JP2012092022A - External skin patch - Google Patents

External skin patch Download PDF

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JP2012092022A
JP2012092022A JP2010238153A JP2010238153A JP2012092022A JP 2012092022 A JP2012092022 A JP 2012092022A JP 2010238153 A JP2010238153 A JP 2010238153A JP 2010238153 A JP2010238153 A JP 2010238153A JP 2012092022 A JP2012092022 A JP 2012092022A
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mass
component
plaster
skin
patch
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Yoshio Sugimoto
義夫 杉本
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Tokuhon Corp
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Tokuhon Corp
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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

PROBLEM TO BE SOLVED: To provide an external skin patch containing an antioxidative component in a water-soluble state and having an excellent preventing effect on skin aging.SOLUTION: The external skin patch contains the following components (a)-(f): (a) an antioxidative component; (b) a hyaluronic acid or a salt thereof; (c) glycerin; (d) agar; (e) locust bean gum; and (f) xanthan gum and has a water-containing plaster body having a pH of 10-12.

Description

本発明は、皮膚老化防止効果に優れる皮膚外用貼付剤に関する。   The present invention relates to a skin external patch excellent in skin aging prevention effect.

アスタキサンチンやコエンザイムQ10等の抗酸化成分は、皮膚の老化を防止し、皮膚の弾力性を増強し、しわ等を防止することから、各種の化粧品やサプリメントに広く用いられている(特許文献1、2等)。 Antioxidants such as astaxanthin and coenzyme Q 10 prevents aging of the skin, enhance the elasticity of the skin, since it prevents wrinkles, are widely used in a variety of cosmetics and supplements (Patent Document 1 2).

一方、貼付剤は、軟膏剤やクリーム等に比べて薬効成分が長時間貼付した局所にとどまっていることから、経皮吸収性が高いことから、医薬の分野では広く利用されている剤形である。しかし、皮膚の最外層は角層で覆われ、外界物質の体内侵入を防御するバリアの働きを有しているため、外用剤にとっては強大な障壁となり、処方した有効成分の効果が十分に発揮できないのが実情である。   On the other hand, the patch is a widely used dosage form in the pharmaceutical field because its medicinal components remain in the local area where it has been applied for a long time compared to ointments and creams. is there. However, the outermost layer of the skin is covered with a stratum corneum and acts as a barrier that prevents external substances from entering the body. Therefore, it is a strong barrier for external preparations, and the effects of the prescribed active ingredients are fully demonstrated. The reality is that you can't.

特開2004−99564号公報JP 2004-99564 A 特開2006−348035号公報JP 2006-348035 A

本発明者がアスタキサンチンやコエンザイムQ10を貼付剤に適用しようとしたところ、これらの抗酸化成分は水溶性が低く、水性膏体中に安定に保持できず、また経皮吸収性が低いため、通常の水性膏体を採用しても十分な効果を得られないことが判明した。
従って、本発明の課題は、抗酸化成分を水に可溶な状態で含有し、かつ優れた皮膚老化防止効果を有する皮膚外用貼付剤を提供することにある。
The present inventors have attempted to apply the astaxanthin and coenzyme Q 10 in patch, these antioxidants have low water solubility, can not be stably maintained in the aqueous plaster in, also due to low percutaneous absorbability, It has been found that a sufficient effect cannot be obtained even when a normal aqueous plaster is used.
Accordingly, an object of the present invention is to provide an external skin patch containing an antioxidant component in a soluble state in water and having an excellent anti-aging effect on skin.

そこで本発明は、抗酸化成分の膏体中への可溶化及び貼付剤としたときの有効性について種々検討したところ、抗酸化成分にヒアルロン酸又はその塩、グリセリン、寒天、ローカストビーンガム及びキサンタンガムを組み合わせ、さらに水性膏体のpHを10〜12になるように調整することにより、皮膚老化防止効果に優れた皮膚外用貼付剤が得られることを見出し、本発明を完成した。   Therefore, the present invention has been variously studied for solubilization of an antioxidant component in a plaster and its effectiveness when used as a patch. As an antioxidant component, hyaluronic acid or a salt thereof, glycerin, agar, locust bean gum and xanthan gum And by adjusting the pH of the aqueous plaster to 10-12, it was found that an external skin patch excellent in skin aging prevention effect was obtained, and the present invention was completed.

すなわち、本発明は、次の成分(a)〜(f):
(a)抗酸化成分、
(b)ヒアルロン酸又はその塩、
(c)グリセリン、
(d)寒天、
(e)ローカストビーンガム、及び
(f)キサンタンガム
を含有し、pHが10〜12である水含有膏体を有する皮膚外用貼付剤を提供するものである。
That is, the present invention includes the following components (a) to (f):
(A) an antioxidant component,
(B) hyaluronic acid or a salt thereof,
(C) glycerin,
(D) Agar,
The present invention provides an external skin patch having a water-containing plaster containing (e) locust bean gum and (f) xanthan gum and having a pH of 10-12.

本発明の皮膚外用貼付剤は、抗酸化成分が水に溶解した状態で安定に保持されており、かつ優れた皮膚老化防止効果を有する。本発明のかかる効果は、ヒアルロン酸又はその塩、グリセリン、寒天、ローカストビーンガム、キサンタンガム及びpH10〜12の水性膏体を組み合わせて用いることにより、角層中の皮脂が除去され、貼付部の皮膚に水分が移行して角層中の水分が飽和状態を形成し角層のバリア機能が低下することで、抗酸化成分の皮膚への移行が促進されることによるものと考えられる。また本発明の貼付剤は、使用感も良好で、効果の持続作用も優れている。   The external skin patch of the present invention is stably held in a state where the antioxidant component is dissolved in water, and has an excellent anti-aging effect on the skin. Such an effect of the present invention is that hyaluronic acid or a salt thereof, glycerin, agar, locust bean gum, xanthan gum and pH 10-12 aqueous paste are used in combination to remove sebum in the stratum corneum, and skin on the patch. This is considered to be because the transfer of antioxidant components to the skin is promoted by the movement of moisture to form a saturated state of the moisture in the stratum corneum and lowering the barrier function of the stratum corneum. In addition, the patch of the present invention has a good feeling of use and an excellent sustained action.

本発明の皮膚外用貼付剤は、膏体中に、(a)抗酸化成分、(b)ヒアルロン酸又はその塩、(c)グリセリン、(d)寒天、(e)ローカストビーンガム、及び(f)キサンタンガムを含有する。   The external skin patch of the present invention comprises (a) an antioxidant component, (b) hyaluronic acid or a salt thereof, (c) glycerin, (d) agar, (e) locust bean gum, and (f ) Contains xanthan gum.

本発明で用いる(a)抗酸化成分としては、抗酸化活性を有する成分であればよいが、アスタキサンチン、コエンザイムQ10が好ましい。これらは1種又は2種を組み合わせて用いることができる。アスタキサンチンは、アスタキサンチンそのものを用いてもよいが、エビ、カニ、紅鮭等からの抽出物であってアスタキサンチンを含むものを用いてもよい。また、コエンザイムQ10は、ユビデカレノン又は補酵素UQ10とも称されるユビキノンである。コエンザイムQ10は、本来ヒト由来の成分であるが、化学合成品を用いることができる。これらは、いずれもビタミンEよりも強い抗酸化力を有することが知られており、皮膚老化防止効果を有し、皮膚にうるおいや弾力を付与する効果を有することが知られている。 The (a) an antioxidant component used in the present invention may be any component having an antioxidant activity, astaxanthin, coenzyme Q 10 are preferred. These can be used alone or in combination. Astaxanthin may be astaxanthin itself, but may also be an extract from shrimp, crab, sockeye salmon and the like containing astaxanthin. Moreover, Coenzyme Q 10 is a ubidecarenone or coenzyme UQ10 also referred ubiquinone. Coenzyme Q 10 is a component of the original human origin, it is possible to use chemical synthesis products. All of these are known to have a stronger antioxidant power than vitamin E, have an anti-skin aging effect, and are known to have an effect of imparting moisture and elasticity to the skin.

成分(a)は、膏体中に皮膚老化防止効果の点から、0.05〜10質量%含有するのが好ましく、0.05〜5質量%含有するのがより好ましく、0.05〜1質量%含有するのがさらに好ましい。このうち、アスタキサンチンの含有量は、膏体中に0.05〜1質量%が好ましく、0.05〜0.5質量%がより好ましく、0.05〜0.25質量%がさらに好ましい。コエンザイムQ10の含有量は、膏体中の0.1〜2質量%が好ましく、0.1〜1質量%がより好ましく、0.1〜0.5質量%がさらに好ましい。 The component (a) is preferably contained in the plaster in an amount of 0.05 to 10% by mass, more preferably 0.05 to 5% by mass, from the viewpoint of the effect of preventing skin aging. More preferably, it is contained by mass%. Among these, the content of astaxanthin is preferably 0.05 to 1% by mass in the plaster, more preferably 0.05 to 0.5% by mass, and further preferably 0.05 to 0.25% by mass. The content of coenzyme Q 10 is preferably 0.1 to 2% by mass in the plaster, more preferably 0.1 to 1% by mass, and still more preferably 0.1 to 0.5% by mass.

本発明で用いる(b)ヒアルロン酸又はその塩としては、ヒアルロン酸又はヒアルロン酸ナトリウムが好ましい。ヒアルロン酸又はその塩としては、ニワトリのトサカ由来のものでも、発酵製造法により得られるものでもよい。またヒアルロン酸又はその塩の分子量も特に限定されず、10万〜150万のものが使用可能であるが、20万〜50万の分子量のものが、保湿効果、保湿効果の持続性、安定配合性、成分(a)の経皮吸収性の点から好ましい。
成分(b)は膏体中に0.5〜3.5質量%、さらに0.5〜3質量%、特に1〜2.5質量%含有するのが、保湿効果、成分(a)の経皮吸収性の点から好ましい。
(B) Hyaluronic acid or a salt thereof used in the present invention is preferably hyaluronic acid or sodium hyaluronate. Hyaluronic acid or a salt thereof may be derived from chicken Tosaka or obtained by fermentation. Further, the molecular weight of hyaluronic acid or a salt thereof is not particularly limited, and those with 100,000 to 1,500,000 can be used. From the viewpoint of properties and transdermal absorbability of component (a).
The component (b) is contained in the plaster in an amount of 0.5 to 3.5% by mass, more preferably 0.5 to 3% by mass, and particularly 1 to 2.5% by mass. It is preferable from the viewpoint of skin absorbability.

本発明で用いる(c)グリセリンとしては、濃グリセリンを用いるのが好ましい。グリセリンは、保湿効果を有し、結果として成分(a)の経皮吸収性向上に寄与する。成分(c)の含有量は、膏体中に30〜50質量%、さらに30〜45質量%、特に35〜45質量%含有するのが、保湿効果及び成分(a)の経皮吸収性の点で好ましい。   As (c) glycerin used in the present invention, concentrated glycerin is preferably used. Glycerin has a moisturizing effect and, as a result, contributes to improvement of the transdermal absorbability of component (a). The content of the component (c) is 30 to 50% by mass, more preferably 30 to 45% by mass, and particularly 35 to 45% by mass in the plaster, for the moisturizing effect and the transdermal absorbability of the component (a). This is preferable.

本発明で用いる(d)寒天としては、天草等の紅藻類から抽出された粘質液を凝固し、乾燥させたものであれば特に制限されない。寒天は膏体の骨格の形成に寄与する。成分(d)の含有量は、膏体中に0.3〜2質量%、さらに0.3〜1.5質量%、特に0.5〜1.5質量%であるのが好ましい。   The (d) agar used in the present invention is not particularly limited as long as the mucus extracted from red algae such as Amakusa is coagulated and dried. Agar contributes to the formation of the plaster skeleton. The content of the component (d) is preferably 0.3 to 2% by mass, more preferably 0.3 to 1.5% by mass, and particularly preferably 0.5 to 1.5% by mass in the plaster.

本発明で用いる(e)ローカストビーンガムは、マメ科のカロブ樹からとれる種子の胚乳部分を原料とする多糖類で、その構造は、マンノースの主鎖にガラクトースの側鎖が平均で4対1の割合で結合した直鎖状のガラクトマンナンを形成する。ローカストビーンガムは無臭性の高い透明性を示す精製タイプのものであれば特に限定されるものではない。寒天のみで得られる膏体の物性は、寒天状のパサパサで粘りがなく、外圧により簡単に崩れやすいものであり、ローカストビーンガムを処方することにより、寒天のみの膏体に増粘弾性、保水性、安定性を付与する成分(e)含有量は、膏体中0.5〜3質量%、さらに0.5〜2.5質量%、特に0.5〜2質量%が好ましい。   (E) Locust bean gum used in the present invention is a polysaccharide made from the endosperm portion of seeds taken from a carob tree of the leguminous family, and its structure is an average of 4 to 1 mannose main chain and galactose side chain To form a linear galactomannan bonded at a ratio of Locust bean gum is not particularly limited as long as it is a purified type exhibiting high odorless transparency. The physical properties of the paste obtained with agar only are agar-like pasapasa and are not sticky and easily collapse due to external pressure. By formulating locust bean gum, the agar-only paste has thickened elasticity and water retention The content of the component (e) that imparts stability and stability is preferably 0.5 to 3% by mass, more preferably 0.5 to 2.5% by mass, and particularly preferably 0.5 to 2% by mass in the plaster.

本発明で用いる(f)キサンタンガムは、微生物(Xanthomonas campestris)から産生される天然多糖類で、その構造はグルコースの主鎖にマンノース、グルクロン酸塩の側鎖が結合し、分岐の多い構造を示す多糖類である。成分(f)は、上記のローカストビーンガムと同時に処方すると膏体にゲル、増粘弾性、保湿性、安定性等を相乗的に付与する。成分(f)の含有量は、膏体中に0.1〜0.8質量%、さらに0.1〜0.7質量%、特に0.2〜0.6質量%が好ましい。   (F) Xanthan gum used in the present invention is a natural polysaccharide produced from a microorganism (Xanthomonas campestris), and its structure shows a branched structure in which the side chain of mannose and glucuronate is bonded to the main chain of glucose. It is a polysaccharide. When component (f) is formulated simultaneously with the locust bean gum, it synergistically imparts gel, thickening elasticity, moisture retention, stability, etc. to the plaster. The content of the component (f) is preferably 0.1 to 0.8 mass%, more preferably 0.1 to 0.7 mass%, and particularly preferably 0.2 to 0.6 mass% in the plaster.

本発明貼付剤の膏体は、pHが10〜12である水含有膏体であるのが、成分(a)の可溶化、安定性及び経皮吸収性の点で重要である。膏体のpHは、pHメータなどにより直接測定することができる。膏体のpHを10〜12に調整するには、水酸化ナトリウム、水酸化カリウム、ジエタノールアミン等のアルカリを添加すればよいが、アルカリイオン水の添加により調整してもよい。当該アルカリイオン水は抗菌・脱脂洗浄・脱臭・防ビ作用等を有し、金属イオン(Na+又はK+)を含まないため皮膚適用時の安全性は極めて高い。膏体中の水の含有量は40〜70質量%、さらに45〜65質量%、特に45〜60質量%が好ましい。 The plaster of the patch of the present invention is a water-containing plaster having a pH of 10 to 12 and is important in terms of solubilization, stability and transdermal absorbability of the component (a). The pH of the plaster can be directly measured with a pH meter or the like. In order to adjust the pH of the plaster to 10 to 12, an alkali such as sodium hydroxide, potassium hydroxide, diethanolamine or the like may be added, but it may be adjusted by adding alkaline ionized water. The alkaline ionized water has antibacterial, degreased cleaning, deodorizing, antibacterial action, and the like, and does not contain metal ions (Na + or K + ), so the safety when applied to the skin is extremely high. The content of water in the plaster is preferably 40 to 70% by mass, more preferably 45 to 65% by mass, and particularly preferably 45 to 60% by mass.

本発明貼付剤の膏体には前記成分以外に、美白成分としてL−アスコルビン酸及びその誘導体(L−アスコルビン酸グリコシド、L−アスコルビン酸モノリン酸エステル等)パルミチン酸ナトリウム、プラセンタエキス、アロエエキス、パントテニールエチルエーテル、トラネキサム酸及びその誘導体、アルブチン、コウジ酸等を配合することができる。また、基剤構成成分として、植物性高分子としてアラビアガム、トラガントガム、カラギーナン、マンナン、動物性高分子としてゼラチン、アルブミン、コラーゲン等を配合することができる。   In addition to the above-mentioned components, the plaster of the patch of the present invention contains L-ascorbic acid and its derivatives (L-ascorbic acid glycoside, L-ascorbic acid monophosphate, etc.) sodium palmitate, placenta extract, aloe extract, Pantotenyl ethyl ether, tranexamic acid and its derivatives, arbutin, kojic acid and the like can be blended. Further, as the base component, gum arabic, tragacanth gum, carrageenan, mannan as vegetable polymer, gelatin, albumin, collagen and the like as animal polymer can be blended.

本発明の貼付剤は、膏体の硬度及び粘弾性が十分に高い場合には膏体のみでの使用が可能となる。一方、膏体の硬度及び粘弾性が十分高くない場合には、膏体を支持体に担持した形態とすることが使用勝手面から好ましく、その支持体の物性は伸縮性を有する不織布、プラスチックフィルム等が挙げられる。
また、支持体を担持した膏体の被覆物として防湿機能を有するフィルムを用いてもよい。貼付剤の品質保持のため、気密性のすぐれた包材に入れて保存した状態で供給するのが好ましい。
When the hardness and viscoelasticity of the plaster are sufficiently high, the patch of the present invention can be used only with the plaster. On the other hand, when the hardness and viscoelasticity of the plaster are not sufficiently high, it is preferable from the viewpoint of ease of use that the plaster is supported on a support, and the physical properties of the support are stretchable nonwoven fabric, plastic film Etc.
Moreover, you may use the film which has a moisture-proof function as a covering of the plaster | support which carry | supported the support body. In order to maintain the quality of the patch, it is preferably supplied in a state of being stored in a packaging material having excellent airtightness.

本発明の貼付剤は、皮膚老化防止の目的で皮膚に貼付して使用するのであることから、顔全面、目のまわり用、目尻用、口の周囲用等の形状(顔パック、部分パック)とするのが好ましい。   Since the patch of the present invention is used after being applied to the skin for the purpose of preventing skin aging, the shape of the entire face, around the eyes, around the eyes, around the mouth, etc. (face pack, partial pack) Is preferable.

次に実施例を挙げて、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ない。なお、下記の各処方において%とは、特に言及しない限りにおいて質量%を意味するものとする。   EXAMPLES Next, although an Example is given and demonstrated further in detail, this invention is not limited to these Examples. In the following formulas, “%” means “% by mass” unless otherwise specified.

実施例1〜5
表1記載の処方の膏体からなる貼付剤を製造した。
Examples 1-5
A patch comprising a paste with the formulation shown in Table 1 was produced.

Figure 2012092022
Figure 2012092022

試験例1(膏体の動的粘弾性の測定と目尻並びに口周囲部位の皮膚弾力性の改善度と使用感試験)
表1に記載した実施例5の貼付剤の膏体の動的粘弾性を測定した。また、表1に示す実施例5の貼付剤を目尻部位と口周囲を貼付対象にして被験者(20〜50歳代34名)に1日1回洗顔直後に貼付し、1カ月継続使用したのち、皮膚弾力性の改善度をキュートメーターを用いて使用前後による皮膚症状の改善度を評価した。また、使用感(しっとり感)については適応前と適応後の皮膚症状を被験者に5段階評価(5:非常によい、4:よい、3:普通、2:やや悪い、1:悪い)させた。
その結果、表2に示すように、実施例5はいずれの試験項目においてもよい弾力性並びに好ましい改善傾向が認められ優れた貼付剤であることが実証された。また、実施例1〜4の貼付剤についても、目尻に貼付したところ、優れた皮膚弾力性の改善効果が得られた。
Test Example 1 (Measurement of dynamic viscoelasticity of plaster and degree of improvement in skin elasticity at the corner of the eye and around the mouth and feeling of use)
The dynamic viscoelasticity of the plaster of the patch of Example 5 described in Table 1 was measured. In addition, after applying the patch of Example 5 shown in Table 1 to the subjects (34 people in their 20s to 50s) once a day after face-washing, applying the patch to the area around the corner of the eye and around the mouth, and continuously using it for 1 month The degree of improvement in skin elasticity was evaluated by using a cutometer to evaluate the degree of improvement in skin elasticity. In addition, regarding the feeling of use (moist feeling), the skin symptoms before and after adaptation were evaluated on a 5-point scale (5: very good, 4: good, 3: normal, 2: slightly bad, 1: bad). .
As a result, as shown in Table 2, Example 5 was proved to be an excellent patch with good elasticity and favorable improvement tendency in any test item. Moreover, when the patches of Examples 1 to 4 were affixed to the corners of the eyes, an excellent skin elasticity improving effect was obtained.

Figure 2012092022
Figure 2012092022

Claims (4)

次の成分(a)〜(f):
(a)抗酸化成分、
(b)ヒアルロン酸又はその塩、
(c)グリセリン、
(d)寒天、
(e)ローカストビーンガム、及び
(f)キサンタンガム
を含有し、pHが10〜12である水含有膏体を有する皮膚外用貼付剤。
The following components (a) to (f):
(A) an antioxidant component,
(B) hyaluronic acid or a salt thereof,
(C) glycerin,
(D) Agar,
(E) An external skin patch having a water-containing plaster containing locust bean gum and (f) xanthan gum and having a pH of 10-12.
成分(a)がアスタキサンチン及びコエンザイムQ10から選ばれる1種又は2種以上である請求項1記載の皮膚外用貼付剤。 One or external skin patch according claim 1 is two or more selected from components (a) astaxanthin and coenzyme Q 10. 膏体中に、成分(a)を0.05〜10質量%、成分(b)を0.5〜3.5質量%、成分(c)を30〜50質量%、成分(d)を0.3〜2質量%、成分(e)を0.5〜3質量%、及び成分(f)を0.1〜0.8質量%含有する請求項1又は2記載の皮膚外用貼付剤。   In the plaster, component (a) is 0.05 to 10% by mass, component (b) is 0.5 to 3.5% by mass, component (c) is 30 to 50% by mass, and component (d) is 0. The external skin patch according to claim 1 or 2, comprising 3 to 2% by mass, 0.5 to 3% by mass of component (e), and 0.1 to 0.8% by mass of component (f). 膏体中に水を40〜70質量%含有する請求項1〜3のいずれか1項記載の皮膚外用貼付剤。   The skin external patch according to any one of claims 1 to 3, wherein the plaster contains 40 to 70% by mass of water.
JP2010238153A 2010-10-25 2010-10-25 External skin patch Pending JP2012092022A (en)

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