WO2008038806A1 - Agent antipruritique - Google Patents

Agent antipruritique Download PDF

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Publication number
WO2008038806A1
WO2008038806A1 PCT/JP2007/069110 JP2007069110W WO2008038806A1 WO 2008038806 A1 WO2008038806 A1 WO 2008038806A1 JP 2007069110 W JP2007069110 W JP 2007069110W WO 2008038806 A1 WO2008038806 A1 WO 2008038806A1
Authority
WO
WIPO (PCT)
Prior art keywords
bht
weight
antipruritic agent
present
antipruritic
Prior art date
Application number
PCT/JP2007/069110
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 WO2008038806A1 publication Critical patent/WO2008038806A1/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
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05—Phenols
    • 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

Definitions

  • the present invention relates to an antipruritic agent excellent in itching suppression effect.
  • “Itching” is defined as "a sensation that causes the skin to break down! / ,! Symptoms associated with itching include a variety of symptoms such as atopic dermatitis, rash, insect bite, dry skin, and hypersensitive skin. Depending on the condition, antihistamines, local anesthetics, moisturizing Agents are used. However, they did not have enough satisfaction for the applicator, such as it took time to take effect!
  • Patent Document 1 discloses an external preparation for skin containing natural fats and oils and an antioxidant. Such external preparations for skin generally contain about 0.001 to 1% of methylhydroxytoluene as a preservative, stabilizer, antioxidant and the like. However, it was not known that butylhydroxytoluene itself has an itching inhibitory effect.
  • Patent Document 1 JP 2000-159678
  • the main object of the present invention is to provide an antipruritic agent capable of effectively suppressing itching such as insect hypersensitivity skin.
  • BHT ptylhydroxytoluene
  • the present invention provides the following antipruritic agents.
  • Item 1 An antipruritic agent containing ptylhydroxytoluene (hereinafter referred to as BHT) as an active ingredient.
  • BHT ptylhydroxytoluene
  • Item 2 The antipruritic agent according to Item 1, wherein BHT is formulated in a dissolved state of 1.5% by weight in 100% by weight of the preparation.
  • Item 3 The antipruritic agent according to Item 2, wherein BHT is blended in a solid state.
  • Item 4 The antipruritic agent according to Item 3, wherein 7.5 to 40% by weight of BHT in a solid state is blended.
  • Item 5. The antipruritic agent according to Item 3 or 4, wherein the particle size of BHT in a solid state is 1000 m or less.
  • Item 6 Any one of Items 3 to 5, wherein BHT having a particle size of less than 350, BHT having a particle size of 350 to 500, BHT having a particle size of 50; The antipruritic agent according to crab.
  • the antipruritic agent of the present invention contains BHT as an active ingredient.
  • BHT exerts an antipruritic effect, and in particular, in the presence of both dissolved and solid BHT, solid BHT provides physical stimulation to the affected area in addition to the dissolved BHT antipruritic action. Because it can be used, it has immediate effect on suppressing itching. In general, when the itchy part is physically stimulated, the itching tends to be further enhanced.
  • the antipruritic agent of the present invention can suppress so-called itch reversal and has an excellent antipruritic effect. is there.
  • itch refers to "a sense that causes the idea of wanting to break the skin” as described above.
  • the antipruritic agent of the present invention is characterized mainly by containing BHT as an active ingredient.
  • BHT a component, production method, application and the like of the antipruritic agent of the present invention will be described.
  • the antipruritic agent of the present invention contains BHT as an active ingredient.
  • Ptylhydroxytoluene is a compound having a white crystal shape and is also called dibutylhydroxytoluene, but both refer to the same compound ([(CH 3) 2 C] 2 CH 3 (CH 2) 3 OH)).
  • BHT traditionally makeup It is blended for uses such as 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 blending amount of BHT in the present invention is not particularly limited, but it is 1.5% by weight or more in 100% by weight of the dissolved BHT, preferably 2 to about 15% by weight, more preferably 5 to about 15% by weight, more preferably 7.5 to about 15% by weight.
  • a particularly excellent antipruritic effect can be obtained and the preparation can be made stable.
  • the BHT is present in a solid state so that it is solid when applied to the affected area.
  • the state of BHT can give an appropriate physical stimulus to the affected area, replace itching with a feeling of irritation, and exert an excellent antipruritic effect.
  • “replacing itching with a sense of irritation” refers to making the skin sensation feel a stimulus other than “itching” (for example, itching) in the short term (instantaneously).
  • the particle diameter of the BHT is about 1000 m or less, preferably (about 1000 to 50 mm 111, more preferably (about 1000 to 00 mm). More preferably, it is about 1000 to about 180 m, where BHT having each particle diameter can be obtained by pulverizing BHT in a mortar or the like and then applying it to a sieve having each diameter.
  • BHT having a particle diameter of less than 350 111, BH having a particle diameter of 350 to 500 111, BH having a particle diameter of 501 to;
  • Preferred combinations include, for example, (a) 501 to; BHT having a particle size of about 1000 Hm and BHT having a particle size of about 350 to 500 ⁇ m (B) A combination of BHT having a particle size of less than 350 m and BHT having a particle size of about 350 to 500 ⁇ m.
  • 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 solid state of the antipruritic agent of the present invention is about 7.5 to 40% by weight, preferably 8 to 100% by weight in consideration of the antipruritic effect and the stability as the preparation. It is about 35% by weight, more preferably about 10-30% by weight.
  • the total amount of BHT in the antipruritic agent of the present invention is about 1.5% by weight or more, preferably about 7.5% by weight or more, more preferably about 9 to 45% by weight, and still more preferably 10 to 35%. It is about 10% by weight, particularly preferably about 10 to 30% by weight. With such a blending amount, the itching suppression effect of the present invention can be exerted more remarkably and can be made stable as a preparation.
  • the antipruritic agent of the present invention is blended with alcohol as necessary in addition to the BHT.
  • the alcohol can be used to dissolve BHT.
  • BHT can be dissolved by adding more than about 3 parts by weight of alcohol to 1 part by weight of BHT.
  • the alcohol used in the present invention is not particularly limited as long as it is generally used in the fields of cosmetics and pharmaceuticals.
  • Lower alcohol having 1 to 6 carbon atoms, preferably 1 to 3 carbon atoms, such as butanol, propanol, isopropanol, butanol, isobutanol; propylene glycol, dipropylene glycol, glycerin, 1,3-butylene glycol, butylene glycol, concentrated glycerin
  • polyhydric alcohols such as polyethylene glycol, maltitol, mannitol and sorbitol. These may be used alone or in combination of two or more.
  • the lower alcohol may be anhydrous or hydrated.
  • (hydrous) ethanol, absolute ethanol, and isopropanol are preferably used.
  • the blending amount of the alcohol in the antipruritic agent of the present invention is not particularly limited as long as the effects of the present invention are not impaired, but for example, about 0 to 92% by weight, preferably about 5 to 92% by weight, and more preferably. It is about 5 to 86.2% by weight, more preferably about 5 to 61% by weight.
  • the amount of alcohol is about 3 parts by weight or less, preferably 2 parts by weight or less, more preferably 1 part by weight or less with respect to 1 part by weight of BHT in the preparation. It is desirable to do.
  • the antipruritic agent of the present invention may contain water, a water-soluble polymer, or the like, if necessary.
  • a water-soluble polymer the ability to use a conventionally known polymer, for example, carboxyvininole polymer, polyvinyl alcohol, polyvinyl methyl ether, polyvinylino pechetil cellulose, pullulan, agar, gelatin, alginic acid and its salt, carrageenan And gums (for example, guar gum, tamarind gum, locust bean gum, cara gum, tragacanth gum) and the like. These may be used alone or in combination of two or more.
  • the amount of water in the antipruritic agent of the present invention is, for example, about 0 to 87% by weight, preferably about 3 to 86.2% by weight, more preferably about 28 to 80% by weight;
  • the blending amount is, for example, 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 35 weight BHT 0/0, the Anorekonore 5-86.
  • the antipruritic agent of the present invention includes, in addition to the above, various components generally used in cosmetics, quasi-drugs, and pharmaceuticals, aqueous components, oily components, moisturizing components, excipients as necessary. Further, thickeners, preservatives, antioxidants, pH adjusters, carriers, fragrances, colorants, drugs and the like can be prepared in various dosage forms singly or in combination of two or more. Further, the antipruritic agent of the present invention may contain a known local anesthetic, anti-inflammatory agent, moisturizing agent, etc.
  • Local anesthetics such as in, diphenhydramine, amino aminoethyl benzoate, desittecitin; chlorfeniramine maleate, diphenhydramine, diphenhydramine hydrochloride, glycyrrhetinic acid, dicalcium glycyrrhizinate, monoammonium glycyrrhizinate, allantoin, methyl salicylate; 1 Refreshing agents such as menthol, dl-menthol, camphor, dl-camphor, menthyl lactate; moisturizers such as urea, salicylic acid, sodium hyaluronate; isopropylmethylphenol (IPMP), quaternary ammonium salts (benzalkonium chloride, chloride) Benzetonium etc.
  • IPMP isopropylmethylphenol
  • IPMP quaternary ammonium salts
  • Chlorhexidine into hydrochloric chlorine disinfectant such Surufuajiajin; nitric Okishikonazoru, butenafine hydrochloride, hydrochloric Amororufuin, hydrochloric Terubinafuin, antifungal agents such as lanoconazole; capsicum tincture, and the like thermal components such Kabusaishin.
  • the dosage form of the antipruritic agent of the present invention includes forces that can be prepared into a conventionally known dosage form according to the method of use and application, for example, ointments, lotions, gels, aerosols and the like.
  • the antipruritic agent of the present invention contains an appropriate amount of a base for obtaining a desired dosage form.
  • a base for obtaining a desired dosage form.
  • examples include, but are not limited to, paraffin, petrolatum, squalane, paraffin, white wax, plastibase, polyethylene glycolore, macrogonole, lauromacronore, silicone oil, silicon, 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 (isopropyl myristate, sorbitan fatty acid esters, etc.)
  • the antipruritic agent of the present invention can be prepared by mixing 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 in the field according to the physical or chemical properties of each component, concentration, instrument stress, etc. For example, the following method can be cited.
  • a water phase is prepared by dissolving a water-soluble component in water. Separately from the aqueous phase, the alcohol-soluble component and BHT are dissolved in alcohol to prepare the alcohol phase. The obtained aqueous phase and alcohol phase are stirred and mixed so as to be homogeneous, whereby the antipruritic agent of the present invention can be obtained. In addition, when blending BHT in a solid state, it can be further added after stirring and mixing.
  • the antipruritic agent of the present invention can be used as an antipruritic agent that reduces itching (itchiness), and the application target is not particularly limited as long as it is used for this purpose.
  • the application target of the antipruritic agent of the present invention include itchy symptoms such as rashes, insect bites, dry skin, and hypersensitive skin.
  • an appropriate amount of the antipruritic agent of the present invention may be spread over the itchy skin. By spreading it out, it is possible to suppress itching by reversing the action of BHT. Furthermore, when BHT is blended in a solid state, moderate physical irritation is involved, so it is possible to control the itching more quickly with the power S.
  • Table 1 shows the evaluation results.
  • CVP carboxybulle polymer
  • HPC hydroxypropylcellulose
  • PG propylene glycol
  • EDTA ethylenediaminetetraacetic acid
  • Comparative Example 3 did not have a shape-retaining property! /, Exhibited a liquid state, and Comparative Example 6 exhibited a cloudy ointment.
  • the antipruritic agent containing two kinds of particle sizes containing BHT in a solid state can exhibit a superior effect of replacing itching with a feeling of irritation, that is, an immediate effect of suppressing itching.
  • This force S was shown.
  • dissolved BHT when contained at a low concentration of 1% by weight in the preparation, it can be used in combination with BHT in a solid state when it is used in combination with a solid state BHT. It has been shown that the action of substituting the sensation with a sense of stimulation supplements the itching effect of dissolved BHT and exerts an excellent itching effect as a whole (Example 6).
  • Formulation examples:! -23 25 and 26 are gel preparations (ointments).
  • Formulation Example 24 is a viscous liquid preparation. Formulation Example 24 requires force S to be filled with a propellant and made into an aerosol.

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

Abstract

L'invention a pour objet un agent antipruritique capable de supprimer le prurit causé par des piqûres d'insectes ou une hypersensibilité de la peau, et de le remplacer par une sensation de stimulation, de façon à supprimer instantanément le prurit. Cet agent antipruritique contient du butylhydroxytoluène en tant que principe actif.
PCT/JP2007/069110 2006-09-29 2007-09-28 Agent antipruritique WO2008038806A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2006-269952 2006-09-29
JP2006269952A JP5565995B2 (ja) 2006-09-29 2006-09-29 鎮痒剤

Publications (1)

Publication Number Publication Date
WO2008038806A1 true WO2008038806A1 (fr) 2008-04-03

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PCT/JP2007/069110 WO2008038806A1 (fr) 2006-09-29 2007-09-28 Agent antipruritique

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WO (1) WO2008038806A1 (fr)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20170093267A (ko) 2009-12-23 2017-08-14 메르크 파텐트 게엠베하 유기 반도성 화합물을 포함하는 조성물

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS63255219A (ja) * 1987-04-11 1988-10-21 Teikoku Seiyaku Kk 鎮痒プラスタ−
JPS63255224A (ja) * 1987-04-11 1988-10-21 Teikoku Seiyaku Kk 鎮痒プラスタ−
JPH04103526A (ja) * 1990-08-21 1992-04-06 Taisho Pharmaceut Co Ltd 皮膚冷却エアゾール剤
JPH07126158A (ja) * 1993-10-27 1995-05-16 Taisho Pharmaceut Co Ltd クロタミトン配合外用剤
JP2001233764A (ja) * 2000-02-22 2001-08-28 Hisamitsu Pharmaceut Co Inc Ｎ−置換−ｏ−トルイジン誘導体からなる鎮痒剤
WO2003047609A1 (fr) * 2001-12-05 2003-06-12 Johnson & Johnson Limited Formulation topique contre les demangeaisons et procede de preparation de celle-ci

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS63255219A (ja) * 1987-04-11 1988-10-21 Teikoku Seiyaku Kk 鎮痒プラスタ−
JPS63255224A (ja) * 1987-04-11 1988-10-21 Teikoku Seiyaku Kk 鎮痒プラスタ−
JPH04103526A (ja) * 1990-08-21 1992-04-06 Taisho Pharmaceut Co Ltd 皮膚冷却エアゾール剤
JPH07126158A (ja) * 1993-10-27 1995-05-16 Taisho Pharmaceut Co Ltd クロタミトン配合外用剤
JP2001233764A (ja) * 2000-02-22 2001-08-28 Hisamitsu Pharmaceut Co Inc Ｎ−置換−ｏ−トルイジン誘導体からなる鎮痒剤
WO2003047609A1 (fr) * 2001-12-05 2003-06-12 Johnson & Johnson Limited Formulation topique contre les demangeaisons et procede de preparation de celle-ci

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JP5565995B2 (ja) 2014-08-06
JP2008088094A (ja) 2008-04-17

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