WO2020130035A1 - Foamable topical composition - Google Patents

Foamable topical composition Download PDF

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Publication number
WO2020130035A1
WO2020130035A1 PCT/JP2019/049587 JP2019049587W WO2020130035A1 WO 2020130035 A1 WO2020130035 A1 WO 2020130035A1 JP 2019049587 W JP2019049587 W JP 2019049587W WO 2020130035 A1 WO2020130035 A1 WO 2020130035A1
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composition according
composition
foam
active ingredient
weight
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PCT/JP2019/049587
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French (fr)
Japanese (ja)
Inventor
強志 桑原
駿介 加茂
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日東メディック株式会社
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Application filed by 日東メディック株式会社 filed Critical 日東メディック株式会社
Priority to JP2020526043A priority Critical patent/JP6781358B1/en
Priority to CN201980083678.1A priority patent/CN113164511A/en
Priority to KR1020217007588A priority patent/KR102584365B1/en
Publication of WO2020130035A1 publication Critical patent/WO2020130035A1/en

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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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/12—Aerosols; Foams
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/727—Heparin; Heparan
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/728—Hyaluronic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/10—Anti-acne agents
    • 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
    • A61P17/16—Emollients or protectives, e.g. against radiation

Definitions

  • the present invention relates to a composition for external use that forms a foam during use.
  • a surfactant is known as a component that forms bubbles.
  • Anionic surfactants are said to have high foaming power but are irritating, and nonionic surfactants are said to have low irritation but low foaming power. No satisfactory foaming power and safety have been obtained.
  • To form a safe and good foam by combining polyoxyethylene alkyl ether and/or polyoxyethylene alkenyl ether as a nonionic surfactant with polyoxyethylene fatty acid ester and/or polyoxyethylene hydrogenated castor oil It is reported that this can be done (Patent Document 1).
  • the amount of the additive is small, and with the smaller amount of the additive, it is possible to produce a foam having a better foam quality, an appropriate foam-holding feeling without dropping, and a foam having a good feeling in use.
  • foamable external compositions There is a strong demand for the development of new foamable external compositions.
  • An object of the present invention is to provide a foamable external composition capable of producing a foam having a better foam quality, an appropriate foam-holding feeling without dropping, and a foam having a good feeling in use.
  • the present inventors have conducted intensive studies in view of such a situation, and have found that the use of a polymer surfactant as a foaming agent achieves a desired purpose. That is, the present invention relates to a composition for external use, which contains a polymeric surfactant as a foaming component and forms foam when used.
  • the formulation of the present invention makes it possible to obtain a new topical composition having a better foam quality, a suitable foam-holding feeling without sagging, and a good feeling of use, particularly gas.
  • a pump former container and a squeeze former container that are not required, it can be used as a non-gas type formulation that exhibits a foamy state at the time of discharge, and a composition suitable for the treatment of skin diseases such as atopic dermatitis can be obtained.
  • Example 3 is a photograph showing the result (foam formation) of Example 1.
  • 5 is a photograph showing the results of Example 2 (foam persistence (evaluated by polyurethane)).
  • 5 is a photograph showing the results of Example 2 (foam persistence (evaluated with Kim towel)).
  • 5 is a photograph showing the result of Example 2 (drip of foam).
  • the external composition of the present invention can be used as a spray agent for foaming a stock solution into a foam at the time of use, or a base thereof.
  • the stock solution means a liquid composition capable of foaming.
  • the composition for external use of the present invention can be used in a foam discharge container in which a stock solution in a container is sprayed by a pump without using a propellant.
  • the foam discharge container is not particularly limited as long as the composition of the present invention can be mixed with air and discharged in a foamed state, and examples thereof include a pump spray (pump former) container that discharges from a pressure pump and a soft container.
  • a squeeze former container or the like that presses the body and discharges is preferably used.
  • the polymer surfactant of the present invention includes ethyl cellulose, methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose (hypromellose), carboxymethyl cellulose, sodium carboxymethyl cellulose, cellulose derivatives such as carboxymethyl ethyl cellulose, polyvinyl alcohol, polyvinylpyrrolidone, polyethylene. At least one selected from glycol and polyacrylic acid.
  • At least one selected, especially hydroxypropylmethyl cellulose (hypromellose) is preferable.
  • hypromellose those having a substitution degree type of 2906 or 2910 stipulated in the Japanese Pharmacopoeia are preferably used.
  • the polymeric surfactant is 0.01 to 10% by weight, preferably 0.1 to 5% by weight, more preferably 0.2 to 3% by weight, particularly about 0.5% by weight, based on the total amount of the composition. , About 0.75% by weight or about 1% by weight.
  • a numerical value is “about”, it includes ⁇ 20%, or ⁇ 10% or ⁇ 5% of the indicated numerical value. According to the present invention, a desired effect can be achieved with only one type of polymeric surfactant.
  • composition of the present invention in addition to the above-mentioned polymer surfactant, if desired, other surfactants that can be used in the fields of pharmaceuticals and cosmetics, such as anionic surfactants, cationic surfactants and amphoteric surfactants. Agents and nonionic surfactants may be added.
  • anionic surfactant for example, N-acyl-N-methylglycine salt, sodium alkylsulfonate, sodium alkyl sulfate, polyoxyethylene alkyl ether carboxylate, sodium lauryl sulfate, etc.
  • a cationic surfactant for example, benzalkonium chloride, benzethonium chloride, an aliphatic amine salt, an aliphatic quaternary ammonium salt, and the like
  • amphoteric surfactant for example, lauryldimethylaminoacetic acid betaine, stearyldimethylaminoacetic acid betaine, 2-alkyl-N.
  • nonionic surfactants such as polyoxyethylene alkyl Ether, polyoxyethylene alkenyl ether, polyoxyethylene hydrogenated castor oil, polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene fatty acid glyceryl, polyoxypropylene polyoxyethylene alkyl ether and polyoxypropylene polyoxyethylene alkenyl Examples thereof include ether.
  • the composition of the present invention may include alcohol.
  • alcohols include monohydric alcohols such as ethanol and isopropyl alcohol, polyethylene glycol, glycerin, 1,3-butylene glycol, erythritol, sorbitol, xylitol, maltitol, propylene glycol, dipropylene glycol, diglycerin, isoprene glycol, 1, Examples are polyhydric alcohols such as 2-pentanediol, 2,4-hexanediol, 1,2-hexanediol, and 1,2-octanediol, which may be contained alone or in combination of two or more. Glycerin, propylene glycol, polyethylene glycol and 1,3-butylene glycol are particularly preferred.
  • the total content of the alcohol is 5 to 60% by weight, preferably 10 to 50% by weight, more preferably 15 to 40% by weight.
  • the composition of the present invention preferably has a pH value in the range of 3-12. A more preferable pH value is 4-10.
  • the pH adjuster for adjusting the pH value of the composition to the above range include potassium dihydrogen phosphate, citric acid, etc., and in the high pH range. Those used for adjustment include sodium hydroxide, potassium hydroxide, sodium lactate, sodium citrate, L-arginine, diisopropanolamine and the like.
  • Particularly preferred pH adjusters include potassium dihydrogen phosphate, potassium hydroxide, sodium citrate, citric acid, diisopropanolamine, sodium edetate and the like.
  • liquid composition according to the present invention in addition to the above components, a preservative (preservative), an antioxidant, a wetting agent, a stabilizer, an ultraviolet absorber, etc., which are commonly used in external preparations for skin. Agents can be included.
  • Examples of the above preservative include methyl paraoxybenzoate, ethyl paraoxybenzoate, paraoxybenzoic acid esters (parabens) such as propyl paraoxybenzoate, sodium benzoate, and phenoxyethanol.
  • the above preservatives may be used alone or in combination of two or more.
  • the content of the preservative in the composition is preferably 0.01 to 1% by weight, more preferably 0.1 to 0.5% by weight.
  • composition of the present invention may be provided as a base for producing a drug or cosmetic by incorporating a pharmaceutically active ingredient or an ingredient effective as a cosmetic, and the composition of the present invention contains the pharmaceutically active ingredient. You can leave.
  • a composition containing a pharmaceutically active ingredient is also an aspect of the present invention.
  • composition of the present invention is used as an external preparation applied to the skin to treat skin inflammation, eczema, atopic dermatitis, psoriasis, acne, scars, pressure ulcers, acne and the like (healing, improvement of symptoms, It is preferably applied to skin diseases such as prevention of deterioration and prevention of onset) and also to hair parts such as the scalp as well as the skin.
  • the active ingredient contained in the composition of the present invention is not particularly limited as long as it is applied to the skin and provided, but steroids, nonsteroidal anti-inflammatory agents, bactericides, antibacterial agents, antifungals. Examples include agents, vitamins, immunosuppressants, mucopolysaccharides, cAMP derivatives, fibroblast growth factors, naphthoic acid derivatives, benzoyl peroxide and the like.
  • the steroids are not particularly limited as long as they have a steroid skeleton, but include cortisone, hydrocortisone, fludrocortisone acetate, prednisolone, methylprednisolone, dexamethasone, betamethasone, clobetasol and its nonsteroidal anti-inflammatory.
  • vitamins examples include vitamin A or a derivative thereof (eg vitamin A oil), vitamin B or a derivative thereof (eg panthenol), vitamin C or a derivative thereof, vitamin D or a derivative thereof (eg active vitamin D3), Vitamin E or a derivative thereof (for example, tocopherol acetate), vitamin K or a derivative thereof, the immunosuppressive agent is tacrolimus, cyclophosphamide, and the like, and the mucopolysaccharide is a heparin-like substance or hyaluronic acid and Examples of the salt and cAMP derivative include bucladesine sodium, fibroblast growth factor such as trafermin, and naphthoic acid derivative such as adapalene.
  • vitamin A or a derivative thereof eg vitamin A oil
  • vitamin B or a derivative thereof eg panthenol
  • vitamin C or a derivative thereof eg active vitamin D3
  • Vitamin E or a derivative thereof for example, tocopherol acetate
  • a topical composition containing a heparin-like substance or a mucopolysaccharide such as hyaluronic acid and a salt thereof is preferably exemplified.
  • the foamable composition containing a heparin-like substance has a blood coagulation suppressing action, a blood flow increasing action, a hematoma regression promoting action, a keratin water retention enhancing action and a fibroblast proliferation inhibiting action, Dry skin disease, sebum deficiency, progressive palmar keratoderma, frostbite, hypertrophic scars/keloids, pain and inflammatory diseases due to blood circulation disorder (induration and pain after injection), thrombophlebitis (including hemorrhoids) ), swelling, hematoma, tendonitis, myalgia, arthritis, and muscular torticollis after trauma (bruises, sprains, and crushes) are also suitable as a therapeutic composition.
  • Example 1 A pump former container was filled with the prepared sample according to the following prescription, and the presence or absence of foam formation at the time of discharge from the container was evaluated (Table 1, FIG. 1).
  • the samples A to I and N are polymeric surfactants.
  • each of the polymer surfactants contained in the foamable external composition of the present invention is effective as a foaming agent alone.
  • Example 2 According to the following formulation, the prepared sample was filled in a pump former container, and the presence or absence of foam formation, foam quality, foam retention time, and the presence or absence of dripping were measured (Tables 3 and 4).
  • condition A a mat of polyurethane material was used as a material close to the skin of a healthy person
  • condition B a Kim towel that assumed relatively severe dry skin was used and discharged onto it (FIGS. 2 and 3). Also, after discharging onto a mat of polyurethane material, it was tilted at about 45° C. and observed whether or not there was dripping (FIG. 4).
  • the combination of polyoxyethylene hydrogenated castor oil 60 with polyoxyethylene cetyl ether or polyoxyethylene lauryl ether does not form bubbles or has low elasticity even when formed, has a short holding time, and drips, Even when the polyhydric alcohol was combined, it was inferior in elasticity and retention time compared to the preparation using hypromellose.
  • Example 3 Using hypromellose with different viscosities, the presence or absence of foam formation was evaluated depending on the concentration. The evaluation criteria of foam quality are the same as in Example 1.
  • Bubbles were formed at a concentration of 0.2% or higher regardless of the viscosity of hypromellose.
  • Example 4 Two compositions containing a heparin-like substance at a concentration of 0.1 or 0.3% were prepared in the formulation shown in the raw material name 2 in Table 2 of Example 2, filled in a pump former container, and foamed. The presence or absence of formation, the retention time of bubbles, and the presence or absence of dripping were measured (Table 5).

Abstract

Provided is a topical composition that contains a polymeric surfactant as a foaming component and that forms foam when being used. This topical composition is used for filling, for example, a pump foamer-type container or a squeeze foamer-type container to be provided.

Description

起泡性外用組成物Foaming external composition
　本発明は、使用時に泡を形成する外用組成物に関する。 The present invention relates to a composition for external use that forms a foam during use.
　従来、皮膚（頭皮を含む）に使用する外用薬として、軟膏剤、クリーム剤、ローション剤など使用されてきたが、近年、垂れ落ちることなく簡便に塗布することができること、また、滑らかに塗り広げることができるなど使用性に優れることから、発泡性液体と噴射剤を使って泡状に噴出するエアゾール型製剤が開発されている。しかしながら、このエアゾール型製剤は噴射剤として液化プロパン等の液化ガス等を使用するため、揮発性有機化合物に関する規制を受け、また使用済みの缶を繰り返し使用することができないなどの環境上の点で問題があり、最近では、ポンプフォーマー容器やスクイズフォーマー容器などを使って、吐出時に泡状を呈するノンガスタイプの製剤も開発されている。 Conventionally, ointments, creams, lotions, etc. have been used as external medicines for the skin (including the scalp), but in recent years, they can be easily applied without dripping and spread smoothly. Since it is excellent in usability such as being able to be used, an aerosol type formulation which is ejected in a foam form using a foaming liquid and a propellant has been developed. However, since this aerosol type formulation uses liquefied gas such as liquefied propane as a propellant, it is subject to regulations on volatile organic compounds and in terms of the environment such as used cans cannot be used repeatedly. There is a problem, and recently, a non-gas type formulation that exhibits a foamy state at the time of discharge has been developed using a pump former container, a squeeze former container, or the like.
　一般に、泡を形成させる成分として界面活性剤が知られている。アニオン性界面活性剤は、起泡力は高いが刺激性があるとされており、非イオン性界面活性剤は、刺激性は低いが起泡力が低いとされており、一種の界面活性剤で起泡力と安全性ともに満足するものは得られていない。非イオン性界面活性剤としてポリオキシエチレンアルキルエーテル及び／又はポリオキシエチレンアルケニルエーテルとポリオキシエチレン脂肪酸エステル及び／又はポリオキシエチレン硬化ヒマシ油とを組み合わせることで、安全で良好な泡を形成することができると報告されている（特許文献１）。 Generally, a surfactant is known as a component that forms bubbles. Anionic surfactants are said to have high foaming power but are irritating, and nonionic surfactants are said to have low irritation but low foaming power. No satisfactory foaming power and safety have been obtained. To form a safe and good foam by combining polyoxyethylene alkyl ether and/or polyoxyethylene alkenyl ether as a nonionic surfactant with polyoxyethylene fatty acid ester and/or polyoxyethylene hydrogenated castor oil It is reported that this can be done (Patent Document 1).
特開２０１７－２１４４０７号公報JP, 2017-214407, A
　しかしながら、皮膚への負担をより少なくするには添加物は少ない方が好ましく、より少ない添加物で、より良好な泡質、垂れ落ちのない適度な泡持ち感、使用感のよい泡を生成できる新しい起泡性外用組成物の開発が強く望まれている。 However, in order to reduce the burden on the skin, it is preferable that the amount of the additive is small, and with the smaller amount of the additive, it is possible to produce a foam having a better foam quality, an appropriate foam-holding feeling without dropping, and a foam having a good feeling in use. There is a strong demand for the development of new foamable external compositions.
　本発明は、より良好な泡質、垂れ落ちのない適度な泡持ち感、使用感のよい泡を生成できる起泡性外用組成物を提供することを課題とする。 An object of the present invention is to provide a foamable external composition capable of producing a foam having a better foam quality, an appropriate foam-holding feeling without dropping, and a foam having a good feeling in use.
　本発明者等は、この様な状況に鑑みて鋭意研究したところ、高分子界面活性剤を起泡剤として使用することで、所望の目的を達成すること見出した。すなわち、本発明は、高分子界面活性剤を起泡成分として含む、使用時に泡を形成する外用組成物に関する。 The present inventors have conducted intensive studies in view of such a situation, and have found that the use of a polymer surfactant as a foaming agent achieves a desired purpose. That is, the present invention relates to a composition for external use, which contains a polymeric surfactant as a foaming component and forms foam when used.
　後述の実施例の結果から明らかな通り、本発明の処方によって、より良好な泡質、垂れ落ちのない適度な泡持ち感、使用感のよい新しい外用組成物を得ることができ、特にガスを必要としないポンプフォーマー容器やスクイズフォーマー容器を使って、吐出時に泡状を呈するノンガスタイプの製剤として使用でき、アトピー性皮膚炎などの皮膚疾患の治療に好適な組成物を得ることができた。 As is clear from the results of the examples described below, the formulation of the present invention makes it possible to obtain a new topical composition having a better foam quality, a suitable foam-holding feeling without sagging, and a good feeling of use, particularly gas. By using a pump former container and a squeeze former container that are not required, it can be used as a non-gas type formulation that exhibits a foamy state at the time of discharge, and a composition suitable for the treatment of skin diseases such as atopic dermatitis can be obtained. It was
実施例１の結果（泡形成）を示す写真である。3 is a photograph showing the result (foam formation) of Example 1. 実施例２の結果（泡の持続性（ポリウレタンで評価））を示す写真である。5 is a photograph showing the results of Example 2 (foam persistence (evaluated by polyurethane)). 実施例２の結果（泡の持続性（キムタオルで評価））を示す写真である。5 is a photograph showing the results of Example 2 (foam persistence (evaluated with Kim towel)). 実施例２の結果（泡の液だれ）を示す写真である。5 is a photograph showing the result of Example 2 (drip of foam).
　本発明の外用組成物は、使用時に原液を泡状にして皮膚に噴霧するためのスプレー剤、あるいはその基剤として使用できる。なお、前記原液とは、起泡可能な液体組成物を意味する。本発明の外用組成物は、噴射剤を使用せずにポンプにより容器内の原液を噴霧する泡吐出容器を用いて使用することが出来る。泡吐出容器としては、本発明の組成物を空気と混合して発泡状態で吐出できるものであれば特に限定されず、例えば、押圧ポンプより吐出するポンプスプレー（ポンプフォーマー）容器、軟質容器の胴部を押圧して吐出するスクイズフォーマー容器等が、好適に用いられる。 The external composition of the present invention can be used as a spray agent for foaming a stock solution into a foam at the time of use, or a base thereof. The stock solution means a liquid composition capable of foaming. The composition for external use of the present invention can be used in a foam discharge container in which a stock solution in a container is sprayed by a pump without using a propellant. The foam discharge container is not particularly limited as long as the composition of the present invention can be mixed with air and discharged in a foamed state, and examples thereof include a pump spray (pump former) container that discharges from a pressure pump and a soft container. A squeeze former container or the like that presses the body and discharges is preferably used.
　本発明の高分子界面活性剤は、エチルセルロース、メチルセルロース、ヒドロキシエチルセルロース、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（ヒプロメロース）、カルボキシメチルセルロース、カルボキシメチルセルロースナトリウム、カルボキシメチルエチルセルロースなどのセルロース誘導体、ポリビニルアルコール、ポリビニルピロリドン、ポリエチレングリコール、ポリアクリル酸から選ばれる少なくとも一種である。好ましくは、セルロース誘導体、ポリビニルアルコール、ポリビニルピロリドン、ポリエチレングリコール、ポリアクリル酸から選ばれる少なくとも一種、より好ましくは、ヒドロキシプロピルメチルセルロース、ヒドロキシエチルセルロース、メチルセルロース、ポリビニルアルコール、ポリビニルピロリドン、ポリエチレングリコール、ポリアクリル酸から選ばれる少なくとも一種、特にヒドロキシプロピルメチルセルロース（ヒプロメロース）が好ましい。ヒプロメロースとしては、日本薬局方に規定の置換度タイプが２９０６または２９１０のものが好適に用いられる。高分子界面活性剤は、組成物全量に対し、０．０１～１０重量％、好ましくは、０．１～5重量％、より好ましくは０．２～３重量％、特に約０．５重量％、約０．７５重量％や約１重量％程度含有するものが例示される。なお、本明細書および請求の範囲において数値について「約」という場合、示された数値の±２０％、または±１０％もしくは±５％の値まで含むものとする。本発明によれば、１種の高分子界面活性剤のみでも所望の効果を達成することができる。 The polymer surfactant of the present invention includes ethyl cellulose, methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose (hypromellose), carboxymethyl cellulose, sodium carboxymethyl cellulose, cellulose derivatives such as carboxymethyl ethyl cellulose, polyvinyl alcohol, polyvinylpyrrolidone, polyethylene. At least one selected from glycol and polyacrylic acid. Preferably, at least one selected from cellulose derivatives, polyvinyl alcohol, polyvinylpyrrolidone, polyethylene glycol, polyacrylic acid, more preferably hydroxypropylmethylcellulose, hydroxyethylcellulose, methylcellulose, polyvinyl alcohol, polyvinylpyrrolidone, polyethylene glycol, polyacrylic acid. At least one selected, especially hydroxypropylmethyl cellulose (hypromellose) is preferable. As hypromellose, those having a substitution degree type of 2906 or 2910 stipulated in the Japanese Pharmacopoeia are preferably used. The polymeric surfactant is 0.01 to 10% by weight, preferably 0.1 to 5% by weight, more preferably 0.2 to 3% by weight, particularly about 0.5% by weight, based on the total amount of the composition. , About 0.75% by weight or about 1% by weight. In addition, in the present specification and claims, when a numerical value is “about”, it includes ±20%, or ±10% or ±5% of the indicated numerical value. According to the present invention, a desired effect can be achieved with only one type of polymeric surfactant.
　本発明の組成物には上記高分子界面活性剤に加え、所望により、医薬品、化粧品分野で使用可能な他の界面活性剤、例えば、アニオン性界面活性剤、カチオン性界面活性剤、両性界面活性剤、非イオン性界面活性剤を追加しても良い。アニオン性界面活性剤としては、例えば、N-アシル-N-メチルグリシン塩、アルキルスルホン酸ナトリウム、アルキル硫酸ナトリウム、ポリオキシエチレンアルキルエーテルカルボン酸塩、ラウリル硫酸ナトリウムなど、カチオン性界面活性剤としては、例えば、塩化ベンザルコニウム、塩化ベンゼトニウム、脂肪族アミン塩、脂肪族4級アンモニウム塩など、両性界面活性剤としては、例えば、ラウリルジメチルアミノ酢酸ベタイン、ステアリルジメチルアミノ酢酸ベタイン、2-アルキル-N-カルボキシメチル-N-ヒドロキシエチルイミダゾリニウムベタイン、ラウリルジメチルアミンオキサイド、ラウリン酸アミドプロピルベタイン、コカミドプロピルベタイン、ラウリルヒドロキシスルホベタインなど、非イオン性界面活性剤としては、例えば、ポリオキシエチレンアルキルエーテル、ポリオキシエチレンアルケニルエーテル、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレン脂肪酸エステル、ポリオキシエチレンソルビタン脂肪酸エステル、ポリオキシエチレン脂肪酸グリセリル、ポリオキシプロピレンポリオキシエチレンアルキルエーテル及びポリオキシプロピレンポリオキシエチレンアルケニルエーテルなどが例示される。 In the composition of the present invention, in addition to the above-mentioned polymer surfactant, if desired, other surfactants that can be used in the fields of pharmaceuticals and cosmetics, such as anionic surfactants, cationic surfactants and amphoteric surfactants. Agents and nonionic surfactants may be added. As the anionic surfactant, for example, N-acyl-N-methylglycine salt, sodium alkylsulfonate, sodium alkyl sulfate, polyoxyethylene alkyl ether carboxylate, sodium lauryl sulfate, etc., as a cationic surfactant , For example, benzalkonium chloride, benzethonium chloride, an aliphatic amine salt, an aliphatic quaternary ammonium salt, and the like, as the amphoteric surfactant, for example, lauryldimethylaminoacetic acid betaine, stearyldimethylaminoacetic acid betaine, 2-alkyl-N. -Carboxymethyl-N-hydroxyethyl imidazolinium betaine, lauryl dimethylamine oxide, lauric amide propyl betaine, cocamidopropyl betaine, lauryl hydroxy sulfobetaine, etc., nonionic surfactants such as polyoxyethylene alkyl Ether, polyoxyethylene alkenyl ether, polyoxyethylene hydrogenated castor oil, polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene fatty acid glyceryl, polyoxypropylene polyoxyethylene alkyl ether and polyoxypropylene polyoxyethylene alkenyl Examples thereof include ether.
　本発明の組成物にはアルコールを含み得る。アルコールとしては、エタノール、イソプロピルアルコールなどの１価アルコール、ポリエチレングリコール、グリセリン、１，３－ブチレングリコール、エリスリトール、ソルビトール、キシリトール、マルチトール、プロピレングリコール、ジプロピレングリコール、ジグリセリン、イソプレングリコール、１，２－ペンタンジオール、２，４－ヘキサンジオール、１，２－ヘキサンジオール、１，２－オクタンジオール等の多価アルコールが例示され、１種あるいは２種以上含み得る。特にグリセリン、プロピレングリコール、ポリエチレングリコール、１，３－ブチレングリコールが好適に例示される。該アルコールの総含有量は、５～６０重量％、好ましくは１０～５０重量％、より好ましくは１５～４０重量％である。 The composition of the present invention may include alcohol. Examples of alcohols include monohydric alcohols such as ethanol and isopropyl alcohol, polyethylene glycol, glycerin, 1,3-butylene glycol, erythritol, sorbitol, xylitol, maltitol, propylene glycol, dipropylene glycol, diglycerin, isoprene glycol, 1, Examples are polyhydric alcohols such as 2-pentanediol, 2,4-hexanediol, 1,2-hexanediol, and 1,2-octanediol, which may be contained alone or in combination of two or more. Glycerin, propylene glycol, polyethylene glycol and 1,3-butylene glycol are particularly preferred. The total content of the alcohol is 5 to 60% by weight, preferably 10 to 50% by weight, more preferably 15 to 40% by weight.
　本発明の組成物は、３～１２の範囲のｐＨ値を有することが好ましい。より好ましいｐＨ値は４～１０である。組成物を上記範囲のｐＨ値に調節するためのｐＨ調節剤としては、低ｐＨ領域に調節するために使用されるものとして、リン酸二水素カリウム、クエン酸などが挙げられ、高ｐＨ領域に調節するため使用されるものとして、水酸化ナトリウム、水酸化カリウム、乳酸ナトリウム、クエン酸ナトリウム、L-アルギニン、ジイソプロパノールアミンなどが挙げられる。特に好ましいｐＨ調節剤として、リン酸二水素カリウム、水酸化カリウム、クエン酸ナトリウム、クエン酸、ジイソプロパノールアミン、エデト酸ナトリウム等が挙げられる。 The composition of the present invention preferably has a pH value in the range of 3-12. A more preferable pH value is 4-10. As the pH adjuster for adjusting the pH value of the composition to the above range, those used for adjusting the low pH range include potassium dihydrogen phosphate, citric acid, etc., and in the high pH range. Those used for adjustment include sodium hydroxide, potassium hydroxide, sodium lactate, sodium citrate, L-arginine, diisopropanolamine and the like. Particularly preferred pH adjusters include potassium dihydrogen phosphate, potassium hydroxide, sodium citrate, citric acid, diisopropanolamine, sodium edetate and the like.
　本発明に係る液体組成物は、上記成分の他に、保存剤(防腐剤)、酸化防止剤、湿潤剤、安定化剤、紫外線吸収剤等、皮膚用外用剤に一般的に使用される添加剤を含むことができる。 The liquid composition according to the present invention, in addition to the above components, a preservative (preservative), an antioxidant, a wetting agent, a stabilizer, an ultraviolet absorber, etc., which are commonly used in external preparations for skin. Agents can be included.
　上記保存剤の例としては、パラオキシ安息香酸メチル、パラオキシ安息香酸エチル、パラオキシ安息香酸プロピル等のパラオキシ安息香酸エステル(パラベン類)、安息香酸ナトリウム、フェノキシエタノールなどが挙げられる。上記保存剤は、一種のみを用いてもよく、複数を併用してもよい。組成物における保存剤の含有量は、０．０１～１重量％の範囲とすることが好ましく、０．１～０．５重量％の範囲とすることがより好ましい。 Examples of the above preservative include methyl paraoxybenzoate, ethyl paraoxybenzoate, paraoxybenzoic acid esters (parabens) such as propyl paraoxybenzoate, sodium benzoate, and phenoxyethanol. The above preservatives may be used alone or in combination of two or more. The content of the preservative in the composition is preferably 0.01 to 1% by weight, more preferably 0.1 to 0.5% by weight.
　本発明の組成物は、医薬有効成分や化粧料として有効な成分を配合して医薬品や化粧品を製造するための基剤として提供されてもよく、また本発明の組成物は医薬有効成分を含んでいてもよい。医薬有効成分を含む組成物も本発明の態様の１つである。 The composition of the present invention may be provided as a base for producing a drug or cosmetic by incorporating a pharmaceutically active ingredient or an ingredient effective as a cosmetic, and the composition of the present invention contains the pharmaceutically active ingredient. You can leave. A composition containing a pharmaceutically active ingredient is also an aspect of the present invention.
　本発明の組成物は、皮膚に適用して供される外用剤として、皮膚の炎症、湿疹、アトピー性皮膚炎、乾癬、アクネ、瘢痕、褥瘡、ざ瘡などの治療（治癒、症状の改善、悪化の防止、発症の予防などを含む）などの皮膚疾患に好適に適用され、皮膚のみならず頭皮のような有毛部への適用にも適している。 The composition of the present invention is used as an external preparation applied to the skin to treat skin inflammation, eczema, atopic dermatitis, psoriasis, acne, scars, pressure ulcers, acne and the like (healing, improvement of symptoms, It is preferably applied to skin diseases such as prevention of deterioration and prevention of onset) and also to hair parts such as the scalp as well as the skin.
　本発明の組成物に配合される有効成分としては、皮膚に適用して供されるものであれば特段の限定はないが、ステロイド類、非ステロイド抗炎症剤、殺菌剤、抗菌剤、抗真菌剤、ビタミン類、免疫抑制剤、ムコ多糖類、ｃＡＭＰ誘導体、線維芽細胞成長因子、ナフトエ酸誘導体、過酸化ベンゾイルなどが例示される。前記ステロイド類としては、ステロイド骨格を有するものであれば特段の限定はないが、コルチゾン、ヒドロコルチゾン、酢酸フルドロコルチゾン、プレドニゾロン、メチルプレドニゾロン、デキサメタゾン、ベタメタゾン、クロベタゾールおよびその誘導体など、前記非ステロイド抗炎症剤としては、インドメタシン、スプロフェン、ケトチフェン、アラントイン、グリチルリチン酸ジカリウム、など、前記殺菌剤としては、グルコン酸クロルヘキシジン、塩化ベンザルコニウムなど、前記抗菌剤としては、テトラサイクリン塩酸塩、クロラムフェニコール、硫酸フラジオマイシン、ナジフロキサシン、クリンダマイシンリン酸エステル、オゼノキサシン、オキシテトラサイクリン塩酸塩、ポリミキシンＢ硫酸塩など、硫酸ゲンタマイシン、フジシン酸ナトリウムなど、前記抗真菌剤としては、テルビナフィン、ブテナフィン、ビフォナゾール、ケトコナゾールなど、前記ビタミン類としては、ビタミンＡ又はその誘導体（例えばビタミンＡ油など）、ビタミンＢ又はその誘導体（例えばパンテノールなど）、ビタミンＣ又はその誘導体、ビタミンＤ又はその誘導体（例えば活性型ビタミンＤ３など）、ビタミンＥ又はその誘導体（例えばトコフェロール酢酸エステルなど）、ビタミンＫ又はその誘導体など、前記免疫抑制剤としては、タクロリムス、シクロホスファミドなど、前記ムコ多糖類としては、へパリン類似物質あるいはヒアルロン酸およびその塩、ｃＡＭＰ誘導体としては、ブクラデシンナトリウムなど、線維芽細胞成長因子としてはトラフェルミンなど、ナフトエ酸誘導体としては、アダパレンなどが例示される。これらの含有量は、０．００１～１０重量％、好ましくは０．０１～１０重量％、より好ましくは０．０１～５重量％である。特に、へパリン類似物質あるいはヒアルロン酸およびその塩のようなムコ多糖類を含む外用組成物が好適に例示される。 The active ingredient contained in the composition of the present invention is not particularly limited as long as it is applied to the skin and provided, but steroids, nonsteroidal anti-inflammatory agents, bactericides, antibacterial agents, antifungals. Examples include agents, vitamins, immunosuppressants, mucopolysaccharides, cAMP derivatives, fibroblast growth factors, naphthoic acid derivatives, benzoyl peroxide and the like. The steroids are not particularly limited as long as they have a steroid skeleton, but include cortisone, hydrocortisone, fludrocortisone acetate, prednisolone, methylprednisolone, dexamethasone, betamethasone, clobetasol and its nonsteroidal anti-inflammatory. As the agent, indomethacin, suprofen, ketotifen, allantoin, dipotassium glycyrrhizinate, etc., the bactericide, chlorhexidine gluconate, benzalkonium chloride, etc., the antibacterial agent, tetracycline hydrochloride, chloramphenicol, sulfuric acid Fradiomycin, nadifloxacin, clindamycin phosphate, ozenoxacin, oxytetracycline hydrochloride, polymyxin B sulfate, etc., gentamicin sulfate, sodium fuzicinate, etc., and the antifungal agents include terbinafine, butenafine, bifonazole, ketoconazole, etc. Examples of vitamins include vitamin A or a derivative thereof (eg vitamin A oil), vitamin B or a derivative thereof (eg panthenol), vitamin C or a derivative thereof, vitamin D or a derivative thereof (eg active vitamin D3), Vitamin E or a derivative thereof (for example, tocopherol acetate), vitamin K or a derivative thereof, the immunosuppressive agent is tacrolimus, cyclophosphamide, and the like, and the mucopolysaccharide is a heparin-like substance or hyaluronic acid and Examples of the salt and cAMP derivative include bucladesine sodium, fibroblast growth factor such as trafermin, and naphthoic acid derivative such as adapalene. The content of these is 0.001 to 10% by weight, preferably 0.01 to 10% by weight, and more preferably 0.01 to 5% by weight. In particular, a topical composition containing a heparin-like substance or a mucopolysaccharide such as hyaluronic acid and a salt thereof is preferably exemplified.
　特に、ヘパリン類似物質を含む起泡性組成物は、ヘパリン類似物質が、血液凝固抑制作用、血流量増加作用、血腫消退促進作用、角質水分保持増強作用および線維芽細胞増殖抑制作用を有するため、乾燥性皮膚疾患、皮脂欠乏症、進行性指掌角皮症、凍瘡、肥厚性瘢痕・ケロイド、血行障害に基づく疼痛と炎症性疾患(注射後の硬結並びに疼痛)、血栓性静脈炎(痔核を含む)、外傷(打撲、捻挫、挫傷)後の腫脹・血腫・腱鞘炎・筋肉痛・関節炎、筋性斜頸等の治療用組成物としても適している。 In particular, the foamable composition containing a heparin-like substance, the heparin-like substance has a blood coagulation suppressing action, a blood flow increasing action, a hematoma regression promoting action, a keratin water retention enhancing action and a fibroblast proliferation inhibiting action, Dry skin disease, sebum deficiency, progressive palmar keratoderma, frostbite, hypertrophic scars/keloids, pain and inflammatory diseases due to blood circulation disorder (induration and pain after injection), thrombophlebitis (including hemorrhoids) ), swelling, hematoma, tendonitis, myalgia, arthritis, and muscular torticollis after trauma (bruises, sprains, and crushes) are also suitable as a therapeutic composition.
　以下に実験例を挙げて本願をさらに詳細に説明し、本願の効果を明らかにするが、これらは単なる例示であって、これらにより本願の範囲が限定されるものではない。 The following will explain the present application in more detail with reference to experimental examples and clarify the effects of the present application, but these are merely examples and the scope of the present application is not limited by these.
　実施例１
　下記処方に従って、調製した検体をポンプフォーマー容器に充填し、容器から吐出時の泡形成の有無を評価した（表１、図１）。
　尚、検体ＡからＩおよびＮが高分子界面活性剤である。 Example 1
A pump former container was filled with the prepared sample according to the following prescription, and the presence or absence of foam formation at the time of discharge from the container was evaluated (Table 1, FIG. 1).
The samples A to I and N are polymeric surfactants.
Figure JPOXMLDOC01-appb-T000001
Figure JPOXMLDOC01-appb-T000001
　本実施例にて用いた各検体の入手元を以下に示す。
Figure JPOXMLDOC01-appb-T000002
 The sources of each sample used in this example are shown below.
Figure JPOXMLDOC01-appb-T000002
　本発明の起泡性外用組成物に配合される高分子界面活性剤はそれぞれ単独で起泡剤として有効であることが分かった。 It was found that each of the polymer surfactants contained in the foamable external composition of the present invention is effective as a foaming agent alone.
　実施例２
　下記処方に従って、調製した検体をポンプフォーマー容器に充填して、泡形成の有無、泡質、泡の保持時間及び液だれの有無を測定した（表３および表４）。条件Ａでは、健常人の皮膚に近い材質としてポリウレタン素材のマットを用い、条件Ｂでは比較的重度の乾燥肌を想定したキムタオルを用いて、その上に吐出させた（図２および図３）。また、ポリウレタン素材のマットに吐出後、約４５℃に傾けて液だれするかどうか観察した（図４）。 Example 2
According to the following formulation, the prepared sample was filled in a pump former container, and the presence or absence of foam formation, foam quality, foam retention time, and the presence or absence of dripping were measured (Tables 3 and 4). In condition A, a mat of polyurethane material was used as a material close to the skin of a healthy person, and in condition B, a Kim towel that assumed relatively severe dry skin was used and discharged onto it (FIGS. 2 and 3). Also, after discharging onto a mat of polyurethane material, it was tilted at about 45° C. and observed whether or not there was dripping (FIG. 4).
Figure JPOXMLDOC01-appb-T000003
Figure JPOXMLDOC01-appb-T000003
Figure JPOXMLDOC01-appb-T000004
Figure JPOXMLDOC01-appb-T000004
　ヒプメロースは単体で良質で安定な泡を形成し、５分後も保持、３分後も液だれしなかった。この効果は、多価アルコールを組み合わせることでさらに改良された。一方、ポリオキシエチレン硬化ヒマシ油６０にポリオキシエチレンセチルエーテルやポリオキシエチレンラウリルエーテルを組み合わせたものは、泡を形成しないか、形成しても弾力が低く、保持時間が短く、液だれし、多価アルコールを組み合わせてもヒプロメロースを用いた製剤と比較して弾力や保持時間などで劣った。 Hypmelose alone formed a good and stable foam, retained after 5 minutes and did not drip after 3 minutes. This effect was further improved by combining the polyhydric alcohols. On the other hand, the combination of polyoxyethylene hydrogenated castor oil 60 with polyoxyethylene cetyl ether or polyoxyethylene lauryl ether does not form bubbles or has low elasticity even when formed, has a short holding time, and drips, Even when the polyhydric alcohol was combined, it was inferior in elasticity and retention time compared to the preparation using hypromellose.
　実施例３
　粘度の異なるヒプロメロースを使って、濃度による泡形成の有無を評価した。尚、泡質の評価基準は実施例１と同様である。 Example 3
Using hypromellose with different viscosities, the presence or absence of foam formation was evaluated depending on the concentration. The evaluation criteria of foam quality are the same as in Example 1.
Figure JPOXMLDOC01-appb-T000005
Figure JPOXMLDOC01-appb-T000005
　ヒプロメロースの粘度に関わらず、濃度０．２％以上で泡を形成した。 Bubbles were formed at a concentration of 0.2% or higher regardless of the viscosity of hypromellose.
　実施例４
　実施例２の表２の原料名２に示す処方に、ヘパリン類似物質を０．１あるいは０．３％の濃度で含む２種の組成物を作成し、ポンプフォーマー容器に充填して、泡形成の有無、泡の保持時間及び液だれの有無を測定した（表５）。
Example 4
Two compositions containing a heparin-like substance at a concentration of 0.1 or 0.3% were prepared in the formulation shown in the raw material name 2 in Table 2 of Example 2, filled in a pump former container, and foamed. The presence or absence of formation, the retention time of bubbles, and the presence or absence of dripping were measured (Table 5).
Figure JPOXMLDOC01-appb-T000006
Figure JPOXMLDOC01-appb-T000006
　表５に示す通り、本発明の組成物を使って、きめ、弾力ともに良好な泡質を有し、垂れ落ちのない適度に泡持ちするヘパリン類似物質含有医薬組成物が得られた。 As shown in Table 5, by using the composition of the present invention, a heparin-like substance-containing pharmaceutical composition having a good foam texture in terms of texture and elasticity and having a proper foaming property without sagging was obtained.

Claims (13)

  1. 　高分子界面活性剤を起泡成分として含む、使用時に泡を形成する外用組成物。 An external composition that contains a polymeric surfactant as a foaming component and forms bubbles during use.
  2. 　高分子界面活性剤がセルロース誘導体、ポリビニルアルコール、ポリビニルピロリドン、ポリエチレングリコール、ポリアクリル酸から選ばれる少なくとも一種である、請求項１に記載の組成物。 The composition according to claim 1, wherein the polymer surfactant is at least one selected from a cellulose derivative, polyvinyl alcohol, polyvinylpyrrolidone, polyethylene glycol, and polyacrylic acid.
  3. 　セルロース誘導体がヒドロキシプロピルメチルセルロース、ヒドロキシエチルセルロース、メチルセルロースから選ばれる少なくとも一種である、請求項２に記載の組成物。 The composition according to claim 2, wherein the cellulose derivative is at least one selected from hydroxypropylmethylcellulose, hydroxyethylcellulose, and methylcellulose.
  4. 　セルロース誘導体がヒドロキシプロピルメチルセルロースである、請求項３に記載の組成物。 The composition according to claim 3, wherein the cellulose derivative is hydroxypropylmethyl cellulose.
  5. 　さらに多価アルコールを含む、請求項１～４のいずれかに記載の組成物。 The composition according to any one of claims 1 to 4, further comprising a polyhydric alcohol.
  6. 　多価アルコールが１，３－ブチレングリコールである、請求項５記載の組成物。 The composition according to claim 5, wherein the polyhydric alcohol is 1,3-butylene glycol.
  7. 　組成物全量に対しヒドロキシプロピルメチルセルロースを０．２～３重量％、１，３－ブチレングリコールを１５～４０重量％含有する、請求項１～６のいずれかに記載の組成物。 The composition according to any one of claims 1 to 6, containing 0.2 to 3% by weight of hydroxypropylmethylcellulose and 15 to 40% by weight of 1,3-butylene glycol with respect to the total amount of the composition.
  8. 　医薬有効成分を少なくとも一種含む、請求項１～７のいずれかに記載の組成物。 The composition according to any one of claims 1 to 7, which contains at least one pharmaceutically active ingredient.
  9. 　医薬有効成分がムコ多糖類である請求項８に記載の組成物。 The composition according to claim 8, wherein the pharmaceutically active ingredient is mucopolysaccharide.
  10. 医薬有効成分の含有量が、組成物全量に対し０．０１～５重量％である、請求項８または９に記載の組成物。 The composition according to claim 8 or 9, wherein the content of the pharmaceutically active ingredient is 0.01 to 5% by weight based on the total amount of the composition.
  11. 　医薬有効成分としてヘパリン類似物質および／またはヒアルロン酸あるいはその塩を含む請求項１０に記載の組成物。 11. The composition according to claim 10, which contains a heparin-like substance and/or hyaluronic acid or a salt thereof as a pharmaceutically active ingredient.
  12. 　請求項１～１１のいずれかに記載の組成物をポンプフォーマー容器またはスクイズフォーマー容器に充填してなる、組成物。 A composition obtained by filling a pump former container or a squeeze former container with the composition according to any one of claims 1 to 11.
  13. 　皮膚疾患の治療のための請求項１～１２のいずれかに記載の組成物。 The composition according to any one of claims 1 to 12 for the treatment of skin diseases.
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WO2023127941A1 (en) * 2021-12-28 2023-07-06 株式会社 資生堂 Sunscreen cosmetic for pump foamer

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