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JP7425536B2 - External composition containing D-chiro-inositol - Google Patents
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JP7425536B2 - External composition containing D-chiro-inositol - Google Patents

External composition containing D-chiro-inositol Download PDF

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JP7425536B2
JP7425536B2 JP2018248587A JP2018248587A JP7425536B2 JP 7425536 B2 JP7425536 B2 JP 7425536B2 JP 2018248587 A JP2018248587 A JP 2018248587A JP 2018248587 A JP2018248587 A JP 2018248587A JP 7425536 B2 JP7425536 B2 JP 7425536B2
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inositol
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公輔 田中
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Kobayashi Pharmaceutical Co Ltd
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K8/9706Algae
    • A61K8/9722Chlorophycota or Chlorophyta [green algae], e.g. Chlorella
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9755Gymnosperms [Coniferophyta]
    • A61K8/9767Pinaceae [Pine family], e.g. pine or cedar
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
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    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/98Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution of animal origin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00Preparations for affecting hair growth

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Description

本発明は、D-chiro-イノシトールを含む外用組成物に関する。 The present invention relates to a topical composition containing D-chiro-inositol.

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 with a hydroxy group, and is known as a vitamin-like substance. There is. Inositol exists in nine stereoisomers depending on the combination of steric configurations of hydroxy groups.

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 growth agent containing inositol as an active ingredient. As in Patent Document 1, "inositol" used in prior documents refers to myo-inositol (cis-1,2,3,5-trans-4 , 6-cyclohexanehexaol) (see, for example, Non-Patent Documents 1 to 3).
Furthermore, the present inventors have discovered that among the stereoisomers of inositol, chiro-inositol is a compound useful as a hair growth agent (see Patent Document 2).

特開2006-28026号公報Japanese Patent Application Publication No. 2006-28026 国際公開第2017/188393号International Publication No. 2017/188393

医薬部外品原料規格2006統合版,薬事日報社,p.318Quasi-drug raw material standards 2006 integrated edition, Yakuji Nipposha, p. 318 医薬品添加物規格2003,薬事日報社,p.101-102Pharmaceutical Excipient Standards 2003, Yakuji Nipposha, p. 101-102 医薬品添加物事典2000,薬事日報社,p.26Dictionary of Pharmaceutical Additives 2000, Yakuji Nipposha, p. 26

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、水溶性ではあるものの、製剤としての使用性に改善の余地があることを確認した。そのような使用性の問題として、具体的には、毛穴への浸透性が低いことを確認した。
Here, the present inventors discovered that among the stereoisomers of inositol, D-chiro-inositol is a compound that has water solubility among the isomers of inositol.
However, in order to take advantage of these properties of D-chiro-inositol, research on compositions containing D-chiro-inositol continues, and although D-chiro-inositol is water-soluble, its usability as a pharmaceutical product has been It was confirmed that there is room for improvement. Specifically, it was confirmed that the usability problem was that the permeability into pores was low.

そこで、本発明は、D-chiro-イノシトールを用いた水溶性製剤としての使用性を向上させることが可能な外用組成物を提供することを目的とする。 Therefore, an object of the present invention is to provide a composition for external use that can improve usability as a water-soluble preparation using 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-イノシトールと特定のエキスと水とを含む組成物が、D-chiro-イノシトールを用いた水溶性製剤としての使用性を向上させることが可能な外用組成物であることを見出し、本発明を完成するに至った。 As a result of extensive research to solve the above problems, the present inventors have discovered that a composition containing D-chiro-inositol, a specific extract, and water has been developed as a water-soluble preparation using D-chiro-inositol. The present inventors have discovered that it is an external composition that can improve the usability of the product, 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、
エキスと、
水と、を含み、
前記エキスが、アブラナ科、ウコギ科、キク科、クロレラ科、ゴマノハグサ科、シソ科、バラ科、フトモモ科、マツ科、マメ科、リンドウ科、及び褐藻類からなる群より選択される1種若しくは2種以上の植物から抽出される植物エキス、又はローヤルゼリーエキスの少なくともいずれかである、外用組成物。
[2] D-chiro-イノシトールの含有量が0.001~20質量%である、[1]に記載の外用組成物。
[3] 前記エキスが、クロレラエキス、オウゴンエキス、ローズマリーエキス、ニンジンエキス、サクラ葉エキス、ユーカリエキス、マツエキス、ダイズエキス、センブリエキス、海藻エキス、又はローヤルゼリーエキスを含む、[1]又は[2]に記載の外用組成物。
[4] 前記エキスの含有量が0.1~30質量%である、[1]~[3]のいずれかに記載の外用組成物。
[5] 頭皮用である、[1]~[4]のいずれかに記載の外用組成物。
That is, the present invention provides the following inventions.
[1] D-chiro-inositol and
Extract and
including water;
The extract is one or more selected from the group consisting of Brassicaceae, Araliaceae, Asteraceae, Chlorellaceae, Phosphoraceae, Lamiaceae, Rosaceae, Myrtaceae, Pinaceae, Fabaceae, Gentianaceae, and Brown algae. A composition for external use that is at least either a plant extract extracted from two or more types of plants or a royal jelly extract.
[2] The external composition according to [1], wherein the content of D-chiro-inositol is 0.001 to 20% by mass.
[3] [1] or [2], wherein the extract contains chlorella extract, scutellariae extract, rosemary extract, carrot extract, cherry leaf extract, eucalyptus extract, pine extract, soybean extract, Japanese japonica extract, seaweed extract, or royal jelly extract. The external composition described in .
[4] The external composition according to any one of [1] to [3], wherein the content of the extract is 0.1 to 30% by mass.
[5] The external composition according to any one of [1] to [4], which is for the scalp.

本発明によれば、D-chiro-イノシトールを用いた水溶性製剤としての使用性を向上させることが可能な外用組成物が提供される。 According to the present invention, a composition for external use that can improve usability as a water-soluble preparation using D-chiro-inositol is provided.

以下、本発明の外用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 external composition of the present invention and specific embodiments thereof. However, the invention is not limited to the specific embodiments described below.

本発明の外用組成物は、D-chiro-イノシトールとエキスと水とを含み、身体の外部に用いられる組成物である。 The external composition of the present invention contains D-chiro-inositol, an extract, and water, and is a composition to be used outside the body.

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。 D-chiro-inositol is not particularly limited, but includes, for example, those extracted from naturally occurring buckwheat, beans, citrus fruits, etc., those purified and extracted from leguminous plants by fermentation, chemically synthesized ones, and Commercially available products may be mentioned. Here, the extraction method is not particularly limited, and any known extraction method can be used.

本発明の外用組成物における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0.1~10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 external 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 even more preferably The content is 0.05 to 15% by weight, even more preferably 0.1 to 10% by weight, and even more preferably 3 to 7% by weight.

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。
As used herein, "mass%" means the mass percentage of the components contained in the composition relative to the mass of the entire composition.
Further, in this specification, when it is written as "X to Y", it means that it is greater than or equal to X and less than or equal to Y.

本発明の外用組成物としては、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。
本発明の外用組成物は、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 external composition of the present invention includes, for example, an agent for cracks and chapped skin, an agent for heat rash and sores, an agent for corns and calluses, an agent for dryness and roughness, an agent for wrinkles and spots, a moisturizing agent, a hair dye, and a hair growth agent. agents, shampoos, conditioners, lotions, creams, milky lotions, hand creams, medicated soaps, and packs.
By containing D-chiro-inositol, the external composition of the present invention can have a vitamin-like action and hair growth activity, and may be used as a hair growth agent.
Specifically, the hair growth activity is an activity related to hair shaft growth promotion, hair growth, hair loss prevention, etc., and preferably an activity related to hair shaft growth promotion and hair growth.

本発明の外用組成物は、アブラナ科、ウコギ科、キク科、クロレラ科、ゴマノハグサ科、シソ科、バラ科、フトモモ科、マツ科、マメ科、リンドウ科、及び褐藻類からなる群より選択される1種若しくは2種以上の植物から抽出される植物エキス、又はローヤルゼリーエキスの少なくともいずれかであるエキスを含む。
このようなエキスを含むことにより、D-chiro-イノシトールを用いた水溶性製剤としての使用性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、D-chiro-イノシトールを用いた水溶性製剤が例えばヒトの皮膚における角質層のような脂溶性バリアを有する層に対して接触した場合に、上述したような特定のエキスが、D-chiro-イノシトールが水に溶解していることによる極性反発を低減させるように変化させることで、上記層に対するD-chiro-イノシトールの表面張力を低下させて浸透性が向上するものと推察される(ただし、要因はこれに限定されない。)。
しました。)。
The topical composition of the present invention is selected from the group consisting of Brassicaceae, Araliaceae, Asteraceae, Chlorellaceae, Phosphoraceae, Lamiaceae, Rosaceae, Myrtaceae, Pinaceae, Fabaceae, Gentianaceae, and Brown algae. The extract includes at least one of a plant extract extracted from one or more types of plants, or a royal jelly extract.
By including such an extract, it becomes possible to improve the usability of a water-soluble preparation using D-chiro-inositol. The reason for this effect is that when a water-soluble preparation using D-chiro-inositol comes into contact with a layer with a fat-soluble barrier such as the stratum corneum of human skin, the above-mentioned specific By changing the extract to reduce the polar repulsion caused by D-chiro-inositol being dissolved in water, the surface tension of D-chiro-inositol to the above layer is lowered and the permeability is improved. (However, the factors are not limited to this.)
Did. ).

本発明のエキスは、上述した特定のエキスであれば特に限定されず、その中から公知のエキスを適宜選択して使用することが可能であり、アブラナ科 Brassicaceaeの植物としては例えばオランダガラシ属 Nasturtium、ヤマガラシ属 Barbarea、イヌガラシ属 Rorippa等の植物が挙げられ、ウコギ科 Araliaceaeの植物としては例えばキヅタ属 Hedera、ヤツデ属 Fatsia、ウコギ属 Eleutherococcus (Acanthopanax) 、トチバニンジン属 Panax等の植物が挙げられ、キク科 Asteraceaeの植物としては例えばゴボウ属 Arctium、ヌマダイコン属 Adenostemma等の植物が挙げられ、クロレラ科 Chlorellaceaeの植物としては例えばクロレラ属 Chlorella、等の植物が挙げられ、ゴマノハグサ科 Scrophulariaceaeの植物としては例えばゴマノハグサ属 Scrophularia L.、ネメシア属 (Nemesia)等の植物が挙げられ、シソ科 Lamiaceaeの植物としては例えばローズマリー属 Rosmarinus、アキギリ属(サルビア属) Salvia、タツナミソウ属 Scutellaria、オドリコソウ属 Lamium等の植物が挙げられ、バラ科 Rosaceaeの植物としては例えばサクラ属(スモモ属)Prunus、ビワ属 Eriobotrya等の植物が挙げられ、フトモモ科 Myrtaceaeの植物としては例えばユーカリ属 Eucalyptus、フトモモ属 Syzygium等の植物が挙げられ、マツ科 Pinaceaeの植物としては例えばマツ属 Pinus、トウヒ属 Picea等の植物が挙げられ、マメ科 Fabaceae syn. Leguminosaeの植物としては例えばダイズ属 Glycine、インゲン属 Phaseolus等の植物が挙げられ、リンドウ科 Gentianaceaeの植物としては例えばセンブリ属 Swertia、ヒメセンブリ属 Lomatogonium、リンドウ属 Gentiana等の植物が挙げられ、褐藻類 Phaeophyceaeの植物としては例えばヒバマタ科 Fucaceae、コンブ科 Laminariaceae、モズク科 Spermatochnaceae等の植物が挙げられる。このようなエキスであれば、抽出する方法は、特に限定されず、天然に存在する動物や植物から抽出する方法、それと同等のものを化学合成する方法、及びそれらの市販品を用いる方法が挙げられる。ここで、具体的に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。例えば、後述する実施例で用いている植物エキスのように、花、葉、茎、根(球根含む)、又は全草から、水、エタノール、BG(1,3-ブチレングリコール)又はこれらの混合液を用いて抽出することが可能であり、なかでも、水およびエタノールの混合液を用いることが好ましい。また、ローヤルゼリーについては、ミツバチ科 Apidae、具体的にはミツバチの分泌物を採取することにより準備することが可能である。ここで、エキスは抽出する際の水、エタノール、BGを含んでいてもよく、これらをさらに添加して希釈してもよい。抽出する際の温度は、例えば抽出する際に用いる水等の沸点より低い温度であることが好ましく、各植物エキスに好適な温度を適宜設定することが可能である。 The extract of the present invention is not particularly limited as long as it is the above-mentioned specific extract, and any known extract can be appropriately selected and used from among them. , Barbarea of the Araliaceae, Rorippa of the Araliaceae, etc. Plants of the Araliaceae Araliaceae include Hedera of the Araliaceae, Fatsia of the Genus Ivy, Eleutherococcus (Acanthopanax), Panax of the Asteraceae, etc. Examples of plants in the Asteraceae family include Arctium, Adenostemma, etc.; plants in the Chlorellaceae family include Chlorella, and examples of plants in the Scrophulariaceae family include Scrophularia. Examples of plants in the Lamiaceae family include Rosmarinus, Salvia, Scutellaria, and Lamium. Examples of plants in the Rosaceae family include Prunus and Eriobotrya; examples of plants in the Myrtaceae family include Eucalyptus and Syzygium; Plants of the Pinaceae include, for example, Pinus and Picea; plants of the Fabaceae syn. Leguminosae include Glycine of the soybean and Phaseolus; Examples of such plants include plants of the genus Swertia, Lomatogonium, and Gentiana, and examples of plants of the brown algae Phaeophyceae include plants of the family Fucaceae, Laminariaceae, Laminariaceae, and Spermatochnaceae. For such extracts, the extraction method is not particularly limited, and examples include methods of extracting from naturally occurring animals and plants, methods of chemically synthesizing equivalents, and methods of using commercially available products. It will be done. Here, the specific extraction method is not particularly limited, and any known extraction method can be used. For example, like the plant extracts used in the Examples below, extracts from flowers, leaves, stems, roots (including bulbs), or whole plants can be extracted from water, ethanol, BG (1,3-butylene glycol), or a mixture thereof. It is possible to extract using a liquid, and it is particularly preferable to use a mixed liquid of water and ethanol. Furthermore, royal jelly can be prepared by collecting the secretions of Apidae, specifically honey bees. Here, the extract may contain water, ethanol, and BG during extraction, and may further be diluted by adding these. The temperature during extraction is preferably lower than the boiling point of water used during extraction, and it is possible to appropriately set a temperature suitable for each plant extract.

本発明のエキスとしては、上記した中では、クロレラ科、シソ科、ウコギ科、バラ科、フトモモ科、マツ科、マメ科、リンドウ科、及び褐藻類の植物から抽出される植物エキス、並びにローヤルゼリーが好ましく、クロレラエキス、オウゴンエキス、ローズマリーエキス、ニンジンエキス、サクラ葉エキス、ユーカリエキス、マツエキス、ダイズエキス、センブリエキス、海藻エキス、及びローヤルゼリーエキスがより好ましい。また、後述する市販のエキスを適宜使用することが可能である。 Among the extracts of the present invention, among those mentioned above, plant extracts extracted from plants of Chlorellaceae, Lamiaceae, Araliaceae, Rosaceae, Myrtaceae, Pinaceae, Fabaceae, Gentianaceae, and Brown algae, and royal jelly are preferred, and chlorella extract, scutellariae extract, rosemary extract, carrot extract, cherry leaf extract, eucalyptus extract, pine extract, soybean extract, Japanese japonica extract, seaweed extract, and royal jelly extract are more preferred. Furthermore, commercially available extracts described below can be used as appropriate.

本発明のエキスは、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種以上のエキスの組み合わせであってもよい。 The extracts of the present invention may be used alone or in combination of two or more. When two or more types are used in combination, a combination of two or more types of extracts may be used.

本発明の外用組成物における本発明のエキスの含有量は、特に限定されないが、固形分量で、通常0.001~70質量%であり、好ましくは0.01~50質量%であり、より好ましくは0.1~30質量%である。 The content of the extract of the present invention in the external composition of the present invention is not particularly limited, but the solid content is usually 0.001 to 70% by mass, preferably 0.01 to 50% by mass, and more preferably is 0.1 to 30% by mass.

本発明の外用組成物における水の含有量は、特に限定されないが、好ましくは5質量%以上であり、より好ましくは8質量%以上であり、さらに好ましくは10質量%以上であり、よりさらに好ましくは15質量%以上である。また、本発明の外用組成物における水の含有量は、95重量%以下であり、好ましくは85重量%以下であり、より好ましくは35質量%以下であり、さらに好ましくは30質量%以下であり、さらにより好ましくは25質量%以下である。
本発明の外用組成物における水の含有量は、上記好ましい上限及び下限を選択してもよく特に限定されるものではないが、5~95重量%であり、好ましくは5~85重量%であり、より好ましくは5~35質量%であり、更により好ましくは10~30質量%である。
水の割合が上記範囲内にあることにより、本発明の外用組成物を含む製剤における使用性を向上させること、特にざらつき感を抑制させることが可能となる。
The content of water in the external composition of the present invention is not particularly limited, but is preferably 5% by mass or more, more preferably 8% by mass or more, still more preferably 10% by mass or more, even more preferably is 15% by mass or more. Further, the water content in the external composition of the present invention is 95% by weight or less, preferably 85% by weight or less, more preferably 35% by weight or less, and still more preferably 30% by weight or less. , even more preferably 25% by mass or less.
The content of water in the external composition of the present invention may be selected from the above preferable upper and lower limits and is not particularly limited, but is 5 to 95% by weight, preferably 5 to 85% by weight. , more preferably 5 to 35% by weight, even more preferably 10 to 30% by weight.
When the proportion of water is within the above range, it becomes possible to improve the usability of the preparation containing the external composition of the present invention, and in particular to suppress the rough feeling.

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, ultrafiltrated water, reverse osmosis water, and distilled water, and water from which ionic impurities have been removed as much as possible, such as ultrapure water.

本発明の外用組成物は、炭素数1~3のモノアルコールをさらに含んでもよい。
炭素数1~3のモノアルコールを含むことにより、抗菌性及び保湿性を付与した外用組成物を得ることができる傾向にある。
The external composition of the present invention may further contain a monoalcohol having 1 to 3 carbon atoms.
By containing a monoalcohol having 1 to 3 carbon atoms, it tends to be possible to obtain a composition for external use that has antibacterial properties and moisturizing properties.

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。
炭素数1~3のモノアルコールは、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。
Monoalcohols having 1 to 3 carbon atoms include methanol, ethanol, n-propanol, and isopropanol, with ethanol and isopropanol being preferred, and ethanol being more preferred.
Monoalcohols having 1 to 3 carbon atoms may be used alone or in combination of two or more.

本発明の外用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。
本発明の外用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 monoalcohol having 1 to 3 carbon atoms in the external composition of the present invention is not particularly limited, but the content of the monoalcohol having 1 to 3 carbon atoms can be set high.
The content of the monoalcohol having 1 to 3 carbon atoms in the external 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. The amount may be 30 to 40% by mass.

本発明の外用組成物は、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、有機アミン等が挙げられる。
The external composition of the present invention may further contain additives that are normally allowed in pharmaceuticals, quasi-drugs, cosmetics, and the like.
Additives include, but are not particularly limited to, excipients, stabilizers, flavoring agents, bases, dispersants, diluents, emulsifiers, transdermal absorption enhancers, preservatives, coloring agents, oils (oils, fats, minerals, etc.). oil, etc.), thickeners, polymers, film-forming agents, ultraviolet absorbers, cell activators, antioxidants, preservatives, fresheners, deodorants, pigments, dyes, fragrances, sugars, amino acids, vitamins, Examples include organic acids and organic amines.

本発明の外用組成物は、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、本発明の外用組成物とすることができる。
The external composition of the present invention is not particularly limited, and can be manufactured by mixing the components included in the present invention. The order in which the components are mixed is not particularly limited.
Further, the conditions for mixing are not particularly limited, and the external composition of the present invention can be prepared according to a conventionally known method.

本発明の外用組成物は、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。本発明の外用組成物は、身体の外部に使用することが可能であり、例えば皮膚用外用組成物、頭髪用外用組成物及び頭皮用外用組成物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、「頭髪用外用組成物」及び「頭皮用外用組成物」は、外用組成物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、「皮膚用外用組成物」は、「頭皮用外用組成物」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組成物を意味する。
The external composition of the present invention can be used as a pharmaceutical, quasi-drug, cosmetic, or the like. The external composition of the present invention can be used outside the body, and can be used, for example, as an external skin composition, a hair composition, and a scalp composition. Used in skin drugs, hair drugs and scalp drugs, quasi-drugs for the skin, quasi-drugs for hair and quasi-drugs for the scalp, and cosmetics for the skin, hair cosmetics and scalp cosmetics. Is possible. More specifically, it can be in the form of an ointment, poultice, liniment, lotion, external solution, spray, cream, gel, milky lotion, hair tonic, or hair spray.
In this specification, "external composition for hair" and "external composition for scalp" may be used in the same or different forms and usage methods as external compositions, but mainly act directly. The difference is whether the location is hair or scalp. Furthermore, the term "external composition for skin" is a concept that includes "external composition for scalp," and means an external composition that is not limited to the scalp but is intended to act directly on the skin.

本発明の方法は、本発明の外用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 present invention includes the step of administering the external composition of the present 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 200 mg. It is 10 mg.

対象への本発明の外用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 external 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 even more preferably per day. 1 to 2 times.

本発明の外用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。 Subjects to whom the external composition of the present invention is administered are not particularly limited, but include, for example, humans and animals such as livestock 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。 EXAMPLES Hereinafter, the present invention will be explained 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。)
[エキス]
ビワ葉エキス(バラ科植物エキス、ビワ Eriobotrya japonicaの葉から抽出されたエキス/エタノールと水、丸善製薬社製の商品名「ビワ抽出液-J」)
クロレラエキス(クロレラ科植物エキス、クロレラ Chlorella vulgaris Chick (Chlorellaceae) から水にて抽出されるエキス/BG(1,3-ブチレングリコール)と水、一丸ファルコス社製の商品名「ビオセルアクト クロレラ B」)
ダイズエキス(フラボステロン)(マメ科植物エキス、非遺伝子組み換えダイズ Glycine max Merrill (Legu minosae) の種子より特殊な方法で抽出したエキス/BG(1,3-ブチレングリコール)と水、一丸ファルコス社製の商品名「フラボステロン SE」)
ゴボウエキス(キク科植物エキス、ゴボウ A. lappaの根から抽出されたエキス/BG(1,3-ブチレングリコール)と水、丸善製薬社製の商品名「ゴボウ抽出液」)
ジオウエキス(ゴマノハグサ科植物エキス、アカヤジオウ Rehmannia glutinosaの根からエタノール溶液により得られる抽出エキス、一丸ファルコス社製の商品名「ファルコレックス ジオウ」)
海藻エキス(褐藻類のヒバマタ科植物エキス、ヒバマタF. distichus ssp. evanescensの全藻から抽出されたエキス/エタノールと水、丸善製薬社製の商品名「カイソウ抽出液」)
マツエキス(マツ科植物エキス、セイヨウアカマツPinus sylvestrisの球果の抽出エキス/BG(1,3-ブチレングリコール)と水、一丸ファルコス社製の商品名「ファルコレックス マツ B」)
ニンジンエキス(ウコギ科植物エキス、オタネニンジンPanax ginsengの根から抽出されたエキス/エタノールと水、丸善製薬社製の商品名「ニンジン抽出液」)
オドリコソウエキス(シソ科植物エキス、オドリコソウ Lamium album var. barbatumの花、葉、茎の抽出エキス/BG(1,3-ブチレングリコール)と水、一丸ファルコス社製の商品名「ファルコレックス オドリコソウ B」)
オランダカラシエキス(アブラナ科植物エキス、オランダカラシ Nasturtium officinale R.Brown (Cruciferae) の葉、茎の抽出エキス/BG(1,3-ブチレングリコール)と水、一丸ファルコス社製の商品名「ファルコレックス オランダカラシ B」)
オウゴンエキス(シソ科植物エキス、オウゴン(コガネバナ Scutellaria baicalensis)の根から抽出されたエキス/エタノールと水、丸善製薬社製の商品名「オウゴン抽出液-J」)
ローズマリーエキス(シソ科植物エキス、ローズマリー rosemaryの葉から抽出されたエキス/エタノールと水、丸善製薬社製の商品名「ローズマリー抽出液-J」)
ローヤルゼリーエキス(ミツバチ科 Apidae昆虫エキス、ミツバチの分泌物(ローヤルゼリー)から抽出されたエキス/エタノールと水、丸善製薬社製の商品名「ローヤルゼリー抽出液-J」)
サクラ葉抽出液(バラ科植物エキス、ソメイヨシノ Cerasus ×yedoensis (Matsum.) Masam. & Suzuki ‘Somei-yoshino’の葉より抽出されたエキス/BG(1,3-ブチレングリコール)と水、一丸ファルコス社製の商品名「サクラエキス B」)
セイヨウキズタエキス(ウコギ科植物エキス、セイヨウキヅタ Hedera helixの抽出エキス/BG(1,3-ブチレングリコール)と水、一丸ファルコス社製の商品名「ファルコレックス セイヨウキズタ B」)
セージエキス(シソ科植物エキス、セージ Salvia officinalisの花や葉、また全草から抽出して得られるエキス/エタノールと水、一丸ファルコス社製の商品名「エコファーム セージ E」)
センブリエキス(リンドウ科植物エキス、センブリ Swertia japonicaの全草から抽出されたエキス/エタノールと水、丸善製薬社製の商品名「センブリ抽出リキッドET」)
ユーカリエキス(フトモモ科植物エキス、ユーカリの葉から抽出されたエキス/エタノールと水、丸善製薬社製の商品名「ユーカリ抽出液」)
[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")
[extract]
Loquat leaf extract (Rosaceae plant extract, extract extracted from the leaves of Loquat Eriobotrya japonica / ethanol and water, product name "Loquat extract - J" manufactured by Maruzen Pharmaceutical Co., Ltd.)
Chlorella extract (Chlorella family plant extract, extract extracted from Chlorella vulgaris Chick (Chlorellaceae) with water/BG (1,3-butylene glycol) and water, product name "Biocellact Chlorella B" manufactured by Ichimaru Falcos)
Soybean extract (flavosterone) (leguminous plant extract, non-genetically modified extract extracted from the seeds of Glycine max Merrill (Legu minosae) using a special method / BG (1,3-butylene glycol) and water, product manufactured by Ichimaru Falcos Name: “Flavosterone SE”)
Burdock extract (Asteraceae plant extract, extract extracted from the roots of Burdock A. lappa/BG (1,3-butylene glycol) and water, trade name "Burdock extract" manufactured by Maruzen Pharmaceutical Co., Ltd.)
Rehmannia glutinosa extract (plant extract of Rehmannia glutinosa, extracted extract obtained from the root of Rehmannia glutinosa with ethanol solution, product name "Falcolex Ziou" manufactured by Ichimaru Falcos Co., Ltd.)
Seaweed extract (Furucaceae plant extract of brown algae, extract extracted from whole algae of F. distichus ssp. evanescens / ethanol and water, product name "Kaiso extract" manufactured by Maruzen Pharmaceutical Co., Ltd.)
Pine extract (Pinaceae plant extract, Pinus sylvestris cone extract/BG (1,3-butylene glycol) and water, product name "Falcolex Pine B" manufactured by Ichimaru Falcos)
Carrot extract (Araliaceae plant extract, extract extracted from the root of Panax ginseng/ethanol and water, trade name "Carrot extract" manufactured by Maruzen Pharmaceutical Co., Ltd.)
Deadlock root extract (Lamiaceae plant extract, flower, leaf, and stem extract of Lamium album var. barbatum / BG (1,3-butylene glycol) and water, product name "Falcolex Deadlock root B" manufactured by Ichimaru Falcos Co., Ltd.)
Dutch mustard extract (Cruciferous plant extract, extract of leaves and stems of Dutch mustard Nasturtium officinale R.Brown (Cruciferae) / BG (1,3-butylene glycol) and water, product name "Falcolex Holland" manufactured by Ichimaru Falcos Co., Ltd.) Mustard B”)
Scutellariae extract (Lamiaceae plant extract, extract extracted from the roots of Scutellaria baicalensis / ethanol and water, trade name "Scutellaria extract - J" manufactured by Maruzen Pharmaceutical Co., Ltd.)
Rosemary extract (Lamiaceae plant extract, extract extracted from rosemary leaves/ethanol and water, trade name "Rosemary Extract - J" manufactured by Maruzen Pharmaceutical Co., Ltd.)
Royal jelly extract (Apidae insect extract, extract extracted from bee secretions (royal jelly)/ethanol and water, product name "Royal Jelly Extract - J" manufactured by Maruzen Pharmaceutical Co., Ltd.)
Sakura leaf extract (Rosaceae plant extract, Someiyoshino Cerasus ×yedoensis (Matsum.) Masam. & Suzuki 'Somei-yoshino' leaf extract/BG (1,3-butylene glycol) and water, Ichimaru Falcos Co., Ltd. (Product name: Sakura Extract B)
Hedera helix extract (Araliaceae plant extract, Hedera helix extract/BG (1,3-butylene glycol) and water, product name "Falcolex Hedera helix B" manufactured by Ichimaru Falcos)
Sage extract (Lamiaceae plant extract, extract obtained by extracting from flowers, leaves, and whole plants of Salvia officinalis/ethanol and water, product name "Eco Farm Sage E" manufactured by Ichimaru Falcos)
Swertia japonica extract (Gentiana family plant extract, extract extracted from the whole plant of Swertia japonica / ethanol and water, product name “Swertia extract liquid ET” manufactured by Maruzen Pharmaceutical Co., Ltd.)
Eucalyptus extract (Myrtaceae plant extract, extract extracted from eucalyptus leaves/ethanol and water, trade name "Eucalyptus extract" manufactured by Maruzen Pharmaceutical Co., Ltd.)
[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とエキスとを溶解させて混合し、各組成物を製剤として調製した。なお、表1に示すエキスの質量は固形分量を示しており、各エキスの溶媒については、凍結乾燥または熱乾燥により乾固化して使用した。
Example 1
DCI and extract were dissolved in purified water and mixed so that each component had the composition shown in Table 1 below, and each composition was prepared as a preparation. Note that the mass of the extract shown in Table 1 indicates the solid content, and the solvent of each extract was used after drying by freeze drying or heat drying.

A.使用性の試験
得られた製剤について、以下の方法で、各組成における製剤による塗布時の使用性(毛穴への浸透性)を評価した。
各組成における製剤を3Lotずつ作成し、それを0.25% Coomassie Brilliant Blue R-250(CBB R-250、東京化成工業社製)の呈色製剤に調製した。次に、C57BL/6マウスの背部体毛をバリカンで1mm長へ刈りそろえた上で、呈色製剤を塗布した。塗布後は速やかに呈色製剤をふき取り、塗布した部分の皮膚を採取し、生切片を作成した。作成した生切片を光学顕微鏡で観察し、毛包への色素到達深度について以下の指標に基づいて評価した。
<使用性>
・毛穴への浸透性
毛根下端へ色素が到達していることが認められた「4点」
毛根深部へ色素が到達していることが認められた「3点」
毛根中深部へ色素が到達していることが認められた「2点」
皮脂腺深部へ色素が到達していることが認められた「1点」
皮脂腺深部へ色素が到達していることが認められない「0点」
A. Usability Test Regarding the obtained formulations, the usability (penetration into pores) of each composition during application was evaluated using the following method.
Three lots of preparations for each composition were prepared, and these were prepared into a coloring preparation of 0.25% Coomassie Brilliant Blue R-250 (CBB R-250, manufactured by Tokyo Kasei Kogyo Co., Ltd.). Next, the hair on the back of the C57BL/6 mouse was trimmed to a length of 1 mm using clippers, and then the coloring preparation was applied. After application, the color preparation was immediately wiped off, the applied skin was collected, and fresh sections were prepared. The prepared raw sections were observed with an optical microscope, and the depth of dye reaching the hair follicles was evaluated based on the following index.
<Usability>
・Penetration into pores: 4 points, indicating that the pigment has reached the lower end of the hair root
``3 points'' indicates that the pigment has reached deep into the hair root
"2 points" indicates that the pigment has reached the middle and deep part of the hair root.
"1 point" indicates that the pigment has reached deep into the sebaceous glands
``0 point'' where it is not recognized that the pigment has reached deep into the sebaceous glands

表1中のDCI及びエキスの含有量以外の数値は、使用性の評価結果の数値である。表1の結果より、DCI含有製剤において特定のエキスを含有することにより、DCIを用いた水溶性製剤としての使用性を向上させることが可能と判断できる。 The numerical values other than the DCI and extract contents in Table 1 are the numerical values of the usability evaluation results. From the results in Table 1, it can be determined that by including a specific extract in a DCI-containing preparation, it is possible to improve the usability of the water-soluble preparation using DCI.

Claims (5)

D-chiro-イノシトールと、
エキスと、
水と、を含み、
人参抽出物を含まず、
前記エキスが、クロレラエキス、オウゴンエキス、ローズマリーエキス、サクラ葉エキス、ユーカリエキス、マツエキス、ダイズエキス、センブリエキス、海藻エキス、ローヤルゼリーエキス、ビワ葉エキス、ゴボウエキス、ジオウエキス、オドリコソウエキス、オランダカラシエキス、セイヨウキズタエキス、及びセージエキスからなる群より選択される1種若しくは2種以上のエキスであり、
D-chiro-イノシトールの含有量が0.1質量%以上であり、
前記エキスの含有量が0.1質量%以上であり、
前記エキスは、D-chiro-イノシトールを含むマメ科植物の抽出物ではない、外用組成物。
D-chiro-inositol,
Extract and
including water;
Contains no ginseng extract,
The extracts include chlorella extract, scutellariae extract, rosemary extract, cherry leaf extract, eucalyptus extract, pine extract, soybean extract, Japanese japonica extract, seaweed extract, royal jelly extract, loquat leaf extract, burdock extract, rhododendron extract, dead networt extract, Dutch mustard extract, One or more extracts selected from the group consisting of Ivy extract and sage extract,
The content of D-chiro-inositol is 0.1% by mass or more,
The content of the extract is 0.1% by mass or more,
A composition for external use, wherein the extract is not a legume extract containing D-chiro-inositol.
D-chiro-イノシトールの含有量が0.1~20質量%である、請求項1に記載の外用組成物。 The external composition according to claim 1, wherein the content of D-chiro-inositol is 0.1 to 20% by mass. 前記エキスが、クロレラエキス、オウゴンエキス、ローズマリーエキス、サクラ葉エキス、ユーカリエキス、マツエキス、ダイズエキス、センブリエキス、海藻エキス、又はローヤルゼリーエキスを含む、請求項1又は2に記載の外用組成物。 The external composition according to claim 1 or 2, wherein the extract includes chlorella extract, scutellariae extract, rosemary extract, cherry leaf extract, eucalyptus extract, pine extract, soybean extract, Japanese japonica extract, seaweed extract, or royal jelly extract. 前記エキスの含有量が0.1~30質量%である、請求項1~3のいずれか一項に記載の外用組成物。 The composition for external use according to any one of claims 1 to 3, wherein the content of the extract is 0.1 to 30% by mass. 頭皮用である、請求項1~4のいずれか一項に記載の外用組成物。 The external composition according to any one of claims 1 to 4, which is for scalp use.
JP2018248587A 2018-12-28 2018-12-28 External composition containing D-chiro-inositol Active JP7425536B2 (en)

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JP2000344632A (en) 1999-06-07 2000-12-12 Ichimaru Pharcos Co Ltd Hair grower containing plant extract
JP2001139435A (en) 1999-11-17 2001-05-22 Oji Paper Co Ltd Hair restorer
JP2011246352A (en) 2010-05-21 2011-12-08 Kikuboshi:Kk Hair styling agent composition
JP2014208714A (en) 2014-08-13 2014-11-06 株式会社ツツミプランニング Hair tonic with dissolution ability of sebum-hardened product blocking pore
CN106474016A (en) 2016-12-16 2017-03-08 深圳市聚华太科技有限公司 A kind of scalp topical composition and scalp tonic liquid
WO2017188393A1 (en) 2016-04-27 2017-11-02 小林製薬株式会社 Hair-growth agent
JP2018138533A (en) 2017-02-24 2018-09-06 共栄化学工業株式会社 Hair Cosmetics

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JP3321712B2 (en) * 1992-06-04 2002-09-09 株式会社林原生物化学研究所 Topical hair restorer containing pine extract

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JP2000344632A (en) 1999-06-07 2000-12-12 Ichimaru Pharcos Co Ltd Hair grower containing plant extract
JP2001139435A (en) 1999-11-17 2001-05-22 Oji Paper Co Ltd Hair restorer
JP2011246352A (en) 2010-05-21 2011-12-08 Kikuboshi:Kk Hair styling agent composition
JP2014208714A (en) 2014-08-13 2014-11-06 株式会社ツツミプランニング Hair tonic with dissolution ability of sebum-hardened product blocking pore
WO2017188393A1 (en) 2016-04-27 2017-11-02 小林製薬株式会社 Hair-growth agent
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