JP5734686B2 - Skin external composition - Google Patents
Skin external composition Download PDFInfo
- Publication number
- JP5734686B2 JP5734686B2 JP2011021628A JP2011021628A JP5734686B2 JP 5734686 B2 JP5734686 B2 JP 5734686B2 JP 2011021628 A JP2011021628 A JP 2011021628A JP 2011021628 A JP2011021628 A JP 2011021628A JP 5734686 B2 JP5734686 B2 JP 5734686B2
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- JP
- Japan
- Prior art keywords
- composition
- acid
- skin
- copolymer
- external
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Landscapes
- Medicinal Preparation (AREA)
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
本発明は、ニキビを効果的に予防又は治療できる安定な皮膚外用組成物に関する。 The present invention relates to a stable external composition for skin that can effectively prevent or treat acne.
アゼライン酸はニキビの治療剤の有効成分として広く使用されてきた化合物である。しかし、アゼライン酸を含むクリームなどの製剤は安定性が悪く、経時的に粘度が低下したり、相分離し易い。特に高濃度のアゼライン酸を含む場合にはアゼライン酸が分散状態になることもあり、製剤が、分離を起こすなど不安定となり易く、粘度低下によって不均一になることもある。このため、流通、保存中に、性状が変化して、商品価値が著しく低下する。 Azelaic acid is a compound that has been widely used as an active ingredient in acne treatments. However, preparations such as creams containing azelaic acid have poor stability, and the viscosity decreases over time and phase separation tends to occur. In particular, when a high concentration of azelaic acid is contained, the azelaic acid may be in a dispersed state, the preparation tends to be unstable such as causing separation, and may become non-uniform due to a decrease in viscosity. For this reason, the property changes during distribution and storage, and the commercial value is significantly reduced.
本発明は、アゼライン酸を含む皮膚外用組成物であって、安定性が良好なものを提供することを主な課題とする。 The main object of the present invention is to provide an external composition for skin containing azelaic acid, which has good stability.
本発明者は上記課題を解決するために研究を重ね、アゼライン酸を含む皮膚外用組成物に、アクリロイルジメチルタウリンアンモニウムとビニル系又はアクリル系単官能性モノマーとの共重合体を添加することにより、組成物の経時的な安定性が改善されることを見出した。
本発明は、上記知見に基づき完成されたものであり、以下の皮膚外用組成物等を提供する。
項1. アゼライン酸と、アクリロイルジメチルタウリンアンモニウムとビニル系又はアクリル系単官能性モノマーとの共重合体を含む皮膚外用組成物。
項2. ビニル系又はアクリル系単官能性モノマーが、下記式(1)
下記一般式(2)
で表されるモノマーである項1に記載の皮膚外用組成物。
項3. アゼライン酸の含有量が、組成物の全量に対して、5〜40重量%である項1又は2に記載の皮膚外用組成物。
項4. さらに、セルロース系増粘剤を含む項1〜3のいずれかに記載の皮膚外用組成物。
項5. さらに、ポリマー粉末を含む項1〜4のいずれかに記載の皮膚外用組成物。
項6. 組成物のpHが3〜6である項1〜5のいずれかに記載の皮膚外用組成物。
項7. アゼライン酸を含む組成物に、アクリロイルジメチルタウリンアンモニウムとビニル系又はアクリル系単官能性モノマーとの共重合体を添加する、アゼライン酸を含む組成物の安定性の向上方法。
項8. アゼライン酸を含む組成物に、アクリロイルジメチルタウリンアンモニウムとビニル系又はアクリル系単官能性モノマーとの共重合体を添加する、アゼライン酸を含む組成物の分離抑制方法。
The present inventor repeated research to solve the above-mentioned problems, and by adding a copolymer of acryloyldimethyltaurine ammonium and a vinyl-based or acrylic monofunctional monomer to a composition for external use containing azelaic acid, It has been found that the stability of the composition over time is improved.
The present invention has been completed based on the above findings, and provides the following external composition for skin.
Item 1. An external composition for skin comprising azelaic acid, a copolymer of ammonium acryloyldimethyltaurate and a vinyl-based or acrylic monofunctional monomer.
Item 2. Vinyl or acrylic monofunctional monomer is represented by the following formula (1)
Item 2. The external composition for skin according to Item 1, which is a monomer represented by:
Item 3. Item 3. The external composition for skin according to Item 1 or 2, wherein the content of azelaic acid is 5 to 40% by weight based on the total amount of the composition.
Item 4. Item 4. The external composition for skin according to any one of Items 1 to 3, further comprising a cellulose-based thickener.
Item 5. Item 5. The external composition for skin according to any one of Items 1 to 4, further comprising a polymer powder.
Item 6. Item 6. The external composition for skin according to any one of Items 1 to 5, wherein the pH of the composition is 3 to 6.
Item 7. A method for improving the stability of a composition containing azelaic acid, comprising adding a copolymer of acryloyldimethyltaurate ammonium and a vinyl or acrylic monofunctional monomer to a composition containing azelaic acid.
Item 8. A method for inhibiting separation of a composition containing azelaic acid, comprising adding a copolymer of acryloyldimethyltaurate ammonium and a vinyl-based or acrylic monofunctional monomer to a composition containing azelaic acid.
本発明の皮膚外用組成物は、アクリロイルジメチルタウリンアンモニウムとビニル系又はアクリル系単官能性モノマーとの共重合体を含有するため、使用感や外観のよい製剤が得られる。さらに、長期保存後にも、粘度低下による不均一や分離が抑制される。このため、ニキビ治療に有効な高濃度のアゼライン酸を含有させることができる。 Since the composition for external use of the skin of the present invention contains a copolymer of acryloyldimethyltaurate ammonium and a vinyl-type or acrylic-type monofunctional monomer, a preparation with good usability and appearance can be obtained. Furthermore, even after long-term storage, nonuniformity and separation due to viscosity reduction are suppressed. For this reason, the high concentration azelaic acid effective for acne treatment can be contained.
以下、本発明を詳細に説明する。
本発明の皮膚外用組成物は、アゼライン酸と、アクリロイルジメチルタウリンアンモニウムとビニル系又はアクリル系単官能性モノマーとの共重合体を含む組成物である。
Hereinafter, the present invention will be described in detail.
The composition for external use of the skin of the present invention is a composition containing azelaic acid, a copolymer of ammonium acryloyldimethyltaurate and a vinyl or acrylic monofunctional monomer.
アゼライン酸
組成物中のアゼライン酸の含有量は、組成物の全量に対して、5重量%以上が好ましく、10重量%以上がより好ましく、15重量%以上がさらにより好ましい。この範囲であれば、ニキビ治療効果が十分に得られる。
また、組成物中のアゼライン酸の含有量は、40重量%以下が好ましく、30重量%以下がより好ましく、25重量%以下がさらにより好ましい。この範囲であれば、十分に組成物を安定化できる。
The content of azelaic acid azelaic acid composition, relative to the total amount of the composition, preferably at least 5 wt%, more preferably at least 10 wt%, even more preferably more than 15 wt%. If it is this range, the acne treatment effect is fully acquired.
The content of azelaic acid in the composition is preferably 40% by weight or less, more preferably 30% by weight or less, and even more preferably 25% by weight or less. If it is this range, a composition can fully be stabilized.
ビニル系又はアクリル系単官能性モノマー
本発明では、アクリロイルジメチルタウリンアンモニウムとビニル系又はアクリル系単官能性モノマーとの共重合体を用いる。このような共重合体にすることで、広範囲の条件で組成物を安定化することができるようになる。
ビニル系又はアクリル系単官能性モノマーは非イオン性であることが好ましく、これにより、一層効果的に組成物が安定化される。また、ビニル系又はアクリル系単官能性モノマーは疎水性であることが好ましく、これにより、一層効果的に組成物が安定化される。
Vinyl or acrylic monofunctional monomer In the present invention, a copolymer of ammonium acryloyldimethyltaurate and a vinyl or acrylic monofunctional monomer is used. By using such a copolymer, the composition can be stabilized under a wide range of conditions.
The vinyl or acrylic monofunctional monomer is preferably nonionic, which stabilizes the composition more effectively. Moreover, it is preferable that a vinyl type or acrylic monofunctional monomer is hydrophobic, and this stabilizes the composition more effectively.
ビニル系又はアクリル系単官能性モノマーとしては、下記式(1)
また、ビニル系又はアクリル系単官能性モノマーとしては、(メタ)アクリル酸系単官能性モノマー、中でも、メタアクリル酸系単官能性モノマーが好ましく挙げられる。中でも、下記一般式(2)
で表されるモノマーが好ましい。
R1は、メチル、エチル、ステアリル、ベヘニルが好ましく、ベヘニルがより好ましい。また、nは1〜80が好ましく、1〜50がより好ましく、10〜30がさらにより好ましい。
この共重合体は、1種を単独で、又は2種以上を組み合わせて使用できる。
Moreover, as a vinyl type or an acrylic type monofunctional monomer, a (meth) acrylic acid type monofunctional monomer, Among these, a methacrylic acid type monofunctional monomer is mentioned preferably. Among them, the following general formula (2)
The monomer represented by these is preferable.
R 1 is preferably methyl, ethyl, stearyl or behenyl, more preferably behenyl. Moreover, 1-80 are preferable, as for n, 1-50 are more preferable, and 10-30 are still more preferable.
This copolymer can be used individually by 1 type or in combination of 2 or more types.
共重合体の含有量
組成物中のアクリロイルジメチルタウレートとビニル系又はアクリル系単官能性モノマーとの共重合体の含有量は、組成物の全量に対して、0.01〜10重量%程度とすることができる。特に、0.1重量%以上が好ましく、0.2重量%以上がより好ましく、0.3重量%以上がさらにより好ましい。この範囲であれば、十分に組成物を安定化できる。
また、組成物中のこの共重合体の含有量は、5重量%以下が好ましく、3重量%以下がより好ましく、1重量%以下がさらにより好ましい。この範囲であれば、滑らかで塗布し易い組成物となる。
アゼライン酸と共重合体との配合比率
本発明の組成物中のアゼライン酸と上記説明した共重合体との配合比率は、重量比で、アゼライン酸:共重合体が、約1:0.00025〜2が好ましく、約1:0.0025〜1がより好ましく、約1:0.0075〜0.2がさらにより好ましい。上記範囲であれば、十分な安定性が得られる。
Content of copolymer The content of the copolymer of acryloyldimethyltaurate and vinyl-based or acrylic monofunctional monomer in the composition is about 0.01 to 10% by weight relative to the total amount of the composition. It can be. In particular, 0.1% by weight or more is preferable, 0.2% by weight or more is more preferable, and 0.3% by weight or more is even more preferable. If it is this range, a composition can fully be stabilized.
Further, the content of the copolymer in the composition is preferably 5% by weight or less, more preferably 3% by weight or less, and still more preferably 1% by weight or less. Within this range, the composition is smooth and easy to apply.
Blending ratio of azelaic acid and copolymer The blending ratio of azelaic acid and the above-described copolymer in the composition of the present invention is about 1: 0.00025 by weight, with azelaic acid: copolymer being about 1: 0.00025. -2 is preferred, about 1: 0.0025-1 is more preferred, and about 1: 0.0075-0.2 is even more preferred. If it is the said range, sufficient stability will be acquired.
セルロース系増粘剤
本発明の皮膚外用組成物は、セルロース系増粘剤を含むことが好ましい。アゼライン酸と、アクリロイルジメチルタウレートとビニル系又はアクリル系単官能性モノマーとの共重合体とを含む組成物は、セルロース系増粘剤を含むことにより、粘度低下が一層効果的に抑制され、組成物の安定性が一層向上する。
セルロース系増粘剤としては、メチルセルロース、エチルセルロース、ヒドロキシエチルセルロース、ヒドロキシメチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、カルボキシメチルセルロース、カルボキシエチルセルロース、又はこれらの薬理学的に許容される塩などが挙げられる。中でも、ヒドロキシエチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロースが好ましく、ヒドロキシプロピルメチルセルロースがより好ましい。
セルロース系増粘剤は、1種を単独で、又は2種以上を組み合わせて使用できる。
組成物中のセルロース系増粘剤の含有量は、組成物の全量に対して、0.01重量%以上が好ましく、0.05重量%以上がより好ましく、0.1重量%以上がさらにより好ましい。この範囲であれば、セルロース系増粘剤の添加による粘度低下抑制効果、及び組成物の安定性向上効果が十分に得られる。また、十分な増粘効果が得られる。
また、組成物中のセルロース系増粘剤の含有量は、0.5重量%以下が好ましく、1重量%以下がより好ましく2重量%以下がさらにより好ましい。この範囲であれば、べたつきが少ない組成物となる。
Cellulose thickener The composition for external use of the skin of the present invention preferably contains a cellulose thickener. The composition containing azelaic acid, a copolymer of acryloyldimethyltaurate and a vinyl-based or acrylic monofunctional monomer, the viscosity reduction is more effectively suppressed by including a cellulose-based thickener, The stability of the composition is further improved.
Examples of the cellulose thickener include methyl cellulose, ethyl cellulose, hydroxyethyl cellulose, hydroxymethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, carboxymethyl cellulose, carboxyethyl cellulose, or a pharmacologically acceptable salt thereof. Among these, hydroxyethyl cellulose, hydroxypropyl cellulose, and hydroxypropyl methylcellulose are preferable, and hydroxypropylmethylcellulose is more preferable.
A cellulosic thickener can be used individually by 1 type or in combination of 2 or more types.
The content of the cellulose-based thickener in the composition is preferably 0.01% by weight or more, more preferably 0.05% by weight or more, and even more preferably 0.1% by weight or more based on the total amount of the composition. preferable. If it is this range, the viscosity fall inhibitory effect by addition of a cellulose thickener and the stability improvement effect of a composition will fully be acquired. In addition, a sufficient thickening effect can be obtained.
In addition, the content of the cellulose-based thickener in the composition is preferably 0.5% by weight or less, more preferably 1% by weight or less, and even more preferably 2% by weight or less. If it is this range, it will become a composition with little stickiness.
ポリマー粉末
本発明の皮膚外用組成物は、ポリマー粉末を含むことが好ましい。これにより、皮膚への塗布時の滑りが良くなり、簡単に皮膚に広げることができるようになる。このため、ニキビを擦らなくて済むようになる。
ポリマー粉末としては、ナイロン粉末、ポリアクリル酸アルキル粉末、メチルシロキサン網状重合体粉末等が挙げられる。
ポリマー粉末は、1種を単独で、又は2種以上を組み合わせて使用できる。
組成物中のポリマー粉末の含有量は、組成物の全量に対して、0.1重量%以上が好ましく、0.5重量%以上がより好ましく、1重量%以上がさらにより好ましい。この範囲であれば、十分に滑りが良くなる。
また、組成物中のポリマー粉末の含有量は、5重量%以下が好ましく、3重量%以下がより好ましく、2重量%以下がさらにより好ましい。この範囲であれば、製剤が不安定にならない。
Polymer powder The composition for external use of the skin of the present invention preferably contains a polymer powder. Thereby, the slip at the time of application | coating to skin improves, and it can spread now on skin easily. For this reason, it becomes unnecessary to rub acne.
Examples of the polymer powder include nylon powder, polyalkyl acrylate powder, and methylsiloxane network polymer powder.
A polymer powder can be used individually by 1 type or in combination of 2 or more types.
The content of the polymer powder in the composition is preferably 0.1% by weight or more, more preferably 0.5% by weight or more, and still more preferably 1% by weight or more based on the total amount of the composition. If it is this range, it will become slippery enough.
Further, the content of the polymer powder in the composition is preferably 5% by weight or less, more preferably 3% by weight or less, and still more preferably 2% by weight or less. If it is this range, a formulation will not become unstable.
pH
本発明の皮膚外用組成物のpHは、約3〜6の酸性範囲であることが好ましく、約3〜5がより好ましく、約3.5〜4.5がさらにより好ましい。この範囲であれば、アゼライン酸によるニキビ治療効果が十分に得られると共に、強い刺激感を感じ難い組成物となる。
pH
The pH of the external composition for skin of the present invention is preferably in the acidic range of about 3-6, more preferably about 3-5, and even more preferably about 3.5-4.5. If it is this range, while the acne treatment effect by azelaic acid will fully be acquired, it will become a composition which is hard to feel a strong irritation feeling.
製剤形態
本発明の外用組成物は、アゼライン酸又はその塩、及びアクリロイルジメチルタウレートとビニル系又はアクリル系単官能性モノマーとの共重合体、さらに必要に応じて、セルロース系増粘剤やポリマー粉末を、医薬品、医薬部外品、又は化粧品に通常使用される基剤又は担体、及び必要に応じて添加剤と共に混合して、医薬品、医薬部外品、又は化粧品用の皮膚外用組成物とすることができる。
Formulation Form The composition for external use of the present invention comprises azelaic acid or a salt thereof, a copolymer of acryloyldimethyltaurate and a vinyl or acrylic monofunctional monomer, and if necessary, a cellulose thickener or a polymer A powder is mixed with a base or carrier usually used for pharmaceuticals, quasi-drugs, or cosmetics, and, if necessary, additives, and a skin external composition for pharmaceuticals, quasi-drugs, or cosmetics. can do.
医薬品用の皮膚外用組成物の形態は特に限定されず、例えば、液剤、懸濁剤、乳剤、クリーム剤、軟膏剤、ゲル剤、リニメント剤、ローション剤、エアゾール剤などが挙げられる。これらの製剤は、第15改正日本薬局方製剤総則に記載の方法等に従い製造することができる。中でも、液剤、懸濁剤、乳剤、クリーム剤、軟膏剤、ゲル剤、ローション剤、エアゾール剤が好ましく、クリーム剤、乳剤、ゲル剤がより好ましい。クリーム剤、乳剤、ゲル剤としては、低級アルコール及び/又は多価アルコールを基剤として含むものが挙げられる。
医薬部外品又は化粧品用の皮膚外用組成物とする場合も、上記の医薬品と同様の形態にすることができる。また、それ以外にも、スティック剤や、不織布に薬液を含浸させたシート剤等が挙げられる。中でも、液剤、懸濁剤、乳剤、クリーム剤、軟膏剤、ゲル剤、ローション剤、シート剤が好ましく、クリーム剤、乳剤、ゲル剤がより好ましい。クリーム剤、乳剤、ゲル剤としては、低級アルコール及び/又は多価アルコールを基剤として含むものが挙げられる。
クリーム剤、乳剤のように、油性基剤と水性基剤とを含む場合は、W/O型でもよく、O/W型でもよいが、O/W型が好ましい。
水を含まない基剤の場合は、軟膏剤や、低級アルコール及び/又は多価アルコール等を基剤とする液剤が好ましい。
医薬部外品又は化粧品用の皮膚外用組成物とする場合の用途としては具体的には、化粧水、乳液、ジェル、クリーム、美容液、日焼け止め用化粧料、パック、マスク、ハンドクリーム、ボディローション、ボディークリームのような基礎化粧料;洗顔料、メイク落とし、ボディーシャンプー、シャンプー、リンス、トリートメントのような洗浄用化粧料などが挙げられる。
The form of the external composition for skin for pharmaceuticals is not particularly limited, and examples thereof include solutions, suspensions, emulsions, creams, ointments, gels, liniments, lotions, and aerosols. These preparations can be produced according to the method described in the 15th revised Japanese Pharmacopoeia General Rules for Preparations. Of these, liquids, suspensions, emulsions, creams, ointments, gels, lotions and aerosols are preferred, and creams, emulsions and gels are more preferred. Examples of creams, emulsions, and gels include those containing a lower alcohol and / or a polyhydric alcohol as a base.
Also when it is set as the composition for external use on the skin for quasi drugs or cosmetics, it can be made into the same form as said pharmaceutical. In addition, a stick agent, a sheet agent obtained by impregnating a nonwoven fabric with a chemical solution, and the like can be given. Of these, liquids, suspensions, emulsions, creams, ointments, gels, lotions, and sheets are preferable, and creams, emulsions, and gels are more preferable. Examples of creams, emulsions, and gels include those containing a lower alcohol and / or a polyhydric alcohol as a base.
When an oily base and an aqueous base are included as in creams and emulsions, they may be W / O type or O / W type, but O / W type is preferred.
In the case of a base not containing water, an ointment or a liquid based on a lower alcohol and / or a polyhydric alcohol is preferred.
Specifically, the skin external composition for quasi-drugs or cosmetics includes skin lotions, emulsions, gels, creams, serums, sunscreen cosmetics, packs, masks, hand creams, bodies Basic cosmetics such as lotions and body creams; cleansing cosmetics such as face wash, makeup remover, body shampoo, shampoo, rinse and treatment.
基剤又は担体
基剤又は担体としては、流動パラフィン、スクワラン、ワセリン、ゲル化炭化水素(プラスチベースなど)、オゾケライト、α−オレフィンオリゴマー、軽質流動パラフィンのような炭化水素;メチルポリシロキサン、架橋型メチルポリシロキサン、高重合メチルポリシロキサン、環状シリコーン、アルキル変性シリコーン、架橋型アルキル変性シリコーン、アミノ変性シリコーン、ポリエーテル変性シリコーン、ポリグリセリン変性シリコーン、架橋型ポリエーテル変性シリコーン、架橋型アルキルポリエーテル変性シリコーン、シリコーン・アルキル鎖共変性ポリエーテル変性シリコーン、シリコーン・アルキル鎖共変性ポリグリセリン変性シリコーン、ポリエーテル変性分岐シリコーン、ポリグリセリン変性分岐シリコーン、アクリルシリコン、フェニル変性シリコーン、シリコーンレジンのようなシリコーン油;セタノール、セトステアリルアルコール、ステアリルアルコール、ベヘニルアルコールのような高級アルコール;エチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロースのようなセルロース誘導体;ポリビニルピロリドン;カラギーナン;ポリビニルブチラート;ポリエチレングリコール;ジオキサン;ブチレングリコールアジピン酸ポリエステル;ミリスチン酸イソプロピル、ミリスチン酸オクチルドデシル、パルミチン酸イソプロピル、パルミチン酸セチル、イソノナン酸イソノニル、テトラ2−エチルヘキサン酸ペンタエリスリット、ホホバ油のようなエステル類;デキストリン、マルトデキストリンのような多糖類;エタノール、イソプロパノールのような低級アルコール;エチレングリコールモノメチルエーテル、エチレングリコールモノエチルエーテル、エチレングリコールモノプロピルエーテル、ジエチレングリコールモノメチルエーテル、ジエチレングリコールモノエチルエーテル、ジエチレングリコールモノプロピルエーテル、ジエチレングリコールモノブチルエーテル、プロピレングリコールモノエチルエーテル、プロピレングリコールモノプロピルエーテル、ジプロピレングリコールモノエチルエーテル、ジプロピレングリコールモノプロピルエーテルのようなグリコールエーテル;ポリエチレングリコール、プロピレングリコール、1,3-ブチレングリコール、グリセリン、イソプレングリコール、ジグリセリン、ジプロピレングリコールなどの多価アルコール;水などの水系基剤などが挙げられる。
中でも、多価アルコール、高級アルコール、炭化水素、エステル類、シリコーン油が好ましく、多価アルコールが、より好ましい。多価アルコールの中では、1,3-ブチレングリコール、プロピレングリコール、イソプレングリコール、グリセリン、ジグリセリン、ジプロピレングリコールが好ましく、1,3-ブチレングリコール、プロピレングリコール、グリセリン、ジグリセリンがさらに好ましい。本発明の組成物の好ましい例として、基剤として多価アルコールを含むクリーム剤、ゲル剤、乳剤が挙げられる。
基剤又は担体は、1種を単独で、又は2種以上を組み合わせて使用できる。
As a base or carrier base or carrier, liquid paraffin, squalane, vaseline, hydrocarbon gel (such as Plastibase), ozokerite, alpha-olefin oligomers, hydrocarbons such as light liquid paraffin; methylpolysiloxane, crosslinked methyl Polysiloxane, Highly polymerized methylpolysiloxane, Cyclic silicone, Alkyl-modified silicone, Cross-linked alkyl-modified silicone, Amino-modified silicone, Polyether-modified silicone, Polyglycerin-modified silicone, Cross-linked polyether-modified silicone, Cross-linked alkyl polyether-modified silicone , Silicone / alkyl chain co-modified polyether modified silicone, silicone / alkyl chain co-modified polyglycerin modified silicone, polyether modified branched silicone, polyglycerin modified branched silicone , Silicone oils such as acrylic silicon, phenyl-modified silicone, and silicone resin; higher alcohols such as cetanol, cetostearyl alcohol, stearyl alcohol, and behenyl alcohol; cellulose derivatives such as ethyl cellulose, hydroxypropyl cellulose, and hydroxypropyl methylcellulose; polyvinylpyrrolidone; Carrageenan; polyvinyl butyrate; polyethylene glycol; dioxane; butylene glycol adipic acid polyester; isopropyl myristate, octyldodecyl myristate, isopropyl palmitate, cetyl palmitate, isononyl isononanoate, pentaerythritol tetra-2-ethylhexanoate, jojoba oil Esters such as dextrin and maltodextrin Lower alcohols such as ethanol and isopropanol; ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, ethylene glycol monopropyl ether, diethylene glycol monomethyl ether, diethylene glycol monoethyl ether, diethylene glycol monopropyl ether, diethylene glycol monobutyl ether, propylene glycol Glycol ethers such as monoethyl ether, propylene glycol monopropyl ether, dipropylene glycol monoethyl ether, dipropylene glycol monopropyl ether; polyethylene glycol, propylene glycol, 1,3-butylene glycol, glycerin, isoprene glycol, diglycerin, Dipropylene grease Examples thereof include polyhydric alcohols such as coal; aqueous bases such as water.
Of these, polyhydric alcohols, higher alcohols, hydrocarbons, esters, and silicone oils are preferable, and polyhydric alcohols are more preferable. Among the polyhydric alcohols, 1,3-butylene glycol, propylene glycol, isoprene glycol, glycerin, diglycerin, and dipropylene glycol are preferable, and 1,3-butylene glycol, propylene glycol, glycerin, and diglycerin are more preferable. Preferable examples of the composition of the present invention include creams, gels and emulsions containing a polyhydric alcohol as a base.
A base or a support | carrier can be used individually by 1 type or in combination of 2 or more types.
添加剤
本発明の外用組成物には、本発明の効果を損なわない範囲で、医薬品、医薬部外品、又は化粧品に添加される公知の添加剤、例えば、酸化防止剤、界面活性剤、増粘剤、保存剤、pH調整剤、安定化剤、刺激軽減剤、防腐剤、着色剤、香料、パール光沢付与剤等を添加することができる。
酸化防止剤としては、ジブチルヒドロキシトルエン、ブチルヒドロキシアニソール、ソルビン酸、亜硫酸ナトリウム、アスコルビン酸、アスコルビン酸誘導体、トコフェロール、トコフェロール誘導体、エリソルビン酸、L−システイン塩酸塩などが挙げられる。
Additives In the composition for external use of the present invention, known additives that are added to pharmaceuticals, quasi drugs, or cosmetics, for example, antioxidants, surfactants, enhancers, within the range that does not impair the effects of the present invention. A sticking agent, a preservative, a pH adjuster, a stabilizer, an irritation reducing agent, an antiseptic, a coloring agent, a fragrance, a pearl luster imparting agent, and the like can be added.
Examples of the antioxidant include dibutylhydroxytoluene, butylhydroxyanisole, sorbic acid, sodium sulfite, ascorbic acid, ascorbic acid derivatives, tocopherol, tocopherol derivatives, erythorbic acid, L-cysteine hydrochloride and the like.
界面活性剤としては、例えば、ソルビタンモノイソステアレート、ソルビタンモノラウレート、ソルビタンモノパルミテート、ソルビタンモノステアレート、ペンタ−2−エチルヘキシル酸ジグリセロールソルビタン、テトラ−2−エチルヘキシル酸ジグリセロールソルビタンのようなソルビタン脂肪酸エステル類;モノステアリン酸プロピレングリコールのようなプロピレングリコール脂肪酸エステル類;ポリオキシエチレン硬化ヒマシ油40(HCO−40)、ポリオキシエチレン硬化ヒマシ油50(HCO−50)、ポリオキシエチレン硬化ヒマシ油60(HCO−60)、ポリオキシエチレン硬化ヒマシ油80などの硬化ヒマシ油誘導体;モノラウリル酸ポリオキシエチレン(20)ソルビタン(ポリソルベート20)、モノステアリン酸ポリオキシエチレン(20)ソルビタン(ポリソルベート60)、モノオレイン酸ポリオキシエチレン(20)ソルビタン(ポリソルベート80)、イソステアリン酸ポリオキシエチレン(20)ソルビタンのようなポリオキシエチレンソルビタン脂肪酸エステル類;ポリオキシエチレンモノヤシ油脂肪酸グリセリル;グリセリンアルキルエーテル;アルキルグルコシド;ポリオキシエチレンセチルエーテルのようなポリオキシアルキレンアルキルエーテル;ステアリルアミン、オレイルアミンのようなアミン類;ポリオキシエチレン・メチルポリシロキサン共重合体、ラウリルPEG−9ポリジメチルシロキシエチルジメチコン、PEG−9ポリジメチルシロキシエチルジメチコンのようなシリコーン系界面活性剤などが挙げられる。 Examples of the surfactant include sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, diglycerol sorbitan penta-2-ethylhexylate, and diglycerol sorbitan tetra-2-ethylhexylate. Sorbitan fatty acid esters; propylene glycol fatty acid esters such as propylene glycol monostearate; polyoxyethylene hydrogenated castor oil 40 (HCO-40), polyoxyethylene hydrogenated castor oil 50 (HCO-50), polyoxyethylene hardened Hardened castor oil derivatives such as castor oil 60 (HCO-60), polyoxyethylene hydrogenated castor oil 80; polyoxyethylene (20) sorbitan (polysorbate 20) monolaurate, monostearate Polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene (20) sorbitan (polysorbate 60), polyoxyethylene monooleate (20) sorbitan (polysorbate 80), polyoxyethylene (20) sorbitan isostearate; Glyceryl alkyl ether; alkyl glucoside; polyoxyalkylene alkyl ether such as polyoxyethylene cetyl ether; amines such as stearylamine and oleylamine; polyoxyethylene / methylpolysiloxane copolymer; And silicone surfactants such as lauryl PEG-9 polydimethylsiloxyethyl dimethicone and PEG-9 polydimethylsiloxyethyl dimethicone.
セルロース系増粘剤以外に増粘剤を含む場合は、例えば、グアーガム、ローカストビーンガム、カラギーナン、キサンタンガム、ポリビニルアルコール、ポリビニルピロリドン、カルボキシビニルポリマー、アクリル酸メタクリル酸アルキル共重合体、ポリエチレングリコール、ベントナイト、アルギン酸、マクロゴール、コンドロイチン硫酸ナトリウムなどが挙げられる。 When a thickener is included in addition to the cellulosic thickener, for example, guar gum, locust bean gum, carrageenan, xanthan gum, polyvinyl alcohol, polyvinyl pyrrolidone, carboxyvinyl polymer, alkyl methacrylate copolymer, polyethylene glycol, bentonite , Alginic acid, macrogol, sodium chondroitin sulfate and the like.
防腐剤、保存剤としては、安息香酸、安息香酸ナトリウム、デヒドロ酢酸、デヒドロ酢酸ナトリウム、パラオキシ安息香酸イソブチル、パラオキシ安息香酸イソプロピル、パラオキシ安息香酸ブチル、パラオキシ安息香酸エチル、パラオキシ安息香酸プロピル、パラオキシ安息香酸ベンジル、パラオキシ安息香酸メチル、フェノキシエタノール、ベンジルアルコール、クロロブタノール、ソルビン酸およびその塩、グルコン酸クロルヘキシジン、アルカンジオールなどが挙げられる。 Examples of preservatives and preservatives include benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl paraoxybenzoate, isopropyl paraoxybenzoate, butyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, paraoxybenzoic acid Examples include benzyl, methyl paraoxybenzoate, phenoxyethanol, benzyl alcohol, chlorobutanol, sorbic acid and its salts, chlorhexidine gluconate, alkanediol and the like.
pH調整剤としては、無機酸(塩酸、硫酸など)、有機酸(乳酸、乳酸ナトリウム、クエン酸、クエン酸ナトリウム、コハク酸、コハク酸ナトリウムなど)、無機塩基(水酸化カリウム、水酸化ナトリウムなど)、有機塩基(トリエタノールアミン、ジイソプロパノールアミン、トリイソプロパノールアミンなど)などが挙げられる。 Examples of pH adjusters include inorganic acids (hydrochloric acid, sulfuric acid, etc.), organic acids (lactic acid, sodium lactate, citric acid, sodium citrate, succinic acid, sodium succinate, etc.), inorganic bases (potassium hydroxide, sodium hydroxide, etc.) ) And organic bases (such as triethanolamine, diisopropanolamine, and triisopropanolamine).
安定化剤としては、ポリアクリル酸ナトリウム、ジブチルヒドロキシトルエン、ビチルヒドロキシアニソールなどが挙げられる。
刺激低減剤としては、甘草エキス、アルギン酸ナトリウムなどが挙げられる。
Examples of the stabilizer include sodium polyacrylate, dibutylhydroxytoluene, and bitylhydroxyanisole.
Examples of the irritation reducing agent include licorice extract and sodium alginate.
添加剤は、1種を単独で、又は2種以上を組み合わせて使用できる。 An additive can be used individually by 1 type or in combination of 2 or more types.
その他の有効成分
本発明の外用組成物は、本発明の効果を損なわない範囲で、その他の有効成分を含むことができる。有効成分の具体例としては、例えば、保湿成分、抗炎症成分、抗菌成分、ビタミン類、ペプチド又はその誘導体、アミノ酸又はその誘導体、細胞賦活化成分、老化防止成分、血行促進成分、角質軟化成分、美白成分、収斂成分などが挙げられる。
Other active ingredients The composition for external use of this invention can contain another active ingredient in the range which does not impair the effect of this invention. Specific examples of active ingredients include, for example, moisturizing ingredients, anti-inflammatory ingredients, antibacterial ingredients, vitamins, peptides or derivatives thereof, amino acids or derivatives thereof, cell activation ingredients, anti-aging ingredients, blood circulation promoting ingredients, keratin softening ingredients, Whitening ingredients, astringent ingredients, etc.
保湿成分としては、グリセリン、1,3−ブチレングリコール、プロピレングリコール、ポリエチレングリコール、ジグリセリントレハロースのような多価アルコール;ヒアルロン酸ナトリウム、ヘパリン類似物質、コンドロイチン硫酸ナトリウム、コラーゲン、エラスチン、ケラチン、キチン、キトサンのような高分子化合物;グリシン、アスパラギン酸、アルギニンのようなアミノ酸;乳酸ナトリウム、尿素、ピロリドンカルボン酸ナトリウムのような天然保湿因子;セラミド、コレステロール、リン脂質のような脂質;カミツレエキス、ハマメリスエキス、チャエキス、シソエキスのような植物抽出エキスなどが挙げられる。 As moisturizing ingredients, polyhydric alcohols such as glycerin, 1,3-butylene glycol, propylene glycol, polyethylene glycol, diglycerin trehalose; sodium hyaluronate, heparin-like substance, sodium chondroitin sulfate, collagen, elastin, keratin, chitin, Macromolecular compounds such as chitosan; amino acids such as glycine, aspartic acid, arginine; natural moisturizing factors such as sodium lactate, urea, sodium pyrrolidonecarboxylate; lipids such as ceramide, cholesterol, phospholipid; chamomile extract, hamamelis Plant extract such as extract, tea extract, perilla extract and the like can be mentioned.
抗炎症成分としては、植物(例えば、コンフリー)に由来する成分、アラントイン、グリチルリチン酸又はその誘導体、酸化亜鉛、塩酸ピリドキシン、酢酸トコフェロール、サリチル酸又はその誘導体、ε-アミノカプロン酸などが挙げられる。 Examples of the anti-inflammatory component include a plant-derived component (eg Comfrey), allantoin, glycyrrhizic acid or a derivative thereof, zinc oxide, pyridoxine hydrochloride, tocopherol acetate, salicylic acid or a derivative thereof, and ε-aminocaproic acid.
抗菌又は殺菌成分としては、クロルヘキシジン、サリチル酸、塩化ベンザルコニウム、アクリノール、イオウ、レゾルシン、エタノール、塩化ベンゼトニウム、アダパレン、過酸化ベンゾイル、クリンダマイシン、クレゾール、グルコン酸及びその誘導体、ポピドンヨード、ヨウ化カリウム、ヨウ素、イソプロピルメチルフェノール、トリクロカルバン、トリクロサン、感光素101号、感光素201号、パラベン、フェノキシエタノール、1,2-ペンタンジオール、塩酸アルキルジアミノグリシン、グルコン酸クロルヘキシジン、パラフェノールスルホン酸亜鉛等が挙げられる。 Antibacterial or bactericidal components include chlorhexidine, salicylic acid, benzalkonium chloride, acrinol, sulfur, resorcin, ethanol, benzethonium chloride, adapalene, benzoyl peroxide, clindamycin, cresol, gluconic acid and its derivatives, popidone iodine, potassium iodide , Iodine, isopropylmethylphenol, triclocarban, triclosan, photosensitizer 101, photosensitizer 201, paraben, phenoxyethanol, 1,2-pentanediol, alkyldiaminoglycine hydrochloride, chlorhexidine gluconate, zinc paraphenolsulfonate, etc. It is done.
ビタミン類としては、レチノール、酢酸レチノール、パルミチン酸レチノール等のレチノール誘導体、レチナール、レチノイン酸、レチノイン酸メチル、レチノイン酸エチル、レチノイン酸レチノール、d−δ−トコフェリルレチノエート、α−トコフェリルレチノエート、β−トコフェリルレチノエート等のビタミンA類;dl−α−トコフェロール、酢酸dl−α−トコフェロール、コハク酸dl−α−トコフェロール、コハク酸dl−α−トコフェロールカルシウム等のビタミンE類;リボフラビン、フラビンモノヌクレオチド、フラビンアデニンジヌクレオチド、リボフラビン酪酸エステル、リボフラビンテトラ酪酸エステル、リボフラビン5’−リン酸エステルナトリウム、リボフラビンテトラニコチン酸エステル等のビタミンB2類;ニコチン酸dl−α−トコフェロール、ニコチン酸ベンジル、ニコチン酸メチル、ニコチン酸β−ブトキシエチル、ニコチン酸1−(4−メチルフェニル)エチル等のニコチン酸類;アスコルビゲン−A、アスコルビン酸ステアリン酸エステル、アスコルビン酸パルミチン酸エステル、ジパルミチン酸L−アスコルビルなどのビタミンC類;メチルヘスペリジン、エルゴカルシフェロール、コレカルシフェロールなどのビタミンD類;フィロキノン、ファルノキノン等のビタミンK類、γ−オリザノール、ジベンゾイルチアミン、ジベンゾイルチアミン塩酸塩;チアミン塩酸塩、チアミンセチル塩酸塩、チアミンチオシアン酸塩、チアミンラウリル塩酸塩、チアミン硝酸塩、チアミンモノリン酸塩、チアミンリジン塩、チアミントリリン酸塩、チアミンモノリン酸エステルリン酸塩、チアミンモノリン酸エステル、チアミンジリン酸エステル、チアミンジリン酸エステル塩酸塩、チアミントリリン酸エステル、チアミントリリン酸エステルモノリン酸塩等のビタミンB1類;塩酸ピリドキシン、酢酸ピリドキシン、塩酸ピリドキサール、5’−リン酸ピリドキサール、塩酸ピリドキサミン等のビタミンB6類;シアノコバラミン、ヒドロキソコバラミン、デオキシアデノシルコバラミン等のビタミンB12類;葉酸、プテロイルグルタミン酸等の葉酸類;ニコチン酸、ニコチン酸アミドなどのニコチン酸類;パントテン酸、パントテン酸カルシウム、パントテニルアルコール(パンテノール)、D−パンテサイン、D−パンテチン、補酵素A、パントテニルエチルエーテル等のパントテン酸類;ビオチン、ビオチシン等のビオチン類;アスコルビン酸、アスコルビン酸ナトリウム、デヒドロアスコルビン酸、アスコルビン酸リン酸エステルナトリウム、アスコルビン酸リン酸エステルマグネシウム等のアスコルビン酸誘導体であるビタミンC類;カルニチン、フェルラ酸、α−リポ酸、オロット酸等のビタミン様作用因子などが挙げられる。 Vitamins include retinol, retinol acetate, retinol palmitate, etc., retinal, retinoic acid, methyl retinoic acid, ethyl retinoic acid, retinol retinoic acid, d-δ-tocopheryl retinoate, α-tocopheryl retinoate Vitamin A such as β-tocopheryl retinoate; vitamin E such as dl-α-tocopherol, dl-α-tocopherol acetate, dl-α-tocopherol succinate, dl-α-tocopherol calcium succinate; riboflavin, Vitamin B2 compounds such as flavin mononucleotide, flavin adenine dinucleotide, riboflavin butyrate, riboflavin tetrabutyrate, riboflavin 5'-phosphate sodium, riboflavin tetranicotinate Nicotinic acids such as dl-α-tocopherol nicotinate, benzyl nicotinate, methyl nicotinate, β-butoxyethyl nicotinate, 1- (4-methylphenyl) ethyl nicotinate; ascorbigen-A, ascorbic acid stearate, ascorbine Vitamin C such as acid palmitate ester, L-ascorbyl dipalmitate; Vitamin D such as methyl hesperidin, ergocalciferol, cholecalciferol; Vitamin K such as phylloquinone, farnoquinone, γ-oryzanol, dibenzoylthiamine, Dibenzoyl thiamine hydrochloride; thiamine hydrochloride, thiamine cetyl hydrochloride, thiamine thiocyanate, thiamine lauryl hydrochloride, thiamine nitrate, thiamine monophosphate, thiamine lysine salt, thiamine triphosphate, Vitamin B1 such as thiamine monophosphate, thiamine monophosphate, thiamine diphosphate, thiamine diphosphate, thiamine triphosphate, thiamine triphosphate monophosphate; pyridoxine hydrochloride, pyridoxine acetate, hydrochloric acid Vitamin B6 such as pyridoxal, 5′-phosphate pyridoxal, pyridoxamine hydrochloride; vitamin B12 such as cyanocobalamin, hydroxocobalamin, deoxyadenosylcobalamin; folic acid such as folic acid, pteroylglutamic acid; nicotinic acid, nicotinamide, etc. Nicotinic acids: Pantothenic acid, calcium pantothenate, pantothenyl alcohol (panthenol), D-pantetheine, D-pantethine, coenzyme A, pantothenyl ethyl ether, etc. Acids; biotins such as biotin and bioticin; vitamins C that are ascorbic acid derivatives such as ascorbic acid, sodium ascorbate, dehydroascorbic acid, sodium ascorbate phosphate sodium, magnesium ascorbate phosphate; carnitine, ferulic acid And vitamin-like agents such as α-lipoic acid and orotic acid.
ペプチド又はその誘導体としては、ケラチン分解ペプチド、加水分解ケラチン、コラーゲン、魚由来コラーゲン、アテロコラーゲン、ゼラチン、エラスチン、エラスチン分解ペプチド、コラーゲン分解ペプチド、加水分解コラーゲン、塩化ヒドロキシプロピルアンモニウム加水分解コラーゲン、エラスチン分解ペプチド、コンキオリン分解ペプチド、加水分解コンキオリン、シルク蛋白分解ペプチド、加水分解シルク、ラウロイル加水分解シルクナトリウム、大豆蛋白分解ペプチド、加水分解大豆蛋白、小麦蛋白、小麦蛋白分解ペプチド、加水分解小麦蛋白、カゼイン分解ペプチド、アシル化ペプチド(パルミトイルオリゴペプチド、パルミトイルペンタペプチド、パルミトイルテトラペプチド等)などが挙げられる。 Peptides or derivatives thereof include keratin-degrading peptide, hydrolyzed keratin, collagen, fish-derived collagen, atelocollagen, gelatin, elastin, elastin-degrading peptide, collagen-degrading peptide, hydrolyzed collagen, hydroxypropylammonium chloride hydrolyzed collagen, elastin-degrading peptide , Conchiolin degrading peptide, hydrolyzed conchiolin, silk proteolytic peptide, hydrolyzed silk, lauroyl hydrolyzed silk sodium, soy proteolytic peptide, hydrolyzed soy protein, wheat protein, wheat proteolytic peptide, hydrolyzed wheat protein, casein degrading peptide Acylated peptides (palmitoyl oligopeptide, palmitoyl pentapeptide, palmitoyl tetrapeptide, etc.).
アミノ酸又はその誘導体としては、ベタイン(トリメチルグリシン)、プロリン、ヒドロキシプロリン、アルギニン、リジン、セリン、グリシン、アラニン、フェニルアラニン、β−アラニン、スレオニン、グルタミン酸、グルタミン、アスパラギン、アスパラギン酸、システイン、シスチン、メチオニン、ロイシン、イソロイシン、バリン、ヒスチジン、タウリン、γ−アミノ酪酸、γ−アミノ−β−ヒドロキシ酪酸、カルニチン、カルノシン、クレアチン等が挙げられる。 As amino acids or their derivatives, betaine (trimethylglycine), proline, hydroxyproline, arginine, lysine, serine, glycine, alanine, phenylalanine, β-alanine, threonine, glutamic acid, glutamine, asparagine, aspartic acid, cysteine, cystine, methionine Leucine, isoleucine, valine, histidine, taurine, γ-aminobutyric acid, γ-amino-β-hydroxybutyric acid, carnitine, carnosine, creatine and the like.
細胞賦活化成分としては、γ-アミノ酪酸、ε-アミノプロン酸などのアミノ酸類;レチノール、チアミン、リボフラビン、塩酸ピリドキシン、パントテン酸類などのビタミン類;グリコール酸、乳酸などのα-ヒドロキシ酸類;タンニン、フラボノイド、サポニン、アラントイン、感光素301号などが挙げられる。
老化防止成分としては、パンガミン酸、カイネチン、ウルソール酸、ウコンエキス、スフィンゴシン誘導体、ケイ素、ケイ酸、N−メチル−L−セリン、メバロノラクトン等が挙げられる。
Cell activation components include amino acids such as γ-aminobutyric acid and ε-aminoproic acid; vitamins such as retinol, thiamine, riboflavin, pyridoxine hydrochloride and pantothenic acids; α-hydroxy acids such as glycolic acid and lactic acid; tannins, Examples include flavonoids, saponins, allantoin, and photosensitizer 301.
Examples of the anti-aging component include pangamic acid, kinetin, ursolic acid, turmeric extract, sphingosine derivative, silicon, silicic acid, N-methyl-L-serine, and mevalonolactone.
血行促進作用成分としては、植物(例えば、オタネニンジン、アシタバ、アルニカ、イチョウ、ウイキョウ、エンメイソウ、オランダカシ、カミツレ、ローマカミツレ、カロット、ゲンチアナ、ゴボウ、コメ、サンザシ、シイタケ、セイヨウサンザシ、セイヨウネズ、センキュウ、センブリ、タイム、チョウジ、チンピ、トウキ、トウニン、トウヒ、ニンジン、ニンニク、ブッチャーブルーム、ブドウ、ボタン、マロニエ、メリッサ、ユズ、ヨクイニン、ローズマリー、ローズヒップ、チンピ、トウキ、トウヒ、モモ、アンズ、クルミ、トウモロコシ)に由来する成分;グルコシルヘスペリジンなどが挙げられる。 Examples of the blood circulation promoting component include plants (e.g., ginseng, ashitaba, arnica, ginkgo, fennel, enmelio, dutch oak, chamomile, roman chamomile, carrot, gentian, burdock, rice, hawthorn, shiitake, hawthorn, prunus, nematode, Assembly, thyme, clove, chimney, spruce, spruce, spruce, carrot, garlic, butcher bloom, grape, button, maronier, melissa, yuzu, yokuinin, rosemary, rosehip, chimpy, touki, spruce, peach, apricot, walnut , A component derived from corn); and glucosyl hesperidin.
角質軟化成分としては、尿素、サリチル酸、グリコール酸、フルーツ酸、フィチン酸、イオウなどが挙げられる。
美白成分としては、アスコルビン酸とその誘導体、アルブチン、トコフェロールなどが挙げられる。
収斂成分としては、パラフェノールスルホン酸亜鉛、酸化亜鉛、メントール、エタノールなどが挙げられる。
Examples of the keratin softening component include urea, salicylic acid, glycolic acid, fruit acid, phytic acid, and sulfur.
Examples of the whitening component include ascorbic acid and its derivatives, arbutin, and tocopherol.
Examples of the astringent component include zinc paraphenol sulfonate, zinc oxide, menthol and ethanol.
その他の有効成分は1種を単独で、又は2種以上を組み合わせて使用できる。 Other active ingredients can be used alone or in combination of two or more.
使用方法
本発明の皮膚外用組成物は、使用対象の皮膚の状態、年齢、性別などによって異なるが、1日数回、適量を皮膚に塗布すればよい。
本発明の皮膚外用組成物は、ニキビの予防又は治療に好適に使用できる。従って、健常人の他、ニキビを有する人が好適な使用対象となる。
Method of Use The external composition for skin of the present invention may be applied to the skin several times a day, although it varies depending on the condition, age, sex, etc. of the target skin.
The external composition for skin of the present invention can be suitably used for the prevention or treatment of acne. Therefore, the person who has an acne other than a healthy person becomes a suitable use object.
その他
本発明は、アゼライン酸を含む組成物(特に、皮膚外用組成物)に、アクリロイルジメチルタウリンアンモニウムとビニル系又はアクリル系単官能性モノマーとの共重合体を添加する、アゼライン酸を含む組成物の安定性の向上方法、詳しくは、アゼライン酸を含む組成物の粘度低下抑制方法、又はアゼライン酸を含む組成物の分離の抑制方法を包含する。各成分の種類や使用量、組成物の性状などは、本発明の皮膚外用組成物について説明した通りである。
In addition, the present invention provides a composition containing azelaic acid, in which a copolymer of acryloyldimethyltaurine ammonium and a vinyl or acrylic monofunctional monomer is added to a composition containing azelaic acid (particularly a composition for external use on the skin). This method includes a method for improving the stability of the composition, specifically, a method for suppressing a decrease in viscosity of a composition containing azelaic acid, or a method for suppressing separation of a composition containing azelaic acid. The type and amount of each component, the properties of the composition, and the like are as described for the composition for external use of the present invention.
以下、本発明を実施例を挙げてより詳細に説明するが、本発明はこれらの実施例に限定されるものではない。
後掲の表1に示す各例において、A成分を加温と攪拌により溶解させておき、B成分のうちナイロン末以外の成分を加温により溶解した後、ナイロン末を添加して分散させておいた。A成分とB成分とをホモミキサーを用いて乳化した後、冷却し、C成分であるアゼライン酸、並びにpH調整用のD成分(精製水、トリエタノールアミン、及び乳酸)を添加し、撹拌して均一にした。これにより、クリームが得られた。
EXAMPLES Hereinafter, although an Example is given and this invention is demonstrated in detail, this invention is not limited to these Examples.
In each example shown in Table 1 below, component A is dissolved by heating and stirring, and components other than nylon powder among components B are dissolved by heating, and then nylon powder is added and dispersed. Oita. After emulsifying component A and component B using a homomixer, cool, add azelaic acid as component C, and component D for pH adjustment (purified water, triethanolamine, and lactic acid), and stir. And even. Thereby, a cream was obtained.
各クリームを50℃の恒温槽内で静置し、2週間後、及び1ヵ月後に外観を目視にて観察した。
また、調合直後のクリームを、20〜50歳の男女10人が、手や顔に塗布して、使用感を評価した。
各クリームの組成と、評価結果を以下の表1に示す。外観は、分離しない場合を○、分離した場合を×で示した。使用感は、非常に滑りが良く極めて良好な使用感である場合を◎、滑りが良く良好な場合を○、製剤がクリーム状でないために、モロモロとした感触がある場合を×で示した。
Each cream was allowed to stand in a thermostat at 50 ° C., and the appearance was visually observed after 2 weeks and 1 month.
In addition, 10 men and women aged 20 to 50 years old applied cream on their hands and face to evaluate the feeling of use.
The composition of each cream and the evaluation results are shown in Table 1 below. Appearance was indicated by ○ when not separated and × when separated. The feeling of use is indicated by ◎ when the feeling is very good and very good feeling, ◯ when the feeling is good and good, and x when the preparation is not creamy and has a feeling of moromi.
コポリマー:アクリロイルジメチルタウリンアンモニウム/ポリビニルピロリドンコポリマー(クラリアントジャパン社、Aristoflex AVC)
増粘剤1:ポリアクリルアミド、水添ポリイソブテン、ラウレス−7、水の混合物(SEPPIC社、SEPIGEL305)
増粘剤2:カルボキシメチルセルロースナトリウム、キサンタン、発酵セルロースの混合物(第一工業製薬、レオアクアCM−100)
Copolymer: Acryloyldimethyltaurine ammonium / polyvinylpyrrolidone copolymer (Clariant Japan, Aristoflex AVC)
Thickener 1: Polyacrylamide, hydrogenated polyisobutene, laureth-7, water mixture (SEPPIC, SEPIGEL 305)
Thickener 2: Mixture of sodium carboxymethylcellulose, xanthan and fermented cellulose (Daiichi Kogyo Seiyaku, Leo Aqua CM-100)
表1から明らかなように、アクリロイルジメチルタウリンアンモニウムとビニル系又はアクリル系単官能性モノマーとの共重合体を含む実施例1では、安定性、及び使用感共に良好であった。さらにヒドロキシプロピルメチルセルロースを含む実施例4も、安定性、及び使用感共に良好であった。さらに、ナイロン末を含む実施例2、3は、一層滑らかで使用感が良好であった。
一方、アクリロイルジメチルタウリンアンモニウムとビニル系又はアクリル系単官能性モノマーとの共重合体に代えて、他の増粘剤を含む比較例1〜4では、保存安定性に欠け、又はさらに使用感も悪かった。
具体的には、実施例1〜4は、使用感が良く、試験期間中も安定な製剤であったが、比較例1〜4は調合直後からクリーム状にならなかったり、調合直後はクリーム状になったものも試験期間中には粘度低下による不均一化や分離を起こした。
As is apparent from Table 1, in Example 1 containing a copolymer of acryloyldimethyltaurate ammonium and a vinyl-based or acrylic monofunctional monomer, both stability and usability were good. Furthermore, Example 4 containing hydroxypropyl methylcellulose also had good stability and usability. Furthermore, Examples 2 and 3 containing nylon powder were smoother and more comfortable to use.
On the other hand, instead of the copolymer of acryloyldimethyltaurate ammonium and a vinyl-based or acrylic monofunctional monomer, Comparative Examples 1 to 4 containing other thickeners lack storage stability or have a feeling of use. It was bad.
Specifically, Examples 1 to 4 had good usability and were stable preparations during the test period, but Comparative Examples 1 to 4 did not become creamy immediately after compounding, or creamed immediately after compounding. Also, during the test period, non-uniformity and separation occurred due to a decrease in viscosity.
処方例
以下に、本発明の皮膚外用剤の処方例を示す。
各成分の含有量の単位は、重量%である。
コポリマーのアクリロイルジメチルタウリンアンモニウム/メタクリル酸ベヘネス−25)クロスポリマーは、例えば、クラリアントジャパン社のAristoflex HBMである。また、アクリロイルジメチルタウリンアンモニウム/ポリビニルピロリドン)コポリマーは、例えば、クラリアントジャパン社のAristoflex AVCである。
Formulation Example A formulation example of the external preparation for skin of the present invention is shown below.
The unit of the content of each component is% by weight.
The copolymer acryloyldimethyltaurate ammonium / beheneth methacrylate-25) crosspolymer is, for example, Aristoflex HBM from Clariant Japan. The acryloyldimethyltaurine ammonium / polyvinylpyrrolidone) copolymer is, for example, Aristoflex AVC manufactured by Clariant Japan.
(1)クリーム
下記表2のA成分を加温と攪拌により溶解させておき、B成分のうちポリアクリル酸アルキル末とメチルシロキサン網状重合体末以外の成分を加温により溶解した後、ポリアクリル酸アルキル末とメチルシロキサン網状重合体を添加して分散させておいた。A成分とB成分とを混合し、撹拌して乳化した後、冷却し、C成分であるアゼライン酸を添加し、撹拌して均一にした。
(2)乳液
下記表3のA成分、B成分をそれぞれ加温と攪拌により溶解させておき、A成分とB成分とを混合し、撹拌して乳化した後、冷却し、C成分であるアゼライン酸を添加し、撹拌して均一にした。
(3)ジェル
下記表4のA成分を加温と攪拌により溶解させ、冷却した後、B成分を添加し、撹拌して均一にした。
(4)ジェル
下記表5のA成分、B成分をそれぞれ加温と攪拌により溶解させておき、B成分にC成分を添加分散させてから、A成分と、B成分及びC成分の分散液とを混合し、撹拌して乳化した後、冷却し、D成分を添加し、撹拌して均一にした。
(5)化粧水
下記表6のA成分の各成分を加温と攪拌により溶解させ、冷却した後にB成分を加えて攪拌して均一にした。
本発明の皮膚外用組成物は、ニキビ治療に有効なアゼライン酸を含み、保存安定性に優れるため、商品価値が高いものである。 The external composition for skin of the present invention contains azelaic acid effective for acne treatment and is excellent in storage stability, and therefore has a high commercial value.
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