External preparation composition

Abstract

This external preparation composition contains the following components (A)-(D): (A) a medicinal component, (B) a water-insoluble polymer, (C) a non-volatile base agent, and (D) a volatile solvent, the component (B) containing two or more types selected from the group consisting of (B1) a cellulose-based polymer, (B2) an acrylic polymer, and (B3) an ethylene-based polymer, and has a viscosity at 25 DEG C of 1.0-10,000 mPa.s (inclusive).

Description

Technical Field

[0001] The present invention relates to an external-use composition. Background Art

[0002] Known liquid skin preparations for external use and patches containing active ingredients such as anti-inflammatory and analgesic ingredients, sterilizing and disinfecting ingredients. However, existing liquid skin preparations for external use have the problems of being easily rubbed off by clothes etc. after being applied to the skin, being difficult to release active ingredients to the skin on a continuous basis. About the patch containing active ingredients, if it is difficult to follow the skin and easily peel off, it is also difficult to release active ingredients to the skin on a continuous basis. On the other hand, there is also the problem of increased skin burden when the high adhesiveness of the patch to the skin is peeled off from the skin. In addition, there are also problems in actual use such as easy rashes and the appearance when the patch is attached to the skin that makes people concerned.

[0003] Therefore, film-forming preparations that can continuously release active ingredients to the skin are being studied. Film-forming preparations can form a film when applied to the skin, so they are more difficult to wipe off than liquid skin external preparations. In addition, even if applied to the skin, they are not as conspicuous as patches, and the burden on the skin when removed from the skin is less, which is also preferred in this regard.

[0004] For example, Japanese Patent Gazette No. 2021-6522 (Patent Document 1) discloses a film-forming skin external composition containing a film-forming polymer including a cellulose polymer and an ethylene polymer, a polyol, and a volatile solvent, which can form the following film and has excellent applicability: the formed film protects the affected area, and although it is firmly in contact with the skin, it has high softness and excellent feel to use without discomfort, and it is difficult to peel off due to movement or friction.

[0005] International Publication No. 2022 / 059618 (Patent Document 2) discloses a film-forming aerosol composition comprising a stock solution containing a film-forming agent and an organic solvent with a predetermined boiling point and a propellant, and comprising an alkyl acrylate-vinyl acetate copolymer as the above-mentioned film-forming agent, which has excellent skin protection and can form a film on the skin that is excellent in both removability after application and water resistance to sweat, etc. Summary of the invention

[0006] The present invention relates to the following contents.

[0007] [1] An external use composition comprising the following components (A) to (D):

[0008] (A) Medicinal ingredients,

[0009] (B) water-insoluble polymers,

[0010] (C) non-volatile base, and

[0011] (D) a volatile solvent, and

[0012] The component (B) includes two or more selected from (B1) a cellulose polymer, (B2) an acrylic polymer, and (B3) a vinyl polymer, and the viscosity of the external preparation composition at 25° C. is 1.0 mPa·s to 10,000 mPa·s.

[0013] [2] A method for using the external preparation composition described in [1], comprising the following steps (I) and (II) in sequence:

[0014] Step (I): a step of applying the external preparation composition to an object, followed by drying to form a film composed of the external preparation composition;

[0015] Step (II): a step of bringing the film into contact with a cleaning agent and then washing with water to remove the film. DETAILED DESCRIPTION

[0016] As described above, Patent Document 1 describes the durability of the formed coating, and Patent Document 2 describes the resistance of the coating to sweat and the like. However, the durability and moisture resistance of the coatings in these prior arts are not sufficient for practical use and there is room for further improvement.

[0017] The present invention relates to an external preparation composition capable of forming a coating film containing a medicinal ingredient and having excellent durability and moisture resistance.

[0018] The present inventors have found that an external preparation composition containing a medicinal ingredient, two or more predetermined water-insoluble polymers, and a predetermined solvent component and having a predetermined viscosity can solve the above-mentioned problems.

[0019] According to the present invention, there can be provided an external preparation composition that can form a coating film containing a medicinal ingredient and having excellent durability and moisture resistance, and a method for using the same.

[0020] [External application composition]

[0021] The present invention relates to an external-use composition, which contains the following components (A) to (D):

[0022] (A) Medicinal ingredients,

[0023] (B) water-insoluble polymers,

[0024] (C) non-volatile base, and

[0025] (D) a volatile solvent, and

[0026] The component (B) comprises two or more selected from (B1) a cellulose polymer, (B2) an acrylic polymer, and (B3) a vinyl polymer, and the viscosity of the external preparation composition at 25° C. is 1.0 mPa·s or more and 10,000 mPa·s or less. Hereinafter, the composition may also be appropriately referred to as the "composition of the present invention".

[0027] <Definition>

[0028] In this specification, the term "external application composition" refers to a composition to be mainly applied to the skin surface.

[0029] In this specification, “containing X” includes X being compounded.

[0030] In this specification, the term "water-insoluble polymer" refers to a polymer having the property that when 1 g of the polymer is immersed in 10 g of ion-exchanged water at 23° C. and 1 atm, more than 0.5 g of the immersed polymer does not dissolve after 24 hours.

[0031] In this specification, the term "non-volatile base" refers to a base that is liquid at 70°C and has a mass reduction rate 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.

[0032] The term "volatile solvent" refers to a component other than water that has a mass reduction rate of 1% or more when 1 g of the solvent is spread in a glass petri dish with a diameter of 48 mm and left at 25°C and normal pressure for 24 hours and is liquid at 25°C.

[0033] In addition, in this specification, when the external preparation composition is applied to the object (skin of the subject) to form a film, the film is difficult to be rubbed off when the subject performs daily life activities, and this situation is referred to as "high durability of the film". In addition, when the film is difficult to wrinkle or peel off even when rubbed under high temperature and high humidity, it is referred to as "high moisture resistance of the film". Specifically, the durability and moisture resistance of the film can be evaluated by the method described in the Examples.

[0034] Furthermore, 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, wherein 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 the components (C) and (D).

[0035] The composition of the present invention can form a coating film containing a medicinal ingredient and having excellent durability and moisture resistance by having the above-mentioned structure. The reason for this is not yet determined, but it is considered as follows.

[0036] The composition of the present invention is a film-forming composition containing a water-insoluble polymer as component (B) and a nonvolatile base as component (C) as film-forming components. 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).

[0037] It is believed that since component (B) is water-insoluble, a highly hydrophobic film can be formed, so the durability and moisture resistance of the film are easily improved, and the stickiness of the film is also suppressed. On the other hand, if only component (B) is used as a film-forming component, there is a concern that the film becomes brittle and the durability is reduced. It is believed that these undesirable situations can be suppressed by using component (B) and component (C) in combination in the present invention.

[0038] Furthermore, it was found that when only one water-insoluble polymer is used as component (B), or when only the same polymer is used even if two or more water-insoluble polymers are used, it is difficult to achieve not only durability of the coating, but also high moisture resistance that does not cause wrinkles or peeling even when the coating is rubbed under high temperature and high humidity. It is believed that the above-mentioned problems can be solved by using two or more specific and different water-insoluble polymers as component (B) in the present invention.

[0039] It is believed that component (D) contributes to the improvement of the quick-drying property of the topical agent composition, the crystallization inhibition effect of component (A), etc. By inhibiting the crystallization of component (A) in the coating, the component (A) as a medicinal ingredient can be effectively slowly released to the object. And then, by making the topical agent composition contain component (D), it is easy to adjust the viscosity to a specified range. It is believed that as a result, the smearability and film formation of the topical agent composition are improved, and the durability and moisture resistance of the formed coating are also further improved.

[0040] The film formed by the composition of the present invention also has the following effects: it is less sticky, has excellent durability and moisture resistance during use, and can be easily removed by washing with a detergent after use (hereinafter also referred to as "removability of the film").

[0041] <Ingredient (A): Medicinal ingredient>

[0042] The composition of the present invention contains a pharmaceutical ingredient as component (A). From the viewpoint of being used for topical composition, component (A) is preferably a skin external medicine component that can be administered percutaneously. Specifically, component (A) is preferably selected from anti-inflammatory and analgesic components, local irritation components, blood circulation promoting components, antihistamine components, herbal medicine components, antipruritic components, local anesthetic components, keratin softening components, bactericidal components, antibacterial / antifungal components, immunosuppressants, antiviral components, hair growth / hair growth components, sebum inhibition components, antiperspirant components, and whitening components. One or more, more preferably including anti-inflammatory and analgesic components, antihistamine components, antipruritic components, bactericidal components, antibacterial / antifungal components, immunosuppressants, antiviral components, hair growth / hair growth components, sebum inhibition components, antiperspirant components, and whitening components. One or more.

[0043] Examples of the anti-inflammatory and analgesic ingredients include ethylene glycol salicylate, methyl salicylate, aspirin, sulpyrine hydrate, acetaminophen, diclofenac sodium, phentermine, ibuprofen, amiprofen, loxoprofen sodium hydrate, naproxen, oxaprofen, ketoprofen, tiaprofenic acid, sulindac, aluminum flufenamic acid, felbinac, mefenamic acid, indomethacin, indomethacin farnesate, acemetacin, procarbazine, Lometasine, bendazolic acid, piroxicam, ampiroxicam, lornoxicam, tenoxicam, meloxicam, etodolac, thiamide hydrochloride, bucolon, flurbiprofen, ifluprofen, lysozyme hydrochloride, bromelain, diphenhydramine hydrochloride, cinchocaine, dimethyl isopropyl azulene, benzethonium chloride, glycyrrhizic acid, dipotassium glycyrrhizinate, zinc oxide, allantoin, heparin analogs, glycyrrhetinic acid, ibuprofen piconol, fluocinolone, difluprednate, clobetasol propionate, betamethasone valerate, etc. Among these, at least one selected from ethylene glycol salicylate, methyl salicylate, diclofenac sodium, loxoprofen sodium hydrate, ketoprofen, indomethacin, piroxicam, flurbiprofen, ifluprofen, glycyrrhizic acid, dipotassium glycyrrhizinate, zinc oxide, allantoin, a heparin analog, glycyrrhetinic acid, picoprofen, fluocinolone, difluprednate, clobetasol propionate, and betamethasone valerate is preferred.

[0044] As the local irritant component, l-menthol, dl-camphor, nonanamide, ammonia, peppermint oil, etc. can be mentioned. Among these, at least one selected from l-menthol, dl-camphor, and nonanamide is preferred.

[0045] Examples of the blood circulation promoting component include benzyl nicotinate, sodium polyvinyl sulfonate, tocopherol acetate, carpronium chloride hydrate, etc. Among these, at least one selected from tocopherol acetate and carpronium chloride hydrate is preferred.

[0046] Examples of the antihistamine component include diphenhydramine, diphenhydramine hydrochloride, diphenhydramine salicylate, chlorpheniramine maleate, etc. Among these, at least one selected from diphenhydramine, diphenhydramine hydrochloride, and chlorpheniramine maleate is preferred.

[0047] Examples of the herbal medicinal ingredients include capsicum, arnica tincture, eucalyptus oil, phellodendron, arnica tincture, houttuynia cordata, peony, wormwood, cinnamon bark, ligusticum chuanxiong, cyperus rotundus, atractylodes, dill, schisandra chinensis, tangerine peel, carrot, magnolol, clove, ginger, gardenia, licorice, fennel, akebia, safflower, magnolia bark, spruce, and artemisia capillaris. Among these, at least one selected from capsicum and arnica tincture is preferred.

[0048] Examples of the antipruritic ingredient include crotamiton, cortisone acetate, azaprozine hydrochloride, benzalkonium chloride, calamine, d-borneol, ammonia water, hydrocortisone, hydrocortisone acetate, hydrocortisone butyrate, dexamethasone, dexamethasone acetate, prednisolone, prednisolone acetate, prednisolone valerate acetate, uffenamate, etc. Among these, preferably, at least one selected from crotamiton, benzalkonium chloride, hydrocortisone, hydrocortisone acetate, hydrocortisone butyrate, dexamethasone, dexamethasone acetate, prednisolone, prednisolone valerate acetate, and uffenamate.

[0049] Examples of the local anesthetic component include lidocaine, mepivacaine, bupivacaine, ropivacaine, levobupivacaine, dibucaine, dibucaine hydrochloride, ethyl aminobenzoate, etc. Among these, at least one selected from lidocaine and dibucaine hydrochloride is preferred.

[0050] Examples of the keratin softening component include urea, sulfur, salicylic acid, and the like.

[0051] Examples of the bactericidal component include chlorhexidine gluconate, sodium copper chlorophyllin, isopropylmethylphenol, cetylpyridinium chloride hydrate, benzethonium chloride, benzalkonium chloride, resorcinol, ethacridine hydrate, chlorhexidine digluconate, mafenide, mafenide hydrochloride, povidone iodine, iodine-potassium iodide, mercurochrome, hydrogen peroxide, cresol, iodoform, thymol, chlorhexidine hydrochloride, adapalene, triclocarban, etc. Among these, preferably one or more selected from isopropylmethylphenol, benzethonium chloride, resorcinol, mafenide, mafenide hydrochloride, chlorhexidine hydrochloride, adapalene, and triclocarban are used.

[0052] Examples of the antibacterial / antifungal ingredient include undecylenic acid, zinc undecylenate, phenyl-11-iodo-10-undecylenate, isoxamide, clotrimazole, econazole nitrate, miconazole nitrate, tioconazole, zinc diethyldithiocarbamate, ciclopirox, siccanin, trichostatin, nitropyrrol, dimethylthioanthracene, 2,4,6-tribromophenyl hexanoate, trimethylcetylammonium pentachlorophenolate, tolcylcerate, tolnaftate, iodine chlorpropene, hibiscus bark, berberine benzoate, dequalinium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate solution, dequalinium acetate, hinokitiol, resorcinol, benzoic acid, chlorobutanol, acetic acid, phenol, iodine tincture, dibenpyraline hydrochloride, diphenhydramine salicylate, diphenylimidazole, chlorpheniramine maleate, cinnamyl hydrochloride Caine, procaine hydrochloride, lidocaine hydrochloride, aluminum allantoin, glycyrrhizic acid and its salts, purple root, angelica, borneol, diethyl phthalate, aluminum chlorohydrate, penicillins, cephems, carbapenems, monobactams, penicillins, aminoglycosides, fosfomycin, chloramphenicol, macrolides, glycopeptides, quinolones, new quinolones, sulfonamides, neomycin sulfate, gentamicin sulfate, pentamidine isethionate, silver sulfadiazine, oxiconazole nitrate, sulconazole nitrate, bifonazole, neconazole hydrochloride, lanoconazole, amorolfine hydrochloride, terbinafine hydrochloride, butenafine hydrochloride, polymyxin B sulfate, colistin sulfate, subtilisin, neomycin sulfate, benzoyl peroxide, nadifloxacin, levofloxacin, clindamycin phosphate, etc. Among these, at least one selected from the group consisting of clotrimazole, miconazole nitrate, pyrrolidone, tolnaftate, hinokitiol, neomycin sulfate, oxiconazole nitrate, bifonazole, lanoconazole, terbinafine hydrochloride, and butenafine hydrochloride is preferred.

[0053] Examples of the immunosuppressant include tacrolimus and the like.

[0054] Examples of the antiviral component include acyclovir and vidarabine.

[0055] Examples of the hair growth and development component include minoxidil, panthenol, and panthenol ethyl ether.

[0056] As the sebum suppressing ingredient, pyridoxine hydrochloride etc. may be mentioned.

[0057] Examples of the antiperspirant ingredient include aluminum chloride, glycopyrronium tosylate hydrate, and sopyrronium bromide.

[0058] Examples of the whitening ingredient include tranexamic acid, vitamin A acid and hydroquinone.

[0059] As the component (A), one or more of the above-mentioned medicinal ingredients can be used.

[0060] Among the above, component (A) is more preferably selected from ethylene glycol salicylate, methyl salicylate, diclofenac sodium, loxoprofen sodium hydrate, ketoprofen, indomethacin, flurbiprofen, dipotassium glycyrrhizinate, zinc oxide, allantoin, heparin analogs, glycyrrhetinic acid, picoprofen, fluocinolone, l-menthol, dl-camphor, vanillyl nonamide, tocopherol acetate, carpronium chloride hydrate, diphenhydramine, diphenhydramine hydrochloride, chlorpheniramine maleate, capsicum, crotamiton, benzalkonium chloride, hydrocortisone, hydrocortisone butyrate, dexamethasone acetate, prednisolone valerate acetate, betamethasone valerate , uffenamate, lidocaine, cinchocaine hydrochloride, urea, sulfur, salicylic acid, isopropyl methylphenol, benzethonium chloride, resorcinol, mafenide, mafenide hydrochloride, chlorhexidine hydrochloride, triclocarban, clotrimazole, miconazole nitrate, tolnaftate, hinokitiol, oxiconazole nitrate, bifonazole, lanoconazole, terbinafine hydrochloride, butenafine hydrochloride, tacrolimus, acyclovir, vidarabine, minoxidil, panthenol, panthenol ethyl ether, pyridoxine hydrochloride, tranexamic acid, retinoic acid, mafenide hydrochloride, aluminum chloride, glycopyrronium tosylate hydrate, and sopironium bromide.

[0061] <Component (B): Water-insoluble polymer>

[0062] The composition of the present invention contains a water-insoluble polymer as component (B). Component (B) is a film-forming component, and it is believed that it can improve the film-forming property of the composition and form a film with high durability and moisture resistance. Furthermore, even when a highly crystalline component (A) is used, the following effects are achieved: the crystallization of component (A) in the film can be suppressed, the formed film is less sticky, and can be easily removed by washing with a detergent.

[0063] From the viewpoint of improving film-forming properties, component (B) is preferably a water-insoluble polymer having film-forming properties. In addition, the definition of "water-insoluble" of component (B) is as described above.

[0064] Component (B) contains two or more selected from the group consisting of (B1) a cellulose-based polymer, (B2) an acrylic polymer, and (B3) a vinyl-based polymer.

[0065] In the present specification, "component (B) contains two or more selected from (B1) a cellulose polymer, (B2) an acrylic polymer, and (B3) a vinyl polymer" specifically means any one of the following aspects (i) to (iv).

[0066] (i) Component (B) contains component (B1) and component (B2), but does not contain component (B3)

[0067] (ii) Component (B) contains component (B1) and component (B3), but does not contain component (B2)

[0068] (iii) Component (B) contains component (B2) and component (B3), but does not contain component (B1)

[0069] (iv) Component (B) includes component (B1), component (B2), and component (B3)

[0070] Therefore, for example, when the component (B) contains two or more components (B1) but does not contain any of the component (B2) and the component (B3), it is regarded as not included in the scope of the present invention.

[0071] Among the above aspects, aspect (i) or (iv) is preferred, and aspect (i) is more preferred, from the viewpoint of improving durability and moisture resistance of the coating, improving the effect of inhibiting crystallization of component (A), and inhibiting stickiness of the coating.

[0072] (Component (B1): Cellulose polymer)

[0073] As the cellulose-based polymer used as the component (B1), water-insoluble substances among polymers having a cellulose skeleton may be mentioned.

[0074] Specific examples of component (B1) include water-insoluble substances such as methyl cellulose, ethyl cellulose, hydroxypropyl methyl cellulose, carboxymethyl cellulose, carboxymethyl ethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose phthalate, hydrophobized (C16-18) hydroxypropyl methyl cellulose, hydroxypropyl methyl cellulose acetate succinate, and cellulose acetate phthalate. Among these, one or more kinds may be used.

[0075] From the viewpoint of improving the durability and moisture resistance of the coating, the viewpoint of improving the crystallization inhibition effect of component (A), and the viewpoint of suppressing the stickiness of the coating, component (B1) is preferably one or more selected from ethyl cellulose, hypromellose phthalate, and hydrophobized (C16-18) hypromellose, and more preferably hypromellose phthalate.

[0076] As component (B1), commercial products may be used. For example, as ethyl cellulose used as component (B1), "Ethocel 100P" manufactured by Nissin Chemical Co., Ltd. may be cited, and as hydroxypropyl methylcellulose phthalate, "HPMCP HP-55", "HPMCP HP-55S", "HPMCP HP-50" manufactured by Shin-Etsu Chemical Co., Ltd. may be cited.

[0077] (Component (B2): acrylic polymer)

[0078] Examples of the acrylic polymer used as component (B2) include water-insoluble polymers containing at least a structural unit derived from a monomer having a (meth)acryloyl group. In this specification, "(meth)acryloyl group" means both an acryloyl group and a methacryloyl group.

[0079] Specific examples of component (B2) include water-insoluble substances such as (acrylate / diacetone acrylamide) copolymers, acrylamide-methoxypolyethylene glycol methacrylate copolymers, alkyl acrylate copolymers, acrylate-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-diacetone acrylamide-acetoacetoxyethyl methacrylate-methyl methacrylate copolymers, 2-ethylhexyl acrylate-vinyl pyrrolidone copolymers, 2-ethylhexyl acrylate-2-ethylhexyl methacrylate-dodecyl methacrylate copolymers, ethyl acrylate-methyl methacrylate copolymers, ethyl acrylate-methyl methacrylate-ethyl trimethylammonium chloride methacrylate copolymers, and methyl methacrylate-butyl methacrylate-dimethylaminoethyl methacrylate copolymers. Among these, one or more kinds thereof may be used.

[0080] Among the above, as the (acrylate / diacetone acrylamide) copolymer, "(alkyl acrylate / diacetone acrylamide) copolymer AMP" in the name of cosmetic ingredient expression can be used, as the acrylamide-methoxy polyethylene glycol methacrylate copolymer, "acrylamide-methoxy polyethylene glycol methacrylate copolymer liquid" described in the Pharmaceutical Additive Standards 2018 (Pharmaceutical Examination and Management Division, Pharmaceutical and Public Health Bureau, Ministry of Health, Labor and Welfare) can be used, as the alkyl acrylate copolymer, "alkyl acrylate copolymer ammonium" in the name of cosmetic ingredient expression can be used, and as the 2-ethylhexyl acrylate-vinyl pyrrolidone copolymer, "Acrylamide-methoxy polyethylene glycol methacrylate copolymer liquid" described in the Pharmaceutical Additive Standards 2018 (Pharmaceutical and Public Health Bureau, Ministry of Health, Labor and Welfare) can be used. The "2-ethylhexyl acrylate-vinyl pyrrolidone copolymer solution" described in the Pharmaceutical Review and Administration Section of the Pharmaceutical and Health Bureau of the Ministry of Health, Labor and Welfare, as the 2-ethylhexyl acrylate-2-ethylhexyl methacrylate-dodecyl methacrylate copolymer, the "2-ethylhexyl acrylate-2-ethylhexyl methacrylate-dodecyl methacrylate copolymer solution" can be used, as the ethyl acrylate-methyl methacrylate copolymer, the "ethyl acrylate-methyl methacrylate copolymer dispersion" can be used, and as the methyl methacrylate-butyl methacrylate-dimethylaminoethyl methacrylate copolymer, the "aminoalkyl methacrylate copolymer E" can be used.

[0081] Moreover, as the ethyl acrylate-methyl methacrylate-trimethylammoniumethyl methacrylate chloride copolymer, "aminoalkyl methacrylate copolymer RS" known as a pharmaceutical additive can be used.

[0082] From the viewpoint of improving the durability and moisture resistance of the coating, the viewpoint of improving the crystallization inhibition effect of the component (A), and the viewpoint of suppressing the stickiness of the coating, the component (B2) preferably contains one or more selected from the group consisting of (acrylate / diacetone acrylamide) copolymers, alkyl acrylate copolymers, and acrylate-vinyl acetate copolymers, and more preferably is an (acrylate / diacetone acrylamide) copolymer.

[0083] As component (B2), commercial products may be used. For example, as the (acrylate / diacetone acrylamide) copolymer used as component (B2), "Plascize L-53" manufactured by Huying Chemical Industry Co., Ltd., as the alkyl acrylate-vinyl acetate copolymer, "Vinysol 2140L" manufactured by Datong Chemical Industry Co., Ltd., and as the alkyl acrylate copolymer, "Vinysol 1086WP" manufactured by Datong Chemical Industry Co., Ltd., etc. may be mentioned.

[0084] (Component (B3): ethylene polymer)

[0085] As the ethylene polymer used as component (B3), water-insoluble substances in polymers that contain at least structural units derived from monomers having vinyl groups and are not the above-mentioned acrylic polymers can be cited. As such ethylene polymers, water-insoluble substances in polyvinyl alcohol, polyvinyl acetate, polyvinyl butyral, etc. can be cited.

[0086] From the viewpoint of improving the durability and moisture resistance of the coating, the viewpoint of improving the crystallization suppressing effect of the component (A), and the viewpoint of suppressing the stickiness of the coating, the component (B3) is preferably polyvinyl butyral.

[0087] As the component (B3), a commercially available product may be used. For example, polyvinyl butyral used as the component (B3) may be "S-LEC B·K" series manufactured by Sekisui Chemical Co., Ltd.

[0088] When (i) component (B) contains component (B1) and component (B2) but does not contain component (B3), component (B1) is preferably one or more selected from ethyl cellulose, hypromellose phthalate, and hydrophobized (C16-18) hypromellose, more preferably hypromellose phthalate, and component (B2) is preferably (acrylate / diacetone acrylamide) copolymer.

[0089] When (ii) the component (B) contains the component (B1) and the component (B3) but does not contain the component (B2), the component (B1) is preferably hypromellose phthalate, and the component (B3) is preferably polyvinyl butyral.

[0090] When (iii) the component (B) includes the components (B2) and (B3) but does not include the component (B1), the component (B2) is preferably an (acrylate / diacetone acrylamide) copolymer, and the component (B3) is preferably polyvinyl butyral.

[0091] When (iv) component (B) includes component (B1), component (B2), and component (B3), component (B1) is preferably hydroxypropyl methylcellulose phthalate, component (B2) is preferably (acrylate / diacetone acrylamide) copolymer, and component (B3) is preferably polyvinyl butyral.

[0092] When the component (B) includes the component (B1) and the component (B2), the mass ratio of the component (B2) to the component (B1) [(B2) / (B1)] is preferably 0.05 or more, more preferably 0.1 or more, further preferably 0.2 or more, further preferably 0.5 or more, further more preferably 1.0 or more, from the viewpoint of improving the durability and moisture resistance of the coating, and preferably 30 or less, more preferably 20 or less, further preferably 15 or less, further more preferably 12 or less, further more preferably 10 or less, from the viewpoint of improving the durability and moisture resistance of the coating and suppressing the stickiness of the coating. Furthermore, the mass ratio of the component (B2) to the component (B1) [(B2) / (B1)] is preferably 0.05 or more and 30 or less, more preferably 0.1 or more and 20 or less, further preferably 0.2 or more and 15 or less, further more preferably 0.5 or more and 12 or less, further more preferably 1.0 or more and 10 or less.

[0093] When the component (B) contains the component (B1) and the component (B3), the mass ratio of the component (B3) to the component (B1) [(B3) / (B1)] is preferably 0.1 or more, more preferably 0.2 or more, further preferably 0.5 or more, further preferably 1.0 or more, further more preferably 2.0 or more, from the viewpoint of improving the durability and moisture resistance of the coating, and from the viewpoint of suppressing the stickiness of the coating, preferably 20 or less, more preferably 15 or less, further preferably 12 or less, further more preferably 10 or less, further more preferably 8 or less. Furthermore, the mass ratio of the component (B3) to the component (B1) [(B3) / (B1)] is preferably 0.1 or more and 20 or less, more preferably 0.2 or more and 15 or less, further preferably 0.5 or more and 12 or less, further more preferably 1.0 or more and 10 or less, further more preferably 2.0 or more and 8 or less.

[0094] When component (B) contains component (B2) and component (B3), the mass ratio of component (B2) to component (B3) [(B2) / (B3)] is preferably 0.05 or more, more preferably 0.1 or more, further preferably 0.2 or more, further preferably 0.5 or more, further more preferably 1.0 or more, from the viewpoint of improving the durability and moisture resistance of the coating, and preferably 30 or less, more preferably 20 or less, further preferably 15 or less, further more preferably 12 or less, further more preferably 10 or less, from the viewpoint of improving the durability and moisture resistance of the coating and suppressing the stickiness of the coating. Furthermore, from the viewpoint of improving the durability and moisture resistance of the coating, the mass ratio of component (B2) to component (B3) [(B2) / (B3)] is preferably from 0.05 to 30, more preferably from 0.1 to 20, further preferably from 0.2 to 15, further preferably from 0.5 to 12, further preferably from 1.0 to 10.

[0095] Component (B) may also contain water-insoluble polymers other than component (B1), component (B2), and component (B3) within a range that does not impair the effects of the present invention. In particular, from the viewpoint of improving the durability and moisture resistance of the coating, the viewpoint of improving the crystallization inhibition effect of component (A), and the viewpoint of suppressing the stickiness of the coating, the total content of component (B1), component (B2), and component (B3) in component (B) is preferably 50% by mass or more, more preferably 60% by mass or more, further preferably 70% by mass or more, further more preferably 80% by mass or more, further more preferably 90% by mass or more, and is 100% by mass or less.

[0096] <Ingredient (C): Non-volatile base>

[0097] The composition of the present invention contains a non-volatile base (except for the substance corresponding to component (A)) as component (C). It is believed that component (C) contributes to improving the durability and moisture resistance of the coating and improving the crystallization inhibition effect of component (A) by using it in combination with component (B).

[0098] The "non-volatile base" of component (C) is as defined above.

[0099] As the component (C), there may be mentioned a lipophilic base agent, a hydrophilic base agent, an amphiphilic base agent and the like, and one or more of these may be used.

[0100] (Lipophilic base)

[0101] Preferred examples of the lipophilic base include polar oils and nonpolar oils.

[0102] Specific examples of polar oils include nonvolatile 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) glycerol fatty acid triesters.

[0103] (i) The fatty acid monoester composed of a fatty acid and a monohydric alcohol may be a monoester of a saturated fatty acid having 8 to 22 carbon atoms and an aliphatic or aromatic ring-containing monohydric alcohol having 1 to 24 carbon atoms, for example, 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, hexyldecyl dimethyloctanoate and the like.

[0104] (ii) fatty acid monoesters or diesters composed of fatty acids and diols include monoesters or diesters of saturated fatty acids having 8 to 22 carbon atoms and aliphatic or aromatic diols having 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, propylene glycol di(caprylic acid / capric acid) ester, propylene glycol diisostearate, and the like.

[0105] (iii) the dicarboxylic acid diester composed of a dicarboxylic acid and a monohydric alcohol may be a diester of an aliphatic or aromatic dicarboxylic acid having 4 to 18 carbon atoms and an aliphatic or aromatic ring-containing monohydric alcohol having 1 to 24 carbon atoms, for example, di-2-ethylhexyl succinate, diisopropyl adipate, dibutyl adipate, diisobutyl adipate, di-2-hexyldecyl adipate, di-2-heptylundecy1 adipate, diethyl sebacate, diisopropyl sebacate, di-2-ethylhexyl sebacate, diisononyl phthalate, diisostearyl malate, and the like.

[0106] (iv) The tricarboxylic acid triester composed of a tricarboxylic acid and a monohydric alcohol may be a triester of an aliphatic or aromatic tricarboxylic acid having 5 to 12 carbon atoms and an aliphatic or aromatic ring-containing monohydric alcohol having 1 to 24 carbon atoms, for example, triisodecyl trimellitate.

[0107] In addition, (v) glycerol fatty acid triesters include triesters of glycerol and saturated fatty acids having 8 to 22 carbon atoms, such as glycerol tri-2-ethylhexanoate, glycerol trimyristate, glycerol tri-2-heptyl undecanoate, glycerol tristearate, and the like.

[0108] As ester oils other than the above (i) to (v), alkyl benzoate, cetyl lactate, myristyl lactate, lanolin acetate, dipentaerythritol fatty acid ester, glyceryl di-2-heptyl undecanoate, castor oil fatty acid methyl ester, N-lauroyl-L-glutamic acid-2-octyldodecyl ester, etc. can also be used.

[0109] Among the above, as the ester oil, more preferably at least one selected from (i) a fatty acid monoester composed of a fatty acid and a monohydric alcohol, and (ii) a fatty acid monoester or diester composed of a fatty acid and a dihydric alcohol, further preferably at least one selected from a fatty acid monoester composed of a fatty acid and a monohydric alcohol having 1 to 24 carbon atoms, and a saturated fatty acid having 8 to 22 carbon atoms and an aliphatic or aromatic dihydric alcohol having 1 to 12 carbon atoms, and further more preferably at least one selected from isopropyl myristate and propylene glycol monocaprate.

[0110] Specific examples of the nonpolar oil include nonvolatile hydrocarbon oils, silicone oils, fluorinated oils, etc. Examples of the hydrocarbon oil include liquid paraffin and squalane, examples of the silicone oil include dimethylpolysiloxane, dimethylcyclopolysiloxane, methylphenylpolysiloxane, methylhydrogenpolysiloxane, and higher alcohol-modified organopolysiloxane, and examples of the fluorinated oil include fluoropolyethers and perfluoroalkylether silicones.

[0111] (Hydrophilic base)

[0112] As the hydrophilic base, one or more selected from polyols and lower amines are preferably used.

[0113] Specific examples of polyols include nonvolatile alkylene glycols, polyalkylene glycols, glycerols, etc. Examples of the alkylene glycols include ethylene glycol, propylene glycol, 1,3-propylene glycol, 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 glycerols include glycerol, diglycerol, triglycerol, etc. Polyethylene glycol, polypropylene glycol, and polyoxyethylene-polyoxypropylene glycol preferably have a weight average molecular weight of less than 10,000.

[0114] In the present specification, the term "lower amine" refers to an amine preferably having a carbon number of 9 or less, and more preferably having a carbon number of 2 or more and 9 or less. The lower amine is preferably an alkanolamine from the viewpoints of non-volatility, improvement of durability and moisture resistance of the coating, improvement of the crystallization inhibition effect of component (A), and inhibition of stickiness of the coating.

[0115] Specific examples of the alkanolamine include triethanolamine, diethanolamine, monoethanolamine, triisopropanolamine, diisopropanolamine, monoisopropanolamine, and 2-amino-2-methylpropanol.

[0116] (Amphiphilic base)

[0117] As the amphiphilic base, preferably, an ionic surfactant or a nonionic surfactant is exemplified, and a nonionic surfactant is preferred.

[0118] Specific examples of the nonionic surfactant include polyoxyethylene alkyl ethers, polyoxyethylene alkenyl ethers, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene fatty acid esters, alkyl glucosides, alkyl glyceryl ethers, sucrose fatty acid esters, polyoxyethylene hydrogenated castor oil, alkyl saccharides, alkyl amine oxides, and alkyl amide amine oxides.

[0119] The alkyl group in polyoxyethylene alkyl ether, alkyl glucoside, alkyl glyceryl ether, alkyl saccharide, alkyl amine oxide, and alkyl amide amine oxide, the alkenyl group in polyoxyethylene alkenyl ether, and the fatty acid in polyoxyethylene sorbitan fatty acid ester, polyoxyethylene fatty acid ester, and sucrose fatty acid ester preferably has 8 to 22 carbon atoms, more preferably 10 to 20 carbon atoms, and even more preferably 12 to 18 carbon atoms.

[0120] Among the above, the nonionic surfactant is preferably at least one selected from polyoxyethylene sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene fatty acid esters, alkyl glucosides, and alkyl glyceryl ethers, and more preferably polyoxyethylene sorbitan fatty acid esters.

[0121] Specific examples of polyoxyethylene sorbitan fatty acid esters include polyoxyethylene sorbitan monolaurate (20 EO) (polysorbate 20), polyoxyethylene sorbitan monostearate (20 EO) (polysorbate 60), polyoxyethylene sorbitan tristearate (20 EO) (polysorbate 65), polyoxyethylene sorbitan oleate (20 EO) (polysorbate 80), and preferably polyoxyethylene sorbitan oleate (20 EO) (polysorbate 80).

[0122] The component (C) may be used alone or in combination of two or more.

[0123] Among the above, component (C) is preferably one or more selected from polar oils, nonpolar oils, polyols, alkanolamines, and nonionic surfactants, more preferably one or more selected from isopropyl myristate, propylene glycol monodecanoate, squalane, 1,3-butylene glycol, dipropylene glycol, polyethylene glycol having a weight average molecular weight of less than 1,000, triethanolamine, diisopropanolamine, 2-amino-2-methylpropanol, and polyoxyethylene sorbitan fatty acid esters, and further preferably contains one or more selected from isopropyl myristate, 1,3-butylene glycol, diisopropanolamine, 2-amino-2-methylpropanol, and polyoxyethylene sorbitan fatty acid esters.

[0124] The amines as the component (C) also include amines constituting the neutralized salt of the water-insoluble polymer as the component (B).

[0125] For example, in the composition of the present invention, as a commercially available product containing component (B) and alkanolamine as component (C), "Plascize L-53P" manufactured by Huying Chemical Industry Co., Ltd., which is a partially neutralized product of (acrylate / diacetone acrylamide) copolymer neutralized with 2-amino-2-methylpropanol, etc. can also be used.

[0126] <Component (D): Volatile solvent>

[0127] The composition of the present invention contains a volatile solvent (except for the substance equivalent to component (A)) as component (D). Component (D) contributes to the improvement of the quick-drying property of the composition, the crystallization inhibition effect of component (A), etc. It is further believed that since the viscosity of the external preparation composition is easily adjusted to a specified range, the spreadability and film formation properties are improved, and the durability and moisture resistance of the formed film are also further improved.

[0128] The "volatile solvent" of the component (D) is as defined above.

[0129] As the component (D), volatile alcohols, ketones, esters, hydrocarbons, silicones and the like may be mentioned.

[0130] The alcohol used as component (D) is preferably a lower alcohol. The so-called "lower alcohol" is preferably an alcohol having 4 or less carbon atoms, and examples thereof include methanol, ethanol, n-propanol, isopropanol, n-butanol, isobutanol, sec-butanol, and tert-butanol.

[0131] 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 polydimethylsiloxane, cyclic siloxane, etc.

[0132] Component (D) can be used alone or in combination of two or more.

[0133] From the viewpoint of improving the spreadability and quick-drying properties of the composition, the solubility or dispersibility of components (A) to (C), and the viewpoint of improving the crystallization inhibition effect of component (A), component (D) is preferably an alcohol having no more than 4 carbon atoms, and more preferably at least one selected from ethanol and isopropyl alcohol.

[0134] <Water>

[0135] The external preparation composition preferably further contains water from the viewpoint of improving the crystallization inhibition effect of component (A) and improving the removability of the film. The water used in the present invention is not particularly limited, and for example, ion exchange water, pure water, distilled water, etc. can be used.

[0136] <Water-soluble polymer>

[0137] The external preparation composition may further contain a water-soluble polymer within a range not impairing the effects of the present invention. The water-soluble polymer is a polymer that is not water-soluble to any of the above components (A) to (D), and examples thereof include carboxyvinyl polymers, polyacrylic acid, and polyvinyl pyrrolidone.

[0138] Among them, from the viewpoint of improving the durability and moisture resistance of the coating, and 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 lower. Specifically, the mass ratio of the water-soluble polymer to the component (B) in the external preparation composition [water-soluble polymer / component (B)] is preferably 2 or less, more preferably 1.5 or less, further preferably 1.3 or less, further preferably 1 or less, further more preferably 0.5 or less, further more preferably 0.1 or less, and further more preferably 0.

[0139] <Other ingredients>

[0140] In addition to the above-mentioned components, the external preparation composition of the present invention may also contain other components usually used in external preparation compositions as appropriate within the scope that does not impair the purpose of the present invention. Such components include, for example, organic acids or inorganic acids, antioxidants, ultraviolet absorbers, preservatives, pH adjusters other than organic acids or inorganic acids, fragrances, pigments, etc.

[0141] <Content>

[0142] The content of each component in the external preparation composition is preferably as follows from the viewpoint of improving the durability and moisture resistance of the film, improving the crystallization inhibitory effect of the component (A), and suppressing the stickiness of the film.

[0143] As the content of the component (A) in the topical agent composition, with respect to the viewpoint of fully showing the effectiveness of the component (A), preferably more than 0.001 mass %, more preferably more than 0.005 mass %, further preferably more than 0.01 mass %, further more preferably more than 0.02 mass %, with respect to the viewpoint that the crystallization inhibition effect of the component (A) is improved, preferably less than 30 mass %, more preferably less than 20 mass %, further preferably less than 15 mass %, further more preferably less than 10 mass %. And, the content of the component (A) in the topical agent composition is preferably less than 30 mass %, more preferably less than 20 mass %, further preferably less than 20 mass %, further preferably less than 0.01 mass % and less than 15 mass %, further more preferably less than 10 mass % and less than 0.02 mass %.

[0144] When component (A) contains an anti-inflammatory and analgesic component, the content of the anti-inflammatory and analgesic component in the external preparation composition is preferably from 0.01 mass % to 30 mass %, more preferably from 0.02 mass % to 20 mass %, further preferably from 0.05 mass % to 15 mass %, further more preferably from 0.05 mass % to 10 mass %, further more preferably from 0.05 mass % to 6.0 mass %.

[0145] When component (A) contains a local irritant component, the content of the local irritant component in the external preparation composition is preferably from 0.001 mass % to 20 mass %, more preferably from 0.005 mass % to 15 mass %, further preferably from 0.01 mass % to 10 mass %, further more preferably from 0.01 mass % to 6.0 mass %.

[0146] When component (A) contains a blood circulation promoting component, the content of the blood circulation promoting component in the external preparation composition is preferably from 0.1 mass % to 30 mass %, more preferably from 0.5 mass % to 20 mass %, further preferably from 1.0 mass % to 15 mass %, further more preferably from 1.0 mass % to 5.0 mass %.

[0147] When component (A) contains an antihistamine component, the content of the antihistamine component in the external preparation composition is preferably 0.01 mass % to 30 mass %, more preferably 0.02 mass % to 20 mass %, further preferably 0.05 mass % to 15 mass %, further more preferably 0.05 mass % to 10 mass %, further more preferably 0.1 mass % to 5.0 mass %, further more preferably 0.1 mass % to 3.0 mass %.

[0148] When component (A) contains a herbal medicinal ingredient, the content of the herbal medicinal ingredient in the external preparation composition is preferably 0.01 mass % to 30 mass %, more preferably 0.02 mass % to 20 mass %, further preferably 0.05 mass % to 15 mass %, further preferably 0.05 mass % to 10 mass %, further more preferably 0.1 mass % to 5.0 mass %, further more preferably 0.1 mass % to 3.0 mass %.

[0149] When component (A) contains an antipruritic ingredient, the content of the antipruritic ingredient in the external preparation composition is preferably 0.01 mass % to 30 mass %, more preferably 0.02 mass % to 20 mass %, further preferably 0.02 mass % to 15 mass %, further more preferably 0.02 mass % to 10 mass %.

[0150] When component (A) contains a local anesthetic component, the content of the local anesthetic component in the external preparation composition is preferably 0.01 mass % to 30 mass %, more preferably 0.02 mass % to 20 mass %, even more preferably 0.02 mass % to 15 mass %, even more preferably 0.02 mass % to 10 mass %, even more preferably 0.02 mass % to 5.0 mass %.

[0151] When component (A) contains a keratin softening component, the content of the keratin softening component in the external preparation composition is preferably 0.1 mass % to 30 mass %, more preferably 0.2 mass % to 20 mass %, and even more preferably 0.5 mass % to 20 mass %.

[0152] When component (A) contains a bactericidal component, the content of the bactericidal component in the external preparation composition is preferably from 0.001 mass % to 20 mass %, more preferably from 0.005 mass % to 15 mass %, further preferably from 0.01 mass % to 10 mass %, further more preferably from 0.01 mass % to 5.0 mass %, further more preferably from 0.01 mass % to 3.0 mass %.

[0153] When component (A) contains an antibacterial / antifungal component, the content of the antibacterial / antifungal component in the external preparation composition is preferably 0.001 mass % to 20 mass %, more preferably 0.005 mass % to 15 mass %, further preferably 0.01 mass % to 10 mass %, further more preferably 0.02 mass % to 5.0 mass %, further more preferably 0.05 mass % to 3.0 mass %.

[0154] When component (A) contains an immunosuppressant, the content of the immunosuppressant in the external preparation composition is preferably 0.01 mass % to 1 mass %, more preferably 0.03 mass % to 0.5 mass %.

[0155] When component (A) contains an antiviral component, the content of the antiviral component in the external preparation composition is preferably from 0.1 mass % to 20 mass %, more preferably from 0.5 mass % to 15 mass %, further preferably from 1.0 mass % to 10 mass %, further more preferably from 1.0 mass % to 5.0 mass %.

[0156] When component (A) contains a hair growth / revitalizing component, the content of the hair growth / revitalizing component in the external preparation composition is preferably from 0.1 mass % to 20 mass %, more preferably from 0.5 mass % to 15 mass %, further preferably from 1.0 mass % to 10 mass %, further more preferably from 1.0 mass % to 5.0 mass %.

[0157] When component (A) contains a sebum suppressing ingredient, the content of the sebum suppressing ingredient in the external preparation composition is preferably 0.001 mass % to 20 mass %, more preferably 0.005 mass % to 15 mass %, further preferably 0.01 mass % to 10 mass %, further more preferably 0.01 mass % to 5.0 mass %, further more preferably 0.01 mass % to 3.0 mass %.

[0158] When component (A) contains an antiperspirant component, the content of the antiperspirant component in the external preparation composition is preferably from 0.1 mass % to 20 mass %, more preferably from 0.5 mass % to 15 mass %, further preferably from 1.0 mass % to 10 mass %, further more preferably from 2.0 mass % to 5.0 mass %.

[0159] When component (A) contains a whitening component, the content of the whitening component in the external preparation composition is preferably from 0.01 mass % to 30 mass %, more preferably from 0.02 mass % to 20 mass %, further preferably from 0.05 mass % to 15 mass %, further more preferably from 0.1 mass % to 10 mass %, further more preferably from 0.2 mass % to 5.0 mass %.

[0160] As the content of the component (B) in the topical agent composition, with respect to the viewpoint that film formation improves, the durability of the film and the viewpoint that moisture resistance improves, preferably 0.01 mass % or more, more preferably 0.05 mass % or more, and further preferably 0.1 mass % or more, and further preferably 0.5 mass % or more, and further more preferably 1.0 mass % or more, with respect to the viewpoint that the durability of the film improves and the viewpoint that the stickiness of the film is suppressed, preferably 30 mass % or less, more preferably 25 mass % or less, and further preferably 20 mass % or less, and further more preferably 15 mass % or less, and further more preferably 10 mass % or less. And, the content of the component (B) in the topical agent composition is preferably 0.01 mass % or more and 30 mass % or less, more preferably 0.05 mass % or more and 25 mass % or less, and further preferably 0.1 mass % or more and 20 mass % or less, and further more preferably 0.5 mass % or more and 15 mass % or less, and further more preferably 1.0 mass % or more and 10 mass % or less.

[0161] When component (B) contains component (B1), the content of component (B1) in the external preparation composition is preferably 0.002 mass% or more, more preferably 0.005 mass% or more, further preferably 0.01 mass% or more, further more preferably 0.02 mass% or more, further more preferably 0.05 mass% or more, further more preferably 0.1 mass% or more, further more preferably 0.2 mass% or more, and is preferably 20 mass% or less, more preferably 15 mass% or less, further preferably 10 mass% or less, further more preferably 8 mass% or less, further more preferably 5 mass% or less. Furthermore, the content of component (B1) in the external preparation composition is preferably from 0.002 mass % to 20 mass %, more preferably from 0.005 mass % to 15 mass %, further preferably from 0.01 mass % to 10 mass %, further preferably from 0.02 mass % to 8 mass %, further more preferably from 0.05 mass % to 5 mass %, further more preferably from 0.1 mass % to 5 mass %, further more preferably from 0.2 mass % to 5 mass %.

[0162] When component (B) contains component (B2), the content of component (B2) in the external preparation composition is preferably 0.003 mass% or more, more preferably 0.005 mass% or more, further preferably 0.01 mass% or more, further more preferably 0.02 mass% or more, further more preferably 0.05 mass% or more, further more preferably 0.1 mass% or more, further more preferably 0.2 mass% or more, further more preferably 0.4 mass% or more, further more preferably 0.5 mass% or more, further more preferably 0.6 mass% or more, and is preferably 25 mass% or less, more preferably 20 mass% or less, further preferably 15 mass% or less, further more preferably 10 mass% or less, further more preferably 8 mass% or less. Furthermore, the content of component (B2) in the external preparation composition is preferably from 0.003 mass % to 25 mass %, more preferably from 0.005 mass % to 25 mass %, further preferably from 0.01 mass % to 20 mass %, further more preferably from 0.02 mass % to 20 mass %, further more preferably from 0.05 mass % to 15 mass %, further more preferably from 0.1 mass % to 15 mass %, further more preferably from 0.2 mass % to 10 mass %, further more preferably from 0.4 mass % to 10 mass %, further more preferably from 0.5 mass % to 8 mass %, further more preferably from 0.6 mass % to 8 mass %.

[0163] When component (B) contains component (B3), the content of component (B3) in the external preparation composition is preferably 0.002 mass% or more, more preferably 0.005 mass% or more, further preferably 0.01 mass% or more, further more preferably 0.02 mass% or more, further more preferably 0.05 mass% or more, further more preferably 0.1 mass% or more, further more preferably 0.2 mass% or more, further more preferably 0.4 mass% or more, further more preferably 0.5 mass% or more, further more preferably 0.6 mass% or more, and is preferably 20 mass% or less, more preferably 15 mass% or less, further preferably 10 mass% or less, further more preferably 8 mass% or less. Furthermore, the content of component (B3) in the external preparation composition is preferably from 0.002 mass % to 20 mass %, more preferably from 0.005 mass % to 20 mass %, further preferably from 0.01 mass % to 15 mass %, further more preferably from 0.02 mass % to 15 mass %, further more preferably from 0.05 mass % to 15 mass %, further more preferably from 0.1 mass % to 10 mass %, further more preferably from 0.2 mass % to 10 mass %, further more preferably from 0.4 mass % to 10 mass %, further more preferably from 0.5 mass % to 8 mass %, further more preferably from 0.6 mass % to 8 mass %.

[0164] As the content of the component (C) in the topical agent composition, with respect to the viewpoint that the film formation improves, the durability of the film and the viewpoint that the moisture resistance improves, preferably 0.001 mass % or more, more preferably 0.005 mass % or more, and further preferably 0.01 mass % or more, and further preferably 0.05 mass % or more, and further more preferably 0.1 mass % or more, with respect to the viewpoint that the stickiness of the film is suppressed, preferably 40 mass % or less, more preferably 30 mass % or less, and further preferably 20 mass % or less, and further more preferably 15 mass % or less. And, the content of the component (C) in the topical agent composition is preferably 0.001 mass % or more and 40 mass % or less, more preferably 0.005 mass % or more and 30 mass % or less, and further preferably 0.01 mass % or more and 20 mass % or less, and further more preferably 0.05 mass % or more and 20 mass % or less, and further more preferably 0.1 mass % or more and 15 mass % or less.

[0165] As the content of the component (D) in the topical agent composition, with respect to the viewpoint that the smearability and quick-drying property of the composition, the durability and moisture resistance of the coating, and the crystallization inhibition effect of the component (A) are improved, preferably more than 10 mass %, more preferably more than 20 mass %, and then preferably more than 30 mass %, and then more preferably more than 40 mass %, with respect to the smearability of the composition and the viewpoint of the coating formation, preferably less than 95 mass %, more preferably less than 90 mass %, and then preferably less than 80 mass %, and then more preferably less than 70 mass %. And, the content of the component (D) in the topical agent composition is preferably less than 10 mass % and less than 95 mass %, more preferably less than 20 mass % and less than 90 mass %, and then preferably less than 30 mass % and less than 80 mass %, and then more preferably less than 40 mass % and less than 70 mass %.

[0166] As the total content of components (A) to (D) in the external agent composition, from the viewpoint of improving the durability and moisture resistance of the coating, the viewpoint of improving the crystallization inhibition effect of component (A), and the viewpoint of suppressing the stickiness of the coating, it is preferably 20% by mass or more, more preferably 30% by mass or more, and further preferably 50% by mass or more, and further preferably 60% by mass or more, and preferably 100% by mass or less, preferably 97% by mass or less, more preferably 95% by mass or less, and further preferably 90% by mass or less. In addition, the total content of components (A) to (D) in the external agent composition is preferably 20% by mass or more and 100% by mass or less, more preferably 30% by mass or more and 97% by mass or less, further preferably 50% by mass or more and 95% by mass or less, and further preferably 60% by mass or more and 90% by mass or less.

[0167] When the external preparation composition contains water, the content of water in the external preparation composition is preferably 1% by mass or more, more preferably 2% by mass or more, further preferably 3% by mass or more, further preferably 5% by mass or more, further preferably 7% by mass or more, further preferably 8% by mass or more, further preferably 10% by mass or more, further more preferably 15% by mass or more, from the viewpoint of improving the spreadability of the external preparation composition, the film forming property, the durability and moisture resistance of the film, the crystallization inhibitory effect of the component (A), the stickiness of the film, and the removability of the film, and is preferably 70% by mass or less, more preferably 60% by mass or less, further preferably 50% by mass or less, further more preferably 45% by mass or less, further more preferably 40% by mass or less, further more preferably 38% by mass or less, further more preferably 35% by mass or less, from the viewpoint of improving the quick-drying property of the composition, the durability and moisture resistance of the film, the crystallization inhibitory effect of the component (A), and the stickiness of the film. Furthermore, the water content in the external preparation composition is preferably from 1 mass % to 70 mass %, more preferably from 2 mass % to 60 mass %, even more preferably from 3 mass % to 50 mass %, even more preferably from 5 mass % to 45 mass %, even more preferably from 7 mass % to 40 mass %, even more preferably from 8 mass % to 38 mass %, even more preferably from 10 mass % to 35 mass %, even more preferably from 15 mass % to 35 mass %.

[0168] The mass ratio of component (A) to component (B) [(A) / (B)] in the external preparation composition 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 improving the crystallization inhibitory effect of component (A); and is preferably 300 or less, more preferably 250 or less, even more preferably 200 or less, even more preferably 100 or less, even more preferably 50 or less, even more preferably 30 or less, even more preferably 20 or less, even more preferably 10 or less, even more preferably 5 or less, and even more preferably 2 or less, from the viewpoint of improving the spreadability and film-forming properties of the composition, improving the durability and moisture resistance of the film, and improving the crystallization inhibitory effect of component (A). Furthermore, the mass ratio of component (A) to component (B) in the external preparation composition [(A) / (B)] is preferably 0.001 to 300, more preferably 0.001 to 250, further preferably 0.002 to 200, further preferably 0.002 to 100, further preferably 0.002 to 50, further more preferably 0.002 to 30, further more preferably 0.002 to 20, further more preferably 0.002 to 10, further more preferably 0.002 to 5, further more preferably 0.003 to 2.

[0169] The mass ratio of component (A) to component (C) [(A) / (C)] in the external preparation composition is preferably 0.001 or more, more preferably 0.002 or more, further preferably 0.003 or more, further preferably 0.005 or more, further more preferably 0.01 or more, from the viewpoint of fully expressing the efficacy of component (A) and improving the crystallization inhibitory effect of component (A); and is preferably 100 or less, more preferably 80 or less, further preferably 70 or less, further preferably 60 or less, further more preferably 50 or less, further more preferably 45 or less, from the viewpoint of improving the spreadability and film-forming properties of the composition, improving the durability and moisture resistance of the film, and improving the crystallization inhibitory effect of component (A). Furthermore, the mass ratio of component (A) to component (C) in the external preparation composition [(A) / (C)] is preferably 0.001 to 100, more preferably 0.002 to 80, further preferably 0.003 to 70, further preferably 0.005 to 60, further more preferably 0.01 to 50, further more preferably 0.01 to 45.

[0170] The mass ratio of component (C) to component (B) in the external preparation 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 film, and preferably 50 or less, more preferably 35 or less, even more preferably 20 or less, even more preferably 10 or less, and even more preferably 5.0 or less from the viewpoint of improving the durability and moisture resistance of the film and suppressing the stickiness of the film. Furthermore, the mass ratio of component (C) to component (B) in the external preparation composition [(C) / (B)] is preferably 0.01 or more and 50 or less, more preferably 0.01 or more and 35 or less, even more preferably 0.02 or more and 20 or less, even more preferably 0.02 or more and 10 or less, and even more preferably 0.03 or more and 5.0 or less.

[0171] The mass ratio of component (A) to the total content of component (B) and component (C) in the external preparation composition [(A) / {(B)+(C)}] is preferably 0.001 or more, more preferably 0.005 or more, further preferably 0.01 or more, further preferably 0.02 or more, further more preferably 0.03 or more, from the viewpoint of fully expressing the efficacy of component (A), and is preferably 20 or less, more preferably 15 or less, further preferably 10 or less, further more preferably 5.0 or less, further more preferably 4.0 or less, further more preferably 3.0 or less, from the viewpoint of improving the durability and moisture resistance of the coating and the effect of improving the crystallization inhibition of component (A). Furthermore, the mass ratio of component (A) to the total content of component (B) and component (C) in the external preparation composition [(A) / {(B)+(C)}] is preferably from 0.001 to 20, more preferably from 0.005 to 15, further preferably from 0.01 to 10, further preferably from 0.02 to 5.0, further preferably from 0.03 to 4.0, further preferably from 0.03 to 3.0.

[0172] When the external preparation composition contains water, the mass ratio of water to component (D) in the external preparation composition [water / (D)] is preferably 0.005 or more, more preferably 0.05 or more, further preferably 0.10 or more, further preferably 0.20 or more, further more preferably 0.50 or more, from the viewpoint of improving the durability and moisture resistance of the film, improving the crystallization inhibitory effect of component (A), suppressing the stickiness of the film, and improving the removability of the film, and is preferably 10 or less, more preferably 8.0 or less, further preferably 5.0 or less, further more preferably 3.0 or less, further more preferably 2.0 or less, further more preferably 1.0 or less, further more preferably 0.7 or less, from the viewpoint 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 the stickiness of the film. Furthermore, the mass ratio of water to component (D) in the external preparation composition [water / (D)] is preferably 0.005 to 10, more preferably 0.05 to 8.0, even more preferably 0.10 to 5.0, even more preferably 0.20 to 3.0, even more preferably 0.50 to 3.0, even more preferably 0.50 to 2.0, even more preferably 0.50 to 1.0, even more preferably 0.50 to 0.7.

[0173] As the mass ratio [(B) / (D)] of the component (B) to the component (D) in the external preparation composition, from the viewpoint of improving the film forming property, it is preferably 0.0001 or more, more preferably 0.0002 or more, further preferably 0.0005 or more, further more preferably 0.001 or more, and from the viewpoint of improving the spreadability and quick-drying property of the composition, it is preferably 1.0 or less, more preferably 0.50 or less, further preferably 0.30 or less, further more preferably 0.20 or less, further more preferably 0.10 or less. In addition, the mass ratio [(B) / (D)] of the component (B) to the component (D) in the external preparation composition is preferably 0.0001 or more and 1.0 or less, more preferably 0.0002 or more and 0.50 or less, further preferably 0.0005 or more and 0.30 or less, further more preferably 0.001 or more and 0.20 or less, further more preferably 0.001 or more and 0.10 or less.

[0174] <Viscosity>

[0175] The viscosity of the external preparation 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 still more preferably 3.0 mPa·s or more from the viewpoint of improving the spreadability of the composition. In addition, from the viewpoint of improving the quick-drying property of the composition and improving 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, and preferably 7,500 mPa·s or less. 0 mPa·s or less, more preferably 5,000 mPa·s or less, further preferably 3,000 mPa·s or less, further more preferably 2,000 mPa·s or less, further more preferably 1,000 mPa·s or less, further more preferably 700 mPa·s or less, further more preferably 500 mPa·s or less, further more preferably 200 mPa·s or less, further more preferably 100 mPa·s or less, further more preferably 50 mPa·s or less. Furthermore, the viscosity of the external preparation composition at 25°C is from 1.0 mPa·s to 10,000 mPa·s, preferably from 1.0 mPa·s to 7,500 mPa·s, more preferably from 1.5 mPa·s to 5,000 mPa·s, further preferably from 1.5 mPa·s to 3,000 mPa·s, further preferably from 1.5 mPa·s to 2,000 mPa·s, further preferably from 2.0 mPa·s to 1,000 mPa·s, further more preferably from 2.0 mPa·s to 700 mPa·s, further more preferably from 2.0 mPa·s to 500 mPa·s, further more preferably from 3.0 mPa·s to 200 mPa·s, further more preferably from 3.0 mPa·s to 100 mPa·s, further more preferably from 3.0 mPa·s to 50 mPa·s.

[0176] The viscosity of the external preparation composition at 25° C. is a value measured by a vibration viscometer for a composition of 1,000 mPa·s or less, and a value measured by a B-type rotational viscometer for a composition of more than 1,000 mPa·s. Specifically, it can be measured by the method described in Examples.

[0177] <Contact angle>

[0178] From the viewpoint of improving the spreadability, film formation, and durability of the film of the composition, the contact angle of the external agent composition relative to the artificial leather after dripping for 10 seconds is preferably 5° or more, more preferably 10° or more, further preferably 15° or more, further preferably 20° or more, further more preferably 25° or more, and preferably 80° or less, more preferably 75° or less, more preferably 70° or less, more preferably 60° or less, and further preferably 55° or less. In addition, the contact angle of the external agent composition relative to the artificial leather after dripping for 10 seconds is preferably 5° or more and 80° or less, more preferably 10° or more and 75° or less, further preferably 15° or more and 70° or less, further more preferably 20° or more and 60° or less, further more preferably 25° or more and 55° or less. In addition, the contact angle of the composition relative to the artificial leather after dripping for 60 seconds is preferably 5° or more, more preferably 10° or more, further preferably 15° or more, further more preferably 18° or more, further more preferably 20° or more, and preferably 70° or less, more preferably 65° or less, more preferably 60° or less, more preferably 55° or less, and further preferably 50° or less. In addition, the contact angle of the external preparation composition relative to the artificial leather after dripping for 60 seconds is preferably 5° or more and 70° or less, more preferably 10° or more and 65° or less, further preferably 15° or more and 60° or less, further more preferably 18° or more and 55° or less, further more preferably 20° or more and 50° or less.

[0179] In addition, as the ratio of the change of the contact angle after 10 seconds to 60 seconds of dripping of the external preparation composition relative to the artificial leather (1-((contact angle after dripping 60 seconds) / (contact angle after dripping 10 seconds))), from the viewpoint of improving the spreadability, film formation, and durability of the film of the composition, it is preferably 0.6 or less, more preferably 0.5 or less, further preferably 0.4 or less, further more preferably 0.3 or less, and further more preferably 0.25 or less. The above-mentioned contact angle can be measured by the method described in the examples at a temperature of 25°C.

[0180] <Dosage form, etc.>

[0181] The external preparation composition of the present invention is preferably used as an external preparation composition for skin.

[0182] The dosage form of the external preparation composition can be any form as long as it has a viscosity within the above range and can be applied to the skin. For example, it can be: an emulsion preparation, a gel preparation, an ointment preparation, a cream preparation, or a foam preparation composed of the external preparation composition of the present invention; an aerosol preparation or a pump spray preparation using the external preparation composition of the present invention. As a foam preparation, it can be exemplified by a preparation in which the external preparation composition of the present invention is filled in a pump bubbler, etc., and sprayed in a foamy state.

[0183] Alternatively, the composition of the present invention may be electrostatically sprayed onto the skin using an electrostatic spray device. Electrostatic spraying is described below.

[0184] The aerosol preparation contains the above-mentioned external preparation composition and a propellant. The aerosol preparation using the external preparation composition of the present invention can provide a cooling sensation or the like by spraying the composition on the skin.

[0185] In the aerosol preparation, the external preparation composition used as the aerosol stock solution and its preferred embodiment are the same as described above. That is, the contents of the components (A) to (D) in the aerosol stock solution and the viscosity of the aerosol stock solution are preferably within the above ranges.

[0186] Examples of propellants used in aerosol preparations include liquefied petroleum gas (LPG) such as ethane, propane, n-butane, isobutane, isopentane, and mixtures thereof; ethers such as dimethyl ether (DME); compressed gases such as nitrogen and carbon dioxide, and one or more of these may be used.

[0187] In an aerosol preparation, there is no particular limitation on the amount ratio of the external agent composition as an aerosol stock solution to the propellant, as long as the external agent composition can be sprayed on the skin. From the viewpoint of aerosol performance and the stability of the aerosol preparation, the mass ratio of the external agent composition to the propellant is preferably in the range of 1:0.01 to 1:10, and more preferably in the range of 1:0.05 to 1:7.5.

[0188] When the propellant is LPG, the mass ratio of the external agent composition to LPG is more preferably 1:0.5 to 1:5, when the propellant is dimethyl ether, the mass ratio of the external agent 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 external agent composition to carbon dioxide is more preferably 1:0.1 to 1:0.5.

[0189] As aerosol containers for aerosol preparations, there can be mentioned known pressure-resistant containers made of metal, plastic, etc., and double-structured containers containing an inner bag inside the pressure-resistant container. In the double-structured container, it is preferred that the external preparation composition as an aerosol stock solution is filled in the inner bag, and the propellant is filled between the pressure-resistant container and the inner bag.

[0190] The method for preparing the aerosol preparation is not particularly limited, and can be prepared, for example, by filling the above-mentioned aerosol container with the external preparation composition as an aerosol stock solution, attaching a valve, and then filling the valve portion with a propellant.

[0191] The pump spray type preparation is a preparation obtained by filling the external preparation composition of the present invention in a pump spray container for use.

[0192] [How to use]

[0193] The present invention also provides a method for using the external preparation composition comprising the following steps (I) and (II) in sequence.

[0194] Step (I): a step of applying the external preparation composition to an object, followed by drying to form a film composed of the external preparation composition;

[0195] Step (II): a step of bringing the film into contact with a cleaning agent and then washing with water to remove the film.

[0196] According to the method of the present invention, in step (I), the above-mentioned topical agent composition is applied to an object, followed by drying, so that a film containing a component (A) as a pharmaceutical ingredient can be formed on the surface of the object. The film is excellent in durability and moisture resistance, and therefore the sustained-release component (A) can be continuously released to the object. In addition, the above-mentioned film can be rinsed with water using a detergent, so the film formed in the process (I) can be easily removed from the object by carrying out process (II).

[0197] <Step (I)>

[0198] The method for applying the external preparation composition to the object in step (I) can be appropriately selected according to the dosage form of the external preparation composition, and examples thereof include methods of application by coating, casting, spraying, etc. Among these, application by coating or spraying is preferred. After the external preparation composition is applied, component (D) is volatilized by natural drying, etc., to form a film containing components (A) to (C) on the surface of the object.

[0199] When applying the external preparation composition directly to the skin, the external preparation composition can be applied by hand or using an application tool such as a metal roller, a plastic roller, a sponge-like porous body, or a pen.

[0200] When the external agent composition is sprayed on the skin, the spraying method of the composition may be, for example, a method using an aerosol, a pump spray, or an electrostatic spray device. Regarding aerosol and pump spray, the external agent composition may be used as a stock solution to prepare the above-mentioned aerosol preparation or pump spray preparation, and the external agent composition may be sprayed on the object using the preparation.

[0201] The electrostatic spray device specifically comprises: a container capable of accommodating the external agent composition, a nozzle for ejecting the external agent composition, a power supply for applying voltage to the nozzle, and a mechanism for transporting the external agent composition from the container to the nozzle. As one embodiment thereof, a handheld type electrostatic spray device having a size that can be held in one hand can be exemplified.

[0202] As the electrostatic spray device, a device exemplified in International Publication No. 2018 / 194140 etc. can be used.

[0203] The object to which the external preparation composition is applied is preferably the skin surface.

[0204] The application site of the external preparation composition is not particularly limited, but is preferably the skin surface of the head, face, neck, hands, arms, feet, legs, buttocks or trunk.

[0205] The amount of the external preparation composition to be applied is not particularly limited, but 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 film, 100 μL / cm 2 Less than, more preferably 50 μL / cm 2 the following.

[0206] The method for drying the external preparation composition after application to the object is preferably natural drying, but a dryer or the like may be used as appropriate.

[0207] As the thickness of the film formed in step (I), from the viewpoint of the ease of forming the film and the viewpoint of improving durability, it is preferably 0.005 mm or more, more preferably 0.01 mm or more, further preferably 0.015 mm or more, further more preferably 0.02 mm or more, and preferably 0.3 mm or less, more preferably 0.1 mm or less, further preferably 0.07 mm or less, further more preferably 0.06 mm or less. In addition, the thickness of the film formed in step (I) is preferably 0.005 mm or more and 0.3 mm or less, more preferably 0.01 mm or more and 0.1 mm or less, further preferably 0.015 mm or more and 0.07 mm or less, further more preferably 0.02 mm or more and 0.06 mm or less. Specifically, the thickness of the film can be measured by the method described in the examples.

[0208] <Step (II)>

[0209] In step (II), the film formed in step (I) is brought into contact with a cleaning agent and then washed with water to remove the film.

[0210] Step (II) is preferably performed after a certain period of time has passed since a film is formed on the surface of the object by step (I), that is, after the effect of component (A) has been exerted. From this viewpoint, the time from step (I) to step (II) is preferably from 0.5 hours to 72 hours, and more preferably from 1 hour to 48 hours.

[0211] The cleaning agent used in step (II) can be any cleaning agent used for cleaning the object. For example, a cleaning agent containing anionic, cationic, or nonionic surfactant components, or a cleaning agent containing an organic solvent can be mentioned, and as specific examples thereof, synthetic detergents, soaps, etc. can be mentioned. When the skin as the object is the scalp, shampoo can be mentioned as the cleaning agent, and when it is the face, facial cleanser can be mentioned. As cleaning agents for skin other than these, soap, hand soap, shower gel, etc. can be mentioned. As the pH value of the cleaning agent, a pH value less than 3 (acidic), a pH value of 3 to 6 (weakly acidic), and a pH value exceeding 6 can be mentioned. From the viewpoint of the removability of the film and the viewpoint of less irritation to the skin, the cleaning agent is preferably a cleaning agent with a pH value of 3 to 6 (weakly acidic), or a cleaning agent with a pH value exceeding 6, and more preferably a cleaning agent with a pH value exceeding 6.

[0212] The pH value of the cleaning agent means the pH value of a 5% aqueous solution at 20°C.

[0213] One embodiment of the method for removing the film formed on the skin surface in step (II) is described. First, the above-mentioned cleanser is brought into contact with the film formed on the skin surface by smearing, casting, spraying, etc. In the case where the cleanser is a solid cleanser such as soap, it is preferred to wet the film on the skin surface or the solid cleanser with water in advance and then bring the two into contact. Alternatively, the cleanser may be foamed in advance and then brought into contact with the film.

[0214] The cleaning agent that has come into contact with the film is allowed to fuse with the film and then washed with water. It is preferred to scrub the film during washing with water. This operation can easily remove the film.

[0215] Example

[0216] Hereinafter, the present invention will be described by way of examples, but the present invention is not limited to the scope of the examples. In addition, in the present examples, various measurements and evaluations were performed by the following methods.

[0217] (Viscosity)

[0218] The viscosity of the external preparation composition at 25°C was measured using a vibration viscometer ("VM-10AL" manufactured by Sekonic Co., Ltd.). In addition, for compositions having a viscosity exceeding 1,000 mPa·s, a B-type rotational viscometer ("TVB-10" manufactured by Toki Sangyo Co., Ltd., SPINDLE: M3, rotation speed: 12 rpm) was used for measurement.

[0219] (Presence or absence of crystals in the film)

[0220] Using Microman (Gilson), 18 μL of the topical composition was applied to an area of ​​1.5 cm × 2 cm on a glass slide and dried on a hot plate ("ceramic hot plate" manufactured by AS ONE (Strain)) set at 32°C for 1 hour. The presence or absence of crystals in the formed film was evaluated by polarizing microscope observation and judged according to the following criteria. The higher the score, the more difficult it is for the crystalline active ingredient to precipitate.

[0221] 5: No crystals were observed at all, 4: Crystals smaller than about 10 μm were observed, 3: Crystals larger than about 10 μm and smaller than 50 μm were observed, 2: Crystals larger than about 50 μm and smaller than 100 μm were observed, 1: Crystals larger than about 100 μm were observed

[0222] (The sticky feeling of the film)

[0223] The panelists were asked to apply 18 μL of the topical composition to an area of ​​1.5 cm × 2 cm on the inner side of the forearm using Microman (manufactured by Gilson), and the stickiness after 2 minutes was evaluated on a 5-level scale. The average of the scores of the 6 panelists (rounded to the second decimal place) is shown in the table. A higher score means a better evaluation result.

[0224] 5: No stickiness at all, 4: Slightly sticky, 3: Slightly sticky, 2: Sticky, 1: Very sticky

[0225] (Durability of coating)

[0226] Ask the panelists to apply 18 μL of the topical composition to an area of ​​1.5 cm × 2 cm on the inner side of the forearm using Microman (Gilson). After application, perform daily activities at an intensity of 3 METs or less in a room at a temperature below 30°C, and visually observe the formed film after a certain period of time to confirm the presence or absence of the remaining film. The longest time to confirm that more than 90% of the film remains is scored according to the following criteria.

[0227] 5: 8 hours later, 4: 4 hours later, 3: 1 hour later, 2: 30 minutes later, 1: 10 minutes later

[0228] (Moisture resistance of the film)

[0229] A professional panelist was asked to apply 50 μL of the external preparation composition to an area of ​​2 cm×2 cm on the inner side of the forearm using a Microman (manufactured by Gilson) and allowed to dry naturally for 10 minutes. After that, the patient was allowed to rest in a constant temperature and humidity chamber at 40°C and 75% for 10 minutes, and the remaining state of the coating when the applied part was rubbed 10 times with a finger was visually observed. The moisture resistance of the coating was determined according to the following criteria.

[0230] 5: No wrinkles or peeling at all, 100% of the film remains; 4: Almost no wrinkles or peeling, more than 90% of the film remains; 3: Slightly wrinkled or peeling, more than 80% of the film remains; 2: Slightly wrinkled or peeling, more than 50% and less than 80% of the film remains; 1: Many wrinkles or peeling, less than 50% of the film remains

[0231] Examples 1 to 102, Comparative Examples 1 to 8 (Preparation and Evaluation of External Use Compositions)

[0232] Component (B) and other components listed in the table were mixed with component (C), component (D), and an appropriate amount of water, and then component (A) was mixed in. Thereafter, the remaining water was mixed in to prepare an external preparation composition.

[0233] The obtained external preparation composition was used for evaluation by the above method. The main components used are shown in Table 1, and the composition of the external preparation composition and the evaluation results are shown in Tables 2 to 11. The blending amount described in each table is the effective ingredient amount (mass %) of each component.

[0234] [Table 1]

[0235]

[0236] [Table 2]

[0237]

[0238] [Table 3]

[0239]

[0240] [Table 4]

[0241]

[0242] [Table 5]

[0243]

[0244] [Table 6]

[0245]

[0246] [Table 7]

[0247]

[0248] [Table 8]

[0249]

[0250] [Table 9]

[0251]

[0252] [Table 10]

[0253]

[0254] [Table 11]

[0255]

[0256] From Tables 2 to 11, it can be seen that the durability and moisture resistance of the coating of the external preparation composition of this Example are good, and the crystallization suppressing effect of the component (A) and the stickiness suppressing effect of the coating are also high.

[0257] In contrast, in Comparative Example 1 not containing component (B), Comparative Examples 2 to 6 in which component (B) does not contain two or more selected from components (B1) to (B3), Comparative Example 7 not containing component (C), and Comparative Example 8 not containing component (D), the effects of the present invention were poor in any of the items.

[0258] In addition, the thickness of the films formed in Examples 1, 2, 4, 7, 12 and 15 using the combination of (B1) cellulose polymer and (B2) acrylic polymer, Example 19 using the combination of (B1) cellulose polymer and (B3) vinyl polymer, and Example 27 using the combination of (B2) acrylic polymer and (B3) vinyl polymer was measured by the following method. The thickness of the films in Examples 1, 2, 4, 7, 9, 12, 13, 15, 19 and 27 was 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.

[0259] (Thickness of coating)

[0260] The external preparation composition was added at 20 μL / cm 2 The film was applied to a polyvinyl chloride insulating tape ("Lead-Removing Type J3447" manufactured by Nitoms Co., Ltd.) and dried on a hot plate heated to 32°C for 10 minutes. The film obtained after drying was peeled off with tweezers, and the thickness of the film was measured using a digital micrometer ("ID-C112XBS" manufactured by Mitutoyo, minimum scale: 0.001 mm).

[0261] Furthermore, regarding Examples 1 to 3 and Comparative Examples 5 to 6, the removability of the film formed using the external preparation composition was evaluated by the following method.

[0262] (Removability of film)

[0263] Have a professional panelist use Microman (manufactured by Gilson) to apply 50 μL of the external agent composition to an area of ​​2 cm × 2 cm on the inner side of the forearm and let it dry naturally for 10 minutes. Afterwards, immerse it in a water bath at about 40°C and visually observe the remaining condition of the film when the film is rubbed 10 times with a finger. Next, bring the foaming detergent (Kao Soap White) into contact with the film, rub it 10 times with a finger, rinse off the foam in a water bath, and visually observe the remaining condition of the film. Regarding the removability of the film, the moisture resistance of the film is also considered, and it is evaluated according to the following evaluation criteria based on the level of removal. A is qualified.

[0264] A: It cannot be removed with warm water at 40°C, but can be removed with a detergent.

[0265] B: Can be removed with warm water at 40°C.

[0266] C: It cannot be removed by using warm water at 40°C or detergent.

[0267] [Table 12]

[0268]

[0269] Examples 103 to 106 (Preparation and evaluation of external use composition)

[0270] Component (B) and other components listed in the table were mixed with component (C), component (D), and an appropriate amount of water, and then component (A) was mixed in. Thereafter, the remaining water was mixed in to prepare an external preparation composition.

[0271] The obtained external preparation composition was evaluated by the above method. Furthermore, the contact angle and its change ratio and spreadability of the composition were evaluated by the following method. The main components used are shown in Table 1, and the composition and evaluation results of the external preparation composition are shown in Table 13. Furthermore, the amount of each component is the effective ingredient amount (mass %).

[0272] (Contact angle of composition and ratio of its change)

[0273] At a temperature of 25° C., 2 μL of the external preparation composition described in Table 13 was dropped onto artificial leather SUPPLALE (manufactured by IDEATEX JAPAN) using an automatic contact angle meter (“DM-501i” manufactured by Kyowa Chemical Industry Co., Ltd.), and the contact angle was measured 10 seconds after dropping and 60 seconds after dropping. In addition, the ratio of the change in the contact angle from 10 seconds after dropping to 60 seconds after dropping was calculated according to the following formula (1).

[0274] The ratio of the change in contact angle = 1-(contact angle after 60 seconds of dripping) / (contact angle after 10 seconds of dripping)...(1)

[0275] (Spreadability)

[0276] The panelists marked the inner forearms of the forearms in a clear area of ​​2 cm x 2 cm, and then applied 24 μL of the external preparation composition described in Table 13 using a Microman (manufactured by Gilson). The spread of the composition was visually confirmed 30 seconds after application, and the spreadability was evaluated according to the following criteria.

[0277] A: Apply in a manner that can be controlled within a range of 2 cm x 2 cm.

[0278] B: It also spreads to the surrounding area of ​​2 cm×2 cm.

[0279] C: dripping from an area of ​​2 cm×2 cm.

[0280] [Table 13]

[0281]

[0282] Table 13 shows that an external preparation composition having high contact angles with respect to artificial leather 10 seconds and 60 seconds after dropping and a small ratio of change in contact angle from 10 seconds to 60 seconds after dropping has better applicability to the skin.

[0283] Formulation Examples 1 to 26 (Preparation of external use composition)

[0284] According to the formulations in Tables 14 to 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. Thereafter, the remaining water was mixed in to prepare an external preparation composition.

[0285] Formulation Examples 27 to 30 (Preparation of Aerosol Preparations)

[0286] According to the formula of Table 16, component (B) and other components are mixed with component (C), component (D), and an appropriate amount of water, and then component (A) is mixed. Thereafter, the remaining water is mixed to prepare an external preparation composition that becomes an aerosol stock solution. After filling it in an aerosol container (manufactured by Toyo Can Co., Ltd.), DME is sealed in such a way that the aerosol stock solution and dimethyl ether (DME) as a propellant become the mass ratio recorded in the table to prepare an aerosol preparation.

[0287] [Table 14]

[0288]

[0289] [Table 15]

[0290]

[0291] [Table 16]

[0292]

[0293] [Industrial Applicability]

[0294] According to the present invention, there can be provided an external preparation composition that can form a coating film containing a medicinal ingredient and having excellent durability and moisture resistance, and a method for using the same.

Claims

1. A composition for external use, wherein Contains the following ingredients (A) to (D): (A) Medicinal ingredients, (B) water-insoluble polymers, (C) non-volatile base, and (D) a volatile solvent, and The component (B) comprises two or more selected from (B1) a cellulose polymer, (B2) an acrylic polymer, and (B3) a vinyl polymer, The viscosity of the external preparation composition at 25° C. is 1.0 mPa·s or more and 10,000 mPa·s or less.

2. The external-use composition according to claim 1, wherein The mass ratio (C) / (B) of the component (C) to the component (B) in the external preparation composition is 0.01 to 50.

3. The external-use composition according to claim 1 or 2, wherein The component (B) includes the component (B1) and the component (B2), and a mass ratio (B2) / (B1) of the component (B2) to the component (B1) is 0.05 to 30.

4. The external-use composition according to claim 1 or 2, wherein The component (B) includes the component (B1) and the component (B3), and a mass ratio (B3) / (B1) of the component (B3) to the component (B1) is 0.1 to 20.

5. The external-use composition according to claim 1 or 2, wherein The component (B) includes the component (B2) and the component (B3), and a mass ratio (B2) / (B3) of the component (B2) to the component (B3) is 0.05 to 30.

6. The composition for external use according to any one of claims 1 to 5, wherein The external preparation composition further contains water, and the content of water in the external preparation composition is 1 mass % to 70 mass %.

7. The composition for external use according to any one of claims 1 to 6, wherein The component (A) comprises one or more selected from anti-inflammatory and analgesic components, local irritant components, blood circulation promoting components, antihistamine components, herbal medicine components, antipruritic components, local anesthetic components, keratin softening components, bactericidal components, antibacterial / antifungal components, immunosuppressants, antiviral components, hair growth / hair development components, sebum suppression components, antiperspirant components, and whitening components.

8. The composition for external use according to any one of claims 1 to 7, wherein The component (C) is at least one selected from polar oils, nonpolar oils, polyols, alkanolamines, and nonionic surfactants.

9. The composition for external use according to any one of claims 1 to 8, wherein The component (D) is an alcohol having 4 or less carbon atoms.

10. The composition for external use according to any one of claims 1 to 9, wherein The content of the component (A) in the external preparation composition is 0.001 mass % to 30 mass %.

11. The composition for external use according to any one of claims 1 to 10, wherein The content of the component (B) in the external preparation composition is 0.01% by mass or more and 30% by mass or less.

12. The composition for external use according to any one of claims 1 to 11, wherein The content of the component (C) in the external preparation composition is 0.001 mass % to 40 mass %.

13. The external-use composition according to any one of claims 1 to 12, wherein The content of the component (D) in the external preparation composition is 10% by mass or more and 95% by mass or less.

14. A method for using the external preparation composition according to any one of claims 1 to 13, wherein: The process comprises the following steps (I) and (II) in sequence: Step (I): a step of applying the external preparation composition to an object, followed by drying to form a film composed of the external preparation composition; Step (II): a step of bringing the film into contact with a cleaning agent and then washing with water to remove the film.

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