JP4615198B2 - Antifungal aerosol topical preparation - Google Patents

Antifungal aerosol topical preparation Download PDF

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JP4615198B2
JP4615198B2 JP2003280287A JP2003280287A JP4615198B2 JP 4615198 B2 JP4615198 B2 JP 4615198B2 JP 2003280287 A JP2003280287 A JP 2003280287A JP 2003280287 A JP2003280287 A JP 2003280287A JP 4615198 B2 JP4615198 B2 JP 4615198B2
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aerosol
external preparation
water
stock solution
antifungal
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JP2005041850A (en
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敏博 白水
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Hisamitsu Pharmaceutical Co Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/12—Aerosols; Foams
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics

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Description

本発明は、抗真菌成分を有効成分としたエアゾール外用剤に関する。   The present invention relates to an aerosol external preparation containing an antifungal component as an active ingredient.

抗真菌剤は、水虫、カンジダ症、タムシなどの真菌感染症を予防または治療するための医薬である。例えば、塩酸ブテナフィンは、ベンジルアミン系抗真菌剤であり、従来より液剤、クリーム剤等の形態での外用剤として用いられているが、この塩酸ブテナフィンのような抗真菌化合物を、アルミニウムエアゾール缶などのエアゾール容器中で水と共存させる場合、該化合物が溶解する際に発生する水素イオンによって、エアゾール缶の金属表面が還元され、水素イオンと当量の金属がイオン化するため、容器の内面を樹脂でコーティングしていても、ピンホール部から金属腐食が見られ、エアゾール剤とすることが困難であった。この点を踏まえ、特許文献１には、水分含量をできるだけ少なくした液体製剤とすることにより、塩酸ブテナフィンの皮膚浸透性を改善させ、上記ピンホール部からの金属腐食を防止する手段が開示されている。しかしながら、角質透過性などの観点からは、水分を含有することが望ましい製剤も多く、そのような場合、前記方法では、角質透過性を十分に確保しつつ、エアゾール缶の腐食を防止することが困難である。
さらに、エアゾール外用製剤が水分を含有することは、適用時の冷感を強め、その持続性を高めることから、痒みを伴なう患者の痒みを緩和することができ、また、水は、皮膚への刺激性が最も少ない成分であることから、アルコールを多く含む製剤に比べ、安全性が高いといった利点を有する。
このように、皮膚浸透性、エアゾール缶の腐食防止をはじめとして、鎮痒性や安全性等、総合的に物性が改善されたエアゾール外用製剤が希求されているが、これを十分に満足するものは未だ得られていないのが現状である。 An antifungal agent is a medicament for preventing or treating fungal infections such as athlete's foot, candidiasis, and beetles. For example, butenafine hydrochloride is a benzylamine antifungal agent and has been conventionally used as an external preparation in the form of a solution, a cream, etc., but this antifungal compound such as butenafine hydrochloride can be used as an aluminum aerosol can etc. When the compound is allowed to coexist with water in the aerosol container, the metal surface of the aerosol can is reduced by the hydrogen ions generated when the compound dissolves, and the metal equivalent to the hydrogen ions is ionized. Even if it was coated, metal corrosion was seen from the pinhole part, and it was difficult to obtain an aerosol agent. In view of this point, Patent Document 1 discloses a means for improving the skin permeability of butenafine hydrochloride and preventing metal corrosion from the pinhole portion by making a liquid preparation with a water content as low as possible. Yes. However, from the viewpoint of keratin permeability and the like, there are many preparations that desirably contain moisture, and in such a case, the method can prevent corrosion of the aerosol can while ensuring sufficient keratin permeability. Have difficulty.
In addition, since the external preparation of aerosol contains water enhances the cooling sensation during application and enhances its persistence, it can alleviate the itching of patients with itching, Since it is the ingredient with the least irritation to the skin, it has the advantage of higher safety compared to a preparation containing a large amount of alcohol.
Thus, there is a need for aerosol preparations with improved physical properties such as skin penetration, prevention of corrosion of aerosol cans, antipruritic properties and safety, etc. The current situation has not yet been obtained.

特開２００１−１８１１８２号公報JP 2001-181182 A

したがって、本発明の課題は、抗真菌成分の皮膚浸透性を改善し、かつ、エアゾール缶の腐食を導くことのないエアゾール外用製剤を提供することにある。   Accordingly, an object of the present invention is to provide an external preparation for aerosol that improves the skin permeability of the antifungal component and does not lead to corrosion of the aerosol can.

本発明者は、鋭意研究した結果、エアゾール外用製剤が、抗真菌成分と水及びＨＬＢ１〜９の親油性の界面活性剤とを配合することからなる原液、および、さらに、アルコールを含有することによって、上記目的を達成できることを見出し、本発明を完成するに至った。   As a result of diligent research, the present inventor has found that an aerosol external preparation contains a stock solution composed of an antifungal component, water and a lipophilic surfactant of HLB 1 to 9, and further contains alcohol. The present inventors have found that the above object can be achieved and have completed the present invention.

すなわち本発明は、塩酸ブテナフィンと、水及びＨＬＢ１〜９の親油性の界面活性剤とを配合してなる原液を含有するエアゾール外用製剤であって、原液中の塩酸ブテナフィンの濃度が０．１〜１０．０ｗｔ％であり、水分濃度が３．０〜９０ｗｔ％であり、ＨＬＢ１〜９の親油性の界面活性剤が、モノイソステアリン酸ジグリセリルまたはモノオレイン酸グリセリンであり、原液がＷ／Ｏ型液状である、前記エアゾール外用製剤に関する。 That is, the present invention is an aerosol external preparation containing a stock solution in which butenafine hydrochloride is mixed with water and a lipophilic surfactant of HLB 1 to 9, wherein the concentration of butenafine hydrochloride in the stock solution is 0.1 to 10.0 wt%, water concentration is 3.0 to 90 wt%, and the lipophilic surfactant of HLB 1 to 9 is diglyceryl monoisostearate or glyceryl monooleate, and the stock solution is W / O type It is related with the said aerosol external preparation which is a liquid .

また、本発明は、原液中のＨＬＢ１〜９の親油性の界面活性剤の濃度が０．１〜１０ｗｔ％である、前記エアゾール外用製剤に関する。
さらに、本発明は、アルコールをさらに含有し、原液中のアルコール濃度が１．０〜７０ｗｔ％である、前記エアゾール外用製剤関する。
また、本発明は、アルコールが、エタノールである、前記エアゾール外用製剤に関する。 Moreover, this invention relates to the said aerosol external preparation whose density | concentration of the lipophilic surfactant of HLB1-9 in stock solution is 0.1-10 wt%.
Furthermore, the present invention relates to the above-mentioned aerosol preparation for external use, which further contains an alcohol and has an alcohol concentration of 1.0 to 70 wt% in the stock solution.
Moreover, this invention relates to the said aerosol external preparation whose alcohol is ethanol .

さらに、本発明は、前記エアゾール外用製剤を含む、抗真菌エアゾール外用製品に関する。 Furthermore, this invention relates to the antifungal aerosol external preparation containing the said aerosol external preparation .

本発明のエアゾール外用製剤の作用メカニズムは、必ずしも明らかではないが、抗真菌成分を含む原液に、水および界面活性剤を用いることにより、外層が油（Ｏｉｌ）、内層が水（Ｗａｔｅｒ）の液となり、そのために抗真菌成分と水が共存する場合でも、抗真菌成分の水への溶解により生じる水素イオンが、エアゾール缶の金属表面と接触しないため、該エアゾール缶を腐食しないと考えられる。
また、本発明のエアゾール外用製剤を用いることにより、とくに塩酸ブテナフィンのように金属腐蝕を惹起しやすい有効成分であっても、皮膚面への付着性が良く、汗などによる塗布面からの脱落を抑制することができる。
さらに、本発明のエアゾール外用製剤は、水を含有することができるので、適用時もしくは適用後の冷感の増強、それによる鎮痒性の向上、または、皮膚への刺激性の低減による安全性の向上といった総合的な物性の改善を図ることができる。 The mechanism of action of the aerosol preparation for external use of the present invention is not necessarily clear, but by using water and a surfactant in a stock solution containing an antifungal component, a liquid in which the outer layer is oil (Oil) and the inner layer is water (Water) Therefore, even when the antifungal component and water coexist, hydrogen ions generated by dissolution of the antifungal component in water do not come into contact with the metal surface of the aerosol can, and therefore it is considered that the aerosol can is not corroded.
In addition, by using the aerosol preparation for external use of the present invention, even an active ingredient that easily causes metal corrosion, such as butenafine hydrochloride, has good adhesion to the skin surface and can be removed from the coated surface by sweat or the like. Can be suppressed.
Furthermore, since the aerosol preparation for external use of the present invention can contain water, the cooling sensation at the time of application or after application is enhanced, thereby improving the antipruritic property or reducing the irritation to the skin. Overall physical properties such as improvement can be improved.

本発明のエアゾール製剤とすることで、抗真菌成分が、皮膚浸透性等を改善するのに十分な量の水分を含有することができ、エアゾール容器内面の腐食を導くことのない、真菌感染症を予防または治療するのに有用なエアゾール外用製剤を得ることが可能となる。   By using the aerosol preparation of the present invention, the antifungal component can contain a sufficient amount of moisture to improve skin permeability and the like, and does not lead to corrosion of the inner surface of the aerosol container, It is possible to obtain an aerosol preparation for external use useful for preventing or treating the above.

本発明で用いられる抗真菌成分は、抗真菌作用を有していれば、特に限定されないが、硝酸ミコナゾール、硝酸エコナゾール、塩酸テルビナフィン、塩酸ネチコナゾール、塩酸ネチコナゾールが挙げられ、典型的には、塩酸ブテナフィンである。   The antifungal component used in the present invention is not particularly limited as long as it has an antifungal action, but examples include miconazole nitrate, econazole nitrate, terbinafine hydrochloride, neticonazole hydrochloride, and neticonazole hydrochloride. It is.

本発明のＨＬＢ１〜９の親油性界面活性剤としては、特に限定されないが、好適な例としては、モノステアリン酸プロピレングリコール、モノステアリン酸グリセリン、モノオレイン酸グリセリンなどのグリセリン脂肪酸エステル、モノオレイン酸ジグリセリル、モノイソステアリン酸ジグリセリル、トリステアリン酸ヘキサグリルなどのポリグリセリン脂肪酸エステル、モノオレイン酸ソルビタン、モノラウリン酸ソルビタン、セスキオレイン酸ソルビタン、トリオレイン酸ソルビタンなどのソルビタン脂肪酸エステル、ポリオキシエチレンヒマシ油３、ポリオキシエチレン硬化ヒマシ油５などが挙げられる。
とくに、好ましくは、モノイソステアリン酸ジグリセリル、モノオレイン酸グリセリンである。
本発明のエアゾール外用製剤は、所望の腐蝕防止効果を得ることができる限り、どのような形態であってもよいが、エアゾール外用製剤に含有される原液が、Ｗ／Ｏ型液状であることが好ましい。 Although it does not specifically limit as lipophilic surfactant of HLB1-9 of this invention, As a suitable example, glycerin fatty acid ester, monooleic acid, such as propylene glycol monostearate, monoglyceryl monostearate, monoglyceryl monooleate Polyglyceryl fatty acid esters such as diglyceryl, diglyceryl monoisostearate, hexagrill tristearate, sorbitan fatty acid esters such as sorbitan monooleate, sorbitan monolaurate, sorbitan sesquioleate, sorbitan trioleate, polyoxyethylene castor oil 3, polyoxyethylene hydrogenated castor oil 5 and the like.
Particularly preferred are diglyceryl monoisostearate and glyceryl monooleate.
The aerosol external preparation of the present invention may be in any form as long as the desired anticorrosion effect can be obtained, but the stock solution contained in the aerosol external preparation should be a W / O liquid. preferable.

本発明で用いられるアルコールは、例えば、メタノール、エタノール、イソプロパノール等の低級アルコールであり、好ましくは、エタノールである。   The alcohol used in the present invention is, for example, a lower alcohol such as methanol, ethanol, isopropanol, and preferably ethanol.

本発明において、塩酸ブテナフィンを用いる場合、本発明の目的を達成することができれば、とくに限定されないが、原液中の塩酸ブテナフィンの濃度は、０.１〜１０．０wt％、水分濃度は、３．０〜９０wt％、アルコールの濃度は、１．０〜７０wt％、および界面活性剤の濃度は、０．１〜１０wt％が好ましい。
また、ｐＨ値は、高いｐＨ値で調製する場合には、抗真菌成分の溶解性が低減することによる結晶の析出を考慮し、３〜８の範囲が好ましい。 In the present invention, when butenafine hydrochloride is used, it is not particularly limited as long as the object of the present invention can be achieved, but the concentration of butenafine hydrochloride in the stock solution is 0.1 to 10.0 wt%, and the water concentration is 3. The concentration of 0 to 90 wt%, the concentration of alcohol is preferably 1.0 to 70 wt%, and the concentration of surfactant is preferably 0.1 to 10 wt%.
In addition, when the pH value is prepared at a high pH value, it is preferably in the range of 3 to 8 in consideration of crystal precipitation due to a decrease in solubility of the antifungal component.

本発明のエアゾール製剤の噴射剤としては公知のものが用いられることができる。すなわち、ジメチルエーテル、液化石油ガス、フロン類、Ｎ２、ＣＯ２ガス、代替フロンガス等の通常のエアゾール剤に噴射剤として用いられるものが使用される。 A well-known thing can be used as a propellant of the aerosol formulation of this invention. That is, what is used as a propellant for normal aerosol agents such as dimethyl ether, liquefied petroleum gas, chlorofluorocarbons, N 2 , CO 2 gas, and alternative chlorofluorocarbon gas is used.

アルミニウム缶は、通常用いられるものであり、すなわち、エポキシ樹脂、フェノール樹脂、ポリアミドイミド樹脂などでコーティングされるものが使用される。
また、本発明で用いられる抗真菌エアゾール外用製品とは、エアゾール外用製剤を含有するエアゾール缶などである。
本発明のエアゾール外用製剤は、その用途に応じて、抗酸化剤、ｐＨ調整剤、防腐剤、保存剤、香料等の製剤上許容される他の配合成分を、適宜含有することができる。 The aluminum can is usually used, that is, an aluminum can coated with an epoxy resin, a phenol resin, a polyamideimide resin, or the like is used.
Moreover, the antifungal aerosol external product used in the present invention includes an aerosol can containing an aerosol external preparation.
The aerosol preparation for external use of the present invention can appropriately contain other formulation components that are acceptable in formulation, such as antioxidants, pH adjusters, preservatives, preservatives, and fragrances, depending on the application.

以下に実施例を示し、本発明をさらに具体的に説明するが、本発明は、これらの実施例に限定されるものではなく、本発明の技術的思想を逸脱しない範囲で種々の変更が可能である。   The present invention will be described more specifically with reference to the following examples. However, the present invention is not limited to these examples, and various modifications can be made without departing from the technical idea of the present invention. It is.

〔実施例１〕
Ａ液：塩酸ブテナフィン１ｇを、エタノール４０ｇに溶解し、モノイソステアリン酸ジグリセリル４ｇ、ミリスチン酸イソプロピル５ｇを加え攪拌する。
Ｂ液：水４５ｇと１，３−ブチレングリコール５ｇを加え攪拌する。
エアゾール缶にＡ液２０ｍｌとＢ液２０ｍｌ及びＬＰガス６０ｍｌを充填したエアゾール剤得る。
実施例１を４０℃に６ヶ月保存した後、缶の内面を調べた結果、孔蝕は観察されなかった。 [Example 1]
Liquid A: 1 g of butenafine hydrochloride is dissolved in 40 g of ethanol, and 4 g of diglyceryl monoisostearate and 5 g of isopropyl myristate are added and stirred.
Liquid B: 45 g of water and 5 g of 1,3-butylene glycol are added and stirred.
An aerosol agent filled with 20 ml of liquid A, 20 ml of liquid B and 60 ml of LP gas in an aerosol can is obtained.
After Example 1 was stored at 40 ° C. for 6 months, the inner surface of the can was examined. As a result, no pitting corrosion was observed.

〔実施例２〕
Ａ液：塩酸ブテナフィン１ｇ、メントール２ｇ、塩酸ジブカイン０．２ｇ、マレイン酸クロルフェニラミン０．５ｇ、グリチルレチン酸０．２ｇ、ジブチルヒドロキシトルエン０．１ｇをエタノール １０ｇに溶解し、モノオレイン酸グリセリン４ｇ、ミリスチン酸オクチルドデシル２ｇを加え攪拌する。
Ｂ液：水７５ｇと１，３−ブチレングリコール５ｇを加え攪拌する。
エアゾール缶にＡ液１０ｍｌとＢ液４０ｍｌ及びＬＰガス５０ｍｌを充填したエアゾール剤得る。
実施例２を４０℃に６ヶ月保存した後、缶の内面を調べた結果、孔蝕は観察されなかった。 [Example 2]
Solution A: 1 g of butenafine hydrochloride, 2 g of menthol, 0.2 g of dibucaine hydrochloride, 0.5 g of chlorpheniramine maleate, 0.2 g of glycyrrhetinic acid and 0.1 g of dibutylhydroxytoluene are dissolved in 10 g of ethanol, 4 g of glyceryl monooleate, Add 2 g of octyldodecyl myristate and stir.
Liquid B: 75 g of water and 5 g of 1,3-butylene glycol are added and stirred.
An aerosol agent filled with 10 ml of liquid A, 40 ml of liquid B and 50 ml of LP gas in an aerosol can is obtained.
After Example 2 was stored at 40 ° C. for 6 months, the inner surface of the can was examined. As a result, no pitting corrosion was observed.

〔実施例３〕
塩酸ブテナフィン１ｇ、メントール２ｇ、リドカイン０．３ｇ、ジフェンヒドラミン０．５ｇ、グリチルレチン酸０．２ｇをエタノール６０ｇに溶解し、モノオレイン酸グリセリン４ｇ、ミリスチン酸イソプロピル３ｇを加え攪拌する。これに水３０ｇを加え攪拌する。
エアゾール缶に上記液５０ｍｌ、液化石油ガス３０ｍｌ及びジメチルエーテル２０ｍｌを充填したエアゾール剤得る。
実施例３を４０℃に６ヶ月保存した後、缶の内面を調べた結果、孔蝕は観察されなかった。 Example 3
1 g of butenafine hydrochloride, 2 g of menthol, 0.3 g of lidocaine, 0.5 g of diphenhydramine and 0.2 g of glycyrrhetinic acid are dissolved in 60 g of ethanol, and 4 g of glycerol monooleate and 3 g of isopropyl myristate are added and stirred. 30 g of water is added to this and stirred.
An aerosol can is obtained by filling an aerosol can with 50 ml of the above liquid, 30 ml of liquefied petroleum gas and 20 ml of dimethyl ether.
After Example 3 was stored at 40 ° C. for 6 months, the inner surface of the can was examined. As a result, no pitting corrosion was observed.

〔実施例４〕
Ａ液：塩酸ブテナフィン３ｇ、メントール１ｇ、塩酸ジブカイン０．５ｇ、マレイン酸クロルフェニラミン０．５ｇをエタノール ３０ｇに溶解し、モノイソステアリン酸ジグリセリル２ｇ、アジピン酸ジイソプロピル３ｇを加え攪拌する。
Ｂ液：水５５ｇとグリセリン５ｇを加え攪拌する。
エアゾール缶にＡ液２４ｍｌとＢ液３６ｍｌ及びＬＰガス４０ｍｌを充填したエアゾール剤得る。
実施例４を４０℃に６ヶ月保存した後、缶の内面を調べた結果、孔蝕は観察されなかった。 Example 4
Solution A: 3 g of butenafine hydrochloride, 1 g of menthol, 0.5 g of dibucaine hydrochloride and 0.5 g of chlorpheniramine maleate are dissolved in 30 g of ethanol, 2 g of diglyceryl monoisostearate and 3 g of diisopropyl adipate are added and stirred.
Liquid B: 55 g of water and 5 g of glycerin are added and stirred.
An aerosol can is obtained by filling an aerosol can with 24 ml of liquid A, 36 ml of liquid B and 40 ml of LP gas.
After Example 4 was stored at 40 ° C. for 6 months, the inner surface of the can was examined. As a result, no pitting corrosion was observed.

〔比較例１〕
塩酸ブテナフィン１ｇ、メントール２ｇ、塩酸ジブカイン０．２ｇ、マレイン酸クロルフェニラミン０．５ｇ、グリチルレチン酸０．２ｇ、ジブチルヒドロキシトルエン０．１ｇを、エタノール ５０ｇに溶解し、ミリスチン酸オクチルドデシル２ｇを加え攪拌する。さらに水４０ｇと１，３−ブチレングリコール５ｇを加え攪拌する。
エアゾール缶に上記液４０ｍｌ及びジメチルエーテル６０ｍｌを充填したエアゾール剤得る。
比較例１を４０℃に６ヶ月保存した後、缶の内面を調べた結果、エアゾール缶に孔蝕が観察され内容物が漏れていた。 [Comparative Example 1]
1 g of butenafine hydrochloride, 2 g of menthol, 0.2 g of dibucaine hydrochloride, 0.5 g of chlorpheniramine maleate, 0.2 g of glycyrrhetinic acid and 0.1 g of dibutylhydroxytoluene are dissolved in 50 g of ethanol, and 2 g of octyldodecyl myristate is added and stirred. To do. Further, 40 g of water and 5 g of 1,3-butylene glycol are added and stirred.
An aerosol can is obtained by filling an aerosol can with 40 ml of the above solution and 60 ml of dimethyl ether.
After Comparative Example 1 was stored at 40 ° C. for 6 months, the inner surface of the can was examined. As a result, pitting corrosion was observed in the aerosol can and the contents were leaked.

Figure 0004615198
Figure 0004615198

本発明のエアゾール製剤とすることで、抗真菌成分が、水分を含有することができ、アルミニウム缶のようなエアゾール容器内面の腐食がみられない、良好な製剤安定性を得ることが可能となる。   By using the aerosol preparation of the present invention, the antifungal component can contain moisture, and it is possible to obtain good preparation stability without corrosion of the inner surface of the aerosol container such as an aluminum can. .

抗真菌成分と、水及びＨＬＢ１〜９の親油性の界面活性剤とを配合してなる原液をエアゾール外用製剤に用いることにより、皮膚浸透性等、総合的に物性を改善し、エアゾール缶の腐食の心配をせずに、真菌感染症の治療等、広範囲な用途に適用することができる。   Aerosol can corrosion by improving the overall physical properties, such as skin permeability, by using an undiluted solution containing antifungal ingredients, water and lipophilic surfactants of HLB1 to 9 for aerosol external preparations It can be applied to a wide range of uses such as the treatment of fungal infections.

Claims (5)

塩酸ブテナフィンと、水及びＨＬＢ１〜９の親油性の界面活性剤とを配合してなる原液を含有するエアゾール外用製剤であって、原液中の塩酸ブテナフィンの濃度が０．１〜１０．０ｗｔ％であり、水分濃度が３．０〜９０ｗｔ％であり、ＨＬＢ１〜９の親油性の界面活性剤が、モノイソステアリン酸ジグリセリルまたはモノオレイン酸グリセリンであり、原液がＷ／Ｏ型液状である、前記エアゾール外用製剤。 An aerosol external preparation containing a stock solution comprising butenafine hydrochloride, water and a lipophilic surfactant of HLB 1 to 9, wherein the concentration of butenafine hydrochloride in the stock solution is 0.1 to 10.0 wt% The water concentration is 3.0 to 90 wt%, the lipophilic surfactant of HLB 1 to 9 is diglyceryl monoisostearate or glyceryl monooleate, and the stock solution is a W / O liquid. Aerosol external preparation . 原液中のＨＬＢ１〜９の親油性の界面活性剤の濃度が０．１〜１０ｗｔ％である、請求項１に記載のエアゾール外用製剤。 The aerosol external preparation according to claim 1, wherein the concentration of the lipophilic surfactant of HLB 1 to 9 in the stock solution is 0.1 to 10 wt% . アルコールをさらに含有し、原液中のアルコール濃度が１．０〜７０ｗｔ％である、請求項２に記載のエアゾール外用製剤。 The aerosol external preparation according to claim 2 , further comprising an alcohol, wherein the alcohol concentration in the stock solution is 1.0 to 70 wt% . アルコールが、エタノールである、請求項３に記載のエアゾール外用製剤。 The aerosol external preparation according to claim 3 , wherein the alcohol is ethanol. 請求項１〜４のいずれかに記載のエアゾール外用製剤を含む、抗真菌エアゾール外用製品。 The antifungal aerosol external product containing the aerosol external preparation in any one of Claims 1-4 .
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