WO2005018320A1 (fr) * 2003-08-12 2005-03-03 The William M. Yarbrough Foundation Composition pour le traitement lie aux organismes piquants et penetrants et aux parasites, et pour le traitement de l'urticaire, et procede d'utilisation

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07126158A (ja) * 1993-10-27 1995-05-16 Taisho Pharmaceut Co Ltd クロタミトン配合外用剤
JPH07173078A (ja) * 1993-12-21 1995-07-11 Taisho Pharmaceut Co Ltd 鎮痒剤組成物
JPH1036883A (ja) * 1996-07-16 1998-02-10 Asahi Chem Ind Co Ltd 皮膚および頭髪洗浄剤組成物
JPH10330217A (ja) * 1997-05-29 1998-12-15 Kose Corp 美白用皮膚外用剤
JPH11106307A (ja) * 1997-09-30 1999-04-20 Pola Chem Ind Inc 亜硫酸塩含有石鹸
JP2004256805A (ja) * 2003-02-07 2004-09-16 Kao Corp 枠練り石鹸組成物
WO2004078157A2 (fr) * 2003-03-04 2004-09-16 The Procter & Gamble Company Regulation de la croissance des poils chez les mammiferes
WO2005018320A1 (fr) * 2003-08-12 2005-03-03 The William M. Yarbrough Foundation Composition pour le traitement lie aux organismes piquants et penetrants et aux parasites, et pour le traitement de l'urticaire, et procede d'utilisation

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2493955A (en) * 2011-08-25 2013-02-27 Hds Ltd Methods and compositions for reducing allergic reactions to fragranced products and perfumes
WO2021204568A1 (fr) 2020-04-07 2021-10-14 Universität Basel Composition topique pour le traitement du prurit

Also Published As

Publication number Publication date
JP5063072B2 (ja) 2012-10-31
JP2008088100A (ja) 2008-04-17

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