JP3575033B2 - External preparation - Google Patents
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- JP3575033B2 JP3575033B2 JP26934893A JP26934893A JP3575033B2 JP 3575033 B2 JP3575033 B2 JP 3575033B2 JP 26934893 A JP26934893 A JP 26934893A JP 26934893 A JP26934893 A JP 26934893A JP 3575033 B2 JP3575033 B2 JP 3575033B2
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- Prior art keywords
- weight
- parts
- acrylate
- external preparation
- ethylhexyl
- 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.)
- Expired - Lifetime
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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
【０００１】
【産業上の利用分野】
本発明はアクリル酸メチル・アクリル酸−２−エチルヘキシル共重合樹脂エマルジョン及びポロシロキサン類を配合し、患部に塗布後製剤の付着性を高めた外用剤に関する。
【０００２】
【従来の技術】
皮膚疾患において例えば水虫・たむしなどの治療に際し、患部に製剤を塗布した場合、汗や衣類との摩擦等により製剤が患部から除かれやすいが、効果的な治療を行うためには、塗布部位に製剤を長時間保持されることが望ましい。
【０００３】
【発明が解決しようとする課題】
しかしながら、従来の軟膏及びクリーム剤の皮膚付着性に関しては、その効果が十分ではなかった。
本発明の目的は、製剤の皮膚付着性を高め、かつ使用感の優れた外用剤を提供することにある。
【０００４】
【課題を解決するための手段】
本発明者らは、前記目的を達成すべく鋭意研究を進めた結果、アクリル酸メチル・アクリル酸−２−エチルヘキシル共重合樹脂エマルジョン及びポリシロキサン類を配合した外用剤を皮膚に塗布すれば、アクリル酸メチル・アクリル酸−２−エチルヘキシル共重合樹脂エマルジョンとポリシロキサン類の相乗効果により、外用剤の皮膚粘着性が顕著に改善され、かつ使用感が優れることを見いだし、本発明を完成した。
【０００５】
すなわち、本発明はアクリル酸メチル・アクリル酸−２−エチルヘキシル共重合樹脂エマルジョン及びポリシロキサン類を配合した外用剤である。
本発明において、ポリシロキサン類とは、メチルポリシロキサン、メチルフェニルポリシロキサン及びシリコーン樹脂などであり、これらを１種または２種以上配合することができる。
前記アクリル酸メチル・アクリル酸−２−エチルヘキシル共重合樹脂エマルジョンの配合量は製剤全量の１〜１０重量％であり、また、ポリシロキサン類の配合量は製剤全量の０．１〜１．０重量％である。
【０００６】
本発明の外用剤は、通常用いられる方法（例えば第１２改正日本薬局方に規定する方法など）に従って調製することができる。その剤形としては、貼付剤、軟膏、クリーム剤及び液剤が挙げられ、このうち軟膏、クリーム剤が好ましい。
【０００７】
本発明の外用剤には、必要に応じて、抗真菌剤（硝酸ミコナゾール、トルナフテートなど）、鎮痒剤（クロタミトンなど）、抗ヒスタミン剤（塩酸ジフェンヒドラミン、塩酸イソチペンジル、マレイン酸クロルフェニラミンなど）、抗炎症剤（例えば、グリチルレチン酸、グリチルリチン酸ジカリウムなど）、局所麻酔剤（例えば、塩酸ジブカイン、リドカイン、塩酸リドカインなど）、界面活性剤（例えば、ポリオキシエチレンソルビタンモノステアレート、ソルビタンモノステアレートなど）、清涼化剤（例えば、メントール、カンフルなど）、ゲル化剤、中和剤、ｐＨ調製剤、溶媒、油成分及び高分子など通常外用剤に配合する成分を本発明の効果を損なわない範囲で加えることができる。
【０００８】
【発明の効果】
本発明により皮膚に対する付着性を高め、かつ使用感の良い外用剤を提供することが可能となった。
【０００９】
【実施例】
以下、実施例及び試験例を挙げて、本発明をさらに詳細に説明する。
試験例 ［アクリル酸メチル・アクリル酸−２−エチルヘキシル共重合樹脂エマルジョン及びポリシロキサン類を配合する製剤の皮膚付着性の評価試験］
（１）被験試料の調製
表１に示す処方の試料をビーカーに入れ、攪拌溶解して均一にすることにより調製した。
【００１０】
【表１】
（２）試験方法
プレパレート用ガラス板に固定した豚皮（商品名：アロアスク，大鵬薬品工業社製）４ｃｍ２に試料約２０ｍｇ（硝酸ミコナゾールとして約２００μｇ）を塗布し、３０分間室温に放置後、日局崩壊試験器を用い、３７±０．５℃生理食塩水中で上下に振とう（２８〜３２回／分）させ、開始時及び一定時間後に、豚皮に付着している製剤中の硝酸ミコナゾールの残存量を測定した。
その結果を表２に示す。
【００１２】
【表２】
実施例１
アクリル酸メチル・アクリル酸−２−エチルヘキシル共重合樹脂エマルジョン５重量部、ポリシロキサン０．３重量部、硝酸ミコナゾール０．５重量部、リドカイン２重量部、尿素３重量部、ハクショクワセリン２０重量部、スクワラン５９．２重量部、デキストラン脂肪酸エステル１０重量部を加温溶解し、軟膏剤を得た。
【００１４】
実施例２
アクリル酸メチル・アクリル酸−２−エチルヘキシル共重合樹脂エマルジョン２．５重量部、ポリシロキサン０．３重量部、硝酸ミコナゾール１重量部、リドカイン２重量部、メントール２重量部、流動パラフィン１０重量部、ポリソルベート６０ ５重量部、ステアリルアルコール１．５重量部、セタノール１．５重量部、プロピレングリコール５重量部をあらかじめ加温し、グリチルリチン酸ジカリウム０．５重量部、尿素５重量部及び精製水７３．７重量部を加温しながら攪拌溶解し、乳化し、クリーム剤を得た。
【００１５】
実施例３
アクリル酸メチル・アクリル酸−２−エチルヘキシル共重合樹脂エマルジョン１０重量部、ポリシロキサン０．８重量部、クロタミトン１０重量部、硝酸ミコナゾール１重量部、リドカイン２重量部、グリチルリチン酸ジカリウム０．５重量部、モノステアリン酸グリセリン３０量部及び精製水５６．５重量部を加温し、攪拌溶解し、乳化させ、クリーム剤を得た。
【００１６】[0001]
[Industrial applications]
The present invention relates to an external preparation containing a methyl acrylate / ethyl-2-ethylhexyl acrylate copolymer resin emulsion and a porosiloxane compound, which are applied to an affected area to enhance the adhesiveness of the preparation after application.
[0002]
[Prior art]
In the treatment of skin diseases, for example, athlete's foot or insects, when the preparation is applied to the affected area, the preparation is easily removed from the affected area due to sweat or friction with clothing, etc. It is desirable that the formulation be retained for an extended period of time.
[0003]
[Problems to be solved by the invention]
However, the effects of conventional ointments and creams on the skin adhesion were not sufficient.
An object of the present invention is to provide an external preparation which enhances the skin adhesion of the preparation and has an excellent feeling upon use.
[0004]
[Means for Solving the Problems]
The present inventors have conducted intensive studies to achieve the above object, and as a result, when an external preparation containing a methyl acrylate / ethyl acrylate 2-ethylhexyl copolymer resin emulsion and polysiloxanes is applied to the skin, The present inventors have found that the synergistic effect of a methyl acrylate / ethyl-2-ethylhexyl copolymer resin emulsion and polysiloxanes significantly improves the skin adhesiveness of the external preparation and provides an excellent feeling in use, thus completing the present invention.
[0005]
That is, the present invention is an external preparation containing a methyl acrylate / 2-ethylhexyl acrylate copolymer resin emulsion and polysiloxanes.
In the present invention, the polysiloxanes include methylpolysiloxane, methylphenylpolysiloxane, silicone resin and the like, and one or more of these can be blended.
The blending amount of the methyl acrylate / -2-ethylhexyl acrylate copolymer resin emulsion is 1 to 10% by weight of the whole preparation, and the blending amount of polysiloxanes is 0.1 to 1.0% by weight of the whole preparation. %.
[0006]
The external preparation of the present invention can be prepared according to a commonly used method (for example, a method prescribed in the 12th revised Japanese Pharmacopoeia). Examples of the dosage form include a patch, an ointment, a cream and a liquid, among which the ointment and the cream are preferred.
[0007]
The external preparation of the present invention may include, if necessary, an antifungal agent (e.g., miconazole nitrate, tolnaftate), an antipruritic (e.g., crotamiton), an antihistamine (e.g., diphenhydramine hydrochloride, isotipendyl hydrochloride, chlorpheniramine maleate), an anti-inflammatory agent (Eg, glycyrrhetinic acid, dipotassium glycyrrhizinate, etc.), local anesthetic (eg, dibucaine hydrochloride, lidocaine, lidocaine hydrochloride, etc.), surfactant (eg, polyoxyethylene sorbitan monostearate, sorbitan monostearate, etc.), cooling Add components that are usually blended with external preparations such as agents (eg, menthol, camphor, etc.), gelling agents, neutralizing agents, pH adjusters, solvents, oil components, and polymers as long as the effects of the present invention are not impaired. Can be.
[0008]
【The invention's effect】
ADVANTAGE OF THE INVENTION By this invention, it became possible to improve the adhesiveness with respect to skin and to provide the external preparation with a good feeling of use.
[0009]
【Example】
Hereinafter, the present invention will be described in more detail with reference to Examples and Test Examples.
Test example [Evaluation test of skin adhesion of a preparation containing a methyl acrylate / ethyl acrylate-2-ethylhexyl copolymer resin emulsion and polysiloxanes]
(1) Preparation of test sample A sample having the formulation shown in Table 1 was placed in a beaker, and dissolved by stirring to prepare a uniform sample.
[0010]
[Table 1]
(2) Test Method About 20 mg (approximately 200 μg as miconazole nitrate) of a sample was applied to 4 cm 2 of pig skin (trade name: Aloask, manufactured by Taiho Pharmaceutical Co., Ltd.) fixed to a glass plate for preparation, and left at room temperature for 30 minutes. Using a disintegration tester in Japan, shake up and down (28-32 times / min) in physiological saline at 37 ± 0.5 ° C. The remaining amount of miconazole nitrate was measured.
Table 2 shows the results.
[0012]
[Table 2]
Example 1
Methyl acrylate / acrylic acid-2-ethylhexyl copolymer resin emulsion 5 parts by weight, polysiloxane 0.3 parts by weight, miconazole nitrate 0.5 parts by weight, lidocaine 2 parts by weight, urea 3 parts by weight, powdered vaseline 20 parts by weight And 59.2 parts by weight of squalane and 10 parts by weight of dextran fatty acid ester were heated and dissolved to obtain an ointment.
[0014]
Example 2
2.5 parts by weight of methyl acrylate / -2-ethylhexyl acrylate copolymer resin emulsion, 0.3 parts by weight of polysiloxane, 1 part by weight of miconazole nitrate, 2 parts by weight of lidocaine, 2 parts by weight of menthol, 10 parts by weight of liquid paraffin, Preliminarily heated 5 parts by weight of polysorbate 60, 1.5 parts by weight of stearyl alcohol, 1.5 parts by weight of cetanol, and 5 parts by weight of propylene glycol, 0.5 part by weight of dipotassium glycyrrhizinate, 5 parts by weight of urea, and 73. 7 parts by weight were stirred and dissolved while being heated and emulsified to obtain a cream.
[0015]
Example 3
Methyl acrylate / ethyl -2-ethylhexyl acrylate copolymer resin emulsion 10 parts by weight, polysiloxane 0.8 parts by weight, crotamiton 10 parts by weight, miconazole nitrate 1 part by weight, lidocaine 2 parts by weight, dipotassium glycyrrhizinate 0.5 part by weight Then, 30 parts by weight of glyceryl monostearate and 56.5 parts by weight of purified water were heated, stirred and dissolved, and emulsified to obtain a cream.
[0016]
Claims (2)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP26934893A JP3575033B2 (en) | 1993-10-28 | 1993-10-28 | External preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP26934893A JP3575033B2 (en) | 1993-10-28 | 1993-10-28 | External preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH07126192A JPH07126192A (en) | 1995-05-16 |
| JP3575033B2 true JP3575033B2 (en) | 2004-10-06 |
Family
ID=17471129
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP26934893A Expired - Lifetime JP3575033B2 (en) | 1993-10-28 | 1993-10-28 | External preparation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP3575033B2 (en) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007277227A (en) * | 2006-03-14 | 2007-10-25 | Mochida Pharmaceut Co Ltd | Cleaning composition containing azole antifungal agent |
| JP5513705B2 (en) * | 2006-03-29 | 2014-06-04 | 小林製薬株式会社 | Hypersensitivity skin itching agent |
| JP5170973B2 (en) * | 2006-03-29 | 2013-03-27 | 小林製薬株式会社 | Topical skin preparation |
| JP5743375B2 (en) * | 2008-09-30 | 2015-07-01 | 小林製薬株式会社 | Candidiasis preventive or therapeutic agent |
| JP2022067658A (en) * | 2020-10-20 | 2022-05-06 | 東光薬品工業株式会社 | External cream agent for skin |
-
1993
- 1993-10-28 JP JP26934893A patent/JP3575033B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| JPH07126192A (en) | 1995-05-16 |
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