JP3608209B2 - Crotamiton combination external preparation - Google Patents
Crotamiton combination external preparation Download PDFInfo
- Publication number
- JP3608209B2 JP3608209B2 JP26928093A JP26928093A JP3608209B2 JP 3608209 B2 JP3608209 B2 JP 3608209B2 JP 26928093 A JP26928093 A JP 26928093A JP 26928093 A JP26928093 A JP 26928093A JP 3608209 B2 JP3608209 B2 JP 3608209B2
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- JP
- Japan
- Prior art keywords
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- parts
- crotamiton
- external preparation
- preparation
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- 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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Description
【０００１】
【産業上の利用分野】
本発明は鎮痒剤としてクロタミトンを配合した外用剤に関する。
【０００２】
【従来の技術】
皮膚疾患において例えば水虫・たむしなどの随伴症状や虫刺され等の蚤痒感を軽減する目的で、クロタミトン等の鎮痒剤を配合した外用剤が使用されている。効果的に蚤痒感を軽減するためには、クロタミトンの配合比を高めることが好ましい。
【０００３】
【発明が解決しようとする課題】
しかしクロタミトンを高濃度に配合した場合、経時的に製剤の変色が認められ、商品価値の著しい低下が問題となっていた。
本発明の目的は、クロタミトンを高濃度に配合することにより鎮痒効果を高め、かつクロタミトンの経時的な変色を抑え、商品価値を高め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、クロタミトンにピロ亜硫酸ナトリウム、エデト酸ナトリウム（以下、ＥＤＴＡ−２Ｎａと略称する。）及びジブチルヒドロキシトルエン（以下、ＢＨＴと略称する。）を配合することにより、調製した外用剤における経時的なクロタミトンの変色を抑えることができることを見いだし、本発明を完成した。
【０００５】
すなわち、本発明はクロタミトン、ピロ亜硫酸ナトリウム、ＥＤＴＡー２Ｎａ 及びＢＨＴを配合した外用剤である。
本発明において、クロタミトンの配合量は製剤全量の１０〜２０重量％、ピロ亜硫酸ナトリウムの配合量は製剤全量の０．０５〜０．３重量％、ＥＤＴＡ−２Ｎａの配合量は製剤全量の０．０５〜０．２重量％、ＢＨＴの配合量は製剤全量の０．０１〜０．２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、軟膏、クリーム剤、ゲル剤、チンキ剤、液剤を挙げることができる。
【０００７】
本発明の外用剤には、必要に応じて、抗真菌剤（例えば、硝酸ミコナゾール、トルナフテート、クロトリマゾールなど）、抗ヒスタミン剤（例えば、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の通常外用剤に配合され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、鎮痒効果を高め、かつクロタミトンの経時的な変色を抑えて商品価値を高めたクロタミトン配合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［クロタミトン含有製剤の経時的外観観察］
（１）被験試料の調製
被験試料を４０℃，相対湿度７５％で６ヶ月間及び室温で１年間保存し、外観変化を肉眼判定により評価した。なお、被験試料は表１に示す処方を攪拌、溶解して均一にすることにより調製した。表１に被験試料の処方及び試験結果を示す。
【００１０】
【表１】
実施例１
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、ポリソルベート６０ ５重量部、プロピレングリコール１０重量部、グリセリンモノステアレート２０重量部、アジピン酸ジイソプロピル２重量部、尿素３重量部、ピロ亜硫酸ナトリウム０．１５重量部、ＥＤＴＡ−２Ｎａ０．１重量部、ＢＨＴ０．０５重量部及び精製水４６．７重量部を加温溶解し、ホモミキサーを用いて乳化し、クリーム剤を得た。
【００１２】
実施例２
クロタミトン１５重量部、塩酸イソチペンジル０．７５重量部、リドカイン２重量部、メントール２重量部、グリチルリチン酸ジカリウム０．５重量部、ピロ亜硫酸ナトリウム０．１５重量部、ＥＤＴＡ−２Ｎａ０．１重量部、ＢＨＴ０．０５重量部、ポリエチレングリコール−３００ １０重量部、カルボキシビニルポリマー０．５重量部、エチルアルコール４５重量部及び精製水１８．４５重量部を攪拌溶解し、ジイソパノールアミン０．５重量部を添加しゲル剤を得た。
【００１３】
実施例３
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、エチルセルロース０．２重量部、ピロ亜硫酸ナトリウム０．１５重量部、ＥＤＴＡ−２Ｎａ０．１重量部、ＢＨＴ０．０５重量部、エチルアルコール８３重量部及び精製水３重量部を攪拌溶解し、チンキ剤を得た。
【００１４】[0001]
[Industrial application fields]
The present invention relates to an external preparation containing crotamiton as an antipruritic agent.
[0002]
[Prior art]
For skin diseases, for example, an external preparation containing an antipruritic agent such as crotamiton has been used for the purpose of reducing the sensation of accompanying symptoms such as athlete's foot and bugs and insect bites. In order to effectively reduce the feeling of wrinkle, it is preferable to increase the mixing ratio of crotamiton.
[0003]
[Problems to be solved by the invention]
However, when crotamiton was blended at a high concentration, discoloration of the preparation was observed over time, and a significant reduction in commercial value was a problem.
An object of the present invention is to provide an external preparation having an increased antipruritic effect by adding crotamiton at a high concentration, suppressing discoloration of crotamiton over time, and increasing commercial value.
[0004]
[Means for Solving the Problems]
As a result of diligent research to achieve the above-mentioned object, the present inventors have found that crotamiton has sodium pyrosulfite, sodium edetate (hereinafter abbreviated as EDTA-2Na) and dibutylhydroxytoluene (hereinafter abbreviated as BHT). .)), It was found that discoloration of crotamiton over time in the prepared external preparation could be suppressed, and the present invention was completed.
[0005]
That is, the present invention is an external preparation containing crotamiton, sodium pyrosulfite, EDTA-2Na and BHT.
In the present invention, the amount of crotamiton is 10 to 20% by weight of the total amount of the preparation, the amount of sodium pyrosulfite is 0.05 to 0.3% by weight of the total amount of the preparation, and the amount of EDTA-2Na is 0. 0% of the total amount of the preparation. The blending amount of 05 to 0.2% by weight and BHT is 0.01 to 0.2% by weight of the total amount of the 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 ointments, creams, gels, tinctures, and liquids.
[0007]
The external preparation of the present invention includes an antifungal agent (for example, miconazole nitrate, tolnaftate, clotrimazole, etc.), an antihistamine agent (for example, diphenhydramine hydrochloride, isothipentyl hydrochloride, chlorpheniramine maleate, etc.), anti-inflammatory as necessary. Agents (eg, glycyrrhetinic acid, dipotassium glycyrrhizinate), local anesthetics (eg, dibucaine hydrochloride, lidocaine, lidocaine hydrochloride, etc.), surfactants (eg, polyoxyethylene sorbitan monostearate, sorbitan monostearate, etc.), A range that does not impair the effects of the present invention for components that are usually blended in external preparations such as cooling agents (eg, menthol, camphor, etc.), gelling agents, neutralizing agents, pH adjusting agents, solvents, oil components, and polymers. Can be added at.
[0008]
【The invention's effect】
According to the present invention, it has become possible to provide a crotamiton-containing external preparation that has an improved antipruritic effect and suppresses discoloration of crotamiton over time and has increased commercial value.
[0009]
【Example】
Hereinafter, the present invention will be described in more detail with reference to Examples and Test Examples.
Test Example [Observation of appearance of crotamiton-containing preparation over time]
(1) Preparation of test sample The test sample was stored at 40 ° C. and relative humidity 75% for 6 months and at room temperature for 1 year, and the appearance change was evaluated by visual inspection. The test sample was prepared by stirring and dissolving the formulation shown in Table 1 to make it uniform. Table 1 shows the formulation of the test sample and the test results.
[0010]
[Table 1]
Example 1
10 parts by weight of crotamiton, 1 part by weight of miconazole nitrate, 2 parts by weight of lidocaine, 5 parts by weight of polysorbate 60, 10 parts by weight of propylene glycol, 20 parts by weight of glycerol monostearate, 2 parts by weight of diisopropyl adipate, 3 parts by weight of urea, pyrosulfurous acid Sodium 0.15 parts by weight, EDTA-2Na 0.1 parts by weight, BHT 0.05 parts by weight and purified water 46.7 parts by weight were dissolved by heating and emulsified using a homomixer to obtain a cream.
[0012]
Example 2
15 parts by weight of crotamiton, 0.75 parts by weight of isothipentyl hydrochloride, 2 parts by weight of lidocaine, 2 parts by weight of menthol, 0.5 parts by weight of dipotassium glycyrrhizinate, 0.15 part by weight of sodium pyrosulfite, 0.1 part by weight of EDTA-2Na, BHT0 .05 parts by weight, 10 parts by weight of polyethylene glycol-300, 0.5 parts by weight of carboxyvinyl polymer, 45 parts by weight of ethyl alcohol and 18.45 parts by weight of purified water were stirred and dissolved, and 0.5 parts by weight of diisopanolamine was added. This was added to obtain a gel.
[0013]
Example 3
10 parts by weight of crotamiton, 1 part by weight of miconazole nitrate, 2 parts by weight of lidocaine, 0.5 parts by weight of dipotassium glycyrrhizinate, 0.2 parts by weight of ethyl cellulose, 0.15 parts by weight of sodium pyrosulfite, 0.1 parts by weight of EDTA-2Na, BHT0 0.05 parts by weight, 83 parts by weight of ethyl alcohol and 3 parts by weight of purified water were stirred and dissolved to obtain a tincture.
[0014]
Claims (1)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP26928093A JP3608209B2 (en) | 1993-10-27 | 1993-10-27 | Crotamiton combination external preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP26928093A JP3608209B2 (en) | 1993-10-27 | 1993-10-27 | Crotamiton combination external preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH07126158A JPH07126158A (en) | 1995-05-16 |
| JP3608209B2 true JP3608209B2 (en) | 2005-01-05 |
Family
ID=17470161
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP26928093A Expired - Lifetime JP3608209B2 (en) | 1993-10-27 | 1993-10-27 | Crotamiton combination external preparation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP3608209B2 (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10105444B2 (en) | 2010-07-08 | 2018-10-23 | Dow Pharmaceutical Sciences, Inc. | Compositions and methods for treating diseases of the nail |
| US10828293B2 (en) | 2013-11-22 | 2020-11-10 | Dow Pharmaceutical Sciences, Inc. | Anti-infective methods, compositions, and devices |
| US10864274B2 (en) | 2013-10-03 | 2020-12-15 | Bausch Health Ireland Limited | Stabilized efinaconazole formulations |
| US11213519B2 (en) | 2008-01-03 | 2022-01-04 | Bausch Health Ireland Limited | Compositions and methods for treating diseases of the nail |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4521899B2 (en) * | 1999-08-27 | 2010-08-11 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | Clotamiton-containing skin external solution |
| JP4549006B2 (en) * | 2002-05-07 | 2010-09-22 | ロート製薬株式会社 | Gel ointment |
| JP5785353B2 (en) * | 2004-02-27 | 2015-09-30 | 大正製薬株式会社 | Ophthalmic agent |
| JP5063072B2 (en) * | 2006-09-29 | 2012-10-31 | 小林製薬株式会社 | Skin external composition |
| JP5565995B2 (en) * | 2006-09-29 | 2014-08-06 | 小林製薬株式会社 | Antipruritic |
-
1993
- 1993-10-27 JP JP26928093A patent/JP3608209B2/en not_active Expired - Lifetime
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11213519B2 (en) | 2008-01-03 | 2022-01-04 | Bausch Health Ireland Limited | Compositions and methods for treating diseases of the nail |
| US11872218B2 (en) | 2008-01-03 | 2024-01-16 | Bausch Health Ireland Limited | Compositions and methods for treating diseases of the nail |
| US10105444B2 (en) | 2010-07-08 | 2018-10-23 | Dow Pharmaceutical Sciences, Inc. | Compositions and methods for treating diseases of the nail |
| US10828369B2 (en) | 2010-07-08 | 2020-11-10 | Dow Pharmaceutical Sciences, Inc. | Compositions and methods for treating diseases of the nail |
| US10864274B2 (en) | 2013-10-03 | 2020-12-15 | Bausch Health Ireland Limited | Stabilized efinaconazole formulations |
| US10828293B2 (en) | 2013-11-22 | 2020-11-10 | Dow Pharmaceutical Sciences, Inc. | Anti-infective methods, compositions, and devices |
| US11654139B2 (en) | 2013-11-22 | 2023-05-23 | Bausch Health Ireland Limited | Anti-infective methods, compositions, and devices |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH07126158A (en) | 1995-05-16 |
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