Film-forming topical composition

Abstract

To provide a topical composition containing ethanol and water, capable of forming a coating layer with practically sufficient adhesion on a skin surface, while exhibiting superior handleability.SOLUTION: A topical composition contains (A) a polyvinyl alcohol, (B) polyacrylic acid or a derivative thereof, (C) alkanolamine, (D) ethanol, and (E) water. The topical composition may contain a further active ingredient.SELECTED DRAWING: None

Description

[Technical field]

[0001] The present invention relates to a topical composition containing ethanol and water, which forms a coating on the body surface after application. [Background technology]

[0002] External compositions that form a film on the skin after application are used for the purposes of protecting affected areas such as wounds, blocking external stimuli to suppress itching, preventing scratching of the skin, and preventing the external composition from adhering to clothing. On the other hand, depending on the type of active ingredient, it is necessary to add a solvent such as ethanol or water to dissolve it in the external composition, and in this case, the coating is not formed or the adhesion of the coating is easily reduced.In addition, the composition is likely to have poor handling properties, such as being difficult to adjust the amount of discharge from the container mouth or dripping on the skin.In particular, ethanol has low surface tension on the surface of the skin or container wall, which significantly reduces the handling properties of the composition, but ethanol is convenient in that it dissolves oily ingredients while being compatible with water, and in some cases it may be desirable to add it in a relatively large amount. Therefore, there is a demand for a composition for external use that contains ethanol and water, is capable of forming a coating on the skin surface that has sufficient adhesion for practical use, and is also easy to handle. Summary of the Invention [Problem to be solved by the invention]

[0003] The present invention aims to provide a composition for external use containing ethanol and water, which is capable of forming a coating having sufficient adhesion for practical use on body surfaces such as the skin and has excellent handleability. [Means for solving the problem]

[0004] The present inventors conducted extensive research to solve the above problems and discovered that by blending an external composition with (A) polyvinyl alcohol, (B) polyacrylic acid or a derivative thereof, and (C) an alkanolamine in addition to (D) ethanol and (E) water, the composition forms a coating with good adhesion after application to a body surface such as the skin, and is easy to handle and less prone to dripping. The present invention has been completed based on the above findings, and provides the following [1] and [2]. [1] A composition for external use comprising (A) polyvinyl alcohol, (B) polyacrylic acid or a derivative thereof, (C) an alkanolamine, (D) ethanol, and (E) water. [2] A composition for external use comprising (A) polyvinyl alcohol, (B) polyacrylic acid or a derivative thereof, (C) an alkanolamine, (D) ethanol, and (E) water, which forms a coating upon application. Effect of the Invention

[0005] Although the composition for external use of the present invention contains ethanol and water, it forms a film after application on the body surface such as the skin. The feeling of use when applied is excellent in adhesion and film-like feeling, and the feeling of use is maintained for a long time. In addition, although the topical composition of the present invention contains ethanol and water, particularly ethanol, which has a low surface tension on body surfaces such as the skin and on the walls of a container, it contains a combination of polyvinyl alcohol, polyacrylic acid or a derivative thereof, and an alkanolamine, so that the composition is less likely to drip during or after application to the skin, and is also less likely to drip when discharged from the opening of the container, and the amount discharged is easily adjusted. In these respects, the topical composition of the present invention has good handleability. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0006] Hereinafter, an embodiment of the present invention will be described in detail. The topical composition of this embodiment is a topical composition containing (A) polyvinyl alcohol, (B) polyacrylic acid or a derivative thereof, (C) an alkanolamine, (D) ethanol, and (E) water.

[0007] (A) Polyvinyl alcohol The polyvinyl alcohol may be unsaponified, completely saponified, or partially saponified. Among them, partially saponified is preferable. The degree of saponification of the partially saponified polyvinyl alcohol may be 75% or more, 82% or more, 85% or more, or 86.5% or more, and may be 95% or less, 92% or less, or 89% or less. Within this range, the effect of the present invention can be sufficiently obtained.

[0008] The concentration of polyvinyl alcohol can be 2% by mass or more, 2.5% by mass or more, or 3% by mass or more, based on the total amount of the composition. Within this range, the effects of the present invention can be sufficiently obtained. The concentration of polyvinyl alcohol can be 5% by mass or less, 4% by mass or less, or 3.5% by mass or less, based on the total amount of the composition. Within this range, the effects of the present invention can be sufficiently obtained.

[0009] The content of polyvinyl alcohol can be 0.04 parts by mass or more, 0.07 parts by mass or more, or 0.08 parts by mass or more per 1 part by mass of water. Within this range, the effects of the present invention can be sufficiently obtained. Furthermore, the content of polyvinyl alcohol can be 0.1 parts by mass or less, 0.09 parts by mass or less, or 0.087 parts by mass or less per 1 part by mass of water. Within this range, the effects of the present invention can be sufficiently obtained.

[0010] (B) Polyacrylic acid or its derivatives Polyacrylic acid or its derivative is a polymer formed by polymerization of a monomer containing a carboxylic acid. Polyacrylic acid or its derivative is neutralized in whole or in part with an alkanolamine. In the topical composition of the present embodiment, polyacrylic acid or its derivative absorbs ethanol or ethanol and water and swells.

[0011] The polyacrylic acid or its derivatives may be either non-crosslinked or crosslinked, but crosslinked polyacrylic acid or its derivatives are preferred. Examples of crosslinked polyacrylic acids include carboxyvinyl polymers. Examples of the derivatives of polyacrylic acid include alkyl acrylate copolymers, alkyl acrylate / alkyl methacrylate copolymers, (acrylic acid / alkyl acrylate (C10-30)) copolymers, alkyl acrylate copolymers, acrylate copolymers, and acrylate crosspolymers. The polyacrylic acid or its derivatives can be used alone or in combination of two or more.

[0012] The concentration of polyacrylic acid or its derivatives can be 0.1% by mass or more, 0.5% by mass or more, or 0.8% by mass or more based on the total amount of the composition. It can also be 3% by mass or less, 2% by mass or less, or 1.5% by mass or less. Within this range, a composition with a suitable viscosity can be obtained, and the effects of the present invention can be fully obtained.

[0013] The content of polyacrylic acid or its derivatives can be 0.1 parts by mass or more, 0.2 parts by mass or more, or 0.25 parts by mass or more, relative to 1 part by mass of polyvinyl alcohol. It can also be 0.5 parts by mass or less, 0.4 parts by mass or less, or 0.3 parts by mass or less. Within this range, a composition with a suitable viscosity can be obtained, and the effects of the present invention can be fully obtained.

[0014] The content of polyacrylic acid or its derivative can be 0.005 parts by mass or more, 0.01 parts by mass or more, 0.015 parts by mass or more, or 0.018 parts by mass or more per 1 part by mass of ethanol. The content of polyacrylic acid can be 0.035 parts by mass or less, 0.03 parts by mass or less, 0.025 parts by mass or less, or 0.02 parts by mass or less per 1 part by mass of ethanol. Within this range, a composition with a suitable viscosity can be obtained, and the effects of the present invention can be fully obtained.

[0015] The total concentration of polyvinyl alcohol and polyacrylic acid or its derivatives can be 2% by mass or more, 3.7% by mass or more, or 4.2% by mass or more based on the total amount of the composition. Within this range, a coating having sufficient strength can be formed. Furthermore, the total concentration of polyvinyl alcohol and polyacrylic acid or its derivatives can be 6% by mass or less, 5% by mass or less, or 4.5% by mass or less based on the total amount of the composition. Within this range, a composition with appropriate viscosity can be obtained, and the effects of the present invention can be fully obtained.

[0016] (C) Alkanolamines Alkanolamines are alkanes that contain an amino group and a hydroxy group. Examples of alkanolamines include primary alkanolamines such as monomethanolamine, monoethanolamine, monoisopropanolamine, 2-amino-2-methyl-1-propanol, 2-amino-2-hydroxymethyl-1,3-propanediol (tromethamine), tris(hydroxymethylamino)methane, and tetrahydroxypropylethylenediamine; secondary alkanolamines such as diethanolamine and diisopropanolamine; and tertiary alkanolamines such as triethanolamine and triisopropanolamine.

[0017] Among these, monoethanolamine, diethanolamine, triethanolamine, monoisopropanolamine, diisopropanolamine, triisopropanolamine, and tetrahydroxypropylethylenediamine are preferred from the viewpoint of solubility in ethanol, and triethanolamine is more preferred. One or more alkanolamines can be used. The alkanolamine may be added in an amount sufficient to give the composition a desired viscosity.

[0018] In addition, the external composition of the present embodiment can contain a basic component other than alkanolamine (amine other than alkanolamine or basic component other than amine) within a range that does not impair the effect of the present invention, but can also not contain it. Examples of basic components other than alkanolamine include inorganic basic components, basic amino acids, etc. Specific examples include sodium hydroxide, potassium hydroxide, calcium hydroxide, magnesium hydroxide, ammonia, glycine, arginine, etc., which are used as basic pH adjusters for external compositions.

[0019] (D) Ethanol The concentration of ethanol can be 35% by mass or more, 45% by mass or more, or 50% by mass or more based on the total amount of the composition. Within this range, the neutralized polyacrylic acid can be easily swollen, and the effects of the present invention can be sufficiently obtained. Furthermore, the concentration of ethanol can be 65% by mass or less, 58% by mass or less, or 55% by mass or less based on the total amount of the composition. Within this range, deterioration of handling properties such as dripping and deterioration of coating adhesion can be suppressed.

[0020] (E)Water The concentration of water can be 30% by mass or more, 38% by mass or more, or 40.2% by mass or more based on the total amount of the composition. Within this range, polyvinyl alcohol can be easily dissolved, and the effects of the present invention can be sufficiently obtained. Furthermore, the concentration of water can be 65% by mass or less, 52% by mass or less, or 48% by mass or less based on the total amount of the composition. Within this range, deterioration of handling properties such as dripping and deterioration of coating adhesion can be suppressed. The content of water can be 0.5 parts by mass or more, 0.7 parts by mass or more, or 0.73 parts by mass or more, and can be 1.3 parts by mass or less, 1 part by mass or less, or 0.8 parts by mass or less, relative to 1 part by mass of ethanol. Within this range, polyvinyl alcohol dissolves in water, and acrylic acid or its derivative absorbs ethanol or ethanol and water and swells in the composition for external use, so that the effects of the present invention can be sufficiently obtained.

[0021] The total concentration of ethanol and water can be 70% by mass or more, 85% by mass or more, or 90% by mass or more based on the total amount of the composition. Within this range, polyvinyl alcohol dissolves in water in the topical composition, and acrylic acid or its derivative absorbs ethanol or ethanol and water to swell, so that the effects of the present invention can be fully achieved. In addition, the total concentration of ethanol and water can be 97% by mass or less, 96% by mass or less, or 95.5% by mass or less based on the total amount of the composition. Within this range, the deterioration of handling properties such as dripping and the deterioration of coating adhesion can be suppressed.

[0022] Bases and Additives The topical composition of this embodiment may contain, in addition to ethanol and water, one or more bases or additives within a range that does not impair the effects of the present invention. Among the bases or additives exemplified below, there are some which correspond to component (A), component (B), component (C), component (D), or component (E) of the present invention, which means that these components can function as bases or additives in addition to achieving the effects of the present invention.

[0023] Examples of the base or additive include an oily base, an aqueous base, an antioxidant, a surfactant, a thickener, a chelating agent, a preservative or antiseptic, a colorant, and a fragrance.

[0024] The oil base may be a polar oil or a non-polar oil. Examples of the polar oil include ester oils, oils and fats, waxes, higher fatty acids, higher alcohols, phytosterols, cholesterol, and other sterols. Examples of the non-polar oil include hydrocarbon oils and silicone oils. The aqueous base may include polyhydric alcohols, such as low molecular weight (non-polymer) polyhydric alcohols having two or more hydroxyl groups, including glycerin, diglycerin, propylene glycol, dipropylene glycol, 1,4-butanediol, ethylene glycol, diethylene glycol, isoprene glycol, 1,3-butylene glycol, 1,3-propanediol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, decanediol, sorbitol, xylitol, erythritol, and mannitol.

[0025] Examples of antioxidants include dibutylhydroxytoluene, butylhydroxyanisole, sorbic acid, sodium sulfite, ascorbic acid, ascorbic acid derivatives, tocopherol, tocopherol derivatives (tocopherol acetate, etc.), tocotrienol, hydrogen sulfite, sodium hyposulfite, erythorbic acid, sodium erythorbate, and L-cysteine ​​hydrochloride.

[0026] Examples of the surfactant include a nonionic surfactant, a cationic surfactant, an anionic surfactant, and an amphoteric surfactant. Examples of nonionic surfactants include sorbitan fatty acid esters such as sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, diglycerol sorbitan penta-2-ethylhexyl acid, and diglycerol sorbitan tetra-2-ethylhexyl acid; propylene glycol fatty acid esters such as propylene glycol monostearate; polyoxyethylene hydrogenated castor oil 40 (HCO-40), polyoxyethylene hydrogenated castor oil 50, and the like. (HCO-50), polyoxyethylene hydrogenated castor oil 60 (HCO-60), polyoxyethylene hydrogenated castor oil 80 and other hydrogenated castor oil derivatives; polyoxyethylene (20) sorbitan monolaurate (polysorbate 20), polyoxyethylene (20) sorbitan monostearate (polysorbate 60), polyoxyethylene (20) sorbitan monooleate (polysorbate 80), polyoxyethylene (20) sorbitan isostearate and other polyoxyethylene sorbitan fatty acid esters; Polyoxyethylene monococonut oil fatty acid glyceryl; glycerin alkyl ethers such as glycerin monooleyl ether and glycerin monosteric ether; glycerin fatty acid esters such as glyceryl oleate, glyceryl myristate, glyceryl stearate, and glyceryl isostearate; polyglyceryl-2 oleate, polyglyceryl-2 stearate, polyglyceryl-10 oleate, polyglyceryl-10 stearate, polyglyceryl-10 laurate, and polyglyceryl distearate. polyglycerin fatty acid esters such as polyglyceryl-10 trioleate, polyglyceryl-10 pentaoleate, and polyglyceryl-10 pentastearate; polyoxyethylene fatty acid esters such as polyoxyl 40 stearate and polyoxyl 55 stearate; alkyl glucosides; polyoxyalkylene alkyl ethers such as polyoxyethylene lauryl ether, polyoxyethylene cetyl ether, polyoxyethylene stearyl ether, and polyoxyethylene behenyl ether;Examples of such surfactants include polyoxyethylene-polyoxypropylene block copolymers such as polyoxyethylene (196) polyoxypropylene (67) glycol, polyoxyethylene (200) polyoxypropylene (70) glycol, polyoxyethylene (20) polyoxypropylene (4) cetyl ether, and polyoxyethylene (10) polyoxypropylene (4) cetyl ether; silicone surfactants such as polyoxyethylene-methylpolysiloxane copolymer, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, and PEG-9 polydimethylsiloxyethyl dimethicone;

[0027] Examples of thickeners include guar gum, locust bean gum, carrageenan, xanthan gum, polyvinylpyrrolidone, polyethylene glycol, bentonite, hyaluronic acid, alginic acid, and cellulose-based thickeners (such as methylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxymethylcellulose, and carboxyethylcellulose).

[0028] Examples of chelating agents include ethylenediaminetetraacetic acid (edetic acid), ethylenediaminetetraacetate (sodium salt (sodium edetate: Japanese Pharmacopoeia, EDTA-2Na, etc.), potassium salt, etc.), phytic acid, gluconic acid, polyphosphoric acid, metaphosphoric acid, etc. Among these, sodium edetate is preferred.

[0029] Examples of preservatives or antiseptics include benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl paraoxybenzoate, isopropyl paraoxybenzoate, butyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, methyl paraoxybenzoate, phenoxyethanol, thymol, isopropylmethylphenol, sorbic acid, potassium sorbate, chlorhexidine gluconate, methylisothiazoline, iodopropynyl butylcarbamate, 1,3-propanediol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, and sodium pyrosulfite.

[0030] Active ingredients The topical composition of the present embodiment can contain various active ingredients (medicinal active ingredients, cosmetic active ingredients, etc.) Examples of the active ingredients include anti-inflammatory agents, antihistamines, antibacterial ingredients, antifungal agents, local anesthetics, antipruritic agents other than antihistamines, moisturizers, cooling agents, ultraviolet absorbing agents or ultraviolet scattering agents, vitamins, and astringent ingredients. Among the active ingredients exemplified below, there are some that correspond to component (A), component (B), or component (C) of the present invention, which means that these ingredients can function as the exemplified pharmacologically or physiologically active ingredients in addition to providing the effects of the present invention. One or more active ingredients may be used as long as the effects of the present invention are not impaired.

[0031] The anti-inflammatory agent may be either a non-steroidal or a steroidal agent. Examples of non-steroidal anti-inflammatory agents include allantoin, glycyrrhizic acid, glycyrrhetinic acid, acetaminophen, epsilon-aminocaproic acid, berberine, azulene, zinc, ufenamate, heparinoids; plant extracts such as licorice extract, sage extract, and rosemary extract; fenamic acid anti-inflammatory agents such as flufenamic acid and tolfenamic acid; arylacetic acid anti-inflammatory agents such as acemetacin, indomethacin, and diclofenac; propionic acid anti-inflammatory agents such as aminoprofen, ibuprofen, ketoprofen, ibuprofen piconol, pranoprofen, and loxoprofen; oxicam anti-inflammatory agents such as piroxicam and meloxicam; methyl salicylate, glycol salicylate, and salts thereof.

[0032] The salt may be any pharma- ceutically or physiologically acceptable salt, and examples of the salt include inorganic acid salts and organic acid salts. Examples of inorganic acid salts include hydrochloride, hydrobromide, nitrate, sulfate, phosphate, etc. Examples of organic acid salts include monocarboxylates such as acetate, trifluoroacetate, butyrate, palmitate, and stearate, polycarboxylates such as fumarate, maleate, succinate, and malonate, oxycarboxylates such as lactate, tartrate, and citrate, and organic sulfonates such as methanesulfonate, toluenesulfonate, tosylate, and napadisilate. Other examples include salts with organic bases (organic amine salts such as methylamine salts, triethylamine salts, triethanolamine salts, morpholine salts, piperazine salts, pyrrolidine salts, tripyridine salts, and picoline salts), and salts with inorganic bases (ammonium salts; alkali metal salts such as sodium salts and potassium salts; alkaline earth metal salts such as calcium salts and magnesium salts; and metal salts such as zinc salts and aluminum salts).

[0033] Examples of non-steroidal anti-inflammatory agents that are salts include dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, indomethacin hydrochloride, diclofenac sodium salt, berberine sulfate, berberine hydrochloride, azulene sulfonate sodium salt, zinc sulfate, zinc lactate, and loxoprofen sodium salt.

[0034] The steroidal anti-inflammatory agents include steroid compounds such as prednisolone, hydrocortisone, cortisone, dexamethasone, betamethasone, and derivatives thereof.

[0035] Representative examples of the derivatives include esters (particularly esters with organic or inorganic acids), salts, and salts of esters. Examples of the ester include esters with organic acids such as valeric acid, acetic acid, succinic acid, butyric acid (butanoic acid), and propionic acid; and esters with inorganic acids such as phosphoric acid. A single molecule may contain a plurality of esters. When a single molecule contains a plurality of esters, the molecule may contain a plurality of esters with one type of acid, or may contain esters with two or more types of acids. Examples of the salt include salts with organic bases (organic amine salts such as methylamine salt, triethylamine salt, triethanolamine salt, morpholine salt, piperazine salt, pyrrolidine salt, tripyridine salt, and picoline salt), and salts with inorganic bases (ammonium salt; alkali metal salts such as sodium salt and potassium salt; alkaline earth metal salts such as calcium salt and magnesium salt; and metal salts such as zinc salt and aluminum salt).

[0036] Specific examples of derivatives of steroid compounds include, for example, cortisone acetate, prednisolone valerate acetate (PVA), prednisolone acetate, dexamethasone acetate, hydrocortisone butyrate (particularly, hydrocortisone-17-butyrate), hydrocortisone acetate, and betamethasone valerate.

[0037] The concentration of the anti-inflammatory agent can be, relative to the total amount of the composition, 0.01% by mass or more, 0.025% by mass or more, 0.05% by mass or more, 0.1% by mass or more, 0.125% by mass or more, 0.2% by mass or more, or 0.5% by mass or more, and can be 6% by mass or less, 5% by mass or less, 2% by mass or less, 1% by mass or less, 0.5% by mass or less, 0.25% by mass or less, or 0.125% by mass or less. The concentration of the nonsteroidal anti-inflammatory agent can be 0.05% by mass or more, 0.2% by mass or more, or 0.5% by mass or more, and can be 6% by mass or less, 5% by mass or less, 2% by mass or less, or 1% by mass or less, based on the total amount of the composition. The concentration of the steroidal anti-inflammatory agent can be, relative to the total amount of the composition, 0.01% by mass or more, 0.025% by mass or more, 0.05% by mass or more, or 0.125% by mass or more, and can be 6% by mass or less, 5% by mass or less, 2% by mass or less, 0.5% by mass or less, 0.25% by mass or less, or 0.125% by mass or less.

[0038] Examples of antihistamines include ethanolamine antihistamines such as diphenhydramine and diphenylpyraline, propylamine antihistamines such as chlorpheniramine, phenothiazine antihistamines such as mequitazine and promethazine, piperazine antihistamines such as cetirizine and meclizine, ketotifen, olopatadine, fexofenadine, epinastine, azelastine, and salts thereof.

[0039] Examples of the salt include salts with organic acids, salts with inorganic acids, salts with organic bases, and salts with inorganic bases, which are exemplified for the anti-inflammatory agent. Specific examples include diphenhydramine hydrochloride, diphenylpyraline hydrochloride, chlorpheniramine maleate, promethazine hydrochloride, cetirizine hydrochloride, meclizine hydrochloride, ketotifen fumarate, olopatadine hydrochloride, fexofenadine hydrochloride, epinastine hydrochloride, and azelastine hydrochloride.

[0040] The concentration of the antihistamine can be 0.1% by weight or more, 0.15% by weight or more, or 0.2% by weight or more, and can be 2% by weight or less, 1% by weight or less, or 0.5% by weight or less, based on the total weight of the composition.

[0041] Examples of antibacterial components include benzoyl peroxide, adapalene, phenolic disinfectants (isopropylmethylphenol, triclosan, phenoxyethanol, etc.), iodine disinfectants (povidone iodine, polyvinyl alcohol iodine, cyclodextrin iodine, etc.), chlorine disinfectants (hypochlorous acid, sodium hypochlorite, calcium hypochlorite, chlorinated isocyanuric acid, etc.), alkyl quaternary ammonium salt disinfectants (cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, dequalinium chloride, etc.), biguanide disinfectants (chlorhexidine hydrochloride, chlorhexidine gluconate, etc.), alkyldiaminoethylglycine hydrochloride, sodium benzoate, ethanol, chlorobutanol, salicylic acid, cresol, etc.

[0042] The concentration of the antibacterial component can be 0.01% by weight or more, 0.03% by weight or more, or 0.05% by weight or more, and can be 0.5% by weight or less, 0.3% by weight or less, or 0.1% by weight or less, based on the total weight of the composition.

[0043] Examples of antifungal agents include azole antifungal agents such as lanoconazole, miconazole, miconazole and its salts (such as miconazole nitrate), efinaconazole, luliconazole, tioconazole, isoconazole, isoconazole and its salts (such as isoconazole nitrate), clotrimazole, bifonazole, oxiconazole and its salts (such as oxiconazole nitrate), and econazole and its salts (such as econazole nitrate); allylamine antifungal agents such as terbinafine hydrochloride; benzylamine antifungal agents such as butenafine hydrochloride; and morpholine antifungal agents such as amorolfine hydrochloride.

[0044] The concentration of the antifungal agent can be 0.05% by mass or more, 0.1% by mass or more, or 0.5% by mass or more, and can be 5% by mass or less, 3% by mass or less, or 1% by mass or less, based on the total amount of the composition.

[0045] Examples of local anesthetics include lidocaine, dibucaine, mepivacaine, procaine, meprylcaine, ethyl aminobenzoate, and oxypolyethoxydodecane.

[0046] Examples of the salt include salts with organic acids, salts with inorganic acids, salts with organic bases, and salts with inorganic bases, which are exemplified for the anti-inflammatory agent. Specific examples include lidocaine hydrochloride, dibucaine hydrochloride, mepivacaine hydrochloride, procaine hydrochloride, meprylcaine hydrochloride, etc.

[0047] The concentration of the local anesthetic may be 0.05% by weight or more, 0.2% by weight or more, or 0.5% by weight or more, and may be 5% by weight or less, 3% by weight or less, or 2% by weight or less, based on the total weight of the composition.

[0048] Examples of antipruritic agents other than antihistamines include crotamiton.

[0049] The concentration of the antipruritic agent other than the antihistamine can be 1% by mass or more, 2% by mass or more, or 4% by mass or more, and can be 10% by mass or less, 8% by mass or less, or 6% by mass or less, based on the total amount of the composition.

[0050] Examples of moisturizing ingredients include heparinoids, sodium chondroitin sulfate, urea, hyaluronic acid or its salts, and the like.

[0051] The concentration of the moisturizing component can be, relative to the total amount of the composition, 0.01% by mass or more, 0.1% by mass or more, 1% by mass or more, 5% by mass or more, or 15% by mass or more, and can be 20% by mass or less, 10% by mass or less, 1% by mass or less, or 0.3% by mass or less.

[0052] Examples of ultraviolet absorbing agents or ultraviolet scattering agents include 2-ethylhexyl paramethoxycinnamate, 2-[4-(diethylamino)-2-hydroxybenzoyl]benzoic acid hexyl ester, 2,4,6-tris[4-(2-ethylhexyloxycarbonyl)anilino]-1,3,5-triazine, t-butylmethoxydibenzoylmethane, ethylhexyl dibenzylidene dioxoimidazolidinepropionate, ethylhexyl triazone, paraaminobenzoic acid and its derivatives, octyl paradimethylaminobenzoate, ethylene glycol salicylate, dihydroxybenzophenone, titanium oxide, and zinc oxide.

[0053] Examples of cooling agents include terpenoids and essential oils. Examples of terpenoids include menthol, anethole, eugenol, camphor, geraniol, cineol, borneol, limonene, and ryuno, etc. These may be in the d-, l-, or dl-form. Examples of essential oils include peppermint oil, cool mint oil, spearmint oil, peppermint oil, fennel oil, cinnamon oil, bergamot oil, eucalyptus oil, rose oil, and lavender oil.

[0054] The concentration of the cooling agent may be 0.01% by mass or more, 0.5% by mass or more, or 1% by mass or more, and may be 15% by mass or less, 12.3% by mass or less, 10% by mass or less, 5% by mass or less, or 2% by mass or less, based on the total amount of the composition.

[0055] Examples of vitamins include vitamin A oil, retinol palmitate, tocopherol, tocopherol acetate, tocopherol succinate, tocopherol calcium succinate, ubiquinone derivatives and salts thereof, riboflavin, flavin mononucleotide, flavin adenine dinucleotide, riboflavin butyrate, riboflavin tetrabutyrate, ascorbic acid, sodium ascorbate, sodium ascorbyl phosphate, magnesium ascorbyl phosphate, ascorbyl palmitate, pyridoxine hydrochloride, pyridoxamine hydrochloride, cyanocobalamin, folic acid, nicotinic acid, nicotinamide, pantothenic acid, calcium pantothenate, pantothenyl alcohol (panthenol), pantothenyl ethyl ether and other pantothenic acids, biotin, and γ-oryzanol.

[0056] The concentration of the vitamins can be 0.001% by mass or more, 0.01% by mass or more, or 0.1% by mass or more, and can be 5% by mass or less, 2% by mass or less, or 1% by mass or less, relative to the total amount of the composition.

[0057] Examples of astringent ingredients include zinc paraphenolsulfonate, zinc oxide, and aluminum chlorohydrin.

[0058] pH The pH of the topical composition of the present embodiment can be 4.5 or more, 4.8 or more, 5 or more, or 5.5 or more, and can be 8 or less, 7 or less, 6.5 or less, 6 or less, or 5.7 or less. Within these ranges, the effects of the present invention can be sufficiently obtained.

[0059] viscosity The viscosity of the topical composition of this embodiment, measured at 25°C with a rotational viscometer (VISCIMETER TVB-15, manufactured by Toki Sangyo Co., Ltd.), can be 15 Pa·s or more, 20 Pa·s or more, 50 Pa·s or more, 80 Pa·s or more, 100 Pa·s or more, or 120 Pa·s or more, and can be 500 Pa·s or less, 300 Pa·s or less, 200 Pa·s or less, 140 Pa·s or less, or 130 Pa·s or less. Within this range, a coating having good handleability and good adhesion can be formed.

[0060] Formulation The topical composition of this embodiment may be in the form of a cream, ointment (oil-soluble ointment, water-soluble ointment), gel, emulsion, or the like. In the case of an emulsion composition such as an emulsion or cream, it may be either an oil-in-water type or a water-in-oil type, but the oil-in-water type is preferred in that the effects of the present invention are more pronounced.

[0061] container Examples of materials for the container that holds the topical composition of this embodiment include containers in which some or all, preferably all, of the surface that comes into contact with the topical composition is made of at least one material selected from the group consisting of polyolefin resin, acrylic resin, polyester, polycarbonate, fluororesin, polyvinyl chloride, polyamide, ABS resin, AS resin, polyacetal, modified polyphenylene ether, polyarylate, polysulfone, polyimide, cellulose acetate, aluminum, and glass.

[0062] From the viewpoint of ease of handling the preparation and ease of molding, preferred materials for the container include aluminum, polyethylene (PE) (including high density polyethylene (HDPE), low density polyethylene (LDPE), very low density polyethylene, linear low density polyethylene (LLDPE), ultra-high molecular weight polyethylene, etc.), polypropylene (PP) (including isotactic polypropylene, syndiotactic polypropylene, atactic polypropylene, etc.), ethylene-propylene copolymer, polymethylpentene, polybutene-1, 1,2-polybutadiene and other polyolefin resins, polyethylene terephthalate, polybutylene terephthalate, polyethylene naphthalate and other polyester resins, and more preferred are polyethylene, polypropylene, and polyethylene terephthalate. The material for the innermost layer of the container is preferably polyethylene (PE) (high density polyethylene (HDPE), low density polyethylene (LDPE), very low density polyethylene, linear low density polyethylene (LLDPE), polypropylene, or aluminum.

[0063] When the container has a lid or cap, the material of the lid or cap can be the same as those exemplified as the container material above. Examples of containers for storing the composition include containers with nozzles, containers with pumps, jar containers, tube containers, containers with holes in the inner plugs, containers with hinge caps, sponge head containers, roll-on containers, and the like.

[0064] Usage and dosage The topical composition of this embodiment may be a pharmaceutical composition, a cosmetic composition, a quasi-drug composition, or the like. The topical composition of the present embodiment can be one for application to the skin (body skin, scalp, etc.), mucous membranes (oral mucosa, anal mucosa, vaginal mucosa, etc.), nails, etc. Among these, a topical composition for skin is preferable. An appropriate amount of the topical composition of this embodiment can be applied (spread, etc.) to the affected area, for example, 1 to 5 times, 1 to 3 times, 1 to 2 times, or 1 time. A dosage form that is applied by spreading is preferred because it can significantly exert the effects of the present invention.

[0065] coating The composition for external use of this embodiment has the above composition and is a composition that forms a film after application, or a composition that is used to form a film after application. In this embodiment, the "film" is a film with no fluidity. Also, it is a film that is solidified to the extent that it does not stick to the hand even when touched. In this embodiment, "capable of forming a film" means that a film can be formed within 30 minutes after applying 1 mL to an area of ​​5 cm x 5 cm on the skin of the forearm at room temperature. The film obtained by applying the composition for external use of this embodiment is suitable for protecting and moisturizing the affected area, and protecting against scratching behavior. In addition, the film obtained by applying the composition for external use of this embodiment is suitable for maintaining a cooling sensation due to the evaporation of ethanol. In addition, in this embodiment, "strong (film)" refers to a film that is strong enough to be able to be picked up and peeled off with fingers without breaking. In addition, in this embodiment, "brittle (film)" refers to a film that is weak enough to be broken when the film formed on the skin is picked up and peeled off with fingers.

[0066] Purpose The topical composition of this embodiment can be used as a pharmaceutical or quasi-drug, particularly as an external preparation thereof, with one or more therapeutic effects such as anti-inflammatory, antibacterial, antipruritic, etc., depending on the active ingredient optionally blended. For example, the topical composition of this embodiment can be suitably used as an external composition with efficacy and effect of itching, dry skin accompanied by itching, rash, hives, eczema, insect bites, lumps and tightness of the skin after a wound or burn (excluding the face), acne, keratosis, cracks and chapped skin, dry skin, dermatitis, rough skin, chilblains (excluding sores), swelling, muscle pain, joint pain after a bruise or sprain, athlete's foot, jock itch, ringworm, heat rash, sores, disinfection of wounds, etc. EXAMPLES

[0067] The present embodiment will be described in more detail below with reference to examples, but the present embodiment is not limited to these. (1) Preparation of topical composition According to the formulation shown in Table 1, a composition for external use was prepared by a conventional method. That is, polyvinyl alcohol and water were heated to 80°C to dissolve polyvinyl alcohol in water, and then cooled. A dispersion liquid was prepared by dispersing carboxyvinyl polymer in ethanol, and the dispersion liquid was added to an aqueous polyvinyl alcohol solution cooled to 60°C. Then, triethanolamine was added, and the mixture was stirred and cooled to room temperature to obtain a composition for external use.

[0068] (2) Sensory evaluation The obtained compositions for external use were filled into plastic tubes, and the film-forming properties, usability, and ease of handling were evaluated by the VAS (Visual Analog Scale) method. That is, six expert panelists applied about 1 mL of each composition for external use to an area of ​​5 cm square on the forearm indoors, and wrote down the answer values ​​for each evaluation item shown in Table 1 on a 10 cm straight line marked with 0 (left end) and 100 (right end). The panelists were blinded to the formulation of each composition. The evaluation items of the VAS evaluation are as follows. Adhesion immediately after application: The strength of adhesion to the skin immediately after application was evaluated. Coating sensation immediately after application: The sensation of being covered immediately after the application process was evaluated. Film sensation 30 minutes after application: After application, as the solvent in the topical composition evaporates and a film forms, the film adheres to the skin, giving the skin a feeling of being pulled. The strength of this sensation was evaluated 30 minutes after application. Fluidity immediately after application: The presence or absence of flow of the topical composition on the skin immediately after it was applied horizontally was evaluated. In other words, the topical composition was deemed to "flow" if it spontaneously spread, diffused, and flowed in a stationary state immediately after application. Dripping during application: The tendency of the composition to drip on the skin was evaluated. In other words, the degree to which the composition for external use flows was evaluated when the application surface was inclined at 45 degrees and held still immediately after application. The more the composition flows, the more it is considered to "droop." Ease of adjusting the amount dispensed from the container opening: Evaluated whether it was easy to dispense the planned amount.

[0069] The average response values ​​are shown in Table 1. [Table 1]

[0070] Comparative Example 1 has the same formulation as Example 1, except that it does not contain 3.5% by mass of polyvinyl alcohol in Example 1, and instead contains 3.5% by mass more absolute alcohol. Comparative Example 2 has the same formulation as Example 1, except that it does not contain 1.0% by mass of carboxyvinyl polymer (crosslinked polyacrylic acid) in Example 1, and instead contains 1.0% by mass more absolute alcohol. Comparative Example 3 has the same formulation as Example 1, except that it does not contain triethanolamine in Example 1.

[0071] The compositions of Examples 1 to 8, which contain polyvinyl alcohol, carboxyvinyl polymer, and triethanolamine, could be discharged in the intended amount without dripping from the opening of the tube container when applied. In addition, they did not flow on the skin under their own weight. Furthermore, a dry film was formed within 30 minutes of application, and the film was maintained thereafter until it was washed off.

[0072] In contrast, the compositions of Comparative Example 1, which did not contain polyvinyl alcohol, and Comparative Example 3, which did not contain triethanolamine, did not solidify or form a film after application to the arm. The composition of Comparative Example 2, which did not contain a carboxyvinyl polymer, formed a film, but it was very brittle and peeled off in pieces within 30 minutes, lacking in adhesion and strength. In addition, the adhesion feeling immediately after application, the coated feeling immediately after application, and the film feeling 30 minutes after application were higher in Example 1 than in Comparative Example 1 not containing polyvinyl alcohol and Comparative Example 2 not containing carboxyvinyl polymer. The coated feeling immediately after application was higher in Example 1 than in Comparative Example 2 not containing carboxyvinyl polymer. Therefore, it is clear that polyvinyl alcohol, carboxyvinyl polymer, and triethanolamine each contribute to film-forming properties, adhesion, and film strength, and also contribute to the sensory film feel.

[0073] Regarding ease of handling, Comparative Example 1, which did not contain polyvinyl alcohol, Comparative Example 2, which did not contain carboxyvinyl polymer, and Comparative Example 3, which did not contain triethanolamine, ran on the skin under their own weight immediately after application. Furthermore, Comparative Examples 1 to 3 were more likely to drip from the container opening than Example 1, and it was difficult to adjust the amount of the product discharged from the container opening. It can be seen that polyvinyl alcohol, carboxyvinyl polymer, and triethanolamine each contribute to improving the handleability by imparting appropriate viscosity and fluidity to the composition.

[0074] (3) Viscosity measurement The viscosity of each composition was measured using a rotational viscometer (VISCIMETER TVB-15, manufactured by Toki Sangyo Co., Ltd.). The rotor, rotation speed, and measurement time were selected according to the viscosity, as appropriate, in accordance with the manual for the device used. The viscosity measurement conditions and measured values ​​are shown in Table 2. [Table 2]

[0075] Formulation examples Formulation examples of the topical composition of this embodiment are shown below. In the formulation examples below, % represents mass %. Water was added so that the total of the components other than triethanolamine was 100 mass %. Formulation Example 1 (pH 4.8) Prednisolone valerate acetate 0.15% Menthol 0.1% Polyvinyl alcohol 2.5% Carboxyvinyl polymer 1.2% Absolute ethanol 60% Water remaining Triethanolamine (appropriate amount) Formulation Example 2 (pH 5.6) Diphenhydramine hydrochloride 1% Crotamiton 2% Polyvinyl alcohol 3.5% Carboxyvinyl polymer 0.8% Absolute ethanol 45% Water remaining Triethanolamine (appropriate amount) Formulation Example 3 (pH 5.2) Heparinoid 0.3% Allantoin 0.2% Polyvinyl alcohol 3% Carboxyvinyl polymer 1% Absolute ethanol 50% Water remaining Triethanolamine (appropriate amount) Formulation Example 4 (pH 6.0) Dipotassium glycyrrhizinate 0.05% Cholesterol 0.01% Polyvinyl alcohol 3% Carboxyvinyl polymer 1% Absolute ethanol 45% Propylene glycol 5% Water remaining Triethanolamine (appropriate amount) Formulation Example 5 (pH 5.5) Isopropyl methylphenol 0.1% Polyvinyl alcohol 3% Carboxyvinyl polymer 1% Absolute ethanol 45% Butylene glycol 5% Water remaining Triethanolamine (appropriate amount) Formulation Example 6 (pH 5.0) Zinc paraphenol sulfonate 1% Benzalkonium chloride 0.05% Polyvinyl alcohol 3% Carboxyvinyl polymer 1.5% Absolute ethanol 50% Water remaining Triethanolamine (appropriate amount)

[0076] The following additional notes are provided with respect to some or all of the above-described embodiments, but the present invention is not limited to the following notes. [Appendix 1] A topical composition comprising (A) polyvinyl alcohol, (B) polyacrylic acid or a derivative thereof, (C) an alkanolamine, (D) ethanol, and (E) water. [Appendix 2] A composition for external use comprising (A) polyvinyl alcohol, (B) polyacrylic acid or a derivative thereof, (C) an alkanolamine, (D) ethanol, and (E) water, which forms a coating upon application. [Appendix 3] The topical composition according to claim 1 or 2, wherein the total content of the components (D) and (E) is 70 to 97% by mass, based on the total amount of the topical composition. [Appendix 4] The topical composition according to any one of claims 1 to 3, wherein the total content of components (A) and (B) is 2 to 6% by mass, based on the total amount of the topical composition. [Appendix 5] The composition for external use according to any one of claims 1 to 4, further comprising an active ingredient. [Appendix 6] The topical composition described in Appendix 5, wherein the active ingredient is prednisolone valerate acetate. [Appendix 7] 7. The topical composition according to claim 5 or 6, wherein the active ingredient is diphenhydramine hydrochloride. [Appendix 8] 8. The composition for external use according to any one of claims 5 to 7, wherein the active ingredient is a heparinoid. [Appendix 9] 9. The composition for external use according to any one of claims 5 to 8, wherein the active ingredient is dipotassium glycyrrhizinate. [Appendix 10] 10. The composition for external use according to any one of claims 5 to 9, wherein the active ingredient is isopropylmethylphenol. [Appendix 11] 11. The composition for external use according to any one of claims 5 to 10, wherein the active ingredient is zinc paraphenolsulfonate. [Industrial Applicability]

[0077] Although the composition for external use of the present invention contains ethanol or water, it can form a film with excellent adhesion and strength on the body surface, so it can be suitably used as a film-forming composition for external use containing an active ingredient that dissolves in ethanol or water. In addition, although it contains ethanol or water, it has appropriate viscosity and fluidity, and is easy to handle. In these respects, the composition for external use of the present invention has high commercial value.

Claims

1. A topical composition comprising (A) polyvinyl alcohol, (B) polyacrylic acid or a derivative thereof, (C) an alkanolamine, (D) ethanol, and (E) water.

2. A composition for external use comprising (A) polyvinyl alcohol, (B) polyacrylic acid or a derivative thereof, (C) an alkanolamine, (D) ethanol, and (E) water, which forms a coating upon application.

3. The topical composition according to claim 1 or 2, wherein the combined content of components (D) and (E) is 70 to 97% by mass, based on the total amount of the topical composition.

4. The topical composition according to claim 1 or 2, wherein the total content of components (A) and (B) is 2 to 6 mass% based on the total amount of the topical composition.

5. The composition for external use according to claim 1 or 2, further comprising prednisolone valerate acetate.

6. The composition for external use according to claim 1 or 2, further comprising diphenhydramine hydrochloride.

7. The composition for external use according to claim 1 or 2, further comprising isopropyl methylphenol.

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