Composition for external application

Abstract

To provide a composition for external application that contains a medicinal component and can form a coating layer with enhanced durability and moisture resistance.SOLUTION: A composition for external application contains the following components (A)-(D): (A) a medicinal component (B), water-insoluble polymers, (C) a nonvolatile base and (D) a volatile solvent. The component (B) includes two or more selected from the group consisting of (B1) a cellulosic polymer, (B2) an acrylic polymer, and (B3) a vinyl polymer. The composition for external application has a viscosity of 1.0 mPa s or more and 10,000 mPa s or less at 25°C.SELECTED DRAWING: None

Description

[Technical field]

[0001] The present invention relates to an external preparation composition. [Background technology]

[0002] Liquid skin topical preparations and patches containing medicinal ingredients such as anti-inflammatory and analgesic ingredients and bactericidal and disinfecting ingredients are known. However, existing liquid skin topical preparations are prone to rubbing off with clothes after application to the skin, making it difficult to continuously release medicinal ingredients to the skin. For patches containing medicinal ingredients, if they are difficult to follow the skin and are easily peeled off, it becomes difficult to continuously release the medicinal ingredients to the skin. On the other hand, patches that are highly adhesive to the skin also have the problem of putting a large burden on the skin when peeled off from the skin. In addition, patches also have practical problems such as being prone to rashes and being unsightly when applied to the skin.

[0003] Therefore, film-forming preparations capable of releasing active ingredients continuously to the skin have been studied. Film-forming preparations can form a film when applied to the skin, so they are less likely to rub off compared to liquid skin preparations. They are also preferred because they are not noticeable when applied to the skin like patches, and they are less stressful on the skin when removed from the skin.

[0004] For example, Patent Document 1 discloses that a film-forming composition for topical skin application containing a film-forming polymer including a cellulose-based polymer and a vinyl-based polymer, a polyhydric alcohol, and a volatile solvent forms a film that protects the affected area and adheres firmly to the skin while having high flexibility, providing an excellent feel when used without any discomfort, and is resistant to movement and rubbing and does not peel off easily, and also has excellent applicability. Patent Document 2 discloses that a film-forming aerosol composition containing a concentrate containing a film-forming agent and an organic solvent of a specified boiling point, and a propellant, in which the film-forming agent is an alkyl acrylate-vinyl acetate copolymer, can form a film on the skin that has excellent skin protection properties, is easy to remove after application, and is water-resistant to sweat, etc. [Prior art documents] [Patent documents]

[0005] [Patent Document 1] Patent Publication No. 2021-6522 [Patent Document 2] International Publication No. 2022 / 059618 Summary of the Invention [Problem to be solved by the invention]

[0006] As described above, Patent Document 1 describes the durability of the coating film formed, and Patent Document 2 describes the resistance of the film to sweat and the like. However, the durability and moisture resistance of the coating films formed by these conventional techniques are not sufficient for practical use, and there is room for further improvement. The present invention relates to a composition for external use which contains a medicinal ingredient and is capable of forming a coating film having excellent durability and moisture resistance. [Means for solving the problem]

[0007] The present inventors have found that the above-mentioned problems can be solved by an external preparation composition which contains a medicinal ingredient, two or more specified water-insoluble polymers, and a specified solvent component and has a specified viscosity. That is, the present invention relates to the following. [1] The following components (A) to (D): (A) Medicinal ingredients (B) Water-insoluble polymer (C) Non-volatile base (D) Volatile Solvents wherein component (B) comprises two or more selected from the group consisting of (B1) a cellulose-based polymer, (B2) an acrylic polymer, and (B3) a vinyl-based polymer, and the viscosity of the topical composition at 25°C is 1.0 mPa s or more and 10,000 mPa s or less. [2] A method for using the topical composition described in [1] above, comprising the following steps (I) and (II) in that order: Step (I): A step of applying the topical composition to an object and then drying the composition to form a coating made of the topical composition. Step (II): A step of contacting the coating with a cleaning agent and then rinsing with water to remove the coating. Effect of the Invention

[0008] According to the present invention, it is possible to provide an external preparation composition which contains a medicinal ingredient and is capable of forming a coating film which is excellent in both durability and moisture resistance, and a method for using the same. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0009] [External application composition] The present invention relates to the following components (A) to (D): (A) Medicinal ingredients (B) Water-insoluble polymer (C) Non-volatile base (D) Volatile Solvents The present invention relates to an external preparation composition comprising the above formula (I), wherein the component (B) comprises two or more selected from the group consisting of (B1) a cellulose-based polymer, (B2) an acrylic polymer, and (B3) a vinyl-based polymer, and wherein the viscosity of the external preparation composition at 25° C. is from 1.0 mPa s to 10,000 mPa s. Hereinafter, the composition may be appropriately referred to as the “composition of the present invention.”

[0010] <Definition> As used herein, the term "external preparation composition" refers to a composition that is primarily applied to the skin surface. In this specification, "containing X" includes those in which X is blended. As used herein, the term "water-insoluble polymer" refers to a polymer that has the property that, when 1 g of the polymer is immersed in 10 g of ion-exchanged water under an environment of 23°C and 1 atmospheric pressure, after 24 hours, more than 0.5 g of the immersed polymer does not dissolve. As used herein, a "non-volatile base" refers to a base that is liquid at 70°C and has a mass loss of less than 1% after 1 g of the base is spread on a glass petri dish with a diameter of 48 mm and left at 25°C and normal pressure for 24 hours. The term "volatile solvent" refers to a solvent that, when 1 g of the solvent is spread on a glass petri dish with a diameter of 48 mm and left at 25°C and normal pressure for 24 hours, exhibits a mass loss of 1% or more, is liquid at 25°C, and contains components other than water. In the present specification, when a coating is formed by applying a topical preparation composition to a target object (a subject's skin) and the coating is not easily rubbed off even when the subject performs daily activities, this is referred to as "high durability of the coating." Furthermore, when the coating is not easily twisted or peeled off even when rubbed under high temperature and high humidity, this is referred to as "high moisture resistance of the coating." The durability and moisture resistance of the coating can be specifically evaluated by the method described in the Examples.

[0011] The composition of the present invention contains component (A): a medicinal ingredient, component (B): a water-insoluble polymer, component (C): a non-volatile base, and component (D): a volatile solvent, but component (A) is a component not contained in any of the other components (B), (C), and (D), and component (B) is a component not contained in any of components (C) and (D).

[0012] The composition of the present invention, having the above-mentioned structure, is capable of forming a coating film which contains a medicinal component and is excellent in both durability and moisture resistance. Although the reason for this is not clear, it is thought to be as follows. The composition of the present invention is a film-forming composition that contains, as film-forming components, a water-insoluble polymer as component (B) and a non-volatile base as component (C). When the composition of the present invention is applied to the skin and then dried, component (D) volatilizes to form a film containing components (A) to (C). Since component (B) is water-insoluble and can form a highly hydrophobic coating, it is believed that the durability and moisture resistance of the coating are easily improved and that the stickiness of the coating is also suppressed. On the other hand, if only component (B) is used as a coating-forming component, there is a concern that the coating becomes brittle and its durability decreases. In the present invention, it is believed that these problems can be suppressed by using component (B) and component (C) in combination. Furthermore, it was found that when only one water-insoluble polymer is used as component (B), or when two or more water-insoluble polymers are used but only the same type of polymer is used, it is difficult to achieve not only the durability of the coating but also a high level of moisture resistance in which the coating is not easily distorted or peeled off even when rubbed under high temperature and high humidity.The present invention is believed to have solved the above problem by using two or more specific and different water-insoluble polymers as component (B).

[0013] Component (D) is believed to contribute to improving the quick-drying property of the topical composition and the effect of inhibiting crystallization of component (A). By inhibiting crystallization in the coating of component (A), the active ingredient component (A) can be effectively sustained-released to the target object. Furthermore, by containing component (D) in the topical composition, it becomes easier to adjust the viscosity to a predetermined range. As a result, it is believed that the application property and film-forming property of the topical composition are improved, and the durability and moisture resistance of the formed coating are also improved.

[0014] In addition, the coating formed by the composition of the present invention has little stickiness, is durable and resistant to moisture during use, and can be easily removed by washing with water and a detergent after use (hereinafter also referred to as "removability of the coating").

[0015] <Ingredient (A): Medicinal ingredient> The composition of the present invention contains a medicinal component as component (A). From the viewpoint of use in an external preparation composition, component (A) is preferably a skin external preparation component that can be administered transdermally. Specifically, component (A) is preferably one or more selected from the group consisting of anti-inflammatory and analgesic components, local stimulating components, blood circulation promoting components, antihistamine components, herbal ingredients, antipruritic components, local anesthetic components, keratin softening components, bactericidal components, antibacterial and antifungal components, immunosuppressants, antiviral components, hair growth and hair growth components, sebum suppressing components, antiperspirant components, and whitening components, and more preferably one or more selected from the group consisting of anti-inflammatory and analgesic components, antihistamine components, antipruritic components, bactericidal components, antibacterial and antifungal components, immunosuppressants, antiviral components, hair growth and hair growth components, sebum suppressing components, antiperspirant components, and whitening components.

[0016] Anti-inflammatory and analgesic ingredients include glycol salicylate, methyl salicylate, aspirin, sulpyrine hydrate, acetaminophen, diclofenac sodium, fenbufen, ibuprofen, aminoprofen, loxoprofen sodium hydrate, naproxen, oxaprofen, ketoprofen, tiaprofenic acid, sulindac, aluminum flufenamate, felbinac, mefenamic acid, indomethacin, indomethacin farnesyl, acemetacin, proglumetacin maleate, bendazac, piroxicam, ampiroxicam, and lorphenesin. Examples of such an active ingredient include xicam, tenoxicam, meloxicam, etodolac, tiaramide hydrochloride, bucolome, flurbiprofen, s-flurbiprofen, lysozyme hydrochloride, bromelain, diphenhydramine hydrochloride, dibucaine, dimethylisopropylazulene, benzethonium chloride, glycyrrhizinic acid, dipotassium glycyrrhizinate, zinc oxide, allantoin, heparinoids, glycyrrhetinic acid, ibuprofen piconol, fluocinolone acetonide, difluprednate, clobetasol propionate, and betamethasone valerate. Among these, one or more selected from the group consisting of glycol salicylate, methyl salicylate, diclofenac sodium, loxoprofen sodium hydrate, ketoprofen, indomethacin, piroxicam, flurbiprofen, es-flurbiprofen, glycyrrhizinic acid, dipotassium glycyrrhizinate, zinc oxide, allantoin, heparinoids, glycyrrhetinic acid, ibuprofen piconol, fluocinolone acetonide, difluprednate, clobetasol propionate, and betamethasone valerate are preferred.

[0017] Examples of the local stimulating component include l-menthol, dl-camphor, nonylic acid vanillylamide, ammonia, peppermint oil, etc. Among these, one or more selected from the group consisting of l-menthol, dl-camphor, and nonylic acid vanillylamide are preferred.

[0018] Examples of blood circulation promoting ingredients include benzyl nicotinate, sodium polyethylene sulfonate, tocopherol acetate, carpronium chloride hydrate, etc. Among these, one or more selected from the group consisting of tocopherol acetate and carpronium chloride hydrate are preferred.

[0019] Examples of the antihistamine component include diphenhydramine, diphenhydramine hydrochloride, diphenhydramine salicylate, chlorpheniramine maleate, etc. Among these, one or more selected from the group consisting of diphenhydramine, diphenhydramine hydrochloride, and chlorpheniramine maleate are preferred.

[0020] Examples of herbal medicine components include chili pepper, arnica tincture, eucalyptus oil, Phellodendron bark, arnica tincture, herb, peony, mugwort, cinnamon bark, cnidium rhizome, magnolia berry, sophora rhizome, star anise, chinese radish, carrot, tallow fruit, clove, ginger, Chinese shiso, licorice, fennel, scutellaria, scutellaria, magnolia, spruce, and inchi. Among these, at least one selected from the group consisting of chili pepper and arnica tincture is preferred.

[0021] Examples of the antipruritic ingredient include crotamiton, cortisone acetate, isothipendyl hydrochloride, benzalkonium chloride, calamine, d-borneol, aqueous ammonia, hydrocortisone, hydrocortisone acetate, hydrocortisone butyrate, dexamethasone, dexamethasone acetate, prednisolone, prednisolone acetate, prednisolone valerate acetate, ufenamate, etc. Among these, one or more selected from the group consisting of crotamiton, benzalkonium chloride, hydrocortisone, hydrocortisone acetate, hydrocortisone butyrate, dexamethasone, dexamethasone acetate, prednisolone, prednisolone valerate acetate, and ufenamate are preferred.

[0022] Examples of local anesthetic components include lidocaine, mepivacaine, bupivacaine, ropivacaine, levopivacaine, dibucaine, dibucaine hydrochloride, ethyl aminobenzoate, etc. Among these, one or more selected from the group consisting of lidocaine and dibucaine hydrochloride are preferred.

[0023] Examples of keratin softening ingredients include urea, sulfur, and salicylic acid.

[0024] Examples of the bactericidal component include chlorhexidine gluconate, copper chlorophyllin sodium, isopropylmethylphenol, cetylpyridinium chloride hydrate, benzethonium chloride, benzalkonium chloride, resorcinol, acrinol hydrate, chlorhexidine gluconate, homosulfamine, homosulfamine hydrochloride, povidone iodine, iodine / potassium iodide, mercurochrome, oxydol, cresol, iodoform, thymol, chlorhexidine hydrochloride, adapalene, trichlorocarbanilide, etc. Among these, one or more selected from the group consisting of isopropylmethylphenol, benzethonium chloride, resorcinol, homosulfamine, homosulfamine hydrochloride, chlorhexidine hydrochloride, adapalene, and trichlorocarbanilide are preferred.

[0025] Antibacterial and antifungal ingredients include undecylenic acid, zinc undecylenate, phenyl-11-iodo-10-undecynoate, exalamide, clotrimazole, econazole nitrate, miconazole nitrate, tioconazole, zinc diethyldithiocarbamate, ciclopirox olamine, siccanin, trichomycin, pyrrolnitrin, thianthol, 2,4,6-tribromophenylcaproic acid ester, trimethylcetylammonium pentane, Rolophenate, tolciclate, tolnaftate, haloprogin, Hibiscus bark, berberine benzoate, dequalinium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate solution, dequalinium acetate, hinokitiol, rebrucin, benzoic acid, chlorobutanol, acetic acid, phenol, tincture of iodine, diphenylpyraline hydrochloride, diphenhydramine salicylate, diphenylimidazole, chlorpheniramine maleate, dibucaine hydrochloride, proline hydrochloride Locaine, lidocaine hydrochloride, aldioxa, glycyrrhizic acid and its salts, Lithospermum Root, Angelica Root, Borneolum, diethyl phthalate, aluminum chlorhydrate, penicillins, cephalosporins, carbapenems, monobactams, penems, aminoglycosides, fosfomycins, chloramphenicols, macrolides, glycopeptides, quinolones, new quinolones, sulfa drugs, fradiomycin sulfate, gentamicin sulfate, penicillins, Examples of such antibacterial agents include tamidine isethionate, silver sulfadiazine, oxiconazole nitrate, sulconazole nitrate, bifonazole, neticonazole hydrochloride, lanoconazole, tenafine hydrochloride, amorolfine hydrochloride, terbinafine hydrochloride, butenafine hydrochloride, polymyxin B sulfate, colistin sulfate, bacitracin, fradiomycin sulfate, benzoyl peroxide, nadifloxan, levofloxan, clindamycin phosphate, etc. Among these, preferred are at least one selected from the group consisting of clotrimazole, miconazole nitrate, pyrrolnitrin, tolnaftate, hinokitiol, fradiomycin sulfate, oxiconazole nitrate, bifonazole, lanoconazole, terbinafine hydrochloride, and butenafine hydrochloride.

[0026] Immunosuppressants include tacrolimus and the like.

[0027] Antiviral components include acyclovir, vidarabine, and the like.

[0028] Hair growth and hair care ingredients include minoxidil, panthenol, pantothenyl ethyl ether, etc.

[0029] Sebum-suppressing ingredients include pyridoxine hydrochloride.

[0030] Antiperspirant ingredients include aluminum chloride, glycopyrronium tosylate hydrate, and sofpironium bromide.

[0031] Examples of whitening ingredients include tranexamic acid, tretinoin, and hydroquinone.

[0032] As the component (A), one or more of the above-mentioned medicinal components can be used. Among the above, component (A) is glycol salicylate, methyl salicylate, diclofenac sodium, loxoprofen sodium hydrate, ketoprofen, indomethacin, flurbiprofen, dipotassium glycyrrhizinate, zinc oxide, allantoin, heparinoids, glycyrrhetinic acid, ibuprofen piconol, fluocinolone acetonide, l-menthol, dl-camphor, vanillylamide nonylate, tocopherol acetate, carpronium chloride hydrate, diphenhydramine, diphenhydramine hydrochloride, chlorpheniramine maleate, capsicum, crotamiton, benzalkonium chloride, hydrocortisone, hydrocortisone butyrate, dexamethasone acetate, prednisolone valerate acetate, betamethasone valerate sulphate. More preferably, the active ingredient contains one or more selected from the group consisting of tert-butyl ether, ufenamate, lidocaine, dibucaine hydrochloride, urea, sulfur, salicylic acid, isopropylmethylphenol, benzethonium chloride, resorcinol, homosulfamine, homosulfamine hydrochloride, chlorhexidine hydrochloride, trichlorocarbanilide, clotrimazole, miconazole nitrate, tolnaftate, hinokitiol, oxiconazole nitrate, bifonazole, lanoconazole, terbinafine hydrochloride, butenafine hydrochloride, tacrolimus, acyclovir, vidarabine, minoxidil, panthenol, pantothenyl ethyl ether, pyridoxine hydrochloride, tranexamic acid, tretinoin, homosulfamine hydrochloride, aluminum chloride, glycopyrronium tosylate hydrate, and sofpironium bromide.

[0033] <Component (B): Water-insoluble polymer> The composition of the present invention contains a water-insoluble polymer as component (B). Component (B) is a film-forming component, and is considered to improve the film-forming properties of the composition and enable the formation of a film with high durability and moisture resistance. Furthermore, even when a highly crystalline component (A) is used, crystallization in the film of component (A) can be suppressed, and the film formed is less sticky and can be easily removed by washing with water using a detergent.

[0034] From the viewpoint of improving the film-forming property, it is preferable that component (B) is a film-forming water-insoluble polymer. The definition of "water-insoluble" for component (B) is as described above.

[0035] The component (B) contains two or more members selected from the group consisting of (B1) a cellulose-based polymer, (B2) an acrylic-based polymer, and (B3) a vinyl-based polymer. In this specification, "component (B) contains two or more members selected from the group consisting of (B1) a cellulose-based polymer, (B2) an acrylic polymer, and (B3) a vinyl-based polymer" specifically means any one of the following embodiments (i) to (iv). (i) Component (B) contains components (B1) and (B2) but does not contain component (B3) (ii) Component (B) contains components (B1) and (B3) but does not contain component (B2). (iii) Component (B) contains components (B2) and (B3) but does not contain component (B1). (iv) Component (B) contains components (B1), (B2), and (B3). Therefore, for example, a case where component (B) contains two or more types of component (B1) but does not contain either component (B2) or component (B3) is not included in the scope of the present invention. Of the above embodiments, from the viewpoints of improving the durability and moisture resistance of the coating, improving the crystallization suppression effect of component (A), and suppressing stickiness of the coating, embodiment (i) or (iv) is preferred, and embodiment (i) is more preferred.

[0036] (Component (B1): Cellulosic polymer) The cellulose-based polymer used as component (B1) includes water-insoluble polymers having a cellulose skeleton. Specific examples of component (B1) include water-insoluble ones among methylcellulose, ethylcellulose, hypromellose, carboxymethylcellulose, carboxymethylethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hypromellose phthalate, hydrophobized (C16-18) hydroxypropylmethylcellulose, hypromellose acetate succinate, phthalcellulose acetate, etc., and one or more of these may be used.

[0037] From the viewpoints of improving the durability and moisture resistance of the coating, improving the crystallization inhibitory effect of component (A), and suppressing stickiness of the coating, component (B1) is preferably one or more selected from the group consisting of ethyl cellulose, hypromellose phthalate, and hydrophobized (C16-18) hydroxypropyl methylcellulose, and more preferably hypromellose phthalate.

[0038] Commercially available products can also be used as component (B1). For example, ethyl cellulose used as component (B1) includes "Ethocel 100P" manufactured by Nisshin Chemical Industry Co., Ltd., and hypromellose phthalate ester includes "HPMCP HP-55", "HPMCP HP-55S", and "HPMCP HP-50" manufactured by Shin-Etsu Chemical Co., Ltd.

[0039] (Component (B2): Acrylic polymer) The acrylic polymer used as component (B2) may be a water-insoluble polymer that contains at least a structural unit derived from a monomer having a (meth)acrylic group. In this specification, "(meth)acrylic" refers to both acrylic and methacrylic. Specific examples of component (B2) include water-insoluble copolymers such as acrylates / diacetoneacrylamide copolymers, acrylamide-methoxypolyethylene glycol methacrylate copolymers, alkyl acrylate copolymers, acrylic ester-vinyl acetate copolymers, 2-ethylhexyl acrylate-methyl acrylate-acrylic acid-glycidyl methacrylate copolymers, 2-ethylhexyl acrylate-vinyl acetate-hydroxyethyl acrylate-glycidyl methacrylate copolymers, 2-ethylhexyl acrylate-diacetoneacrylamide-acetoacetoxyethyl methacrylate-methyl methacrylate copolymers, 2-ethylhexyl acrylate-vinylpyrrolidone copolymers, 2-ethylhexyl acrylate-2-ethylhexyl methacrylate-dodecyl methacrylate copolymers, ethyl acrylate-methyl methacrylate copolymers, ethyl acrylate-methyl methacrylate-trimethylammonium ethyl methacrylate chloride copolymers, and methyl methacrylate-butyl methacrylate-dimethylaminoethyl methacrylate copolymers. One or more of these copolymers may be used.

[0040] Of the above, for the (acrylates / diacetone acrylamide) copolymer, use the cosmetic ingredient label name "(alkyl acrylate / diacetone acrylamide) copolymer AMP." For the acrylamide-methoxy polyethylene glycol methacrylate copolymer, use "acrylic acid amide-methoxy polyethylene glycol methacrylate copolymer liquid" as specified in the Pharmaceutical Excipients Standards 2018 (Pharmaceutical and Food Safety Bureau, Ministry of Health, Labour and Welfare). For the alkyl acrylate copolymer, use the cosmetic ingredient label name "alkyl acrylate copolymer ammonium." For the 2-ethylhexyl acrylate-vinylpyrrolidone copolymer, use the cosmetic ingredient label name "alkyl acrylate copolymer ammonium." As the 2-ethylhexyl acrylate-2-ethylhexyl methacrylate-dodecyl methacrylate copolymer, "2-ethylhexyl acrylate-2-ethylhexyl methacrylate-dodecyl methacrylate copolymer solution" described in the Pharmaceutical and Food Safety Bureau, Pharmaceutical and Food Safety Bureau, Ministry of Labor and Welfare can be used; as the 2-ethylhexyl acrylate-2-ethylhexyl methacrylate-dodecyl methacrylate copolymer, "2-ethylhexyl acrylate-2-ethylhexyl methacrylate-dodecyl methacrylate copolymer solution" can be used; as the ethyl acrylate-methyl methacrylate copolymer, "ethyl acrylate-methyl methacrylate copolymer dispersion" can be used; and as the methyl methacrylate-butyl methacrylate-dimethylaminoethyl methacrylate copolymer, "Aminoalkyl methacrylate copolymer E" can be used. As the ethyl acrylate-methyl methacrylate-trimethylammonium ethyl methacrylate chloride copolymer, "aminoalkyl methacrylate copolymer RS," known as a pharmaceutical additive, can be used.

[0041] From the viewpoints of improving the durability and moisture resistance of the coating, improving the crystallization suppression effect of component (A), and suppressing stickiness of the coating, component (B2) is more preferably an acrylates / diacetoneacrylamide copolymer.

[0042] Commercially available products can also be used as component (B2). For example, an acrylates / diacetone acrylamide copolymer used as component (B2) is “Pluscise L-53” manufactured by GOO Chemical Industry Co., Ltd., an alkyl acrylate / vinyl acetate copolymer is “Vinisole 2140L” manufactured by Daido Chemical Industry Co., Ltd., and an alkyl acrylate copolymer is “Vinisole 1086WP” manufactured by Daido Chemical Industry Co., Ltd.

[0043] (Component (B3): vinyl polymer) The vinyl polymer used as component (B3) is a water-insoluble polymer that contains at least a structural unit derived from a monomer having a vinyl group and does not belong to the above-mentioned acrylic polymers. Examples of the vinyl polymer include water-insoluble ones among polyvinyl alcohol, polyvinyl acetate, polyvinyl butyral, etc. From the viewpoints of improving the durability and moisture resistance of the coating, improving the crystallization suppression effect of component (A), and suppressing stickiness of the coating, polyvinyl butyral is preferred as component (B3).

[0044] As component (B3), commercially available products can also be used. For example, the polyvinyl butyral used as component (B3) is the “S-LEC B·K” series manufactured by Sekisui Chemical Co., Ltd.

[0045] (i) In the case where component (B) contains components (B1) and (B2) but does not contain component (B3), component (B1) is preferably one or more selected from the group consisting of ethyl cellulose, hypromellose phthalate, and hydrophobized (C16-18) hydroxypropyl methylcellulose, more preferably hypromellose phthalate, and component (B2) is preferably an acrylates / diacetoneacrylamide copolymer. (ii) In the case where component (B) contains components (B1) and (B3) but does not contain component (B2), component (B1) is preferably hypromellose phthalate, and component (B3) is preferably polyvinyl butyral. (iii) In the case where component (B) contains components (B2) and (B3) but does not contain component (B1), component (B2) is preferably an acrylates / diacetone acrylamide copolymer, and component (B3) is preferably polyvinyl butyral. (iv) In the case where component (B) contains components (B1), (B2), and (B3), component (B1) is preferably hypromellose phthalate, component (B2) is preferably an acrylates / diacetoneacrylamide copolymer, and component (B3) is preferably polyvinyl butyral.

[0046] When component (B) contains component (B1) and component (B2), the mass ratio of component (B2) to component (B1) [(B2) / (B1)] is, from the viewpoint of improving the durability and moisture resistance of the coating, preferably 0.05 or more, more preferably 0.1 or more, even more preferably 0.2 or more, still more preferably 0.5 or more, and still more preferably 1.0 or more; and from the viewpoint of improving the durability and moisture resistance of the coating and preventing the coating from becoming sticky, it is preferably 30 or less, more preferably 20 or less, even more preferably 15 or less, still more preferably 12 or less, and still more preferably 10 or less.

[0047] When component (B) contains component (B1) and component (B3), the mass ratio of component (B3) to component (B1) [(B3) / (B1)] is, from the viewpoint of improving the durability and moisture resistance of the coating, preferably 0.1 or more, more preferably 0.2 or more, even more preferably 0.5 or more, still more preferably 1.0 or more, and still more preferably 2.0 or more; and from the viewpoint of improving the durability and moisture resistance of the coating and preventing the coating from becoming sticky, it is preferably 20 or less, more preferably 15 or less, even more preferably 12 or less, still more preferably 10 or less, and still more preferably 8 or less.

[0048] When component (B) contains component (B2) and component (B3), the mass ratio of component (B2) to component (B3) [(B2) / (B3)] is, from the viewpoint of improving the durability and moisture resistance of the coating, preferably 0.05 or more, more preferably 0.1 or more, even more preferably 0.2 or more, still more preferably 0.5 or more, and still more preferably 1.0 or more; and from the viewpoint of improving the durability and moisture resistance of the coating and preventing the coating from becoming sticky, it is preferably 30 or less, more preferably 20 or less, even more preferably 15 or less, still more preferably 12 or less, and still more preferably 10 or less.

[0049] Component (B) may contain water-insoluble polymers other than components (B1), (B2), and (B3) within the scope of the present invention. However, from the viewpoint of improving the durability and moisture resistance of the coating, improving the crystallization suppression effect of component (A), and suppressing the stickiness of the coating, the total content of components (B1), (B2), and (B3) in component (B) is preferably 50% by mass or more, more preferably 60% by mass or more, even more preferably 70% by mass or more, still more preferably 80% by mass or more, and even more preferably 90% by mass or more, and 100% by mass or less.

[0050] <Component (C): Non-volatile base> The composition of the present invention contains a non-volatile base as component (C) (excluding those corresponding to component (A)). It is believed that component (C), when used in combination with component (B), contributes to improving the durability and moisture resistance of the coating film, as well as to improving the crystallization suppression effect of component (A). The "non-volatile base" of component (C) is as defined above.

[0051] Examples of the component (C) include lipophilic bases, hydrophilic bases, and amphiphilic bases, and one or more of these can be used.

[0052] (Lipophilic base) The lipophilic base preferably includes polar oils, non-polar oils, and the like. Specific examples of polar oils include non-volatile synthetic ester oils, and more preferably at least one selected from the group consisting of (i) fatty acid monoesters composed of fatty acids and monohydric alcohols, (ii) fatty acid monoesters or diesters composed of fatty acids and dihydric alcohols, (iii) dicarboxylic acid diesters composed of dicarboxylic acids and monohydric alcohols, (iv) tricarboxylic acid triesters composed of tricarboxylic acids and monohydric alcohols, and (v) glycerin fatty acid triesters.

[0053] (i) Examples of fatty acid monoesters composed of fatty acids and monohydric alcohols include monoesters of saturated fatty acids having 8 to 22 carbon atoms and aliphatic or aromatic ring-containing monohydric alcohols having 1 to 24 carbon atoms, such as cetyl octanoate, cetyl 2-ethylhexanoate, ethyl laurate, hexyl laurate, isopropyl myristate, myristyl myristate, hexadecyl myristate, 2-hexyldecyl myristate, octyldodecyl myristate, isopropyl palmitate, ethylhexyl palmitate, hexadecyl palmitate, 2-hexyldecyl palmitate, 2-heptylundecyl palmitate, butyl stearate, 2-ethylhexyl stearate, isocetyl stearate, isocetyl isostearate, isononyl isononanoate, isotridecyl isononanoate, and hexyldecyl dimethyloctanoate.

[0054] (ii) Examples of fatty acid monoesters or diesters composed of fatty acids and dihydric alcohols include monoesters or diesters of saturated fatty acids having from 8 to 22 carbon atoms and aliphatic or aromatic dihydric alcohols having from 1 to 12 carbon atoms, such as propylene glycol monocaprate, ethylene glycol di-2-ethylhexanoate, ethylene glycol dilaurate, ethylene glycol distearate, neopentyl glycol dicaprate, neopentyl glycol diethylhexanoate, propanediol di(caprylic / capric acid), and propanediol diisostearate.

[0055] (iii) Examples of dicarboxylate diesters composed of dicarboxylic acids and monohydric alcohols include diesters of aliphatic or aromatic dicarboxylic acids having 4 to 18 carbon atoms and aliphatic or aromatic ring-containing monohydric alcohols having 1 to 24 carbon atoms, such as 2-ethylhexyl succinate, diisopropyl adipate, dibutyl adipate, diisobutyl adipate, 2-hexyldecyl adipate, di-2-heptylundecyl adipate, diethyl sebacate, diisopropyl sebacate, di-2-ethylhexyl sebacate, diisononyl phthalate, and diisostearyl malate.

[0056] (iv) Examples of tricarboxylic acid triesters composed of tricarboxylic acids and monohydric alcohols include triesters of aliphatic or aromatic tricarboxylic acids having from 5 to 12 carbon atoms and aliphatic or aromatic ring-containing monohydric alcohols having from 1 to 24 carbon atoms, such as triisodecyl trimellitate.

[0057] Furthermore, (v) examples of glycerin fatty acid triesters include triesters of glycerin and saturated fatty acids having 8 to 22 carbon atoms, such as glycerin tri-2-ethylhexanoate, glycerin trimyristate, glycerin tri-2-heptylundecanoate, and tristearin.

[0058] As ester oils other than the above (i) to (v), alkyl benzoate, cetyl lactate, myristyl lactate, lanolin acetate, dipentaerythritol fatty acid esters, di-2-heptylundecanoic acid glycerin, castor oil fatty acid methyl esters, N-lauroyl-L-glutamic acid-2-octyldodecyl, and the like can also be used.

[0059] Among the above, the ester oil is more preferably one or more selected from the group consisting of (i) fatty acid monoesters composed of fatty acids and monohydric alcohols, and (ii) fatty acid monoesters or diesters composed of fatty acids and dihydric alcohols, even more preferably one or more selected from the group consisting of fatty acid monoesters composed of fatty acids and monohydric alcohols having 1 to 24 carbon atoms, and monoesters or diesters of saturated fatty acids having 8 to 22 carbon atoms and aliphatic or aromatic dihydric alcohols having 1 to 12 carbon atoms, and even more preferably one or more selected from the group consisting of isopropyl myristate and propylene glycol monocaprate.

[0060] Specific examples of non-polar oils include non-volatile hydrocarbon oils, silicone oils, fluorine oils, etc. Examples of the hydrocarbon oils include liquid paraffin, squalane, etc. Examples of the silicone oils include dimethylpolysiloxane, dimethylcyclopolysiloxane, methylphenylpolysiloxane, methylhydrogenpolysiloxane, higher alcohol-modified organopolysiloxane, etc. Examples of the fluorine oils include fluoropolyether, perfluoroalkyl ether silicone, etc.

[0061] (Hydrophilic base) The hydrophilic base is preferably at least one selected from the group consisting of polyols and lower amines. Specific examples of polyols include non-volatile alkylene glycols, polyalkylene glycols, glycerins, etc. Examples of the alkylene glycols include ethylene glycol, propylene glycol, 1,3-propanediol, 1,3-butylene glycol (1,3-butanediol), 1,2-pentanediol, etc. Examples of the polyalkylene glycols include diethylene glycol, dipropylene glycol, polyethylene glycol, polypropylene glycol, polyoxyethylene-polyoxypropylene glycol, etc. Examples of the glycerins include glycerin, diglycerin, triglycerin, etc. It is preferable that the polyethylene glycol, polypropylene glycol, and polyoxyethylene-polyoxypropylene glycol have a weight average molecular weight of less than 10,000.

[0062] In this specification, the term "lower amine" refers preferably to an amine having 9 or less carbon atoms, more preferably having from 2 to 9 carbon atoms. The lower amine is preferably an alkanolamine from the viewpoints of non-volatility, improving the durability and moisture resistance of the coating, improving the crystallization inhibitory effect of component (A), and suppressing stickiness of the coating. Specific examples of alkanolamines include triethanolamine, diethanolamine, monoethanolamine, triisopropanolamine, diisopropanolamine, monoisopropanolamine, and 2-amino-2-methylpropanol.

[0063] (Amphiphilic base) The amphiphilic base preferably includes an ionic or nonionic surfactant, with nonionic surfactants being preferred. Specific examples of nonionic surfactants include polyoxyethylene alkyl ethers, polyoxyethylene alkenyl ethers, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene sorbit fatty acid esters, polyoxyethylene fatty acid esters, alkyl glucosides, alkyl glyceryl ethers, fatty acid sucrose esters, polyoxyethylene hydrogenated castor oil, alkyl saccharides, alkylamine oxides, and alkylamidoamine oxides. The alkyl group in the polyoxyethylene alkyl ether, alkyl glucoside, alkyl glyceryl ether, alkyl saccharide, alkyl amine oxide, and alkyl amidoamine oxide, the alkenyl group in the polyoxyethylene alkenyl ether, and the fatty acid in the polyoxyethylene sorbitan fatty acid ester, polyoxyethylene fatty acid ester, and fatty acid sucrose ester preferably have 8 or more and 22 or less carbon atoms, more preferably 10 or more and 20 or less carbon atoms, and even more preferably 12 or more and 18 or less carbon atoms.

[0064] Among the above, the nonionic surfactant is preferably one or more selected from the group consisting of polyoxyethylene sorbitan fatty acid esters, polyoxyethylene sorbit fatty acid esters, polyoxyethylene fatty acid esters, alkyl glucosides, and alkyl glyceryl ethers, and more preferably polyoxyethylene sorbitan fatty acid esters. Specific examples of polyoxyethylene sorbitan fatty acid esters include polyoxyethylene sorbitan monolaurate (20 E.O.) (polysorbate 20), polyoxyethylene sorbitan monostearate (20 E.O.) (polysorbate 60), polyoxyethylene sorbitan tristearate (20 E.O.) (polysorbate 65), polyoxyethylene sorbitan oleate (20 E.O.) (polysorbate 80), and the like, with polyoxyethylene sorbitan oleate (20 E.O.) (polysorbate 80) being preferred.

[0065] The component (C) can be used alone or in combination of two or more. Among the above, component (C) is preferably one or more selected from the group consisting of polar oils, non-polar oils, polyols, alkanolamines, and nonionic surfactants, more preferably one or more selected from the group consisting of isopropyl myristate, propylene glycol monocaprate, squalane, 1,3-butylene glycol, dipropylene glycol, polyethylene glycols having a weight average molecular weight of less than 1,000, triethanolamine, diisopropanolamine, 2-amino-2-methylpropanol, and polyoxyethylene sorbitan fatty acid esters, and even more preferably one or more selected from the group consisting of isopropyl myristate, 1,3-butylene glycol, diisopropanolamine, 2-amino-2-methylpropanol, and polyoxyethylene sorbitan fatty acid esters.

[0066] The amine as component (C) also includes amines that form neutralized salts of the water-insoluble polymer as component (B). For example, in the composition of the present invention, a commercially available product containing component (B) and the alkanolamine component (C) may be “Plussize L-53P” manufactured by GOO Chemical Industry Co., Ltd., which contains a partial neutralization product of an (acrylates / diacetoneacrylamide) copolymer with 2-amino-2-methylpropanol.

[0067] <Component (D): Volatile solvent> The composition of the present invention contains a volatile solvent as component (D) (excluding those corresponding to component (A)). Component (D) contributes to improving the quick-drying property of the composition and the crystallization-inhibiting effect of component (A). Furthermore, it is believed that by making it easier to adjust the viscosity of the topical composition to a predetermined range, the application property and film-forming property are improved, and the durability and moisture resistance of the formed film are also further improved. The "volatile solvent" of component (D) is as defined above.

[0068] Examples of the component (D) include volatile alcohols, ketones, esters, hydrocarbons, silicones, and the like. The alcohol used as component (D) is preferably a lower alcohol. The "lower alcohol" is preferably an alcohol having 4 or less carbon atoms, such as methanol, ethanol, n-propyl alcohol, isopropyl alcohol, n-butyl alcohol, isobutyl alcohol, sec-butyl alcohol, and tert-butyl alcohol. Examples of ketones used as component (D) include acetone, ethyl methyl ketone, methyl isobutyl ketone, etc.; examples of esters include methyl acetate, ethyl acetate, butyl acetate, etc.; examples of hydrocarbons include volatile liquid paraffin, etc.; and examples of silicones include linear polydimethylsiloxanes, cyclic siloxanes, etc.

[0069] The component (D) can be used alone or in combination of two or more. From the viewpoints of improving the coatability and quick-drying property of the composition, the solubility or dispersibility of components (A) to (C), and the crystallization-inhibiting effect of component (A), component (D) is preferably an alcohol having 4 or less carbon atoms, and more preferably one or more selected from the group consisting of ethanol and isopropyl alcohol.

[0070] <Water> The topical composition preferably further contains water from the viewpoint of improving the crystallization suppression effect of component (A) and improving the removability of the coating. The water used in the present invention is not particularly limited, and for example, ion-exchanged water, pure water, distilled water, etc. can be used.

[0071] <Water-soluble polymer> The topical composition may further contain a water-soluble polymer within the range not impairing the effects of the present invention. The water-soluble polymer is a water-soluble polymer that does not fall under any of the above components (A) to (D), and examples thereof include carboxyvinyl polymer, polyacrylic acid, polyvinylpyrrolidone, etc. However, from the viewpoint of improving the durability and moisture resistance of the coating, and from the viewpoint of suppressing the stickiness of the coating, the mass ratio of the water-soluble polymer to the component (B) [water-soluble polymer / component (B)] is preferably low. Specifically, the mass ratio of the water-soluble polymer to the component (B) in the topical preparation composition [water-soluble polymer / component (B)] is preferably 2 or less, more preferably 1.5 or less, even more preferably 1.3 or less, even more preferably 1 or less, even more preferably 0.5 or less, even more preferably 0.1 or less, and even more preferably 0.

[0072] <Other ingredients> In addition to the above-mentioned components, the topical composition of the present invention may appropriately contain other components that are usually blended in topical compositions, so long as the purpose of the present invention is not impaired. Examples of such components include organic or inorganic acids, antioxidants, ultraviolet absorbers, preservatives, pH adjusters other than organic or inorganic acids, fragrances, pigments, etc.

[0073] <Content> The content of each component in the topical composition is preferably as follows, from the viewpoints of improving the durability and moisture resistance of the coating, improving the crystallization inhibitory effect of component (A), and suppressing stickiness of the coating.

[0074] The content of component (A) in the topical preparation composition is, from the viewpoint of fully expressing the efficacy of component (A), preferably 0.001% by mass or more, more preferably 0.005% by mass or more, even more preferably 0.01% by mass or more, and even more preferably 0.02% by mass or more, and, from the viewpoint of improving the crystallization inhibitory effect of component (A), preferably 30% by mass or less, more preferably 20% by mass or less, even more preferably 15% by mass or less, and even more preferably 10% by mass or less.

[0075] When component (A) contains an anti-inflammatory and analgesic component, the content of the anti-inflammatory and analgesic component in the topical preparation composition is preferably 0.01% by mass or more and 30% by mass or less, more preferably 0.02% by mass or more and 20% by mass or less, even more preferably 0.05% by mass or more and 15% by mass or less, still more preferably 0.05% by mass or more and 10% by mass or less, and even more preferably 0.05% by mass or more and 6.0% by mass or less.

[0076] When component (A) contains a local irritating component, the content of the local irritating component in the topical composition is preferably 0.001% by mass or more and 20% by mass or less, more preferably 0.005% by mass or more and 15% by mass or less, even more preferably 0.01% by mass or more and 10% by mass or less, and even more preferably 0.01% by mass or more and 6.0% by mass or less.

[0077] When component (A) contains a blood circulation-promoting component, the content of the blood circulation-promoting component in the topical composition is preferably 0.1% by mass or more and 30% by mass or less, more preferably 0.5% by mass or more and 20% by mass or less, even more preferably 1.0% by mass or more and 15% by mass or less, and even more preferably 1.0% by mass or more and 5.0% by mass or less.

[0078] When component (A) contains an antihistamine component, the content of the antihistamine component in the topical composition is preferably 0.01% by mass or more and 30% by mass or less, more preferably 0.02% by mass or more and 20% by mass or less, even more preferably 0.05% by mass or more and 15% by mass or less, even more preferably 0.05% by mass or more and 10% by mass or less, even more preferably 0.1% by mass or more and 5.0% by mass or less, and even more preferably 0.1% by mass or more and 3.0% by mass or less.

[0079] When component (A) contains a herbal ingredient, the content of the herbal ingredient in the topical composition is preferably 0.01% by mass or more and 30% by mass or less, more preferably 0.02% by mass or more and 20% by mass or less, even more preferably 0.05% by mass or more and 15% by mass or less, even more preferably 0.05% by mass or more and 10% by mass or less, even more preferably 0.1% by mass or more and 5.0% by mass or less, and even more preferably 0.1% by mass or more and 3.0% by mass or less.

[0080] When component (A) contains an antipruritic component, the content of the antipruritic component in the topical preparation composition is preferably 0.01% by mass or more and 30% by mass or less, more preferably 0.02% by mass or more and 20% by mass or less, even more preferably 0.02% by mass or more and 15% by mass or less, and even more preferably 0.02% by mass or more and 10% by mass or less.

[0081] When component (A) contains a local anesthetic component, the content of the local anesthetic component in the topical composition is preferably 0.01% by mass or more and 30% by mass or less, more preferably 0.02% by mass or more and 20% by mass or less, even more preferably 0.02% by mass or more and 15% by mass or less, even more preferably 0.02% by mass or more and 10% by mass or less, and even more preferably 0.02% by mass or more and 5.0% by mass or less.

[0082] When component (A) contains a keratin softening component, the content of the keratin softening component in the topical composition is preferably 0.1% by mass or more and 30% by mass or less, more preferably 0.2% by mass or more and 20% by mass or less, and even more preferably 0.5% by mass or more and 20% by mass or less.

[0083] When component (A) contains a bactericidal component, the content of the bactericidal component in the topical composition is preferably 0.001% by mass or more and 20% by mass or less, more preferably 0.005% by mass or more and 15% by mass or less, even more preferably 0.01% by mass or more and 10% by mass or less, still more preferably 0.01% by mass or more and 5.0% by mass or less, and even more preferably 0.01% by mass or more and 3.0% by mass or less.

[0084] When component (A) contains an antibacterial and / or antifungal component, the content of the antibacterial and / or antifungal component in the topical composition is preferably from 0.001% to 20% by mass, more preferably from 0.005% to 15% by mass, even more preferably from 0.01% to 10% by mass, still more preferably from 0.02% to 5.0% by mass, and even more preferably from 0.05% to 3.0% by mass.

[0085] When component (A) contains an immunosuppressant, the content of the immunosuppressant in the topical preparation composition is preferably from 0.01% by mass to 1% by mass, more preferably from 0.03% by mass to 0.5% by mass.

[0086] When component (A) contains an antiviral component, the content of the antiviral component in the topical preparation composition is preferably 0.1 mass% or more and 20 mass% or less, more preferably 0.5 mass% or more and 15 mass% or less, even more preferably 1.0 mass% or more and 10 mass% or less, and still more preferably 1.0 mass% or more and 5.0 mass% or less.

[0087] When component (A) contains a hair growth / hair care ingredient, the content of the hair growth / hair care ingredient in the topical composition is preferably 0.1% by mass or more and 20% by mass or less, more preferably 0.5% by mass or more and 15% by mass or less, even more preferably 1.0% by mass or more and 10% by mass or less, and even more preferably 1.0% by mass or more and 5.0% by mass or less.

[0088] When component (A) contains a sebum-suppressing component, the content of the sebum-suppressing component in the topical composition is preferably 0.001% by mass or more and 20% by mass or less, more preferably 0.005% by mass or more and 15% by mass or less, even more preferably 0.01% by mass or more and 10% by mass or less, even more preferably 0.01% by mass or more and 5.0% by mass or less, and even more preferably 0.01% by mass or more and 3.0% by mass or less.

[0089] When component (A) contains an antiperspirant component, the content of the antiperspirant component in the topical preparation composition is preferably 0.1% by mass or more and 20% by mass or less, more preferably 0.5% by mass or more and 15% by mass or less, even more preferably 1.0% by mass or more and 10% by mass or less, and still more preferably 2.0% by mass or more and 5.0% by mass or less.

[0090] When component (A) contains a whitening ingredient, the content of the whitening ingredient in the topical composition is preferably 0.01% by mass or more and 30% by mass or less, more preferably 0.02% by mass or more and 20% by mass or less, even more preferably 0.05% by mass or more and 15% by mass or less, even more preferably 0.1% by mass or more and 10% by mass or less, and even more preferably 0.2% by mass or more and 5.0% by mass or less.

[0091] The content of component (B) in the topical composition is, from the viewpoint of improving film formability and improving the durability and moisture resistance of the film, preferably 0.01 mass% or more, more preferably 0.05 mass% or more, even more preferably 0.1 mass% or more, still more preferably 0.5 mass% or more, and even more preferably 1.0 mass% or more, and from the viewpoint of improving the durability of the film and suppressing stickiness of the film, it is preferably 30 mass% or less, more preferably 25 mass% or less, even more preferably 20 mass% or less, still more preferably 15 mass% or less, and even more preferably 10 mass% or less.

[0092] When component (B) contains component (B1), the content of component (B1) in the topical composition is preferably 0.002 mass% or more, more preferably 0.005 mass% or more, even more preferably 0.01 mass% or more, even more preferably 0.02 mass% or more, even more preferably 0.05 mass% or more, even more preferably 0.1 mass% or more, even more preferably 0.2 mass% or more, and is preferably 20 mass% or less, more preferably 15 mass% or less, even more preferably 10 mass% or less, even more preferably 8 mass% or less, and even more preferably 5 mass% or less.

[0093] When component (B) contains component (B2), the content of component (B2) in the topical preparation composition is preferably 0.003% by mass or more, more preferably 0.005% by mass or more, even more preferably 0.01% by mass or more, even more preferably 0.02% by mass or more, even more preferably 0.05% by mass or more, even more preferably 0.1% by mass or more, even more preferably 0.2% by mass or more, even more preferably 0.4% by mass or more, even more preferably 0.5% by mass or more, even more preferably 0.6% by mass or more, and preferably 25% by mass or less, more preferably 20% by mass or less, even more preferably 15% by mass or less, even more preferably 10% by mass or less, and even more preferably 8% by mass or less.

[0094] When component (B) contains component (B3), the content of component (B3) in the topical preparation composition is preferably 0.002% by mass or more, more preferably 0.005% by mass or more, even more preferably 0.01% by mass or more, even more preferably 0.02% by mass or more, even more preferably 0.05% by mass or more, even more preferably 0.1% by mass or more, even more preferably 0.2% by mass or more, even more preferably 0.4% by mass or more, even more preferably 0.5% by mass or more, even more preferably 0.6% by mass or more, and preferably 20% by mass or less, more preferably 15% by mass or less, even more preferably 10% by mass or less, and even more preferably 8% by mass or less.

[0095] The content of component (C) in the topical composition is, from the viewpoint of improving film formability and improving the durability and moisture resistance of the film, preferably 0.001% by mass or more, more preferably 0.005% by mass or more, even more preferably 0.01% by mass or more, still more preferably 0.05% by mass or more, and even more preferably 0.1% by mass or more, and from the viewpoint of suppressing stickiness of the film, is preferably 40% by mass or less, more preferably 30% by mass or less, even more preferably 20% by mass or less, and even more preferably 15% by mass or less.

[0096] The content of component (D) in the topical composition is preferably 10% by mass or more, more preferably 20% by mass or more, even more preferably 30% by mass or more, and even more preferably 40% by mass or more, from the viewpoints of improving the coatability and quick-drying properties of the composition, the durability and moisture resistance of the coating, and the crystallization-inhibiting effect of component (A); and from the viewpoints of maintaining the coatability and coating formability of the composition, it is preferably 95% by mass or less, more preferably 90% by mass or less, even more preferably 80% by mass or less, and even more preferably 70% by mass or less.

[0097] The total content of components (A) to (D) in the topical preparation composition is, from the viewpoints of improving the durability and moisture resistance of the coating, improving the crystallization inhibitory effect of component (A), and suppressing stickiness of the coating, preferably 20% by mass or more, more preferably 30% by mass or more, even more preferably 50% by mass or more, and even more preferably 60% by mass or more, and is 100% by mass or less, preferably 97% by mass or less, more preferably 95% by mass or less, and even more preferably 90% by mass or less.

[0098] When the topical preparation composition contains water, the content of water in the topical preparation composition is, from the viewpoints of improving the application property, film formability, durability and moisture resistance of the film, improving the crystallization inhibitory effect of component (A), suppressing stickiness of the film, and improving removability of the film, preferably 1% by mass or more, more preferably 2% by mass or more, even more preferably 3% by mass or more, still more preferably 5% by mass or more, still more preferably 7% by mass or more, still more preferably 8% by mass or more, still more preferably 10% by mass or more, and still more preferably 15% by mass or more; and from the viewpoints of improving the quick-drying property of the composition, improving the durability and moisture resistance of the film, improving the crystallization inhibitory effect of component (A), and suppressing stickiness of the film, preferably 70% by mass or less, more preferably 60% by mass or less, even more preferably 50% by mass or less, still more preferably 45% by mass or less, still more preferably 40% by mass or less, still more preferably 38% by mass or less, and still more preferably 35% by mass or less.

[0099] The mass ratio of component (A) to component (B) in the topical preparation composition [(A) / (B)] is preferably 0.001 or more, more preferably 0.002 or more, and even more preferably 0.003 or more, from the viewpoint of fully expressing the efficacy of component (A) and from the viewpoint of improving the crystallization inhibitory effect of component (A); and from the viewpoint of improving the coatability and film formability of the composition, improving the durability and moisture resistance of the film, and improving the crystallization inhibitory effect of component (A), it is preferably 300 or less, more preferably 250 or less, even more preferably 200 or less, still more preferably 100 or less, still more preferably 50 or less, still more preferably 30 or less, still more preferably 20 or less, still more preferably 10 or less, still more preferably 5 or less, and even more preferably 2 or less.

[0100] The mass ratio of component (A) to component (C) in the topical preparation composition [(A) / (C)] is preferably 0.001 or more, more preferably 0.002 or more, even more preferably 0.003 or more, still more preferably 0.005 or more, and still more preferably 0.01 or more, from the viewpoint of fully expressing the efficacy of component (A) and from the viewpoint of improving the crystallization inhibitory effect of component (A), and is preferably 100 or less, more preferably 80 or less, even more preferably 70 or less, still more preferably 60 or less, still more preferably 50 or less, and still more preferably 45 or less, from the viewpoint of improving the coatability and film formability of the composition, improving the durability and moisture resistance of the film, and improving the crystallization inhibitory effect of component (A).

[0101] The mass ratio of component (C) to component (B) in the topical composition [(C) / (B)] is preferably 0.01 or more, more preferably 0.02 or more, and even more preferably 0.03 or more, from the viewpoint of improving the durability and moisture resistance of the coating, and from the viewpoint of preventing the coating from becoming sticky, is preferably 50 or less, more preferably 35 or less, even more preferably 20 or less, still more preferably 10 or less, and even more preferably 5.0 or less.

[0102] The mass ratio of component (A) to the total content of components (B) and (C) in the topical preparation composition [(A) / {(B)+(C)}] is, from the viewpoint of fully expressing the efficacy of component (A), preferably 0.001 or more, more preferably 0.005 or more, even more preferably 0.01 or more, still more preferably 0.02 or more, and still more preferably 0.03 or more, and from the viewpoint of improving the durability and moisture resistance of the coating and improving the crystallization inhibitory effect of component (A), is preferably 20 or less, more preferably 15 or less, even more preferably 10 or less, still more preferably 5.0 or less, still more preferably 4.0 or less, and still more preferably 3.0 or less.

[0103] When the topical preparation composition contains water, the mass ratio of water to component (D) in the topical preparation composition [water / (D)] is, from the viewpoints of improving the durability and moisture resistance of the coating, improving the crystallization inhibitory effect of component (A), suppressing stickiness of the coating, and improving removability of the coating, preferably 0.005 or more, more preferably 0.05 or more, even more preferably 0.10 or more, still more preferably 0.20 or more, and still more preferably 0.50 or more; and from the viewpoints of improving the quick-drying property of the composition, improving the durability and moisture resistance of the coating, improving the crystallization inhibitory effect of component (A), and suppressing stickiness of the coating, it is preferably 10 or less, more preferably 8.0 or less, even more preferably 5.0 or less, still more preferably 3.0 or less, still more preferably 2.0 or less, still more preferably 1.0 or less, and still more preferably 0.7 or less.

[0104] The mass ratio of component (B) to component (D) in the topical composition [(B) / (D)] is, from the viewpoint of improving film-forming properties, preferably 0.0001 or more, more preferably 0.0002 or more, even more preferably 0.0005 or more, and even more preferably 0.001 or more, and from the viewpoint of improving the application property and quick-drying property of the composition, is preferably 1.0 or less, more preferably 0.50 or less, even more preferably 0.30 or less, even more preferably 0.20 or less, and even more preferably 0.10 or less.

[0105] <Viscosity> The viscosity of the topical composition at 25°C is 1.0 mPa·s or more, preferably 1.5 mPa·s or more, more preferably 2.0 mPa·s or more, and even more preferably 3.0 mPa·s or more, from the viewpoint of improving the application property of the composition. Also, from the viewpoint of improving the quick-drying property of the composition and the durability and moisture resistance of the coating, it is 200,000 mPa·s or less, 150,000 mPa·s or less, 130,000 mPa·s or less, 100,000 mPa·s or less, 50,000 mPa·s or less, 30,000 mPa·s or less, 20,000 mPa·s or less, 10,000 mPa·s or less, preferably 7,500 mPa·s or less, More preferably, it is 5,000 mPa·s or less, even more preferably 3,000 mPa·s or less, even more preferably 2,000 mPa·s or less, even more preferably 1,000 mPa·s or less, even more preferably 700 mPa·s or less, even more preferably 500 mPa·s or less, even more preferably 200 mPa·s or less, even more preferably 100 mPa·s or less, and even more preferably 50 mPa·s or less. The viscosity of the topical composition at 25°C is a value measured using a vibration viscometer for compositions of 1,000 mPa·s or less, and a B-type rotational viscometer for compositions of more than 1,000 mPa·s. Specifically, the viscosity can be measured using the method described in the examples.

[0106] <Contact angle> From the viewpoint of improving the application property of the composition, the film-forming property, and the durability of the film, the contact angle of the topical composition on artificial leather 10 seconds after it is dropped is preferably 5° or more, more preferably 10° or more, even more preferably 15° or more, even more preferably 20° or more, even more preferably 25° or more, and also preferably 80° or less, more preferably 75° or less, more preferably 70° or less, more preferably 60° or less, and even more preferably 55° or less. In addition, the contact angle of the composition on artificial leather 60 seconds after it is dropped is preferably 5° or more, more preferably 10° or more, even more preferably 15° or more, even more preferably 20° or more, and also preferably 70° or less, more preferably 65° or less, more preferably 60° or less, more preferably 55° or less, and even more preferably 50° or less. Furthermore, the rate of change in the contact angle of the topical composition on artificial leather from 10 seconds to 60 seconds after application (1-((contact angle 60 seconds after application) / (contact angle 10 seconds after application))) is preferably 0.6 or less, more preferably 0.5 or less, even more preferably 0.4 or less, still more preferably 0.3 or less, and even more preferably 0.25 or less, from the viewpoints of improving the application properties of the composition, the film formability, and the durability of the film. The above contact angle can be measured at a temperature of 25°C by the method described in the Examples.

[0107] <Dosage form, etc.> The topical composition of the present invention is preferably used as a topical composition for skin. The dosage form of the topical composition may be any dosage form that has a viscosity within the above range and is applicable to the skin. For example, the topical composition of the present invention may be a lotion preparation, a gel preparation, an ointment preparation, a cream preparation, or a foam preparation; the topical composition of the present invention may be an aerosol preparation or a pump spray preparation; etc. The foam preparation may be a preparation in which the topical composition of the present invention is filled in a pump former or the like and discharged in the form of foam. The compositions of the present invention may also be electrostatically sprayed onto the skin using an electrostatic spray device, as described below.

[0108] The aerosol formulation contains the topical composition and a propellant. The aerosol formulation using the topical composition of the present invention can provide a cooling sensation or the like by spraying the composition onto the skin. In the aerosol formulation, the topical composition used as the aerosol concentrate and the preferred embodiments thereof are the same as those described above. That is, the contents of the components (A) to (D) in the aerosol concentrate and the viscosity of the aerosol concentrate are preferably within the above-mentioned ranges. Propellants used in aerosol formulations include liquefied petroleum gas (LPG), which is ethane, propane, normal butane, isobutane, isopentane, and mixtures thereof; ethers such as dimethyl ether (DME); compressed gases such as nitrogen and carbon dioxide; and the like. One or more of these may be used.

[0109] In an aerosol formulation, the mass ratio of the topical preparation composition, which is an aerosol concentrate, to the propellant is not particularly limited as long as it is possible to spray the topical preparation composition onto the skin. From the viewpoints of aerosol performance and stability of the aerosol formulation, the mass ratio of the topical preparation composition to the propellant is preferably in the range of 1:0.01 to 1:10, and more preferably 1:0.05 to 1:7.5. When the propellant is LPG, the mass ratio of the topical preparation composition to LPG is more preferably 1:0.5 to 1:5; when the propellant is dimethyl ether, the mass ratio of the topical preparation composition to dimethyl ether is more preferably 1:0.1 to 1:5; and when the propellant is carbon dioxide, the mass ratio of the topical preparation composition to carbon dioxide is more preferably 1:0.1 to 1:0.5.

[0110] Examples of aerosol containers used for aerosol preparations include known pressure-resistant containers made of metal, plastic, etc., and double-structure containers in which an inner bag is housed inside a pressure-resistant container. In the case of double-structure containers, it is preferable to fill the inner bag with the topical agent composition, which is an aerosol concentrate, and fill the space between the pressure-resistant container and the inner bag with a propellant.

[0111] The method for preparing the aerosol formulation is not particularly limited. For example, the aerosol formulation can be prepared by filling the aerosol container with the topical composition, which is an aerosol concentrate, attaching a valve, and then filling the propellant through the valve.

[0112] The pump spray type preparation is a preparation in which the topical composition of the present invention is filled into a pump spray container for use.

[0113] [How to use] The present invention also provides a method for using an external preparation composition, which comprises the following steps (I) and (II) in that order: Step (I): A step of applying the topical composition to an object and then drying the composition to form a coating made of the topical composition. Step (II): A step of contacting the coating with a cleaning agent and then rinsing with water to remove the coating. According to the method of the present invention, in step (I), the topical preparation composition is applied to an object and then dried, thereby forming a coating containing the active ingredient component (A) on the surface of the object. The coating has excellent durability and moisture resistance, and can continuously release the ingredient (A) to the object. In addition, the coating can be washed off with water using a detergent, so that the coating formed in step (I) can be easily removed from the object by performing step (II).

[0114] <Process (I)> In step (I), the method of applying the topical composition to the object can be appropriately selected depending on the formulation of the topical composition, and examples of the method include application by coating, casting, spraying, etc. Among these, application by coating or spraying is preferable. After application of the topical composition, component (D) volatilizes by natural drying, etc., and a coating containing components (A) to (C) is formed on the surface of the object.

[0115] When applying the topical composition directly to the skin, the topical composition can be applied by hand or with an applicator such as a metal roller, a plastic roller, a sponge-like porous body, or a brush. When the topical composition is sprayed onto the skin, the method of spraying the composition includes a method using an aerosol, a pump spray, or an electrostatic spray device. For aerosol and pump spray, the topical composition is used as a stock solution to prepare the aerosol formulation or pump spray formulation, and the topical composition can be sprayed onto the target using the formulation. Specifically, the electrostatic spray device includes a storage unit capable of storing the topical preparation composition, a nozzle for ejecting the topical preparation composition, a power source for applying a voltage to the nozzle, and a means for delivering the topical preparation composition from the storage unit to the nozzle. One embodiment of the electrostatic spray device is a handy electrostatic spray device having a size that can be held in one hand. As the electrostatic spray device, those exemplified in International Publication No. 2018 / 194140, etc. can be used.

[0116] The object to which the topical composition is applied is preferably the skin surface. The site to which the topical composition is applied is not particularly limited, but preferred examples include the skin surface of the head, face, neck, hands, arms, feet, legs, buttocks, or trunk.

[0117] The amount of the topical composition to be applied is not particularly limited, but from the viewpoint of effectively exerting the efficacy of component (A), it is preferably 0.5 μL / cm 2 More preferably, 1 μL / cm 2 More preferably, 3 μL / cm 2 From the viewpoint of the appearance (transparency) of the formed coating, the concentration is preferably 100 μL / cm 2 Less than or equal to 50 μL / cm 2 The following is the result.

[0118] The method for drying the topical composition after application to the object is preferably natural drying, but a device such as a hair dryer can also be used as appropriate.

[0119] From the viewpoint of ease of forming the coating and of improving durability, the thickness of the coating formed in step (I) is preferably 0.005 mm or more, more preferably 0.01 mm or more, even more preferably 0.015 mm or more, still more preferably 0.02 mm or more, and is preferably 0.3 mm or less, more preferably 0.1 mm or less, even more preferably 0.07 mm or less, and still more preferably 0.06 mm or less. Specifically, the thickness of the coating can be measured by the method described in the Examples.

[0120] <Process (II)> In step (II), the coating formed in step (I) is brought into contact with a cleaning agent, and then washed with water to remove the coating. It is preferable to carry out step (II) after a certain period of time has elapsed since the formation of a coating on the surface of the object in step (I), i.e., after component (A) has exerted its effect. From this viewpoint, the time from step (I) until carrying out step (II) is preferably 0.5 hours or more and 72 hours or less, more preferably 1 hour or more and 48 hours or less.

[0121] The detergent used in step (II) may be any detergent for washing the object. For example, detergents containing anionic, cationic, or nonionic surface active ingredients and detergents containing organic solvents are included, and specific examples thereof include synthetic detergents and soaps. When the skin of the object is the scalp, the detergent may be shampoo, and when the skin is the face, the detergent may be face wash. Other detergents for the skin include soap, hand soap, body soap, and the like. The pH of the detergent may be less than pH 3 (acidic), pH 3 to 6 (weakly acidic), or pH 6 or more. From the viewpoint of removability of the coating and less irritation to the skin, the detergent is preferably pH 3 to 6 (weakly acidic), or pH 6 or more, and more preferably pH 6 or more. The pH of the detergent refers to the pH of a 5% aqueous solution at 20°C. In step (II), one embodiment of the method for removing the coating formed on the skin surface will be described. First, the cleaning agent is brought into contact with the coating formed on the skin surface by application, casting, spraying, or the like. When the cleaning agent is a solid cleaning agent such as soap, it is preferable to wet the coating on the skin surface or the solid cleaning agent with water before contacting the two. The cleaning agent may also be foamed before contacting the coating. After the cleaning agent that has been in contact with the coating has been allowed to blend into the coating, the coating is washed with water. It is preferable to scrub the coating when washing with water. This operation makes it possible to easily remove the coating. EXAMPLES

[0122] The present invention will be described below with reference to examples, but the present invention is not limited to the scope of the examples. In the examples, various measurements and evaluations were carried out by the following methods.

[0123] (viscosity) The viscosity of the topical composition at 25°C was measured using a vibration viscometer ("VM-10AL" manufactured by Sekonic Corporation). For compositions with a viscosity exceeding 1,000 mPa s, the viscosity was measured using a B-type rotational viscometer ("TVB-10" manufactured by Toki Sangyo Co., Ltd., SPINDLE: M3, rotation speed: 12 rpm).

[0124] (Presence or absence of crystals in the coating) 18 μL of the topical composition was applied to an area of ​​1.5 cm × 2 cm on a glass slide using a Microman (Gilson), and dried for 1 hour on a hot plate (AzOne Corporation's "Ceramic Hot Plate") set at 32°C. The presence or absence of crystals in the formed coating was evaluated by observation with a polarizing microscope, and judged according to the following criteria. The higher the score, the less likely precipitation of crystalline medicinal ingredients occurs. 5: no crystals observed, 4: crystals less than about 10 μm observed, 3: crystals greater than about 10 μm and less than 50 μm observed, 2: crystals greater than about 50 μm and less than 100 μm observed, 1: crystals greater than about 100 μm observed

[0125] (Sticky coating) A panel of experts applied 18 μL of the topical composition to an area of ​​1.5 cm × 2 cm on the inside of the forearm using a Microman (manufactured by Gilson), and evaluated the stickiness after 2 minutes on a 5-point scale. The average scores (rounded to the nearest tenth) of the six expert panelists are shown in the table. The higher the score, the better the evaluation result. 5: Not sticky at all, 4: Slightly sticky, 3: Slightly sticky, 2: Sticky, 1: Very sticky

[0126] (Durability of the coating) A panel of experts applied 18 μL of the topical composition to an area of ​​1.5 cm × 2 cm on the inside of the forearm using a Microman (Gilson). After application, participants performed daily activities with an exercise intensity of 3 METs or less in a room at 30°C or less, and the formed coating was visually observed after a certain period of time to confirm whether the coating remained or not. The longest time during which 90% or more of the coating remained was scored according to the following criteria. 5: 8 hours later, 4: 4 hours later, 3: 1 hour later, 2: 30 minutes later, 1: 10 minutes later

[0127] (Moisture resistance of coating) A panelist applied 50μL of the topical composition to an area of ​​2cm x 2cm on the inside of the forearm using a Microman (Gilson), and allowed to air dry for 10 minutes.Then, the panelist rested for 10 minutes in a constant temperature and humidity room at a temperature of 40℃ and a humidity of 75%.The applied area was rubbed with a finger 10 times, and the remaining film was visually observed.The moisture resistance of the film was judged according to the following criteria. 5: No wrinkling or peeling at all, 100% of the coating remains, 4: Almost no wrinkling or peeling, 90% or more of the coating remains, 3: Slight wrinkling or peeling, 80% or more of the coating remains, 2: Wrinkling or peeling, 50% to less than 80% of the coating remains, 1: Considerable wrinkling or peeling, less than 50% of the coating remains

[0128] Examples 1 to 102 and Comparative Examples 1 to 8 (Preparation and Evaluation of Topical Compositions) Component (B) and other components shown in the table were mixed with components (C), (D) and an appropriate amount of water, and then component (A) was mixed in. The remaining water was then mixed in to prepare a topical preparation composition. The obtained topical composition was evaluated by the above-mentioned method. The main ingredients used are shown in Table 1, and the composition of the topical composition and the evaluation results are shown in Tables 2 to 11. The blending amount shown in each table is the amount of active ingredient (mass%) of each ingredient.

[0129] [Table 1]

[0130] [Table 2]

[0131] [Table 3]

[0132] [Table 4]

[0133] [Table 5]

[0134] [Table 6]

[0135] [Table 7]

[0136] [Table 8]

[0137] [Table 9]

[0138] [Table 10]

[0139] [Table 11]

[0140] From Tables 2 to 11, it can be seen that the topical composition of this example has good coating durability and moisture resistance, and further has a high effect of suppressing crystallization of component (A) and stickiness of the coating. In contrast, Comparative Example 1, which did not contain component (B), Comparative Examples 2 to 6, in which component (B) did not contain two or more kinds selected from the group consisting of components (B1) to (B3), Comparative Example 7, which did not contain component (C), and Comparative Example 8, which did not contain component (D), were inferior to the effects of the present invention in any of the items.

[0141] The thicknesses of the coatings formed in Examples 1, 2, 4, 7, 12, and 15, which used a combination of (B1) cellulose polymer and (B2) acrylic polymer, Example 19, which used a combination of (B1) cellulose polymer and (B3) vinyl polymer, and Example 27, which used a combination of (B2) acrylic polymer and (B3) vinyl polymer, were measured by the following method. The thicknesses of the coatings in Examples 1, 2, 4, 7, 9, 12, 13, 15, 19, and 27 were 0.028 mm, 0.019 mm, 0.008 mm, 0.028 mm, 0.051 mm, 0.029 mm, 0.070 mm, 0.098 mm, 0.031 mm, and 0.020 mm, respectively.

[0142] (Coating thickness) The topical composition was applied to a vinyl tape (Nitoms Corporation, "Lead-free type J3447") at 20 μL / cm 2The coating was applied and dried for 10 minutes on a hot plate heated to 32° C. After drying, the resulting coating was peeled off with tweezers, and the thickness of the coating was measured using a digimatic indicator (Mitutoyo "ID-C112XBS", minimum display: 0.001 mm).

[0143] Furthermore, the removability of the coatings formed using the topical preparation compositions was evaluated by the following method for Examples 1 to 3 and Comparative Examples 5 and 6. The results are shown in Table 12. (Removability of coating) A specialist panel applied 50 μL of the topical composition to an area of ​​2 cm × 2 cm on the inside of the forearm using a Microman (manufactured by Gilson), and allowed to dry naturally for 10 minutes. After that, the coating was immersed in a water bath at about 40°C, and the remaining state of the coating was visually observed when the coating was rubbed with a finger 10 times. Next, a foamed detergent (Kao Soap White) was brought into contact with the coating, and the coating was rubbed with a finger 10 times, and the foam was washed away in a water bath, and the remaining state of the coating was visually observed. The removability of the coating was evaluated according to the following evaluation criteria depending on the stage of removal, taking into account the moisture resistance of the coating. Pass was rated as A. A: It cannot be removed with lukewarm water at 40°C, but it can be removed if a cleaning agent is used. B: It can be removed with lukewarm water at 40℃. C: Cannot be removed even with warm water (40°C) or cleaning agents.

[0144] [Table 12]

[0145] Examples 103 to 106 (Preparation and Evaluation of Topical Compositions) Component (B) and other components shown in the table were mixed with component (C), component (D), and an appropriate amount of water, and then component (A) was mixed in. The remaining water was then mixed in to prepare a topical preparation composition. The obtained topical composition was evaluated by the above method. Furthermore, the thickness of the coating, the contact angle of the composition and its rate of change, and the applicability were evaluated by the following method. The main components used are shown in Table 1, and the composition of the topical composition and the evaluation results are shown in Table 13. The blending amount shown in the table is the amount of active ingredient (mass%) of each component.

[0146] (Contact angle of composition and rate of change) At 25° C., 2 μL of the topical composition shown in Table 13 was dropped onto artificial leather Suplarle (Ideatex Japan) using an automatic contact angle meter (Kyowa Chemical Industry Co., Ltd., “DM-501i”), and the contact angle was measured 10 seconds and 60 seconds after the drop was applied. The rate of change in the contact angle from 10 seconds to 60 seconds after the drop was applied was calculated using the following formula (1). Rate of change in contact angle = 1 - (contact angle after 60 seconds on contact) / (contact angle after 10 seconds on contact) (1)

[0147] (Applicability) After marking the inside of the forearm of a specialist panelist to indicate an area of ​​2 cm x 2 cm, 24 μL of the topical composition shown in Table 13 was applied using a Microman (Gilson). The spread of the composition 30 seconds after application was visually confirmed, and the applicability was judged according to the following criteria. A: It can be applied within an area of ​​2cm x 2cm. B: Bleeding also occurs around the 2cm x 2cm area. C: Dripping from a 2cm x 2cm area.

[0148] [Table 13]

[0149] Table 13 shows that topical preparation compositions that have high contact angles on artificial leather 10 seconds and 60 seconds after application and that have a small rate of change in contact angle from 10 seconds to 60 seconds after application have better applicability to skin.

[0150] Formulation Examples 1 to 26 (Preparation of topical compositions) According to the formulations in Tables 14 and 15, component (B) and other components were mixed with component (C), component (D), and an appropriate amount of water, and then component (A) was mixed in. The remaining water was then mixed in to prepare a topical preparation composition.

[0151] Formulation Examples 27-30 (Preparation of aerosol formulations) According to the recipe in Table 16, component (B) and other components were mixed with component (C), component (D), and an appropriate amount of water, and then component (A) was mixed in. The remaining water was then mixed in to prepare an external preparation composition that would be an aerosol concentrate. This was then filled into an aerosol container (manufactured by Toyo Seikan Co., Ltd.), and dimethyl ether (DME), a propellant, was sealed in such that the mass ratio of the aerosol concentrate to DME was as shown in the table, to prepare an aerosol formulation.

[0152] [Table 14]

[0153] [Table 15]

[0154] [Table 16] [Industrial Applicability]

[0155] According to the present invention, it is possible to provide an external preparation composition which contains a medicinal ingredient and is capable of forming a coating film which is excellent in both durability and moisture resistance, and a method for using the same.

Claims

1. The following ingredients (A) to (D): (A) Medicinal ingredients (B) Water-insoluble polymer (C) Non-volatile base (D) Volatile solvents A topical composition containing, The aforementioned component (B) comprises (B1) a cellulose polymer and (B2) an acrylic polymer. The mass ratio of component (B2) to component (B1) [(B2) / (B1)] is 0.05 or more and 30 or less. The aforementioned component (B) is a polymer that, when immersed in 10 g of deionized water at 23°C and 1 atm, has the property that more than 0.5 g of the immersed polymer does not dissolve after 24 hours. A topical preparation composition having a viscosity of 1.0 mPa·s or more and 10,000 mPa·s or less at 25°C.

2. The following components (A) to (D): (A) Medicinal ingredients (B) Water-insoluble polymer (C) Non-volatile base (D) Volatile solvents A topical composition containing, The aforementioned component (B) includes (B2) an acrylic polymer and (B3) a vinyl polymer. The mass ratio of component (B2) to component (B3) [(B2) / (B3)] is 0.05 or more and 30 or less. The aforementioned component (B) is a polymer that, when immersed in 10 g of deionized water at 23°C and 1 atm, has the property that more than 0.5 g of the immersed polymer does not dissolve after 24 hours. A topical preparation composition having a viscosity of 1.0 mPa·s or more and 10,000 mPa·s or less at 25°C.

3. The topical preparation composition according to claim 1 or 2, wherein the mass ratio of component (C) to component (B) in the topical preparation composition [(C) / (B)] is 0.01 or more and 50 or less.

4. The topical preparation composition according to claim 1 or 2, wherein the topical preparation composition further contains water, and the water content in the topical preparation composition is 1% by mass or more and 70% by mass or less.

5. The topical composition according to claim 1 or 2, wherein component (A) contains one or more selected from the group consisting of anti-inflammatory and analgesic components, local irritants, blood circulation promoting components, antihistamine components, herbal components, antipruritic components, local anesthetic components, keratolytic components, bactericidal components, antibacterial and antifungal components, immunosuppressants, antiviral components, hair growth and hair restoration components, sebum suppressing components, antiperspirant components, and whitening components.

6. The component (A) is glycol salicylate, methyl salicylate, diclofenac sodium, loxoprofen sodium hydrate, ketoprofen, felbinac, indomethacin, flurbiprofen, dipotassium glycyrrhizinate, zinc oxide, allantoin, heparinoid, glycyrrhetinic acid, ibuprofen piconol, fluocinolone acetonide, l-menthol, dl-camphor, nonylic acid vanillylamide, tocopherol acetate, carpronium chloride hydrate, diphenhydramine, diphenhydramine hydrochloride, chlorpheniramine maleate, capsicum, capsicum tincture, crotamiton, benzalkonium chloride, hydrocortisone, hydrocortisone acetate, hydrocortisone butyrate, dexamethasone acetate, prednisolone valerate acetate, A topical composition according to claim 1 or 2, comprising one or more selected from the group consisting of betamethasone valerate, ufenamate, lidocaine, dibucaine hydrochloride, urea, sulfur, salicylic acid, isopropylmethylphenol, benzethonium chloride, resorcinol, homosulfamine, homosulfamine hydrochloride, chlorhexidine hydrochloride, adapalene, trichlorocarbanilide, clotrimazole, miconazole nitrate, tolnaftate, hinokitiol, oxiconazole nitrate, bifonazole, lanoconazole, terbinafine hydrochloride, butenafine hydrochloride, tacrolimus, acyclovir, vidarabine, minoxidil, panthenol, pantothenyl ethyl ether, pyridoxine hydrochloride, tranexamic acid, tretinoin, aluminum chloride, glycopyrronium tosylate hydrate, and sofpyrronium bromide.

7. The topical composition according to Claim 1, wherein the component (B1) comprises one or more selected from the group consisting of methylcellulose, ethylcellulose, hypromellose, carboxymethylcellulose, carboxymethylethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hypromellose phthalate, hydrophobized (C16-18) hydroxypropylmethylcellulose, hypromellose acetate succinate, and phthalcellulose acetate.

8. The topical composition according to claim 1 or 2, wherein the component (B2) comprises one or more selected from the group consisting of (acrylates / diacetone acrylamide) copolymer, acrylamide / methoxypolyethylene glycol methacrylate copolymer, alkyl acrylate copolymer, acrylic acid ester / vinyl acetate copolymer, 2-ethylhexyl acrylate / methyl acrylate / acrylic acid / glycidyl methacrylate copolymer, 2-ethylhexyl acrylate / vinyl acetate / hydroxyethyl acrylate / glycidyl methacrylate copolymer, 2-ethylhexyl acrylate / diacetone acrylamide / acetoacetoxyethyl methacrylate / methyl methacrylate copolymer, 2-ethylhexyl acrylate / vinylpyrrolidone copolymer, 2-ethylhexyl acrylate / 2-ethylhexyl methacrylate / dodecyl methacrylate copolymer, ethyl acrylate / methyl methacrylate copolymer, ethyl acrylate / methyl methacrylate / methacrylate-derived trimethylammonium ethyl copolymer, and methyl methacrylate / butyl methacrylate / dimethylaminoethyl methacrylate copolymer.

9. The topical composition according to claim 2, wherein the component (B3) comprises one or more selected from the group consisting of polyvinyl alcohol, polyvinyl acetate, and polyvinyl butyral.

10. The topical composition according to claim 1 or 2, wherein the component (C) is one or more selected from the group consisting of polar oils, non-polar oils, polyols, alkanolamines, and nonionic surfactants.

11. The topical preparation composition according to claim 1 or 2, wherein the content of component (A) in the topical preparation composition is 0.001% by mass or more and 30% by mass or less.

12. The topical preparation composition according to claim 1 or 2, wherein the content of component (B) in the topical preparation composition is 0.01% by mass or more and 30% by mass or less.

13. The topical preparation composition according to claim 1 or 2, wherein the content of component (C) in the topical preparation composition is 0.001% by mass or more and 40% by mass or less.

14. The topical preparation composition according to claim 1 or 2, wherein the content of component (D) in the topical preparation composition is 10% by mass or more and 95% by mass or less.