JPS58124716A - Liquid drug for external use - Google Patents

Liquid drug for external use

Info

Publication number
JPS58124716A
JPS58124716A JP853582A JP853582A JPS58124716A JP S58124716 A JPS58124716 A JP S58124716A JP 853582 A JP853582 A JP 853582A JP 853582 A JP853582 A JP 853582A JP S58124716 A JPS58124716 A JP S58124716A
Authority
JP
Japan
Prior art keywords
indomethacin
crotamiton
acetone
glycols
esters
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.)
Granted
Application number
JP853582A
Other languages
Japanese (ja)
Other versions
JPH0476969B2 (en
Inventor
Yoshinari Yamahira
山平　良也
Tetsuo Noguchi
哲男 野口
Katsuhiko Shima
島　勝彦
Chikako Matsuzaka
松坂　千賀子
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sumitomo Chemical Co Ltd
Original Assignee
Sumitomo Chemical Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Sumitomo Chemical Co Ltd filed Critical Sumitomo Chemical Co Ltd
Priority to JP853582A priority Critical patent/JPS58124716A/en
Publication of JPS58124716A publication Critical patent/JPS58124716A/en
Publication of JPH0476969B2 publication Critical patent/JPH0476969B2/ja
Granted legal-status Critical Current

Links

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

PURPOSE:To provide a liquid drug for external use, having high solubility, excellent feeling to the skin and sufficiently high drug effect, and useful as a non- steroidal antiphlogistic and analgesic agent, by using indomethacin as an active component. CONSTITUTION:The objective drug can be prepared by dissolving indomethacin in a base consisting of a lower alcohol and/or acetone, crotamiton, and glycols (e.g. propylene glycol, butylene glycol, etc.) and/or their esters (e.g. polyethylene glycol monolaurate) by stirring. The amounts of lower alcohol and/or acetone, crotamiton, and glycols and/or their esters are preferably 50-90 V/V%, 0.5- 20 W/V%, and 5-50 W/V%, respectively. EFFECT:The addition of crotamiton to the base is effective to the prevention of the crystallization at the coating part of the vessel caused by the rapid evaporation of the solvent.

Description

【発明の詳細な説明】 本発明は、有効成分としてインドメタシンを含有する外
用液剤に関するものである。さらに詳しくはインドメタ
シン、低級アルコールおよび／またはアセトン、クロタ
ミトン、グリコール類および／またはそのエステルから
なることを特徴とする外用液剤であろう インドメタ’、ｔ　ンハ、１−　（ｐ−ｃｈｌｏｒｏｂ
ｅｎｚｏｙｌ）−５−ｒｎｅｔ、ｈｏｘｙ　−２−ｍｅ
ｔｈｙｌｉｎｄｏｌｅ　−９−ａｏｅｔｉ。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a liquid preparation for external use containing indomethacin as an active ingredient. More specifically, it is a liquid preparation for external use that is characterized by consisting of indomethacin, lower alcohols and/or acetone, crotamiton, glycols and/or esters thereof.
enzoyl)-5-rnet, hoxy-2-me
thylindole-9-aoeti.

ａｏｉｄ　（分子式Ｃ１ｅＨ１ｓ０１Ｎ０４、分子量８
５７．７９　）の化学名を有するすぐれた非ステロイド
性消炎鎮痛剤であろう インドメタシンは周知のごとく水ｌこ対する溶解性は小
さく外用液剤に使用し得る基剤の中でも高い溶解性を示
すものはきわめて少なく、溶媒の蓋散によって容Ｓ塗布
部に結晶が折用したり、また基剤の選択によりその安定
性も左右されるため基剤のくみあわせもむつかしく、従
来すぐれた特徴を有する外用液剤はみいだされていなか
った。aoid (molecular formula C1eH1s01N04, molecular weight 8
Indomethacin, which is an excellent non-steroidal anti-inflammatory analgesic with the chemical name 57.79), has low solubility in water as is well known, and among the bases that can be used for external liquid preparations, one that shows high solubility is External liquid preparations with excellent characteristics are extremely rare, and crystals may break into the application area due to dispersion of the solvent, and the stability is affected by the selection of the base material, making it difficult to combine the base materials. It had not been discovered.

本発明はこれらの点を克服し得た新規なる発明であり、
実用り大きな価値を有するものである。インドメタシン
の外用液剤としての具備すべき条件は、インドメタシン
が安定に溶解し、使用感がすぐれており、十分に薬効が
発現されることであろうそれにはエチルアルコール、変
性エチルアルコール、プロピルアルコールなどの低級ア
ルコールおよび／またはアセトン、グリコール類および
／またはそのエステルを基剤として使用する処方が知ら
れている。The present invention is a novel invention that can overcome these points,
It has great practical value. The conditions that must be met for indomethacin as a topical liquid preparation are that indomethacin should be stably dissolved, have an excellent feeling of use, and have sufficient medicinal efficacy. Formulations using lower alcohols and/or acetone, glycols and/or their esters as bases are known.

しかし、本発明者がさらに検討した結果、上記基剤にク
ロタミトンを添加することにより、塗布後すみやかな溶
媒の蒸散によりて容器の塗布部に結晶が析出することを
防ぐことができることを見い出しｔ二。However, as a result of further investigation, the present inventor found that by adding crotamiton to the above-mentioned base material, it is possible to prevent the precipitation of crystals in the coated area of the container due to the quick evaporation of the solvent after coating. .

ここで使用するグリコール類はプロピレングリコール、
ブチレングリコール、ポリエチレングリコールなどが、
そのエステルはモノラウリン酸ポリエチレングリコール
等が適轟である。The glycols used here are propylene glycol,
Butylene glycol, polyethylene glycol, etc.
Suitable esters include polyethylene glycol monolaurate.

また、これら基剤は低級アルコールおよび／またはアセ
トン５０〜ｇ５ｖ７ｖ＊、クロタミトン０．５〜２０Ｖ
Ｖ％、グリコール類および／またはそのエステル５〜５
　ｇ　Ｗ／Ｖ＊になるように混合するのが使用感の点か
ら好ましい、低級アルコールおよび／またはアセトンの
一部を精製水にかえることも可能であるがその量は液剤
の２６Ｖ／Ｖ４以下に限定される。In addition, these bases include lower alcohol and/or acetone 50~5v7v*, crotamiton 0.5~20V*
V%, glycols and/or their esters 5-5
From the viewpoint of usability, it is preferable to mix so that the ratio is W/V*.It is also possible to replace part of the lower alcohol and/or acetone with purified water, but the amount should be below 26V/V4 of the liquid. Limited.

本発明で提供する製剤は、きわめて調製条件が容易であ
り単にインドメタシンを基剤中で攪拌溶解するだけでよ
い。The preparation provided by the present invention is extremely easy to prepare, and it is sufficient to simply stir and dissolve indomethacin in the base.

このようにして調製した製剤は、安定性にすぐれている
だけでなく、溶媒蒸散後容器塗布部の結晶析出を防げる
特徴を有していることが実験例１からも明らかである。It is clear from Experimental Example 1 that the preparation prepared in this manner not only has excellent stability, but also has the characteristic of preventing crystal precipitation in the container application area after solvent evaporation.

実験例１ ポリプロピレン製液剤容器（塗布部はスポンジ）に実施
例２で調製した液剤を充填後、スポンジ部分をぬらして
から、キャップをしめ２週間後にキャップをあけて様子
を１！察したうなお、スポンジ（色はブルー）に白い結
晶が肉眼で誌められないものを「変化なし」、認められ
た木のを「スポンジに結晶析出が認められた」と判定し
た。Experimental Example 1 After filling a polypropylene liquid container (the application part is a sponge) with the liquid prepared in Example 2, wet the sponge part, close the cap, and after 2 weeks, open the cap and check the situation. As a result, if white crystals were not visible to the naked eye on the sponge (blue in color), it was judged as ``no change'', and if white crystals were observed, it was judged as ``crystal precipitation was observed on the sponge.''

（検体数　１０本） 液剤ムの処方 インドメタシン　　　　１１ プロピレングリコール　１０？ 精製水　　　　　　　　５？ エチルアルコール　　　全量１００ｗ１を以下に実施例
を示すが、本発明はこれらに限定されるものではない。(Number of samples: 10) Liquid formulation Indomethacin 11 Propylene glycol 10? Purified water 5? Examples are shown below using a total amount of 100 w1 ethyl alcohol, but the present invention is not limited thereto.

実施例１ インドメタシンＩＰ、ポリエチレングリコール４００　
１０）、クロタミトン１？にエチルアルコール５０−を
加えてインドメタシンを溶解したのち、精製水５−を加
えイソプロピルアルコールを加えて全量を１００−とじ
、インドメタシン外用液剤を得た。Example 1 Indomethacin IP, polyethylene glycol 400
10), Crotamiton 1? After adding 50% of ethyl alcohol to dissolve indomethacin, 5% of purified water was added, and isopropyl alcohol was added, and the total volume was adjusted to 100% to obtain a topical solution of indomethacin.

実施例２ インドメタシン２Ｆ、モノラウリン酸ポリエチレングリ
コール（１０Ｅ、０．）１５）１クロタミトン２７、ア
ジピン酸ジイソプロピル４ｉに８アセチル化蔗糖変性ア
ルコールを加えて全量を１００−とし、インドメタシン
外用液剤を得た。Example 2 Indomethacin 2F, polyethylene glycol monolaurate (10E, 0.) 15) 1 crotamiton 27, and diisopropyl adipate 4i were added with 8 acetylated sucrose denatured alcohol to make the total amount 100-, to obtain a topical solution of indomethacin.

実施例８ インドメタシン０．５ｙ−、プロピレングリコールｌ（
ＭＬ、モノラウリン酸ポリエチレングリコール（１０Ｂ
、０．）　ｌ　Ｏｆ、クロタミトン０．５Ｆにアセトン
２０−、エチルアルコール２０ｄを加えインドメタシン
を溶解したのち、精製水１０１１ｄを加え、エチルアル
コールを加えて全量を１００ｍとし、インドメタシン外
用液剤を得た。Example 8 Indomethacin 0.5y-, propylene glycol l (
ML, polyethylene glycol monolaurate (10B
, 0. ) l Of, 20 d of acetone and 20 d of ethyl alcohol were added to 0.5 F of crotamiton to dissolve indomethacin, and then 1011 d of purified water was added, and ethyl alcohol was added to make a total volume of 100 ml to obtain a topical solution of indomethacin.

Claims (1)

【特許請求の範囲】 下記式で示されるインドメタシン、低級アルコールおよ
び／またはアセトン、クロタミトン、グリコール類およ
び／またはそのエステルからなることを特徴とする外用
液剤。 インドメタシン[Scope of Claims] An external liquid preparation comprising indomethacin represented by the following formula, lower alcohol and/or acetone, crotamiton, glycols and/or esters thereof. indomethacin
JP853582A 1982-01-21 1982-01-21 Liquid drug for external use Granted JPS58124716A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP853582A JPS58124716A (en) 1982-01-21 1982-01-21 Liquid drug for external use

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP853582A JPS58124716A (en) 1982-01-21 1982-01-21 Liquid drug for external use

Publications (2)

Publication Number Publication Date
JPS58124716A true JPS58124716A (en) 1983-07-25
JPH0476969B2 JPH0476969B2 (en) 1992-12-07

Family

ID=11695838

Family Applications (1)

Application Number Title Priority Date Filing Date
JP853582A Granted JPS58124716A (en) 1982-01-21 1982-01-21 Liquid drug for external use

Country Status (1)

Country Link
JP (1) JPS58124716A (en)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE1000381A4 (en) * 1987-03-13 1988-11-16 Pharlyse Sa PHARMACEUTICAL PREPARATION BASED indomethacin.
JP2002029971A (en) * 2000-07-14 2002-01-29 Teikoku Seiyaku Co Ltd Indomethacin water-soluble cataplasm
JP2002029970A (en) * 2000-07-14 2002-01-29 Teikoku Seiyaku Co Ltd Cataplasm
WO2007046318A1 (en) * 2005-10-17 2007-04-26 Kowa Co., Ltd. Liquid preparation for external application containing indomethacin

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5636411A (en) * 1979-08-31 1981-04-09 Sumitomo Chem Co Ltd Liquid agent for external use
JPS5798209A (en) * 1980-12-09 1982-06-18 Kowa Co Remedy for dermatopathy for external use

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5636411A (en) * 1979-08-31 1981-04-09 Sumitomo Chem Co Ltd Liquid agent for external use
JPS5798209A (en) * 1980-12-09 1982-06-18 Kowa Co Remedy for dermatopathy for external use

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE1000381A4 (en) * 1987-03-13 1988-11-16 Pharlyse Sa PHARMACEUTICAL PREPARATION BASED indomethacin.
JP2002029971A (en) * 2000-07-14 2002-01-29 Teikoku Seiyaku Co Ltd Indomethacin water-soluble cataplasm
JP2002029970A (en) * 2000-07-14 2002-01-29 Teikoku Seiyaku Co Ltd Cataplasm
WO2007046318A1 (en) * 2005-10-17 2007-04-26 Kowa Co., Ltd. Liquid preparation for external application containing indomethacin
US8673960B2 (en) 2005-10-17 2014-03-18 Kowa Co., Ltd. External liquid preparation containing indomethacin

Also Published As

Publication number Publication date
JPH0476969B2 (en) 1992-12-07

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