WO2020004201A1 - COMPOSITION INCLUDING D-chiro-INOSITOL - Google Patents

COMPOSITION INCLUDING D-chiro-INOSITOL Download PDF

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Publication number
WO2020004201A1
WO2020004201A1 PCT/JP2019/024381 JP2019024381W WO2020004201A1 WO 2020004201 A1 WO2020004201 A1 WO 2020004201A1 JP 2019024381 W JP2019024381 W JP 2019024381W WO 2020004201 A1 WO2020004201 A1 WO 2020004201A1
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Prior art keywords
composition
inositol
surfactant
chiro
acid
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PCT/JP2019/024381
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French (fr)
Japanese (ja)
Inventor
信哉 宅見
公輔 田中
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小林製薬株式会社
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Publication of WO2020004201A1 publication Critical patent/WO2020004201A1/en

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    • 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
    • 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
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/45—Derivatives containing from 2 to 10 oxyalkylene groups
    • 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
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/86—Polyethers
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00—Preparations for affecting hair growth

Definitions

  • the present invention relates to a composition comprising D-chiro-inositol.
  • the present invention also relates to an external preparation containing the composition.
  • Inositol (1,2,3,4,5,6-cyclohexanehexaol) has a structure in which one hydrogen atom on each carbon of cyclohexane is replaced by one hydroxy group, and is known as a vitamin-like active substance. I have. Inositol has nine types of stereoisomers depending on the combination of hydroxy group configurations.
  • Patent Document 1 discloses a hair restorer containing inositol as an active ingredient.
  • “inositol” used in the prior art refers to myo-inositol (cis-1,2,3,5-trans-4) as an additive for pharmaceuticals, quasi-drugs, cosmetics, and the like. , 6-cyclohexanehexaol) (see, for example, Non-Patent Documents 1 to 3).
  • the present inventors have found that among stereoisomers of inositol, chiro-inositol is a compound useful as a hair restorer (see Patent Document 2).
  • D-chiro-inositol is a water-soluble compound among the isomers of inositol.
  • D-chiro-inositol was found to be an inositol stereoisomer as well as in aqueous solution. It has been found that a precipitate tends to be formed.
  • an object of the present invention is to provide a composition capable of suppressing the precipitation of D-chiro-inositol.
  • the present inventors have made intensive studies to solve the above-mentioned problems, and as a result, in an aqueous solution containing D-chiro-inositol, the composition further containing a surfactant suppresses the precipitation of D-chiro-inositol.
  • the present inventors have found that the composition can be used, and have completed the present invention.
  • a composition comprising D-chiro-inositol, a surfactant, and water.
  • the surfactant comprises a nonionic surfactant.
  • the nonionic surfactant comprises polyoxyethylene hydrogenated castor oil or polyoxyethylene polyoxypropylene alkyl ether.
  • An external preparation containing the composition according to any one of [1] to [5].
  • An external preparation for scalp comprising the composition according to any one of [1] to [5].
  • composition capable of suppressing the precipitation of D-chiro-inositol.
  • composition of the present invention is a composition containing D-chiro-inositol, a surfactant, and water.
  • D-chiro-inositol examples include, but are not particularly limited to, those extracted from naturally occurring buckwheat, beans, citrus, etc., those extracted and purified from legumes by fermentation, those chemically synthesized, and Commercial products can be mentioned.
  • the extraction method is not particularly limited, and a known extraction method can be used.
  • the content of D-chiro-inositol in the composition of the present invention is not particularly limited, but is preferably 0.001 to 20% by mass, more preferably 0.01 to 20% by mass, and still more preferably 0 to 20% by mass. 0.05 to 15% by mass, more preferably 1 to 10% by mass, still more preferably 3 to 7% by mass.
  • % by mass means the mass percentage of the components contained in the composition with respect to the mass of the entire composition.
  • X to Y means that it is X or more and Y or less.
  • the composition of the present invention can be used as an external preparation.
  • external preparations include, for example, agents for cracks and irrigations, agents for rashes and sores, agents for sea urchin and octopus, agents for dryness and irritations, agents for wrinkles and spots, humectants, hair dyes, hair restorers, shampoos, Rinse, conditioner, lotion, cream, milky lotion, hand cream, medicated soap, pack and the like can be mentioned.
  • the composition of the present invention contains D-chiro-inositol, a composition having a vitamin-like effect and a hair-growth activity can be obtained, and may be used as a hair-growth agent.
  • the hair growth activity is, specifically, an activity relating to hair shaft growth promotion, hair growth, prevention of hair loss, and the like, and preferably an activity relating to hair shaft growth promotion and hair growth.
  • the composition of the present invention contains a surfactant.
  • a surfactant By including a surfactant, it becomes possible to suppress the precipitation of D-chiro-inositol in an aqueous solution containing D-chiro-inositol.
  • a surfactant in the composition of the present invention it becomes possible to improve the feeling of use in a preparation containing the composition of the present invention. It is presumed that the factor that exerts such effects is due to the fact that the surfactant improves the solubility of D-chiro-inositol in an aqueous solution (however, the factor is not limited to this).
  • the surfactant examples include, but are not particularly limited to, a nonionic surfactant, a cationic surfactant, an anionic surfactant, and an amphoteric surfactant.
  • a nonionic surfactant is preferable from the viewpoint that a good feeling in use can be obtained.
  • One type of surfactant may be used alone, or two or more types may be used in combination.
  • the HLB value of the surfactant is not particularly limited, but is preferably 2 to 17, more preferably 6 to 17, and even more preferably 12 to 17.
  • HLB is an abbreviation for hydrophile-lipophile balance, and is one of the indices indicating the effect of a surfactant.
  • the HLB value when two or more surfactants are contained is a weighted average of the HLB values of each surfactant.
  • the nonionic surfactant means a surfactant that does not exhibit ionicity in an aqueous solution.
  • Nonionic surfactants include, but are not particularly limited to, for example, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene sorbitan oleate, monoesters of oleic acid and glycerin, and oleic acid. Esters of diglycerin.
  • polyoxyethylene hydrogenated castor oil and polyoxyethylene polyoxypropylene alkyl ether are preferred from the viewpoint of suppressing the precipitation of D-chiro-inositol and obtaining a good feeling in use.
  • the cationic surfactant and the anionic surfactant mean a surfactant that becomes a cation and an anion when dissociated in an aqueous solution, respectively, and the amphoteric surfactant has a pH of the aqueous solution in the aqueous solution.
  • Means a surfactant that becomes one of a cation, an anion, and a zwitterion depending on the Examples of the cationic surfactant include, but are not particularly limited to, alkyldimethylamine, alkyltrimethylammonium salt, and dialkyldimethylammonium salt.
  • the anionic surfactant include, but are not particularly limited to, fatty acid salts and alkyl sulfates.
  • Examples of the amphoteric surfactant include, but are not particularly limited to, alkylamino fatty acid salts, alkyl betaines, and alkylamine oxides.
  • the content of the surfactant in the composition of the present invention is not particularly limited, but is usually 0.1 to 10% by mass, preferably 0.5 to 7% by mass, and more preferably 1 to 5% by mass. It is.
  • the composition of the present invention may further include an organic acid or a salt thereof.
  • the composition of the present invention preferably contains an organic acid and a salt of the organic acid.
  • the feeling of use in a preparation containing the composition of the present invention can be improved. It tends to be. It is presumed that such an effect is attributable to the fact that the organic acid or a salt thereof exerts a chelating effect and functions to reduce the stimulus contributed by a solvent other than water, for example, a monoalcohol having 1 to 3 carbon atoms. (However, the factor is not limited to this.)
  • the organic acid means an organic compound which is acidic alone in water.
  • the organic acid is not particularly limited as long as it is an organic compound exhibiting acidity, and examples thereof include monocarboxylic acids and polycarboxylic acids, and organic sulfonic acids. Among these, polyvalent carboxylic acids are preferable from the viewpoint that a good feeling in use can be obtained.
  • the monocarboxylic acid means an organic compound having one carboxylic acid in the molecule
  • the polyvalent carboxylic acid means an organic compound having two or more carboxylic acids in the molecule
  • the organic sulfonic acid means an organic compound having at least one sulfonic acid in a molecule.
  • a monocarboxylic acid For example, Formic acid, acetic acid, propionic acid, and valeric acid are mentioned.
  • polyvalent carboxylic acid examples include, but are not particularly limited to, dicarboxylic acid, tricarboxylic acid, and tetracarboxylic acid, and include, for example, citric acid, edetic acid, phthalic acid, isophthalic acid, terephthalic acid, succinic acid, fumaric acid, and maleic acid. Acids, malic acid, and tartaric acid. Among these, citric acid and edetic acid are preferred.
  • Organic sulfonic acids include, but are not limited to, methanesulfonic acid, benzenesulfonic acid, and taurine.
  • the salt in the organic acid salt is not particularly limited, and includes, for example, a sodium salt, a potassium salt, a calcium salt, and a magnesium salt. Of these, sodium salts are preferred.
  • the organic acids or salts thereof may be used alone or in combination of two or more. When two or more kinds are used in combination, a combination of two or more kinds of organic acids or a combination of two or more kinds of salts of organic acids may be used. These may be used in combination. When an organic acid and a salt of the organic acid are used, the organic acid and the organic acid of the salt of the organic acid may be the same or different, but the organic acid and the salt of the organic acid are used in combination. Is preferred.
  • the content of the organic acid or a salt thereof in the composition of the present invention is not particularly limited, but is usually 0.001 to 5% by mass, preferably 0.01 to 3% by mass, more preferably 0.03% by mass. To 1% by mass, more preferably 0.05 to 1% by mass.
  • composition of the present invention contains water.
  • D-chiro-inositol contained in the composition of the present invention can be handled as an aqueous solution.
  • water examples include pure water such as ion-exchanged water, ultrafiltration water, reverse osmosis water, and distilled water, and water from which ionic impurities such as ultrapure water have been removed as much as possible.
  • composition of the present invention may further contain a mono- and / or polyhydric alcohol having 1 to 3 carbon atoms.
  • a monoalcohol having 1 to 3 carbon atoms and / or a polyhydric alcohol By containing a monoalcohol having 1 to 3 carbon atoms and / or a polyhydric alcohol, a composition having antibacterial properties and moisture retention tends to be obtained.
  • the monoalcohol having 1 to 3 carbon atoms is methanol, ethanol, n-propanol and isopropanol, preferably ethanol and isopropanol, and more preferably ethanol.
  • the polyhydric alcohol means an alcohol having two or more hydroxyl groups in a molecule.
  • glycerin ethylene glycol, diethylene glycol, triethylene glycol, propylene glycol (1,2-propanediol), dipropylene glycol, trimethylolpropane, 1,3-propylene glycol ( 1,3-propanediol), isobutylene glycol (2-methyl-1,2-propanediol), 1,2-butanediol, 1,3-butyleneglycol (1,3-butanediol), 1,4-butane Diol, 2-butene-1,4-diol, 1,2-pentanediol, 1,5-pentanediol, 2-methyl-2,4-pentanediol, 1,2-hexanediol, 1,6-hexanediol , 2-ethyl-1,3-hexanediol, 1, - heptanediol
  • the content of the mono-alcohol having 1 to 3 carbon atoms in the composition of the present invention is not particularly limited, but the content of the mono-alcohol having 1 to 3 carbon atoms can be set high.
  • the content of the monoalcohol having 1 to 3 carbon atoms in the composition of the present invention is usually 80% by mass or less, may be 60% by mass or less, may be 30 to 60% by mass, and may be 30 to 50% by mass. Or 30 to 40% by mass.
  • the content of the polyhydric alcohol in the composition of the present invention is not particularly limited, but is usually 0.1% by mass or more, preferably 0.5% by mass, more preferably 0.5 to 30% by mass. And more preferably 0.5 to 20% by mass, and still more preferably 0.5 to 15% by mass.
  • the composition of the present invention may further include a monoterpene.
  • a monoterpene By containing a monoterpene, there is a tendency that a refreshing feeling can be imparted and a composition excellent in suppressing the precipitation of D-chiro-inositol can be obtained.
  • monoterpene examples include, but are not particularly limited to, monoterpene hydrocarbons such as limonene, pinene, and camphor; monoterpene alcohols such as citronellol, geraniol, linalool, menthol, terpineol, and borneol; monoterpenes such as citronellal, citral, and safranal Aldehydes; monoterpene ketones such as menthone, carbomentone, and yonone; Preferably, it is a monoterpene alcohol, and more preferably, menthol. These monoterpenes may be d-, l-, or dl-form.
  • menthol for example, l-menthol and d-menthol are preferred, and l-menthol is more preferred. It may be used as a mixture of 1-menthol and d-menthol. Monoterpenes may be used alone or in combination of two or more.
  • the content of the monoterpene in the composition of the present invention is not particularly limited, but in addition to imparting a refreshing feeling, suppressing precipitation of D-chiro-inositol, suppressing dripping and irritating feeling (crisp feeling) of the obtained composition. And 0.01 to 10% by mass, more preferably 0.05 to 2% by mass, and still more preferably 0.1 to 1.0% by mass because of excellent suppression of separation of the monoterpene itself. %, And still more preferably 0.7 to 1.0% by mass.
  • composition of the present invention may further contain additives that are generally acceptable in pharmaceuticals, quasi-drugs, cosmetics, and the like.
  • additives include, but are not limited to, excipients, stabilizers, odor correctors, bases, dispersants, diluents, emulsifiers, transdermal absorption enhancers, preservatives, coloring agents, oils (oils, fats, minerals, Oil, etc.), thickeners, polymers, film-forming agents, ultraviolet absorbers, cell activators, antioxidants, preservatives, fresheners, deodorants, pigments, dyes, fragrances, sugars, amino acids, vitamins, Organic acids, organic amines, plant extracts and the like can be mentioned.
  • the composition of the present invention is not particularly limited, and can be produced by mixing components contained in the present invention.
  • the order of mixing the components is not particularly limited.
  • the conditions for mixing are not particularly limited, and the composition of the present invention can be obtained according to a conventionally known method.
  • the composition of the present invention when used as an external preparation, it can be used as a drug, a quasi-drug, a cosmetic or the like.
  • it can be used as an external preparation for skin, an external preparation for hair, and an external preparation for scalp, and more specifically, a dermatological drug, a hair drug and a scalp drug, a quasi-drug for skin, and a hair
  • It can be used for quasi-drugs and quasi-drugs, as well as skin cosmetics, hair cosmetics and scalp cosmetics. More specifically, it can be in the form of an ointment, cataplasm, liniment, lotion, topical solution, dusting agent, cream, gel, emulsion, hair tonic, hair spray.
  • the “external preparation for hair” and the “external preparation for scalp” may be the same or different in the form and usage as the external preparation. Or scalp.
  • “external preparation for skin” is a concept including “external preparation for scalp” and means an external preparation that acts directly on the skin without being limited to the scalp.
  • the method of the invention comprises the step of administering a composition of the invention to a subject.
  • the dose of D-chiro-inositol per administration to a subject is not particularly limited, but is preferably 0.005 to 200 mg, more preferably 0.05 to 100 mg, and still more preferably 0.5 to 100 mg. 10 mg.
  • the frequency of administration of the composition of the present invention to a subject is not particularly limited, but is preferably 1 to 6 times per day, more preferably 1 to 3 times per day, and still more preferably 1 to 3 times per day. ⁇ 2 times.
  • composition of the present invention is administered is not particularly limited, and includes, for example, humans, animals such as domestic animals and pets.
  • Example 1 DCI was dissolved in purified water so that each component had the composition shown in Table 1 below, a surfactant was added, and the remaining volume was diluted and mixed with purified water to prepare each composition as a preparation.
  • Formulation stability test The obtained preparations were evaluated for DCI precipitation in surfactants of each type and content by the following method. Formulations of each composition were prepared in 3 lots, DCI precipitation was induced by a low-temperature cycle (12 hours 5 ° C incubation, 12 hours -20 ° C repeated for 28 days), and visually evaluated based on the following indices did. The evaluation results are shown in Table 1 (the number of N is 3). In all lots, no precipitation of crystals was observed " ⁇ " Even with 1Lot, slight precipitation of crystalline material was observed " ⁇ " Even with 1 Lot, a small number of crystals were precipitated. Even with 1 Lot, many crystals precipitated
  • Degree of improvement (%) 100 ⁇ (Average of questionnaire results in formulations without surfactant in Table 1 ⁇ Average of questionnaire results in formulations containing surfactant) / Questionnaire results in formulations without surfactant in Table 1
  • the average relative value of the results of the questionnaire in the “surfactant-containing preparation” when the value was 100.0 was calculated as the degree of improvement.

Abstract

[Problem] To provide a composition that makes it possible to suppress deposition of D-chiro-inositol. [Solution] This composition includes D-chiro-inositol, a surfactant, and water.

Description

Ｄ－ｃｈｉｒｏ－イノシトールを含む組成物Composition comprising D-chiro-inositol

　本発明は、Ｄ－ｃｈｉｒｏ－イノシトールを含む組成物に関する。また、本発明は、該組成物を含む外用剤に関する。
The present invention relates to a composition comprising D-chiro-inositol. The present invention also relates to an external preparation containing the composition.

　イノシトール（１，２，３，４，５，６－シクロヘキサンヘキサオール）は、シクロヘキサンの各炭素上の水素原子が１つずつヒドロキシ基に置換した構造を有し、ビタミン様作用物質として知られている。イノシトールは、ヒドロキシ基の立体配置の組み合わせにより、９種類の立体異性体が存在する。
Inositol (1,2,3,4,5,6-cyclohexanehexaol) has a structure in which one hydrogen atom on each carbon of cyclohexane is replaced by one hydroxy group, and is known as a vitamin-like active substance. I have. Inositol has nine types of stereoisomers depending on the combination of hydroxy group configurations.

　特許文献１には、イノシトールを有効成分として含有する育毛剤が開示されている。特許文献１におけるように、先行文献において使用される「イノシトール」とは、医薬品、医薬部外品又は化粧品等の添加物として、ｍｙｏ－イノシトール（シス－１，２，３，５－トランス－４，６－シクロヘキサンヘキサオール）の立体異性体を通常意味する（例えば非特許文献１～３参照）。

　また、本発明者らは、イノシトールの立体異性体の内、ｃｈｉｒｏ－イノシトールが、育毛剤として有用な化合物であることを見出した（特許文献２参照）。
Patent Document 1 discloses a hair restorer containing inositol as an active ingredient. As in Patent Document 1, “inositol” used in the prior art refers to myo-inositol (cis-1,2,3,5-trans-4) as an additive for pharmaceuticals, quasi-drugs, cosmetics, and the like. , 6-cyclohexanehexaol) (see, for example, Non-Patent Documents 1 to 3).

In addition, the present inventors have found that among stereoisomers of inositol, chiro-inositol is a compound useful as a hair restorer (see Patent Document 2).

特開２００６－２８０２６号公報JP 2006-28026 A 国際公開第２０１７／１８８３９３号WO 2017/188393


　ここで、本発明者らは、イノシトールの立体異性体の内、Ｄ－ｃｈｉｒｏ－イノシトールは、イノシトールの異性体の中でも水溶性を有する化合物であることを見出した。

　しかしながら、これらのＤ－ｃｈｉｒｏ－イノシトールの特性を生かすべく、Ｄ－ｃｈｉｒｏ－イノシトールを含む組成物についての研究を続ける中で、Ｄ－ｃｈｉｒｏ－イノシトールは、イノシトールの立体異性体の内でも水溶液中で析出物を生成し易い傾向にあることを発見した。
Here, the present inventors have found that, among the stereoisomers of inositol, D-chiro-inositol is a water-soluble compound among the isomers of inositol.

However, while continuing to study compositions containing D-chiro-inositol in order to take advantage of these properties of D-chiro-inositol, D-chiro-inositol was found to be an inositol stereoisomer as well as in aqueous solution. It has been found that a precipitate tends to be formed.

　そこで、本発明は、Ｄ－ｃｈｉｒｏ－イノシトールの析出を抑制することの可能な組成物を提供することを目的とする。
Accordingly, an object of the present invention is to provide a composition capable of suppressing the precipitation of D-chiro-inositol.

　本発明者らは、上記課題を解決するために鋭意研究を重ねた結果、Ｄ－ｃｈｉｒｏ－イノシトールを含む水溶液内において、界面活性剤をさらに含む組成物が、Ｄ－ｃｈｉｒｏ－イノシトールの析出を抑制することの可能な組成物であることを見出し、本発明を完成するに至った。
The present inventors have made intensive studies to solve the above-mentioned problems, and as a result, in an aqueous solution containing D-chiro-inositol, the composition further containing a surfactant suppresses the precipitation of D-chiro-inositol. The present inventors have found that the composition can be used, and have completed the present invention.

　すなわち、本発明は、以下の発明を提供する。

［１］　Ｄ－ｃｈｉｒｏ－イノシトールと界面活性剤と水とを含む、組成物。

［２］　Ｄ－ｃｈｉｒｏ－イノシトールの含有量が０．００１～２０質量％である、［１］に記載の組成物。

［３］　界面活性剤がノニオン性界面活性剤を含む、［１］又は［２］に記載の組成物。

［４］　界面活性剤のＨＬＢ値が、２～１７である、［１］～［３］のいずれかに記載の組成物。

［５］　ノニオン性界面活性剤がポリオキシエチレン硬化ヒマシ油又はポリオキシエチレンポリオキシプロピレンアルキルエーテルを含む、［１］～［４］のいずれかに記載の組成物。

［６］　［１］～［５］のいずれかに記載の組成物を含む外用剤。

［７］　［１］～［５］のいずれかに記載の組成物を含む頭皮用外用剤。
That is, the present invention provides the following inventions.

[1] A composition comprising D-chiro-inositol, a surfactant, and water.

[2] The composition according to [1], wherein the content of D-chiro-inositol is 0.001 to 20% by mass.

[3] The composition according to [1] or [2], wherein the surfactant comprises a nonionic surfactant.

[4] The composition according to any one of [1] to [3], wherein the surfactant has an HLB value of 2 to 17.

[5] The composition according to any one of [1] to [4], wherein the nonionic surfactant comprises polyoxyethylene hydrogenated castor oil or polyoxyethylene polyoxypropylene alkyl ether.

[6] An external preparation containing the composition according to any one of [1] to [5].

[7] An external preparation for scalp, comprising the composition according to any one of [1] to [5].

　本発明によれば、Ｄ－ｃｈｉｒｏ－イノシトールの析出を抑制することの可能な組成物が提供される。
According to the present invention, there is provided a composition capable of suppressing the precipitation of D-chiro-inositol.

　以下、本発明の組成物及びその具体的な実施形態を説明することにより、本発明を明らかにする。しかし、本発明は、以下で説明する具体的な実施形態に限定されるものではない。
Hereinafter, the present invention will be clarified by describing the composition of the present invention and specific embodiments thereof. However, the present invention is not limited to the specific embodiments described below.

　本発明の組成物は、Ｄ－ｃｈｉｒｏ－イノシトールと界面活性剤と水とを含む組成物である。
The composition of the present invention is a composition containing D-chiro-inositol, a surfactant, and water.

　Ｄ－ｃｈｉｒｏ－イノシトールとしては、特に限定されないが、例えば、天然に存在する蕎麦、豆類、柑橘類等から抽出したもの、発酵法によりマメ科植物から精製して抽出したもの、化学合成したもの、及び市販品が挙げられる。ここで、抽出する方法としては、特に限定されず、公知の抽出法を用いることができる。
Examples of D-chiro-inositol include, but are not particularly limited to, those extracted from naturally occurring buckwheat, beans, citrus, etc., those extracted and purified from legumes by fermentation, those chemically synthesized, and Commercial products can be mentioned. Here, the extraction method is not particularly limited, and a known extraction method can be used.

　本発明の組成物におけるＤ－ｃｈｉｒｏ－イノシトールの含有量は、特に限定されないが、好ましくは０．００１～２０質量％であり、より好ましくは０．０１～２０質量％であり、さらに好ましくは０．０５～１５質量％であり、よりさらに好ましくは１～１０質量％であり、さらにより好ましくは３～７質量％である。
The content of D-chiro-inositol in the composition of the present invention is not particularly limited, but is preferably 0.001 to 20% by mass, more preferably 0.01 to 20% by mass, and still more preferably 0 to 20% by mass. 0.05 to 15% by mass, more preferably 1 to 10% by mass, still more preferably 3 to 7% by mass.

　本明細書において、「質量％」とは、組成物全体の質量に対する組成物に含有される成分の質量百分率を意味する。

　また、本明細書において「Ｘ～Ｙ」と表記する場合は、Ｘ以上Ｙ以下であることを意味する。
In the present specification, “% by mass” means the mass percentage of the components contained in the composition with respect to the mass of the entire composition.

Further, in the present specification, the expression “X to Y” means that it is X or more and Y or less.

　本発明の組成物は、外用剤として使用し得る。外用剤としては、例えば、ひび・あかぎれ用剤、あせも・ただれ用剤、うおのめ・たこ用剤、かさつき・あれ用剤、しわ・しみ用剤、保湿剤、染毛剤、育毛剤、シャンプー、リンス、コンディショナー、化粧水、クリーム、乳液、ハンドクリーム、薬用石鹸、及びパック等が挙げられる。

　本発明の組成物は、Ｄ－ｃｈｉｒｏ－イノシトールを含むことにより、ビタミン様作用や育毛活性を付与した組成物を得ることができ、育毛剤として使用してもよい。

　育毛活性は、具体的には、毛幹成長促進、発毛、脱毛防止等に関する活性であり、好ましくは毛幹成長促進及び発毛に関する活性である。
The composition of the present invention can be used as an external preparation. Examples of external preparations include, for example, agents for cracks and irrigations, agents for rashes and sores, agents for sea urchin and octopus, agents for dryness and irritations, agents for wrinkles and spots, humectants, hair dyes, hair restorers, shampoos, Rinse, conditioner, lotion, cream, milky lotion, hand cream, medicated soap, pack and the like can be mentioned.

Since the composition of the present invention contains D-chiro-inositol, a composition having a vitamin-like effect and a hair-growth activity can be obtained, and may be used as a hair-growth agent.

The hair growth activity is, specifically, an activity relating to hair shaft growth promotion, hair growth, prevention of hair loss, and the like, and preferably an activity relating to hair shaft growth promotion and hair growth.

　本発明の組成物は、界面活性剤を含む。

　界面活性剤を含むことにより、Ｄ－ｃｈｉｒｏ－イノシトールを含む水溶液において、Ｄ－ｃｈｉｒｏ－イノシトールの析出を抑制することが可能となる。また、本発明の組成物において、界面活性剤を含むことにより、本発明の組成物を含む製剤における使用感を向上させることが可能となる。このような効果を奏する要因は、界面活性剤がＤ－ｃｈｉｒｏ－イノシトールの水溶液に対する溶解性を向上させることによるものと推察される（ただし、要因はこれに限定されない。）。
The composition of the present invention contains a surfactant.

By including a surfactant, it becomes possible to suppress the precipitation of D-chiro-inositol in an aqueous solution containing D-chiro-inositol. In addition, by including a surfactant in the composition of the present invention, it becomes possible to improve the feeling of use in a preparation containing the composition of the present invention. It is presumed that the factor that exerts such effects is due to the fact that the surfactant improves the solubility of D-chiro-inositol in an aqueous solution (however, the factor is not limited to this).

　界面活性剤としては、特に限定されないが、ノニオン性界面活性剤、カチオン性界面活性剤、アニオン性界面活性剤、及び両性界面活性剤が挙げられる。これらの中では、良好な使用感が得られるという観点から、ノニオン性界面活性剤が好ましい。

　界面活性剤は、１種を単独で使用してもよく、２種以上を組み合わせて使用してもよい。
Examples of the surfactant include, but are not particularly limited to, a nonionic surfactant, a cationic surfactant, an anionic surfactant, and an amphoteric surfactant. Among these, a nonionic surfactant is preferable from the viewpoint that a good feeling in use can be obtained.

One type of surfactant may be used alone, or two or more types may be used in combination.

　界面活性剤のＨＬＢ値は、特に限定されないが、２～１７であることが好ましく、６～１７であることがより好ましく、１２～１７であることがさらに好ましい。ＨＬＢ値がこのような範囲にある界面活性剤を用いることにより、Ｄ－ｃｈｉｒｏ－イノシトールの析出が軽減される傾向にある。なお、ＨＬＢは、親水親油バランス（hydrophile-lipophile balance）の略称であり、界面活性剤が果たす効果を表す指標の一つであり、ＨＬＢ値が大きいほど親水性が高いことを示す。本発明におけるＨＬＢ値とは、Daviesの式であるＨＬＢ＝７＋Σ（親水基の基数）－Σ（親油基の基数）によって算出した値をいう（以下、単に「ＨＬＢ値」という場合に同じ。）。また、２種以上の界面活性剤を含有する場合のＨＬＢ値は、各界面活性剤のＨＬＢ値の加重平均値である。
The HLB value of the surfactant is not particularly limited, but is preferably 2 to 17, more preferably 6 to 17, and even more preferably 12 to 17. By using a surfactant having an HLB value in such a range, the precipitation of D-chiro-inositol tends to be reduced. HLB is an abbreviation for hydrophile-lipophile balance, and is one of the indices indicating the effect of a surfactant. The larger the HLB value, the higher the hydrophilicity. The HLB value in the present invention refers to a value calculated by HLB = 7 + Σ (the number of hydrophilic groups) −Σ (the number of lipophilic groups) which is a formula of Davies (hereinafter, simply referred to as “HLB value”). ). The HLB value when two or more surfactants are contained is a weighted average of the HLB values of each surfactant.

　ノニオン性界面活性剤とは、水溶液中でイオン性を示さない界面活性剤を意味する。

　ノニオン性界面活性剤としては、特に限定されないが、例えば、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンポリオキシプロピレンアルキルエーテル、オレイン酸ポリオキシエチレンソルビタン、オレイン酸とグリセリンのモノエステル、及びオレイン酸とジグリセリンのエステルが挙げられる。これらの中では、Ｄ－ｃｈｉｒｏ－イノシトールの析出の抑制の観点及び良好な使用感が得られるという観点から、ポリオキシエチレン硬化ヒマシ油及びポリオキシエチレンポリオキシプロピレンアルキルエーテルが好ましい。
The nonionic surfactant means a surfactant that does not exhibit ionicity in an aqueous solution.

Nonionic surfactants include, but are not particularly limited to, for example, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene sorbitan oleate, monoesters of oleic acid and glycerin, and oleic acid. Esters of diglycerin. Among these, polyoxyethylene hydrogenated castor oil and polyoxyethylene polyoxypropylene alkyl ether are preferred from the viewpoint of suppressing the precipitation of D-chiro-inositol and obtaining a good feeling in use.

　カチオン性界面活性剤及びアニオン性界面活性剤とは、それぞれ、水溶液中で解離したときに陽イオン及び陰イオンとなる界面活性剤を意味し、両性界面活性剤は、水溶液中で該水溶液のｐＨに応じて陽イオン、陰イオン、及び両性イオンのいずれかとなる界面活性剤を意味する。

　カチオン性界面活性剤としては、特に限定されないが、例えば、アルキルジメチルアミン、アルキルトリメチルアンモニウム塩、及びジアルキルジメチルアンモニウム塩が挙げられる。

　アニオン性界面活性剤としては、特に限定されないが、例えば、脂肪酸塩、及びアルキル硫酸塩が挙げられる。

　両性界面活性剤としては、特に限定されないが、例えば、アルキルアミノ脂肪酸塩、アルキルベタイン、及びアルキルアミンオキシドが挙げられる。
The cationic surfactant and the anionic surfactant mean a surfactant that becomes a cation and an anion when dissociated in an aqueous solution, respectively, and the amphoteric surfactant has a pH of the aqueous solution in the aqueous solution. Means a surfactant that becomes one of a cation, an anion, and a zwitterion depending on the

Examples of the cationic surfactant include, but are not particularly limited to, alkyldimethylamine, alkyltrimethylammonium salt, and dialkyldimethylammonium salt.

Examples of the anionic surfactant include, but are not particularly limited to, fatty acid salts and alkyl sulfates.

Examples of the amphoteric surfactant include, but are not particularly limited to, alkylamino fatty acid salts, alkyl betaines, and alkylamine oxides.

　本発明の組成物における界面活性剤の含有量は、特に限定されないが、通常０．１～１０質量％であり、好ましくは０．５～７質量％であり、より好ましくは１～５質量％である。
The content of the surfactant in the composition of the present invention is not particularly limited, but is usually 0.1 to 10% by mass, preferably 0.5 to 7% by mass, and more preferably 1 to 5% by mass. It is.

　本発明の組成物は、有機酸又はその塩をさらに含んでもよい。また、特に限定されないが、本発明の組成物は、有機酸と有機酸の塩とを含むことが好ましい。

　有機酸又はその塩を含むことにより、水以外の溶媒、例えば炭素数１～３のモノアルコールをさらに含む場合であっても、本発明の組成物を含む製剤における使用感を向上させることが可能となる傾向にある。このような効果を奏する要因は、有機酸又はその塩がキレート作用を発揮し、水以外の溶媒、例えば炭素数１～３のモノアルコールが寄与する刺激を緩和するよう機能することによるものと推察される（ただし、要因はこれに限定されない。）。
The composition of the present invention may further include an organic acid or a salt thereof. Although not particularly limited, the composition of the present invention preferably contains an organic acid and a salt of the organic acid.

By containing an organic acid or a salt thereof, even when the composition further contains a solvent other than water, for example, a monoalcohol having 1 to 3 carbon atoms, the feeling of use in a preparation containing the composition of the present invention can be improved. It tends to be. It is presumed that such an effect is attributable to the fact that the organic acid or a salt thereof exerts a chelating effect and functions to reduce the stimulus contributed by a solvent other than water, for example, a monoalcohol having 1 to 3 carbon atoms. (However, the factor is not limited to this.)

　有機酸とは、水中において単体で酸性を示す有機化合物を意味する。

　有機酸としては、酸性を示す有機化合物であれば特に限定されないが、モノカルボン酸及び多価カルボン酸、並びに有機スルホン酸が挙げられる。これらの中では、良好な使用感が得られるという観点から、多価カルボン酸が好ましい。
The organic acid means an organic compound which is acidic alone in water.

The organic acid is not particularly limited as long as it is an organic compound exhibiting acidity, and examples thereof include monocarboxylic acids and polycarboxylic acids, and organic sulfonic acids. Among these, polyvalent carboxylic acids are preferable from the viewpoint that a good feeling in use can be obtained.

　モノカルボン酸とは、分子内にカルボン酸を１個もつ有機化合物を意味し、多価カルボン酸とは、分子内にカルボン酸を２個以上もつ有機化合物を意味する。

　有機スルホン酸とは、分子内にスルホン酸を少なくとも１個もつ有機化合物を意味する。

　モノカルボン酸としては、特に限定されないが、例えば、ギ酸、酢酸、プロピオン酸、及び吉草酸が挙げられる。

　多価カルボン酸としては、特に限定されないが、ジカルボン酸、トリカルボン酸、テトラカルボン酸等が挙げられ、例えば、クエン酸、エデト酸、フタル酸、イソフタル酸、テレフタル酸、コハク酸、フマル酸、マレイン酸、リンゴ酸、及び酒石酸が挙げられる。これらの中では、クエン酸及びエデト酸が好ましい。

　有機スルホン酸としては、特に限定されないが、メタンスルホン酸、ベンゼンスルホン酸、及びタウリンが挙げられる。

　有機酸の塩における塩としては、特に限定されないが、例えば、ナトリウム塩、カリウム塩、カルシウム塩、及びマグネシウム塩が挙げられる。これらの中では、ナトリウム塩が好ましい。
The monocarboxylic acid means an organic compound having one carboxylic acid in the molecule, and the polyvalent carboxylic acid means an organic compound having two or more carboxylic acids in the molecule.

The organic sulfonic acid means an organic compound having at least one sulfonic acid in a molecule.

Although it does not specifically limit as a monocarboxylic acid, For example, Formic acid, acetic acid, propionic acid, and valeric acid are mentioned.

Examples of the polyvalent carboxylic acid include, but are not particularly limited to, dicarboxylic acid, tricarboxylic acid, and tetracarboxylic acid, and include, for example, citric acid, edetic acid, phthalic acid, isophthalic acid, terephthalic acid, succinic acid, fumaric acid, and maleic acid. Acids, malic acid, and tartaric acid. Among these, citric acid and edetic acid are preferred.

Organic sulfonic acids include, but are not limited to, methanesulfonic acid, benzenesulfonic acid, and taurine.

The salt in the organic acid salt is not particularly limited, and includes, for example, a sodium salt, a potassium salt, a calcium salt, and a magnesium salt. Of these, sodium salts are preferred.

　有機酸又はその塩は、１種を単独で使用してもよく、２種以上を組み合わせて使用してもよい。２種以上を組み合わせて使用する場合、２種以上の有機酸の組み合わせであってもよく、２種以上の有機酸の塩の組み合わせであってもよく、有機酸と有機酸の塩を2種以上組み合わせて用いてもよい。

　有機酸と有機酸の塩とを用いる場合において、有機酸と、有機酸の塩の有機酸とは、同一でも異なっていてもよいが、有機酸と、当該有機酸の塩とを組み合わせて用いることが好ましい。
The organic acids or salts thereof may be used alone or in combination of two or more. When two or more kinds are used in combination, a combination of two or more kinds of organic acids or a combination of two or more kinds of salts of organic acids may be used. These may be used in combination.

When an organic acid and a salt of the organic acid are used, the organic acid and the organic acid of the salt of the organic acid may be the same or different, but the organic acid and the salt of the organic acid are used in combination. Is preferred.

　本発明の組成物における有機酸又はその塩の含有量は、特に限定されないが、通常０．００１～５質量％であり、好ましくは０．０１～３質量％であり、より好ましくは０．０３～１質量％であり、さらに好ましくは０．０５～１質量％である。
The content of the organic acid or a salt thereof in the composition of the present invention is not particularly limited, but is usually 0.001 to 5% by mass, preferably 0.01 to 3% by mass, more preferably 0.03% by mass. To 1% by mass, more preferably 0.05 to 1% by mass.

　本発明の組成物は、水を含む。

　水を含むことにより、本発明の組成物に含まれるＤ－ｃｈｉｒｏ－イノシトールを水溶液として扱うことができる。
The composition of the present invention contains water.

By containing water, D-chiro-inositol contained in the composition of the present invention can be handled as an aqueous solution.

　水としては、例えば、イオン交換水、限外濾過水、逆浸透水、及び蒸留水等の純水、並びに超純水のような、イオン性不純物を極力除去したものが挙げられる。
Examples of the water include pure water such as ion-exchanged water, ultrafiltration water, reverse osmosis water, and distilled water, and water from which ionic impurities such as ultrapure water have been removed as much as possible.

　本発明の組成物は、炭素数１～３のモノアルコール及び／又は多価アルコールをさらに含んでもよい。

　炭素数１～３のモノアルコール及び／又は多価アルコールを含むことにより、抗菌性及び保湿性を付与した組成物を得ることができる傾向にある。
The composition of the present invention may further contain a mono- and / or polyhydric alcohol having 1 to 3 carbon atoms.

By containing a monoalcohol having 1 to 3 carbon atoms and / or a polyhydric alcohol, a composition having antibacterial properties and moisture retention tends to be obtained.

　炭素数１～３のモノアルコールとしては、メタノール、エタノール、ｎ－プロパノール、及びイソプロパノールであり、エタノール、イソプロパノールが好ましく、エタノールがさらに好ましい。

　多価アルコールとは、分子内に水酸基を２個以上もつアルコールを意味する。　多価アルコールとしては、特に限定されないが、例えば、グリセリン、エチレングリコール、ジエチレングリコール、トリエチレングリコール、プロピレングリコール（１，２－プロパンジオール）、ジプロピレングリコール、トリメチロールプロパン、１，３－プロピレングリコール（１，３－プロパンジオール）、イソブチレングリコール（２－メチル－１，２－プロパンジオール）、１，２－ブタンジオール、１，３－ブチレングリコール（１，３－ブタンジオール）、１，４－ブタンジオール、２－ブテン－１，４－ジオール、１，２－ペンタンジオール、１，５－ペンタンジオール、２－メチル－２，４－ペンタンジオール、１，２－ヘキサンジオール、１，６－ヘキサンジオール、２－エチル－１，３－ヘキサンジオール、１，７－ヘプタンジオール、及び１，８－オクタンジオール等が挙げられる。これらの中では、グリセリン、プロピレングリコール、及び１，３－ブチレングリコールが好ましい。

　炭素数１～３のモノアルコール及び多価アルコールは、それぞれ独立に、１種を単独で使用してもよく、２種以上を組み合わせて使用してもよい。
The monoalcohol having 1 to 3 carbon atoms is methanol, ethanol, n-propanol and isopropanol, preferably ethanol and isopropanol, and more preferably ethanol.

The polyhydric alcohol means an alcohol having two or more hydroxyl groups in a molecule. Although it does not specifically limit as a polyhydric alcohol, For example, glycerin, ethylene glycol, diethylene glycol, triethylene glycol, propylene glycol (1,2-propanediol), dipropylene glycol, trimethylolpropane, 1,3-propylene glycol ( 1,3-propanediol), isobutylene glycol (2-methyl-1,2-propanediol), 1,2-butanediol, 1,3-butyleneglycol (1,3-butanediol), 1,4-butane Diol, 2-butene-1,4-diol, 1,2-pentanediol, 1,5-pentanediol, 2-methyl-2,4-pentanediol, 1,2-hexanediol, 1,6-hexanediol , 2-ethyl-1,3-hexanediol, 1, - heptanediol, and 1,8-octanediol, and the like. Of these, glycerin, propylene glycol and 1,3-butylene glycol are preferred.

Mono- and polyhydric alcohols having 1 to 3 carbon atoms may be used alone or in combination of two or more.

　本発明の組成物における炭素数１～３のモノアルコールの含有量は、特に限定されないが、炭素数１～３のモノアルコールの含有量を高く設定することも可能である。

　本発明の組成物における炭素数１～３のモノアルコールの含有量は、通常８０質量％以下であり、６０質量％以下としてもよく、３０～６０質量％としてもよく、３０～５０質量％としてもよく、３０～４０質量％としてもよい。
The content of the mono-alcohol having 1 to 3 carbon atoms in the composition of the present invention is not particularly limited, but the content of the mono-alcohol having 1 to 3 carbon atoms can be set high.

The content of the monoalcohol having 1 to 3 carbon atoms in the composition of the present invention is usually 80% by mass or less, may be 60% by mass or less, may be 30 to 60% by mass, and may be 30 to 50% by mass. Or 30 to 40% by mass.

　本発明の組成物における多価アルコールの含有量は、特に限定されないが、通常０．１質量％以上であり、好ましくは０．５質量％であり、より好ましくは０．５～３０質量％であり、さらに好ましくは０．５～２０質量％であり、よりさらに好ましくは０．５～１５質量％である。
The content of the polyhydric alcohol in the composition of the present invention is not particularly limited, but is usually 0.1% by mass or more, preferably 0.5% by mass, more preferably 0.5 to 30% by mass. And more preferably 0.5 to 20% by mass, and still more preferably 0.5 to 15% by mass.

　本発明の組成物は、モノテルペンをさらに含んでもよい。

　モノテルペンを含むことにより、清涼感を付与するとともに、Ｄ－ｃｈｉｒｏ－イノシトールの析出抑制により優れた組成物を得ることができる傾向にある。
The composition of the present invention may further include a monoterpene.

By containing a monoterpene, there is a tendency that a refreshing feeling can be imparted and a composition excellent in suppressing the precipitation of D-chiro-inositol can be obtained.

　モノテルペンとしては、特に制限されないが、リモネン、ピネン、カンフル等のモノテルペン系炭化水素；シトロネロール、ゲラニオール、リナロール、メントール、テルピネオール、ボルネオール等のモノテルペン系アルコール；シトロネラール、シトラール、サフラナール等のモノテルペン系アルデヒド；メントン、カルボメントン、ヨノン等のモノテルペン系ケトン等が挙げられる。好ましくはモノテルペン系アルコールであり、より好ましくはメントールである。これらのモノテルペンは、ｄ－，ｌ－，ｄｌ－体のいずれでもよい。特にメントールとしては、例えば、ｌ－メントール及びｄ－メントールが好ましく、ｌ－メントールがより好ましい。ｌ－メントール及びｄ－メントールの混合物として使用してもよい。

　モノテルペンは、１種を単独で使用してもよく、２種以上を組み合わせて使用してもよい。
Examples of the monoterpene include, but are not particularly limited to, monoterpene hydrocarbons such as limonene, pinene, and camphor; monoterpene alcohols such as citronellol, geraniol, linalool, menthol, terpineol, and borneol; monoterpenes such as citronellal, citral, and safranal Aldehydes; monoterpene ketones such as menthone, carbomentone, and yonone; Preferably, it is a monoterpene alcohol, and more preferably, menthol. These monoterpenes may be d-, l-, or dl-form. Particularly as menthol, for example, l-menthol and d-menthol are preferred, and l-menthol is more preferred. It may be used as a mixture of 1-menthol and d-menthol.

Monoterpenes may be used alone or in combination of two or more.

　本発明の組成物におけるモノテルペンの含有量は、特に限定されないが、清涼感の付与に加え、Ｄ－ｃｈｉｒｏ－イノシトールの析出抑制、得られる組成物の液だれ及び刺激感（ぴりぴり感）の抑制、ならびにモノテルペン自体の分離の抑制に優れることから、好ましくは０．０１～１０質量％であり、より好ましくは０．０５～２質量％であり、さらに好ましくは０．１～１．０質量％であり、よりさらに好ましくは０．７～１．０質量％である。
The content of the monoterpene in the composition of the present invention is not particularly limited, but in addition to imparting a refreshing feeling, suppressing precipitation of D-chiro-inositol, suppressing dripping and irritating feeling (crisp feeling) of the obtained composition. And 0.01 to 10% by mass, more preferably 0.05 to 2% by mass, and still more preferably 0.1 to 1.0% by mass because of excellent suppression of separation of the monoterpene itself. %, And still more preferably 0.7 to 1.0% by mass.

　本発明の組成物は、医薬品、医薬部外品又は化粧品等で通常許容される添加物をさらに含んでもよい。

　添加物としては、特に限定されないが、例えば、賦形剤、安定剤、矯臭剤、基剤、分散剤、希釈剤、乳化剤、経皮吸収促進剤、保存剤、着色剤、油分（油脂、鉱物油等）、増粘剤、ポリマー、皮膜形成剤、紫外線吸収剤、細胞賦活剤、酸化防止剤、防腐剤、清涼剤、消臭剤、顔料、染料、香料、糖類、アミノ酸類、ビタミン類、有機酸、有機アミン、植物抽出物等が挙げられる。
The composition of the present invention may further contain additives that are generally acceptable in pharmaceuticals, quasi-drugs, cosmetics, and the like.

Examples of the additive include, but are not limited to, excipients, stabilizers, odor correctors, bases, dispersants, diluents, emulsifiers, transdermal absorption enhancers, preservatives, coloring agents, oils (oils, fats, minerals, Oil, etc.), thickeners, polymers, film-forming agents, ultraviolet absorbers, cell activators, antioxidants, preservatives, fresheners, deodorants, pigments, dyes, fragrances, sugars, amino acids, vitamins, Organic acids, organic amines, plant extracts and the like can be mentioned.

　本発明の組成物は、特に限定されず、本発明に含まれる成分を混合することにより製造することができる。各成分を混合する順番は特に限定されない。

　また、混合する場合の条件も、特に限定されず、従来公知の方法に従って、本発明の組成物とすることができる。
The composition of the present invention is not particularly limited, and can be produced by mixing components contained in the present invention. The order of mixing the components is not particularly limited.

The conditions for mixing are not particularly limited, and the composition of the present invention can be obtained according to a conventionally known method.

　本発明の組成物を外用剤として用いる場合、医薬品、医薬部外品又は化粧品等として使用することが可能である。例えば皮膚用外用剤、頭髪用外用剤及び頭皮用外用剤に使用することが可能であり、より具体的には皮膚用医薬品、頭髪用医薬品及び頭皮用医薬品、皮膚用医薬部外品、頭髪用医薬部外品及び頭皮用医薬部外品、並びに皮膚用化粧品、頭髪用化粧品及び頭皮用化粧品に使用することが可能である。より具体的には、軟膏、パップ、リニメント、ローション、外用液剤、散布剤、クリーム、ジェル、乳液、ヘアトニック、ヘアスプレーの形態とすることが可能である。

　本明細書において、「頭髪用外用剤」及び「頭皮用外用剤」は、外用剤として使用する形態や用法が同一であっても異なっていてもよいが、主として直接的に作用する箇所が頭髪であるのか頭皮であるのかの点で異なる。また、「皮膚用外用剤」は、「頭皮用外用剤」を含む概念であり、頭皮に限定されず皮膚に直接的に作用するための外用剤を意味する。
When the composition of the present invention is used as an external preparation, it can be used as a drug, a quasi-drug, a cosmetic or the like. For example, it can be used as an external preparation for skin, an external preparation for hair, and an external preparation for scalp, and more specifically, a dermatological drug, a hair drug and a scalp drug, a quasi-drug for skin, and a hair It can be used for quasi-drugs and quasi-drugs, as well as skin cosmetics, hair cosmetics and scalp cosmetics. More specifically, it can be in the form of an ointment, cataplasm, liniment, lotion, topical solution, dusting agent, cream, gel, emulsion, hair tonic, hair spray.

In the present specification, the “external preparation for hair” and the “external preparation for scalp” may be the same or different in the form and usage as the external preparation. Or scalp. Further, “external preparation for skin” is a concept including “external preparation for scalp” and means an external preparation that acts directly on the skin without being limited to the scalp.

　本発明の方法は、本発明の組成物を対象に投与する工程を含む。対象への１投与あたりのＤ－ｃｈｉｒｏ－イノシトールの投与量は、特に限定されないが、好ましくは０．００５～２００ｍｇであり、より好ましくは０．０５～１００ｍｇであり、さらに好ましくは０．５～１０ｍｇである。
The method of the invention comprises the step of administering a composition of the invention to a subject. The dose of D-chiro-inositol per administration to a subject is not particularly limited, but is preferably 0.005 to 200 mg, more preferably 0.05 to 100 mg, and still more preferably 0.5 to 100 mg. 10 mg.

　対象への本発明の組成物の投与回数は、特に限定されないが、好ましくは１日あたり１～６回であり、より好ましくは１日あたり１～３回であり、さらに好ましくは１日あたり１～２回である。
The frequency of administration of the composition of the present invention to a subject is not particularly limited, but is preferably 1 to 6 times per day, more preferably 1 to 3 times per day, and still more preferably 1 to 3 times per day. ~ 2 times.

　本発明の組成物を投与する対象は、特に限定されないが、例えば、ヒト、家畜・愛玩動物等の動物が挙げられる。
The subject to which the composition of the present invention is administered is not particularly limited, and includes, for example, humans, animals such as domestic animals and pets.

　以下、実施例によって本発明を更に詳細に説明するが、本発明はこれらの実施例に限定されるものではない。
Hereinafter, the present invention will be described in more detail with reference to Examples, but the present invention is not limited to these Examples.

　本実施例において用いる成分は、以下のとおりである。

［Ｄ－ｃｈｉｒｏ－イノシトール］

　Ｄ－ｃｈｉｒｏ－イノシトール（和光純薬工業社製、以下「DCI」と略する。）

［界面活性剤］

　ＨＣＯ－１０（ポリオキシエチレン（１０）硬化ヒマシ油、ＨＬＢ値：６．５、日光ケミカルズ社製）

　ＨＣＯ－２０（ポリオキシエチレン（２０）硬化ヒマシ油、ＨＬＢ値：１０．５、日光ケミカルズ社製）

　ＨＣＯ－４０（ポリオキシエチレン（４０）硬化ヒマシ油、ＨＬＢ値：１２．５、日光ケミカルズ社製）

　ＨＣＯ－５０（ポリオキシエチレン（５０）硬化ヒマシ油、ＨＬＢ値：１３．５、日光ケミカルズ社製）

　ＨＣＯ－６０（ポリオキシエチレン（６０）硬化ヒマシ油、ＨＬＢ値：１４、日光ケミカルズ社製）

　ＰＰＧ－８セテス－２０（セタノールに酸化エチレン及び酸化プロピレンを付加重合したもの、ＨＬＢ値：１２．５、日光ケミカルズ社製、以下「PBC44」と略する。）

　ＰＰＧ－４セテス－２０（ポリオキシエチレンポリオキシプロピレンセチルエーテル、ＨＬＢ値：１６．５、日光ケミカルズ社製、以下「PBC34」と略する。）

　ポリソルベート８０（オレイン酸ポリオキシエチレンソルビタン、ＨＬＢ値：１５、日光ケミカルズ社製）

　オレイン酸グリセリル（オレイン酸とグリセリンのモノエステル、ＨＬＢ値：２．５、日光ケミカルズ社製）

　オレイン酸ポリグリセリル－２（オレイン酸とジグリセリンのエステル、ＨＬＢ値：５．５、日光ケミカルズ社製）

　ラウリル硫酸ナトリウム（日光ケミカルズ社製）

　ラウロイルメチルタウリン酸ナトリウム（日光ケミカルズ社製）

　ステアラミドプロピルジメチルアミン（日光ケミカルズ社製）

［水］

　精製水
The components used in this example are as follows.

[D-chiro-inositol]

D-chiro-inositol (manufactured by Wako Pure Chemical Industries, Ltd .; hereinafter abbreviated as "DCI")

[Surfactant]

HCO-10 (polyoxyethylene (10) hydrogenated castor oil, HLB value: 6.5, manufactured by Nikko Chemicals)

HCO-20 (polyoxyethylene (20) hydrogenated castor oil, HLB value: 10.5, manufactured by Nikko Chemicals)

HCO-40 (polyoxyethylene (40) hydrogenated castor oil, HLB value: 12.5, manufactured by Nikko Chemicals)

HCO-50 (polyoxyethylene (50) hardened castor oil, HLB value: 13.5, manufactured by Nikko Chemicals)

HCO-60 (polyoxyethylene (60) hydrogenated castor oil, HLB value: 14, Nikko Chemicals Co., Ltd.)

PPG-8 ceteth-20 (addition polymerization of ethylene oxide and propylene oxide to cetanol, HLB value: 12.5, manufactured by Nikko Chemicals, hereinafter abbreviated as "PBC44")

PPG-4 Ceteth-20 (polyoxyethylene polyoxypropylene cetyl ether, HLB value: 16.5, manufactured by Nikko Chemicals Co., Ltd .; hereinafter abbreviated as “PBC34”)

Polysorbate 80 (polyoxyethylene sorbitan oleate, HLB value: 15, manufactured by Nikko Chemicals)

Glyceryl oleate (monoester of oleic acid and glycerin, HLB value: 2.5, manufactured by Nikko Chemicals)

Polyglyceryl-2 oleate (ester of oleic acid and diglycerin, HLB value: 5.5, manufactured by Nikko Chemicals)

Sodium lauryl sulfate (Nikko Chemicals)

Sodium lauroylmethyltaurate (Nikko Chemicals)

Stearamidopropyldimethylamine (Nikko Chemicals)

[water]

purified water

実施例１

　各成分を下記表１に示す組成になるように、精製水にDCIを溶解させ、界面活性剤を添加し、残容量を精製水で希釈、混合し、各組成物を製剤として調製した。
Example 1

DCI was dissolved in purified water so that each component had the composition shown in Table 1 below, a surfactant was added, and the remaining volume was diluted and mixed with purified water to prepare each composition as a preparation.

Ａ．製剤安定性試験

　得られた製剤について、以下の方法で、各種類及び含有量の界面活性剤におけるDCIの析出について評価した。

　各組成における製剤を3Lotずつ作成し、低温サイクル（12時間5℃インキュベートの後、12時間-20℃を28日間繰り返す）によりDCIの析出を誘導して、目視により、以下の指標に基づいて評価した。評価結果を表１に示す（Ｎ数は３である）。

　全てのLotで、結晶物の析出はみられない「◎」

　1Lotでも、わずかな結晶物の析出がみられた「〇」

　1Lotでも、少数の結晶物の析出がみられた「△」

　1Lotでも、多数の結晶物の析出がみられた「×」
A. Formulation stability test

The obtained preparations were evaluated for DCI precipitation in surfactants of each type and content by the following method.

Formulations of each composition were prepared in 3 lots, DCI precipitation was induced by a low-temperature cycle (12 hours 5 ° C incubation, 12 hours -20 ° C repeated for 28 days), and visually evaluated based on the following indices did. The evaluation results are shown in Table 1 (the number of N is 3).

In all lots, no precipitation of crystals was observed "◎"

Even with 1Lot, slight precipitation of crystalline material was observed "〇"

Even with 1 Lot, a small number of crystals were precipitated.

Even with 1 Lot, many crystals precipitated

Ｂ．使用感の試験

　得られた製剤について、以下の方法で、界面活性剤含有製剤による塗布時の使用感（ざらつき感及びべたつき感）を評価した。

　評価モニター10名が製剤0.5ｇを、頭皮に塗布した塗布時のざらつき感及び腕に塗布した塗布時のべたつき感を評価した。具体的には次のとおりに評価した。ざらつき感及びべたつき感について、以下のとおり評点化したVisual Analogue Scaleによるアンケートを実施することにより評価した。

＜使用感＞

・ざらつき感

　ざらつき感がなく、使用性として問題なし「1点」

　ざらつき感が強く、使用性として問題である「10点」

・べたつき感

　べたつき感が十分感じられ、使用性として問題なし「1点」

　べたつき感が非常に少なく、使用性として問題である「10点」

次に、そのアンケート結果を平均し、下記式に従って各改善度（％）を算出することにより、評価結果を表４にまとめた（Ｎ数は１０である）。

　改善度（％）＝１００×（表１における界面活性剤を用いない製剤におけるアンケート結果の平均－界面活性剤含有製剤におけるアンケート結果の平均）／表１における界面活性剤を用いない製剤におけるアンケート結果の平均

　上記式において、「表１における界面活性剤を用いない製剤」と「界面活性剤含有製剤」には、それぞれDCIの含有量が同じ製剤同士を選択して改善度を算出しており、具体的には「５質量％」、「０．１質量％」のいずれかのDCIの含有量が同じ製剤同士を選択した上で、「表１における界面活性剤を用いない製剤」におけるアンケート結果の平均を１００．０としたときの「界面活性剤含有製剤」におけるアンケート結果の平均の相対値を、改善度として算出した。
B. Test of usability

With respect to the obtained preparation, the feeling of use (roughness and stickiness) at the time of application with the surfactant-containing preparation was evaluated by the following method.

Ten evaluation monitors evaluated the rough feeling at the time of application of 0.5 g of the preparation to the scalp and the sticky feeling at the time of application to the arm. Specifically, evaluation was made as follows. Roughness and stickiness were evaluated by conducting a questionnaire using the Visual Analogue Scale, which was rated as follows.

<Usability>

・ Roughness

No roughness, no problem in usability "1 point"

"10 points" with strong roughness and usability issues

・ Sticky feeling

Good feeling of stickiness, no problem in usability "1 point"

"10 points" with very little sticky feeling and a problem in usability

Next, the results of the questionnaire were averaged, and the degree of improvement (%) was calculated according to the following formula, whereby the evaluation results were summarized in Table 4 (the number of N is 10).

Degree of improvement (%) = 100 × (Average of questionnaire results in formulations without surfactant in Table 1−Average of questionnaire results in formulations containing surfactant) / Questionnaire results in formulations without surfactant in Table 1 The average of

In the above formula, the “formulations without surfactants” and the “surfactant-containing preparations” in Table 1 each select preparations having the same DCI content and calculate the degree of improvement. The average of the results of the questionnaire for “Formulations without surfactants in Table 1” after selecting formulations with the same DCI content of either “5% by mass” or “0.1% by mass” The average relative value of the results of the questionnaire in the “surfactant-containing preparation” when the value was 100.0 was calculated as the degree of improvement.

Figure JPOXMLDOC01-appb-T000001
Figure JPOXMLDOC01-appb-T000001

　表１の結果より、製剤に界面活性剤を添加することにより、DCIの析出を効果的に抑制できると判断できる。また、DCI含有製剤によるざらつき感及びべたつき感が、界面活性剤を添加することにより改良されたことを確認した。
From the results in Table 1, it can be determined that the addition of a surfactant to the preparation can effectively suppress the precipitation of DCI. It was also confirmed that the roughness and stickiness of the DCI-containing preparation were improved by adding a surfactant.

Claims (7)


  1. 　Ｄ－ｃｈｉｒｏ－イノシトールと界面活性剤と水とを含む、組成物。
    A composition comprising D-chiro-inositol, a surfactant and water.

  2. 　Ｄ－ｃｈｉｒｏ－イノシトールの含有量が０．００１～２０質量％である、請求項１に記載の組成物。
    The composition according to claim 1, wherein the content of D-chiro-inositol is 0.001 to 20% by mass.

  3. 　界面活性剤がノニオン性界面活性剤を含む、請求項１又は２に記載の組成物。
    The composition according to claim 1 or 2, wherein the surfactant comprises a nonionic surfactant.

  4. 　界面活性剤のＨＬＢ値が、２～１７である、請求項１～３のいずれか一項に記載の組成物。
    The composition according to any one of claims 1 to 3, wherein the HLB value of the surfactant is 2 to 17.

  5. 　ノニオン性界面活性剤がポリオキシエチレン硬化ヒマシ油又はポリオキシエチレンポリオキシプロピレンアルキルエーテルを含む、請求項１～４のいずれか一項に記載の組成物。
    The composition according to any one of claims 1 to 4, wherein the nonionic surfactant comprises polyoxyethylene hydrogenated castor oil or polyoxyethylene polyoxypropylene alkyl ether.

  6. 　請求項１～５のいずれか一項に記載の組成物を含む外用剤。
    An external preparation containing the composition according to any one of claims 1 to 5.

  7. 　請求項１～５のいずれか一項に記載の組成物を含む頭皮用外用剤。
    An external preparation for scalp, comprising the composition according to any one of claims 1 to 5.
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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006028026A (en) * 2004-07-12 2006-02-02 Doctor Program Kk Hair-growing agent
JP2009108023A (en) * 2007-10-11 2009-05-21 Rohto Pharmaceut Co Ltd Hair grower
WO2017188393A1 (en) * 2016-04-27 2017-11-02 小林製薬株式会社 Hair-growth agent
JP2019085339A (en) * 2017-11-01 2019-06-06 小林製薬株式会社 Composition containing d-chiro-inositol
JP2019085342A (en) * 2017-11-01 2019-06-06 小林製薬株式会社 Composition containing d-chiro-inositol

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006028026A (en) * 2004-07-12 2006-02-02 Doctor Program Kk Hair-growing agent
JP2009108023A (en) * 2007-10-11 2009-05-21 Rohto Pharmaceut Co Ltd Hair grower
WO2017188393A1 (en) * 2016-04-27 2017-11-02 小林製薬株式会社 Hair-growth agent
JP2019085339A (en) * 2017-11-01 2019-06-06 小林製薬株式会社 Composition containing d-chiro-inositol
JP2019085342A (en) * 2017-11-01 2019-06-06 小林製薬株式会社 Composition containing d-chiro-inositol

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