JPS62292716A - Ointment base - Google Patents

Ointment base

Info

Publication number
JPS62292716A
JPS62292716A JP61135569A JP13556986A JPS62292716A JP S62292716 A JPS62292716 A JP S62292716A JP 61135569 A JP61135569 A JP 61135569A JP 13556986 A JP13556986 A JP 13556986A JP S62292716 A JPS62292716 A JP S62292716A
Authority
JP
Japan
Prior art keywords
agent
ointment
ointment base
drug
base
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
JP61135569A
Other languages
Japanese (ja)
Other versions
JPH0511093B2 (en
Inventor
Shoichi Murata
昌一 村田
Shigenobu Okada
岡田 穣伸
Kenji Hara
健次 原
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.)
Kao Corp
Original Assignee
Kao Corp
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 Kao Corp filed Critical Kao Corp
Priority to JP61135569A priority Critical patent/JPS62292716A/en
Publication of JPS62292716A publication Critical patent/JPS62292716A/en
Publication of JPH0511093B2 publication Critical patent/JPH0511093B2/ja
Granted legal-status Critical Current

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  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

PURPOSE:To provide an ointment base containing propylene glycol, polyethylene glycol, gelation agent, glycerol and alkaline agent, capable of easily dissolving a hardly soluble drug, improving the releasability and absorbability of a drug and fully exhibiting its effect. CONSTITUTION:The objective base can be produced by compounding (A) 5-30(wt)%, preferably 5-20% propylene glycol, (B) 5-50%, preferably 10-50% polyethylene glycol (having an average molecular weight of preferably 200-400), (C) 0.1-5% gelation agent such as carboxyvinyl polymer, CMC, sodium alginate, etc., (D) 10-40%, preferably 10-30% glycerol as moisture-retaining agent and (E) 0.1-3% alkaline agent (e.g. monoethanolamine, sodium hydroxide, etc.). Especially excellent effect can be attained in an ointment produced by compounding said ointment base with an adrenal cortical hormone as an anti- inflammatory agent in combination with dibucaine hydrochloride as a local anesthetic.

Description

【発明の詳細な説明】 3、発明の詳細な説明 〔産業上の利用分野〕 本発明は軟膏基剤、更に詳しくは、難溶性薬物をよく溶
解し、薬物の放出性、吸収性を向上させて当該薬物の効
果を充分に発揮させることができると共に、使用感のよ
い水溶性軟膏基剤に関する。
[Detailed Description of the Invention] 3. Detailed Description of the Invention [Field of Industrial Application] The present invention provides an ointment base, more specifically, an ointment base that dissolves poorly soluble drugs and improves drug release and absorption. The present invention relates to a water-soluble ointment base that can fully exhibit the effects of the drug and is comfortable to use.

〔従来の技術〕[Conventional technology]

難溶性薬物を外用に使用する場合、その治療効果は、薬
物の基剤への溶解性と相関するとされており、例えば副
腎皮質ホルモン含有軟膏は、上腕部看白性試験において
、完全溶解型のものは非溶解型に比較して約5培の効力
があることが報告されている。
When a poorly soluble drug is used externally, its therapeutic effect is said to be correlated with the solubility of the drug in the base.For example, an ointment containing adrenocortical hormone was found to be completely soluble in an upper arm visibility test. It has been reported that the non-dissolved version is about 5 times more effective than the non-dissolved version.

〔発明が解決しようとする問題点〕[Problem that the invention seeks to solve]

しかし、従来、難溶性薬物、特に副腎皮質ホルモンを完
全に溶解する軟膏基剤は提供されておらず、当該薬物の
効果を完全に発現させることは困難であると考えられて
いたofた、一方従来の軟膏基剤はワセリン等の油脂性
のものであるため、使用部位がべとつくと共に、衣類等
に付着するという欠点があった。
However, to date, no ointment base has been provided that completely dissolves poorly soluble drugs, especially adrenocortical hormones, and it has been thought that it is difficult to fully express the effects of the drug. Since conventional ointment bases are oil-based such as petrolatum, they have the disadvantage of being sticky on the application site and adhering to clothing and the like.

〔問題点を解決するための手段〕[Means for solving problems]

斯かる実情において、本発明者は鋭意研究を行った結果
、上記問題点を克服した軟膏基剤を得ることに成功した
Under these circumstances, the inventors of the present invention conducted intensive research and succeeded in obtaining an ointment base that overcomes the above-mentioned problems.

すなわち、本発明は、プロピレングリコール5〜30f
fi1%1.1elJ工チレングリコール5〜50重!
俤、グル化剤0.1〜5重量優、グリセリンlO〜40
重量俤及びアルカリ剤0.1〜3重量%を含有する軟膏
基剤を提供するものである。
That is, the present invention provides propylene glycol 5-30f
fi1%1.1elJ engineered tylene glycol 5-50 weight!
迤, Gluing agent 0.1-5% by weight, Glycerin 10-40
The present invention provides an ointment base containing 0.1 to 3% by weight of an alkaline agent.

ゾロピレングリコールは一般の軟膏基剤として使用され
ているものであるが、一般に高含量で用いると皮膚刺激
があると考えられている。しかし5通常の外用剤の使用
形態において、基剤中30重量%(以下、単に優と表示
する)以下の場合には重篤な刺激性は認められない。従
って、本発明においては、プロピレングリコールは全組
成の5〜30%、好ましくは5〜20%になるように配
合される。
Zoropylene glycol is commonly used as an ointment base, but is generally thought to cause skin irritation when used in high concentrations. However, in the usual usage form of external preparations, serious irritation is not observed when the amount is 30% by weight or less (hereinafter simply referred to as "excellent") in the base. Therefore, in the present invention, propylene glycol is blended in an amount of 5 to 30%, preferably 5 to 20% of the total composition.

ポリエチレングリコールは、凝固点及び水に対する溶解
性の点から、平均分子量200〜600、特に200〜
400のもの(破りエチレングリコール200〜400
)が好ましい。またその配合量は、難溶性薬物の溶解性
の点からすれば多い程よいが、あまり多いと基剤系が不
安定となるので、これらを考慮し、全組成の5〜50%
、好ましくは10〜30%配合される。
Polyethylene glycol has an average molecular weight of 200 to 600, particularly 200 to 600, in terms of freezing point and water solubility.
400 (broken ethylene glycol 200-400)
) is preferred. In addition, from the viewpoint of solubility of the poorly soluble drug, the larger the amount is, the better, but if it is too large, the base system will become unstable.
, preferably 10 to 30%.

グル化剤としては、例えば、アクリル酸の重合した酸性
高分子であるカルボキシビニル?リマー、メチルセルロ
ース、カルボ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、
アルギン酸ナトリウム等が挙げられる。この中でも、粘
度が適当でしかも温度変化による粘度の変動が少なく、
また経日安定性がよい等の点から、カルゴキシビニル?
リフ−#940又は#941が特に好ましい。このグル
化剤の配合量によってグル化状態及び粘度が異なり、ま
た軟膏の粘度は添加される難溶性薬物の種類によっても
異なるので、グル化剤の配合量はその都度決定されるが
、通常全組成の0.1〜5%配合される。
Examples of gluing agents include carboxyvinyl, which is an acidic polymer made from polymerized acrylic acid. Rimmer, methylcellulose, carboxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose,
Examples include sodium alginate. Among these, the viscosity is suitable and there is little fluctuation in viscosity due to temperature changes.
Also, since it has good stability over time, cargoxyvinyl?
Rif-#940 or #941 is particularly preferred. The gluing state and viscosity vary depending on the amount of the gluing agent, and the viscosity of the ointment also differs depending on the type of poorly soluble drug added, so the amount of the gluing agent is determined on a case-by-case basis. It is added in an amount of 0.1 to 5% of the composition.

グリセリンは保湿剤として冷加されるものであり、ゲル
化剤によるゲル化への影響を考慮し、局方グリセリンを
使用するのが好ましい。その配合量は、ゲル化剤及び難
溶性薬物の溶解性の点から、10〜40%、好ましくは
10〜30%である。
Glycerin is a moisturizing agent that is cooled, and in consideration of the influence of gelling agents on gelation, it is preferable to use pharmacopoeial glycerin. The blending amount is 10 to 40%, preferably 10 to 30% from the viewpoint of solubility of the gelling agent and the poorly soluble drug.

アルカリ剤としては、モノエタノールアミン、ジェタノ
ールアミン、トリエタノールアミン、水酸化ナトリウム
、炭酸ナトリウム等が使用される。このアルカリ剤はグ
ル化剤を中和するために使用されるものであり、その配
合量は全組成のO,1〜3%が好ましい。
As the alkaline agent, monoethanolamine, jetanolamine, triethanolamine, sodium hydroxide, sodium carbonate, etc. are used. This alkaline agent is used to neutralize the gluing agent, and its amount is preferably 1 to 3% of the total composition.

本発明の軟膏基剤に配合して効果の同上がみられる難溶
性薬物としては、例えば、ヒドロコルチゾン、酢酸ヒド
ロコルチゾン、ゾレトニゾロン、酢酸ゾレドニゾロン等
の則腎皮質ホルモン;アミノ安息香酸エチル、塩酸テト
ラカイン、塩酸ゾロカイン、塩酸ゾプカイン、塩酸リド
カイン等の局所麻酔剤;インドメタシン、ブフエキサマ
ツク、フルフェナム酸ブチル、ビタミンA等の鎮痛、鎮
痒、収斂、消炎剤が挙げられる。この中でも、抗炎症剤
の副腎皮質ホルモンと局所麻酔剤の塩酸ゾプカインを併
用して本発明軟膏基剤に配合して得られる軟膏は特に優
れた効果’kWする。これらの薬物の配合量は、一般の
外用剤への配合量に準ずればよいが、従来の外用剤への
配合量より少ない量で高い効果が得られる。
Examples of sparingly soluble drugs that can be combined with the ointment base of the present invention and exhibit the same effects as above include renal cortical hormones such as hydrocortisone, hydrocortisone acetate, zoletnisolone, and zolednisolone acetate; ethyl aminobenzoate, tetracaine hydrochloride, and hydrochloric acid. Local anesthetics such as zorocaine, zopcaine hydrochloride, and lidocaine hydrochloride; analgesic, antipruritic, astringent, and antiinflammatory agents such as indomethacin, bufexamac, butyl flufenamate, and vitamin A. Among these, an ointment obtained by combining adrenocortical hormone, an anti-inflammatory agent, and zopcaine hydrochloride, a local anesthetic, into the ointment base of the present invention has particularly excellent effects. The amount of these drugs to be blended may be the same as that in general external preparations, but high effects can be obtained with a smaller amount than in conventional external preparations.

本発明の軟膏基剤2用いて軟膏を調表するには、例えば
、難溶性薬物を7″ロビレングリコール及ヒ、jelJ
エチレングリコールの混合液に溶解させ、これにゲル化
剤の水膨潤液及びグリセリンを添加し、最後にアルカリ
剤を加えてグル化させる方法によって行われる。面この
際粘度調節剤としてぼりビニルピロリドンを添加するこ
ともできる。
To prepare an ointment using the ointment base 2 of the present invention, for example, a sparingly soluble drug may be mixed with 7'' robylene glycol and gel J.
This is carried out by dissolving in a mixed solution of ethylene glycol, adding thereto a water-swelling solution of a gelling agent and glycerin, and finally adding an alkaline agent to cause gluing. At this time, vinylpyrrolidone can also be added as a viscosity modifier.

〔実施例〕〔Example〕

次に実施例を挙げて説明する。 Next, an example will be given and explained.

実施例1゜ 下記組成の軟膏金調裂し、ヒト上腕部の、Qソチテスト
により薬物(酢酸ヒドロコルチゾン)の効果を評価した
Example 1 An ointment having the following composition was cut into pieces, and the effect of the drug (hydrocortisone acetate) was evaluated using the QSochi test on human upper arms.

(1)  組成 本発明軟膏: 酢酸ヒドロコルチゾン  0.1   C重11ノロピ
レングリコール 15.O ?ジエチレングリコール200 45.0カルボキシビ
ニル?リマー*0.5 グリセリン       10.0 トリエタノールアミン    1.0 精製水     28,4 (注)*カーボ?−ル#941(ミツヤ化工社製)比較
軟11F: 酢酸ヒドロコルチゾン    0.1(重量%)ワセリ
ン          70゜9スノQン60    
      5.0ラノリン         24.
0 (2)評価方法 79ツチテストは軟膏閉鎖貼付17時間後1、Qツチを
除去し、貼付部位全水洗いし、除去1時間後及び3時間
後に貼付部の蒼白度?相対的に数値化(0:不変、1:
境界線が不明瞭であるが中心が蒼白、2:境界線が明瞭
な蒼白、3:境界面が明らかで強い蒼白)した0尚値は
10名の平均値で示した。
(1) Composition Ointment of the present invention: Hydrocortisone acetate 0.1 C-11 noropyrene glycol 15. O? Diethylene glycol 200 45.0 carboxyvinyl? Rimmer *0.5 Glycerin 10.0 Triethanolamine 1.0 Purified water 28.4 (Note) *Carbo? -L #941 (manufactured by Mitsuya Kako Co., Ltd.) Comparative soft 11F: Hydrocortisone acetate 0.1 (wt%) Vaseline 70°9 Suno Q-on 60
5.0 Lanolin 24.
0 (2) Evaluation method 79 Tsuchi test: 17 hours after application of ointment, Q Tsuchi is removed, the entire application area is washed with water, and 1 hour and 3 hours after removal, the pallor level of the application area is evaluated. Relatively quantified (0: unchanged, 1:
The score of 0 was expressed as the average value of 10 patients.

(3)結果 第1表(蒼白度〕 以上の試験から明らかな如く、本発明の軟膏基剤を使用
して調製した本発明状fは比較軟膏に比較し約5倍の効
果を示した0 実施例2゜ 下記組成の軟−1!Ff!:調表し、使用試ti!lヲ
したところ、効力、使用感ともにすぐれたものであった
(3) Results Table 1 (pallor level) As is clear from the above tests, the present invention f prepared using the ointment base of the present invention showed about 5 times the effect compared to the comparative ointment. Example 2 Soft-1!Ff! of the following composition: When prepared and tested in use, it was found to be excellent in both efficacy and feeling of use.

組成: デレドニゾロン      0.05(重量%)塩酸ゾ
ブカイン      0.20 プロピレングリコール  20.00 ポリエチレングリコール200 35.00* カルボキシビニル?リマ−0,80 グリセリン      25.00 ゾエタノールアミン    0.50 精裂水     18.45 (注)*カーボ?−ル#940(ミツヤ化工社製)〔発
明の効果〕 本発明軟膏基剤は難溶性薬物をよく溶解し、薬物の効果
を完全に発現させることができるので、少量の薬物の配
合によって高い効果を得ることができると共に、これに
よって調製された軟膏はべとつきがなく使用感が優れて
いるという特長’に!する。
Composition: Delednisolone 0.05 (wt%) Zobucaine hydrochloride 0.20 Propylene glycol 20.00 Polyethylene glycol 200 35.00* Carboxyvinyl? Limer 0.80 Glycerin 25.00 Zoethanolamine 0.50 Semena water 18.45 (Note) *Carbo? -L #940 (manufactured by Mitsuya Kako Co., Ltd.) [Effects of the invention] The ointment base of the present invention can dissolve poorly soluble drugs well and fully express the effects of the drug, so it is highly effective with a small amount of drug. In addition to this, the ointment prepared using this method has the advantage of not being sticky and having an excellent feeling of use! do.

以上that's all

Claims (1)

【特許請求の範囲】[Claims] 1、プロピレングリコール5〜30重量%、ポリエチレ
ングリコール5〜50重量%、ゲル化剤0.1〜5重量
%、グリセリン10〜40重量%及びアルカリ剤0.1
〜3重量%を含有する軟膏基剤。
1. Propylene glycol 5-30% by weight, polyethylene glycol 5-50% by weight, gelling agent 0.1-5% by weight, glycerin 10-40% by weight, and alkali agent 0.1
Ointment base containing ~3% by weight.
JP61135569A 1986-06-11 1986-06-11 Ointment base Granted JPS62292716A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP61135569A JPS62292716A (en) 1986-06-11 1986-06-11 Ointment base

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP61135569A JPS62292716A (en) 1986-06-11 1986-06-11 Ointment base

Publications (2)

Publication Number Publication Date
JPS62292716A true JPS62292716A (en) 1987-12-19
JPH0511093B2 JPH0511093B2 (en) 1993-02-12

Family

ID=15154878

Family Applications (1)

Application Number Title Priority Date Filing Date
JP61135569A Granted JPS62292716A (en) 1986-06-11 1986-06-11 Ointment base

Country Status (1)

Country Link
JP (1) JPS62292716A (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2302808A (en) * 1995-07-04 1997-02-05 Surtech Int Ltd Propylene glycol with low potency corticosteroids for topical treatment of the scalp
JP2002531526A (en) * 1998-12-04 2002-09-24 ジョンソン・アンド・ジョンソン・コンシューマー・カンパニーズ・インコーポレイテッド Topical skin preparation in anhydrous state

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59122420A (en) * 1982-12-28 1984-07-14 Otsuka Pharmaceut Factory Inc Local ointment

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59122420A (en) * 1982-12-28 1984-07-14 Otsuka Pharmaceut Factory Inc Local ointment

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2302808A (en) * 1995-07-04 1997-02-05 Surtech Int Ltd Propylene glycol with low potency corticosteroids for topical treatment of the scalp
JP2002531526A (en) * 1998-12-04 2002-09-24 ジョンソン・アンド・ジョンソン・コンシューマー・カンパニーズ・インコーポレイテッド Topical skin preparation in anhydrous state

Also Published As

Publication number Publication date
JPH0511093B2 (en) 1993-02-12

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