External preparation composition

Abstract

The present invention addresses the problem of providing a composition for external application which has excellent adhesion to the skin.　The composition for external application of the present invention is characterized by comprising (A) at least one polyhydric alcohol having a molecular weight of 100 to 200 and (B) at least one non-polymeric cationic compound. The component (B) may be a compound, a basic amino acid, an alkanolamine or an alkylamine each containing a metal that can be converted to a cation having a valency of 2 or more in an aqueous solution, and the component (A) may be glucose, sorbitol, fructose, xylitol or erythritol.

Description

[Technical field]

[0001] The present invention relates to an external preparation composition, more specifically, to an external preparation composition having excellent adhesion to the skin. [Background technology]

[0002] Antiperspirants are used by applying them to the skin. Generally, antiperspirants are applied to areas of the body where friction occurs due to contact with other parts of the body or clothing, such as the armpits and back. Therefore, there is a problem that the formulation may peel off from the application site due to friction, and therefore there is a demand for the development of a formulation that adheres better to the application site.

[0003] Patent Document 1 discloses an antiperspirant composition that spreads smoothly when applied, and the resin adheres to the skin even after application, maintaining a dry feeling. This composition contains a deodorant component and specific spherical resin particles. In the antiperspirant composition of Patent Document 1, it is the resin particles that adhere to the skin, not the preparation itself containing the deodorant component.

[0004] On the other hand, Patent Document 2 discloses an antiperspirant composition that does not cause a feeling of tightness or stickiness on the skin after application, has excellent antiperspirant effect and formulation stability, and can suppress darkening of the armpits. This composition contains (A) an antiperspirant component such as an aluminum compound, (B) a specific polyoxypropylene stearyl ether, (C) an anti-inflammatory component, (D) at least one selected from trimethylglycine, sodium pyrrolidone carboxylate, sorbitol, serine, and glycine, (E1) / (E2) a specific polyoxyethylene stearyl ether, and (F) water. The antiperspirant composition of Patent Document 2 does not consider its adhesion to the skin. [Prior art documents] [Patent documents]

[0005] [Patent Document 1] JP 2004-059501 A [Patent Document 2] JP 2018-203683 A Summary of the Invention [Problem to be solved by the invention]

[0006] An object of the present invention is to provide an external preparation composition that has excellent adhesion to the skin. [Means for solving the problem]

[0007] As a result of extensive investigations aimed at solving the above problems, the inventors discovered that by combining a polyhydric alcohol having a specific molecular weight with a cationic non-polymerizable compound, it is possible to provide an external preparation composition having excellent adhesion to the skin, and thus completed the present invention.

[0008] That is, the present invention provides [1] (A) at least one polyhydric alcohol having a molecular weight of 100 to 200, and (B) at least one non-polymerizable cationic compound The present invention relates to an external preparation composition comprising the above compound.

[0009] [2] In the composition [1] above, the number of hydroxy groups in component (A) is preferably 4 or more.

[0010] [3] In the composition of [1] or [2] above, the component (B) is preferably one or more selected from the group consisting of compounds containing a metal that becomes a divalent or higher cation in an aqueous solution, basic amino acids, alkanolamines, and alkylamines.

[0011] [4] In the above compositions [1] to [3], the component (A) is preferably one or more selected from the group consisting of glucose, sorbitol, fructose, xylitol, and erythritol.

[0012] [5] In the composition of [1] to [4] above, component (B) is preferably at least one selected from the group consisting of zinc para - phenolsulfonate, chlorohydroxyaluminum, alum, arginine, and lysine.

[0013] [6] In the composition of [1] to [5] above, the concentration of component (A) is preferably 4 to 20% by weight.

[0014] [7] The external preparation composition of [1] to [6] above is suitable for use as an antiperspirant composition.

[0015] [8] In the composition of [1] to [7] above, when the total amount of component (A) is 1 part by weight, the total amount of component (B) is preferably 0.01 to 25 parts by weight.

[0016] [9] As a preferred embodiment of the composition of [1] above, (A) 1 to 20% by weight of at least one polyhydric alcohol selected from the group consisting of xylitol and erythritol, and (B) 1 to 20% by weight of at least one non - polymerizable cationic compound selected from the group consisting of zinc para - phenolsulfonate, chlorohydroxyaluminum, and alum An antiperspirant composition containing the above is exemplified.

[0017]

[10] As a more preferred embodiment of the composition of [1] above, (A) 1 to 15% by weight of erythritol, and (B) 1 to 20% by weight of at least one non - polymerizable cationic compound selected from the group consisting of zinc para - phenolsulfonate and chlorohydroxyaluminum; Containing, When the total amount of component (A) is 1 part by weight, the total amount of component (B) is in the range of 1 to 3 parts by weight, An antiperspirant composition is exemplified.

[0018]

[11] The compositions according to the above [1] to

[10] are characterized by having a film-forming ability.

[0019]

[12] The present invention also relates to the use of (A) at least one polyhydric alcohol having a molecular weight of 100 to 200 for reacting with (B) at least one non-polymerizable cationic compound to produce a coating that adheres to the skin. In this use, preferred examples, concentrations, parts by weight, combinations, and applications of the components (A) and (B) are as described in [2] to

[10] above. Effect of the Invention

[0020] According to the present invention, it is possible to provide an external preparation composition that has excellent adhesion to the skin. [Brief description of the drawings]

[0021] [Figure 1] FIG. 1 is a photograph showing the device and test method used in the adhesion (coating strength) evaluation test of Test Example 1. [Diagram 2] FIG. 2 is a set of photographs illustrating the test method for the astringency evaluation test in Test Example 2. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0022] The composition of the present invention is characterized by containing (A) at least one polyhydric alcohol having a molecular weight of 100 to 200, and (B) at least one non-polymerizable cationic compound. According to the present invention, a preparation exhibiting high adhesion to the skin can be obtained by blending both the (A) component and the (B) component. Although the mechanism by which the composition of the present invention exhibits excellent skin adhesion is not clear, it is considered possible that the (A) component and the (B) component form a film on the skin due to the interaction between the hydroxyl group generated from the (A) component and the cation of the (B) component, which allows the (A) component and the (B) component to adhere to the skin.

[0023] Usually, compositions that form a film on the skin contain a polymer as a film-forming component. In contrast, the composition of the present invention does not contain a polymer, but contains a polyhydric alcohol as component (A) and a cationic compound (non-polymer) as component (B). Although both components (A) and (B) are low molecular weight, they can form a film on the skin, and thus exhibit high adhesion to the skin.

[0024] The component (A) used in the topical composition of the present invention is a polyhydric alcohol having a molecular weight in the range of 100 to 200 (ie, a molar mass of 100 to 200 g / mol). From the viewpoint of further enhancing the effects of the present invention, the polyhydric alcohol preferably has 2 to 9 hydroxy groups, more preferably 3 to 6 hydroxy groups, and particularly preferably 4 to 5 hydroxy groups. The component (A) used in the topical composition of the present invention is preferably a polyhydric alcohol having a linear carbon chain, because a linear chain is more likely to form a coating, although the mechanism is unclear. From the viewpoint of further enhancing the effect of the present invention, preferred (A) components of the present invention include sugars having a hydroxyl group and a molecular weight of 100 to 200, and more preferably monosaccharides or monosaccharide alcohols. Preferred examples of (A) components include glucose (molecular weight about 180), sorbitol (molecular weight about 182), fructose (molecular weight about 180), xylitol (molecular weight about 152), erythritol (also called erythritol) (molecular weight about 122), 1,6-hexanediol (molecular weight about 118), 1,8-octanediol (molecular weight about 146), 1,9-nonanediol (molecular weight about 160), 1,10-decanediol (molecular weight about 174), 1,11-undecanediol (molecular weight about 188), and 1,2-decanediol (molecular weight about 174). Particularly preferred (A) components are erythritol, xylitol, and sorbitol, more preferably erythritol and xylitol, and most preferably erythritol. The (A) component of the present invention is generally commercially available and therefore easily available.

[0025] The molecular weight of the component (A) used in the topical composition of the present invention is not particularly limited, but is preferably 100 to 200, more preferably 110 to 190, and even more preferably 120 to 160. Polyhydric alcohols with a molecular weight below 100 are not preferred because many of them are liquid at room temperature, making it difficult to form a coating. Polyhydric alcohols with a molecular weight above 200 are not preferred because the coating they form has low adhesion to the skin, probably because their crystallinity is too high. The component (A) used in the topical composition of the present invention is preferably solid at room temperature (e.g., 15 to 25°C).

[0026] In the topical composition of the present invention, the above component (A) may be used alone or in combination of two or more kinds. The content of component (A) of the present invention is not particularly limited, but from the viewpoint of further enhancing the effects of the present invention, the content is preferably 0.01 to 25 weight % (w / w%), more preferably 1 to 20 weight %, even more preferably 3 to 15 weight %, particularly preferably 5 to 12 weight %, and most preferably 7 to 10 weight %, based on the total weight of the composition.

[0027] The component (B) used in the topical composition of the present invention is a non-polymerizable cationic compound. In this specification, a "non-polymerizable" compound means that it is not a polymer formed by polymerization of a monomer. In addition, the "non-polymerizable" compound of the present invention is not a monomer that is polymerized to form a polymer. The component (B) of the present invention is preferably a low molecular weight compound having a molecular weight of 500 or less. In addition, when the component (B) is a hydrate, the molecular weight is H 2 It means the molecular weight excluding O. Specific examples of the component (B) include compounds containing metals that become divalent or higher cations in an aqueous solution, basic amino acids, alkanolamines, and alkylamines.

[0028] When the component (B) is a compound containing a metal that becomes a divalent or higher cation in an aqueous solution, specific examples thereof include aluminum-based compounds (i.e., aluminum compounds that become a trivalent cation [Al 3+ ]), and zinc compounds such as zinc paraphenolsulfonate (i.e., divalent cations [Zn 2+ ]) are mentioned. All of the above compounds have an antiperspirant effect and are known as aluminum-based antiperspirant components and zinc-based antiperspirant components. By using the above antiperspirant component as component (B), the antiperspirant component and the polyhydric alcohol of component (A) form a film on the skin and adhere to the skin. Therefore, according to the present invention, the antiperspirant component itself can be directly adhered to the skin. That is, according to the present invention, it is possible to provide an antiperspirant composition that is difficult to remove from the skin and has a high antiperspirant effect.

[0029] Examples of the basic amino acid of component (B) include arginine, lysine, histidine, tryptophan, and ornithine. These basic amino acids are preferred because they are known to have antibacterial properties.

[0030] Examples of the (B) component that is an alkanolamine include ethanolamine, diethanolamine, triethanolamine, isopropanolamine, diisopropanolamine, triisopropanolamine, methylethanolamine, methyldiethanolamine, 2-amino-2-hydroxymethyl-1,3-propanediol, 2-amino-2-methyl-1-propanol, and 2-amino-2-methyl-1,3-propanediol. These alkanolamines are preferred because they are known to have antibacterial properties.

[0031] Examples of alkylamines in the component (B) include cetyltrimethylammonium bromide, cetylpyridinium bromide, and benzalkonium chloride. These alkylamines are preferred because they are known to have antibacterial properties.

[0032] By using a basic amino acid, alkanolamine, or alkylamine known to have the antibacterial activity as the (B) component, the (B) component having the antibacterial activity and the polyhydric alcohol of the (A) component form a film on the skin and adhere to the skin. Therefore, according to the present invention, the antibacterial component itself can be directly adhered to the skin. In other words, according to the present invention, it is possible to provide a composition that is difficult to remove from the skin and has a high antibacterial effect. Such a composition is useful as a deodorant agent.

[0033] Particularly preferred components (B) are compounds containing a metal that becomes a divalent or higher cation in an aqueous solution. Among these, aluminum chlorohydrate, zinc paraphenolsulfonate, and alum (e.g., AlK(SO 4 ) 2 12H 2 O) is more preferred, aluminum chlorohydrate and zinc paraphenolsulfonate are particularly preferred, and aluminum chlorohydrate is further preferred.

[0034] In the topical composition of the present invention, the above component (B) may be used alone or in combination of two or more kinds. The content of component (B) of the present invention is not particularly limited, but from the viewpoint of further enhancing the effects of the present invention, the content is preferably 0.1 to 20 weight % (w / w%), more preferably 0.3 to 15 weight %, even more preferably 1 to 12 weight %, and particularly preferably 5 to 10 weight %, based on the total weight of the composition.

[0035] In the topical composition of the present invention, when the total amount of component (A) is taken as 1 part by weight, the total amount of component (B) is, from the viewpoint of further enhancing the effects of the present invention, preferably 0.01 to 25 parts by weight, more preferably 0.1 to 8 parts by weight, even more preferably 0.375 to 5 parts by weight, even more preferably 1 to 3 parts by weight, and particularly preferably 1.25 to 1.5 parts by weight.

[0036] The topical composition of the present invention is particularly suitable for use as a preparation requiring improved adhesion to the skin, such as an antiperspirant or deodorant, and is particularly suitable for use as an antiperspirant.

[0037] The present invention can be used to adhere the topical composition to the skin where application is desired, and can also be used to adhere for a long time. By improving adhesion, it is possible to provide a topical composition that is resistant to friction. In particular, by adhering an antibacterial component, it is possible to keep the application site clean and suppress body odor. Therefore, the topical composition of the present invention may be used to keep the application site clean or suppress odor at the application site.

[0038] The topical composition of the present invention may further contain a cooling agent in addition to the above-mentioned (A) and (B) components. The cooling agent is not particularly limited, but for example, menthol, menthyl glyceryl ether, menthyl lactate, peppermint oil, peppermint oil, camphor, and icilin can be used, and among them, menthol is preferable. The cooling agent may be used alone or in combination of two or more kinds.

[0039] When a cooling agent is blended in the topical composition of the present invention, the content is not particularly limited, but is preferably 0.001 to 10% by weight, more preferably 0.01 to 5% by weight, and even more preferably 0.1 to 1% by weight, based on the total weight of the composition.

[0040] The topical composition of the present invention may further contain a surfactant in addition to the above-mentioned components (A) and (B). The surfactant is not particularly limited, and examples thereof include glycerin alkyl ethers such as isostearyl glyceryl ether (monomyristyl glyceryl ether, diisostearyl glyceryl ether, etc.), myristyl glyceryl ether (monomyristyl glyceryl ether, dimyristyl glyceryl ether, etc.), and lauryl glyceryl ether (monolauryl glyceryl ether, dilauryl glyceryl ether, etc.); POE-branched alkyl ethers such as polyoxyethylene (hereinafter sometimes referred to as POE)-octyldodecyl alcohol and POE-2-decyltetradecyl alcohol; POE-alkyl ethers such as POE-oleyl alcohol ether and POE-cetyl alcohol ether; sorbitan esters such as sorbitan monooleate, sorbitan monoisostearate, and sorbitan monolaurate; POE-sorbitan esters such as POE-sorbitan monooleate, POE-sorbitan monoisostearate, and POE-sorbitan monolaurate; glycerin monooleate, glycerol fatty acid esters such as glycerol monostearate and glycerol monomyristate; POE-glycerol fatty acid esters such as POE-glycerol monooleate, POE-glycerol monostearate and POE-glycerol monomyristate; POE-hydrogenated castor oil fatty acid esters such as POE-dihydrocholesterol ester, POE-hydrogenated castor oil and POE-hydrogenated castor oil isostearate; POE-alkylaryl ethers such as POE-octylphenyl ether; POE-glycerol alkyl ethers such as POE-monostearyl glyceryl ether and POE-monomyristyl glyceryl ether; POE·POP alkyl ethers such as polypropylene glycol (hereinafter sometimes referred to as PPG)-4 ceteth-1, PPG-6 decyltetradeceth-20 and polyoxyethylene polyoxypropylene butyl ether (hereinafter polyoxypropylene may be referred to as POP); POP polyglyceryl ethers such as POP diglyceryl ether; POE·POP glyceryl ether;Examples of the surfactant include various nonionic surfactants such as polyglycerol fatty acid esters, such as diglyceryl monostearate, decaglyceryl decastearate, decaglyceryl decastearate, diglyceryl diisostearate, and polyglyceryl monolaurate. Examples of the surfactant include naturally derived surfactants, such as lecithin, hydrogenated lecithin, saponin, sodium surfactin, cholesterol, and bile acid. Preferred surfactants are nonionic surfactants. In the topical preparation composition of the present invention, the above surfactants may be used alone or in combination of two or more.

[0041] When a surfactant is blended in the topical preparation composition of the present invention, its content is not particularly limited, but from the viewpoint of further enhancing the effects of the present invention, it is preferably 0.1 to 20% by weight, more preferably 0.5 to 10% by weight, and even more preferably 1 to 5% by weight, based on the total weight of the composition.

[0042] The topical composition of the present invention may further contain a lower alcohol in addition to the components (A) and (B). In this specification, the lower alcohol means a monohydric alcohol having 1 to 6 carbon atoms. The lower alcohol is not particularly limited as long as it is pharmaceutical or physiologically acceptable. Specific examples include, but are not limited to, ethanol, propanol, isopropanol, n-butyl alcohol, s-butyl alcohol, t-butyl alcohol, isobutyl alcohol, pentyl alcohol, and hexyl alcohol. From the viewpoint of easily exerting the effects of the present invention more effectively, ethanol, propanol, isopropanol, n-butyl alcohol, s-butyl alcohol, t-butyl alcohol, and isobutyl alcohol are preferable, ethanol and isopropanol are more preferable, and ethanol is even more preferable. In the topical composition of the present invention, the above-mentioned lower alcohol may be used alone or in combination of two or more kinds.

[0043] When a lower alcohol is blended in the topical preparation composition of the present invention, its content is not particularly limited, but from the viewpoint of further enhancing the effects of the present invention, the content is preferably 0.1 to 95 wt % (e.g., 1 to 60 wt %), 5 to 80 wt % (e.g., 5 to 50 wt %), more preferably 7 to 75 wt % (e.g., 7 to 40 wt %), and particularly preferably 8 to 10 wt % relative to the total composition.

[0044] The topical composition of the present invention may further contain an oil in addition to the components (A) and (B). The oil is not particularly limited, but examples thereof include hydrocarbons, oils and fats, waxes, ester oils, higher alcohols, higher fatty acids, and silicone oils.

[0045] Examples of hydrocarbons include paraffin, ceresin, isoparaffin, hard fat, microcrystalline wax, polybutene, polyethylene powder, liquid paraffin, squalane, petrolatum, gelled hydrocarbons (such as Plastibase), ozokerite, α-olefin oligomer, light liquid paraffin, and light liquid paraffin.

[0046] Examples of fats and oils include hydrogenated oils such as hydrogenated palm oil and hydrogenated rice bran oil; avocado oil, linseed oil, camellia oil, macadamia nut oil, corn oil, olive oil, safflower oil, apricot kernel oil, cinnamon oil, jojoba oil, grape seed oil, sunflower oil, almond oil, camellia oil, rapeseed oil, sesame oil, cacao butter, coconut oil, hydrogenated coconut oil, palm oil, palm kernel oil, Japan wax kernel oil, Japan wax, wheat germ oil, rice germ oil, rice bran oil, cottonseed oil, soybean oil, peanut oil, tea seed oil, evening primrose oil, kukui nut oil, hazelnut oil, and shea butter.

[0047] Examples of waxes include waxes such as candelilla wax, rice bran wax, cotton wax, carnauba wax, lanolin, isopropyl lanolate, POE lanolin alcohol ether, POE lanolin alcohol acetate, polyethylene glycol lanolate, POE hydrogenated lanolin alcohol ether, shellac wax, and beeswax.

[0048] Examples of ester oils include isopropyl myristate, cetyl octanoate, octyldodecyl myristate, isopropyl palmitate, isopropyl isostearate, octyl palmitate, octyl isopalmitate, cetyl palmitate, butyl stearate, hexyl laurate, myristyl myristate, decyl oleate, isodecyl oleate, hexyldecyl dimethyloctanoate, diisopropyl sebacate, di-2-ethylhexyl sebacate, 2-hexyldecyl myristate, 2-hexyldecyl palmitate, adipine, Diisopropyl acetate, 2-hexyldecyl adipate, isononyl isononanoate, isotridecyl isononanoate, cetyl lactate, myristyl lactate, lanolin acetate, isocetyl stearate, isocetyl isostearate, isostearyl isostearate, cholesteryl 12-hydroxystearate, cholesteryl stearate, cholesteryl oleate, phytosteryl macadamiate, phytosteryl oleate, dextrin palmitate, inulin stearate, hydrogenated jojoba oil, ethylene glycol di-2-ethylhexyl ester, 2-ethylhexyl ester Cetyl ethylhexanoate, dipentaerythritol fatty acid ester, N-alkyl glycol monoisostearate, neopentyl glycol dicaprate, diisostearyl malate, di-2-heptylundecanoate glycerin, tri-2-ethylhexyl trimellitate, tritridecyl trimellitate, trimethylolpropane tri-2-ethylhexyl acid, trimethylolpropane triisostearate, pentaerythritol tetra-2-ethylhexanoate, glycerin tri-2-ethylhexanoate, trimethylolpropane triisostearate, Cetyl 2-ethylhexanoate, glycerin trimyristate, tri(caprylic / capric)glyceryl, tri(caprylic / capric / myristic / stearic)glyceryl, tri-2-heptylundecanoic acid glyceride, castor oil fatty acid methyl ester, oleyl oleate, 2-heptylundecyl palmitate, diisobutyl adipate, di(phytosteryl / octyldodecyl) lauroyl glutamate, di(octyldodecyl / phytosteryl / behenyl) lauroyl glutamate, di-2-heptylundecyl adipate,Ethyl laurate, bisethoxydiglycol cyclohexane-1,4-dicarboxylate, 2-ethylhexyl succinate, diethoxyethyl succinate, triethyl citrate, decaglyceryl (eicosandioate / tetradecanedioate), ethyl acetate, butyl acetate, amyl acetate, triethyl citrate, phytosteryl / isostearyl / cetyl / stearyl / behenyl dimer dilinoleate, polyglyceryl-2 triisostearate, dimer dilinoleyl dimer dilinoleate, dipentaerythritol tripolyhydroxystearate Examples of ester oils include erythrityl, tri(behenic acid / isostearic acid / eicosanedioic acid)glyceryl, (eicosanedioic acid / tetradecanedioic acid)polyglyceryl-10, bisethoxydiglycol cyclohexanedicarboxylate, bis(triethylene glycol monoethyl ether) 1,4-cyclohexanedicarboxylate, bis(diethylene glycol monoethyl ether) adipate, bis(triethylene glycol monoethyl ether) adipate, diethoxyethyl succinate, and diethylhexyl succinate.

[0049] Examples of higher alcohols include higher alcohols having 12 to 22 carbon atoms and sterols. Preferred examples of the higher alcohols include linear saturated alcohols (solid at room temperature) such as lauryl alcohol, myristyl alcohol, cetanol, cetostearyl alcohol, stearyl alcohol, arachyl alcohol, and behenyl alcohol; unsaturated alcohols (liquid at room temperature) such as oleyl alcohol and selachyl alcohol; branched alcohols (liquid at room temperature) such as hexyldecanol, isostearyl alcohol, octyldodecanol, decyltetradecanol, lanolin alcohol, and isostearyl glyceryl ether; and sterols such as phytosterol and cholesterol.

[0050] Examples of higher fatty acids that can be used include saturated or unsaturated straight-chain or branched-chain fatty acids having 12 to 22 carbon atoms. For example, preferred examples include straight-chain saturated fatty acids (solid at room temperature) such as lauric acid, myristic acid, palmitic acid, stearic acid, margaric acid, arachidonic acid, and behenic acid; unsaturated fatty acids (liquid at room temperature) such as oleic acid, linoleic acid, linolenic acid, arachidonic acid, palmitoleic acid, eicosapentaenoic acid, paccenic acid, and docosahexaenoic acid; branched fatty acids such as lanolin fatty acid; and 12-hydroxystearic acid.

[0051] Examples of silicone oils include siloxanes such as methylpolysiloxane, methylphenylpolysiloxane, decamethylcyclopentasiloxane, methylcyclopentasiloxane, highly polymerized methylpolysiloxane, octamethylcyclotetrasiloxane, methylhydrogenpolysiloxane, methyltrimethicone, dimethiconol, and dimethiconol crosspolymer; alkyl-modified silicones such as caprylyl methicone, amino-modified silicones such as aminopropyl dimethicone and amodimethicone, crosslinked methylpolysiloxane, crosslinked alkyl-modified silicone, amino-modified silicone, polyether-modified silicone, polyglycerin-modified silicone, crosslinked polyether-modified silicone, crosslinked alkylpolyether-modified silicone, silicone-alkyl chain co-modified polyether-modified silicone, silicone-alkyl chain co-modified polyglycerin-modified silicone, polyether-modified branched silicone, polyglycerin-modified branched silicone, acrylic silicone, phenyl-modified silicone, and silicone resin.

[0052] When an oil is blended in the topical composition of the present invention, the content thereof is not particularly limited, but from the viewpoint of further enhancing the effects of the present invention, the content is preferably 0.01 to 70% by weight, more preferably 0.1 to 60% by weight, even more preferably 5 to 50% by weight, and particularly preferably 10 to 40% by weight, based on the total weight of the composition.

[0053] In addition to the above-mentioned components, the topical agent composition of the present invention may further contain various components such as moisturizing components, bactericidal components, anti-inflammatory components, sebum-absorbing components, UV-scattering components, UV-absorbing components, components having DNA damage prevention and / or repair effects, whitening components, cell activation components, antioxidant components, anti-aging components, keratin softening components, and vitamins, either alone or in combination of two or more, in order to add other useful effects. These components are not particularly limited as long as they can be used in the fields of medicines, quasi-drugs, and cosmetics, and any components can be appropriately selected and used. Specific examples of such components include isopropylmethylphenol, glycyrrhetinic acid, glycyrrhizinic acid and its salts, and triclosan.

[0054] The vitamins may be either water-soluble or oil-soluble, and examples of such vitamins include retinol derivatives such as retinol, retinol acetate, retinol palmitate, retinol propionate, and retinol linoleate, hydrogenated retinol, retinal, retinoic acid, methyl retinoate, ethyl retinoate, retinol retinoic acid, d-δ-tocopheryl retinoate, α-tocopheryl retinoate, and β-tocopheryl retinoate; provitamin A such as β-carotene, α-carotene, γ-carotene, δ-carotene, lycopene, zeaxanthin, cryptoxanthin, and echinenone; dl-α-tocopherol, dl-α-tocopherol succinate, and dl-α-tocopherol succinate; Vitamin E such as calcium, d-δ-tocopherol, tocopherol nicotinate, dl-α-tocopherol acetate, tocopherol linoleate, tocopherol linoleate / oleate, potassium ascorbyl / tocopheryl phosphate, and ascorbyl tocopheryl maleate; Vitamin B2 such as riboflavin, flavin mononucleotide, flavin adenine dinucleotide, riboflavin butyrate, riboflavin tetrabutyrate, riboflavin 5'-phosphate sodium, and riboflavin tetranicotinate; Nicotinic acids such as methyl nicotinate, nicotinic acid, benzyl nicotinate, nicotinamide, β-butoxyethyl nicotinate, and 1-(4-methylphenyl)ethyl nicotinate;Ascorbyl stearate, disodium isostearyl ascorbyl phosphate, L-ascorbyl dipalmitate, ascorbyl tetraisopalmitate (ascorbyl tetra-2-hexyldecanoate), trisodium ascorbyl palmitate phosphate, methylsilanol ascorbate, ascorbic acid, sodium ascorbate, dehydroascorbic acid, sodium ascorbyl phosphate, magnesium ascorbyl phosphate, disodium ascorbyl sulfate Vitamin C such as ascorbic acid glucoside, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, glyceryl ascorbic acid, bisglyceryl ascorbic acid, hexyl 3-glyceryl ascorbic acid, 3-glyceryl ascorbic acid, myristyl 3-glyceryl ascorbic acid, and 3-laurylglyceryl ascorbic acid; Vitamin D such as methylhesperidin, ergocalciferol, and cholecalciferol; Vitamin K such as phylloquinone and farnoquinone. Vitamin B1 such as thiamine and its salts (e.g., dibenzoylthiamine hydrochloride, thiamine hydrochloride, and thiamine diphosphate); Vitamin B6 such as pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, pyridoxal 5'-phosphate, and pyridoxamine hydrochloride; Vitamin B12 such as cyanocobalamin, hydroxocobalamin, and deoxyadenosylcobalamin; folic acids such as folic acid and pteroylglutamic acid; pantothenic acid, calcium pantothenate, pantothenyl a Pantothenic acids such as alcohol (panthenol), D-pantetheine, D-pantethine, coenzyme A, pantothenyl ethyl ether, and calcium pantetheine sulfonate; biotins such as biotin and biocytin; and vitamin-like factors such as carnitine, ferulic acid, α-lipoic acid, orotic acid, orotic acid, γ-oryzanol, pyrroloquinoline quinone, hesperidin, glucosyl herperidin, glucuronamide, ubiquinone, and salts thereof.

[0055] In addition to the above-mentioned components, the topical agent composition of the present invention can be prepared by appropriately blending components that are commonly used in the fields of medicines, quasi-drugs, cosmetics, etc., depending on the application or dosage form. The components that can be blended are not particularly limited, and can include additives such as bases or carriers, fragrances, antioxidants, preservatives, pH adjusters, chelating agents, stabilizers, irritation reducers, preservatives, colorants, and dispersants. These components can be blended alone or in any combination of two or more.

[0056] The composition of the present invention may contain water (purified water). When the topical preparation composition of the present invention contains water, the content of water is not particularly limited, but from the viewpoint of further enhancing the effect of the present invention, the content of water is preferably 0.001 to 85% by weight, more preferably 10 to 55% by weight, based on the total weight of the composition.

[0057] The topical composition of the present invention preferably does not contain liquefied petroleum gas or isostearic acid, and particularly preferably does not contain a combination of liquefied petroleum gas and isostearic acid.

[0058] The topical composition of the present invention can be prepared in any formulation form known in the fields of medicines, quasi-drugs, cosmetics, etc. Specific examples of the formulation form suitable for application to the skin include, but are not limited to, roll-on, sheet (not for application but for wiping), cream (preferably W / O type), stick, lotion, gel, spray (e.g., aerosol), spray (mist), powder, etc. From the viewpoint of obtaining the effect of the present invention more reliably, the topical composition of the present invention is more preferably in the form of roll-on, sheet, cream, or stick. Such a formulation form can be prepared by any method known to those skilled in the art.

[0059] As a preferred embodiment of the topical composition of the present invention, (A) 1 to 20% by weight (more preferably 3 to 15% by weight, particularly preferably 5 to 12% by weight, and even more preferably 7 to 10% by weight) of at least one polyhydric alcohol (particularly, erythritol) selected from the group consisting of glucose, sorbitol, fructose, xylitol, and erythritol (more preferably, the group consisting of xylitol and erythritol); and (B) 1 to 20% by weight (more preferably 1 to 15% by weight, particularly preferably 1 to 12% by weight, and even more preferably 5 to 10% by weight) of at least one non-polymerizable cationic compound (particularly, aluminum chlorohydrate) selected from the group consisting of zinc paraphenolsulfonate, aluminum chlorohydrate, alum, arginine, and lysine (more preferably, the group consisting of zinc paraphenolsulfonate, aluminum chlorohydrate, and alum); The antiperspirant composition (particularly preferably, an antiperspirant composition in the form of a roll-on, sheet, cream, or stick) containing In the antiperspirant composition, when the total amount of the component (A) is taken as 1 part by weight, the total amount of the component (B) is preferably in the range of 0.1 to 8 parts by weight (more preferably 0.375 to 5 parts by weight, particularly preferably 1 to 3 parts by weight, and even more preferably 1.25 to 1.5 parts by weight). The antiperspirant composition preferably contains benzalkonium chloride (also called benzalkonium chloride) and / or isopropylmethylphenol in an amount of 0.01 to 0.2% by weight (more preferably 0.03 to 0.1% by weight, respectively). The antiperspirant composition preferably further contains water (purified water) and / or ethanol (for example, absolute ethanol).

[0060] As a more preferred embodiment of the topical composition of the present invention, (A) 1 to 15% by weight (more preferably 3 to 15% by weight, particularly preferably 5 to 12% by weight, and even more preferably 7 to 10% by weight) of erythritol; and (B) 1 to 20% by weight (more preferably 1 to 15% by weight, particularly preferably 1 to 12% by weight, and even more preferably 5 to 10% by weight) of at least one non-polymerizable cationic compound selected from the group consisting of zinc p-phenolsulfonate and aluminum chlorohydrate (particularly, aluminum chlorohydrate); Contains An example of an antiperspirant composition (particularly preferably an antiperspirant composition in the form of a roll-on, sheet, cream, or stick) is one in which the total amount of the component (B) is in the range of 1 to 3 parts by weight (more preferably 1.25 to 1.5 parts by weight) when the total amount of the component (A) is 1 part by weight. The antiperspirant composition preferably contains benzalkonium chloride and / or isopropyl methylphenol (preferably both) in an amount of 0.01 to 0.2% by weight (more preferably 0.03 to 0.1% by weight), and further preferably contains water (purified water) and / or ethanol (e.g., absolute ethanol).

[0061] The method of using the topical composition of the present invention may vary depending on the skin condition, age, sex, season, and other conditions of the subject. In general, an appropriate amount (about 0.001 to 0.1 g / cm) is applied to any part of the skin where it is desired to exert an antiperspirant or antibacterial effect (preferably the face, behind the ears, neck, décolleté, back, armpits, hands, feet, etc.). 2 The composition of the present invention may be applied by any method known in the art, such as application of a dose of about 100 mg / kg or more (about 1 to 5 times a day). The topical composition of the present invention may be used regularly several times a day (for example, about 1 to 5 times a day), or may be used irregularly at a desired timing to exert the antiperspirant or antibacterial effect. The period of use is not particularly limited, and may be, for example, a few days (for example, about 3 days) to about 3 months, preferably about 1 week to about 1 month.

[0062] The pH of the topical composition of the present invention can be appropriately set depending on the types of components (A) and (B), the types and contents of other blended components, the formulation form, the method of use, etc. There are no limitations as long as it is within a physiologically or pharma- ceutical acceptable range, but from the viewpoint of safety, such as skin irritation, the pH of the composition can be, for example, 2 to 9, preferably about 3 to 8, and more preferably about 5 to 7.

[0063] The container that fills the topical agent composition of the present invention is not particularly limited. It may be used as a container for topical pharmaceuticals, quasi-drugs, or cosmetics. For example, the container that contacts the topical agent composition includes a part or all of the surface, preferably all of the surface, 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.

[0064] From the viewpoint of ease of handling, preferred materials for the container in which the topical agent composition of the present invention is filled include polyethylene (PE) (including high density polyethylene (HDPE), low density polyethylene (LDPE), very low density polyethylene, linear low density polyethylene (LLDPE), and ultra-high molecular weight polyethylene, etc.); polypropylene (PP) (including isotactic polypropylene, syndiotactic polypropylene, and atactic polypropylene, etc.); polyolefin resins such as ethylene-propylene copolymer, polymethylpentene, polybutene-1, and 1,2-polybutadiene; and polyester resins such as polyethylene terephthalate, polybutylene terephthalate, and polyethylene naphthalate. Polyethylene or polypropylene is more preferred.

[0065] In the preceding paragraph, the preferred compound names of the essential and optional components used in the composition of the present invention have been described, but the composition of the present invention also includes compositions obtained by arbitrarily combining these and compositions obtained by arbitrarily combining the content (concentration) ranges of each component. In addition, the above-mentioned numerical ranges of concentration, pH, weight parts, etc. can also be arbitrarily combined, and when multiple numerical ranges are described, the upper limit or lower limit of each numerical range can also be arbitrarily combined.

[0066] The composition of the present invention will be described in more detail below with reference to Test Examples and Examples, but the present invention is not limited to these Examples.

[0067] <Test Example 1: Evaluation of Adhesion (Coating Strength)> The topical agent composition of the present invention is prepared, applied to one side of a flexible sheet, and dried to form a coating on the sheet.Then, the sheet with the coating formed on its surface is gradually curved, and the amount of the coating peeled off from the sheet is measured to evaluate the adhesion of the coating (i.e., the less the amount of the coating peeled off from the sheet, the higher the adhesion of the coating).The evaluation method is described in more detail below.

[0068] The topical agent composition (aqueous solution) shown in Table 1 was prepared. 1 mL of this aqueous solution was dropped onto the center (position of 7 cm long and 3.5 cm wide) of a rectangular silicone rubber sheet with a thickness of 0.1 mm, length of 14 cm, and width of 7 cm, and dried at 25°C and humidity of 50±5% for two days. Then, the upper and lower ends of the silicone rubber sheet were fixed vertically to an AUTOGRAPH AGS-X 5kN (Shimadzu Corporation) equipped with a screw plane type gripper. At this time, the upper and lower ends of the silicone rubber sheet were fixed so that the upper surface of the gripper teeth of the upper gripper and the upper end of the silicone rubber sheet were in the same position, and the lower surface of the gripper teeth of the lower gripper and the lower end of the silicone rubber sheet were in the same position. In addition, the left and right sides of the silicone rubber sheet were fixed so that the center of each gripper tooth and the center of the silicone rubber sheet were aligned. Then, a compression test was started (i.e., the upper gripper was brought close to the lower gripper). The compression (approach) speed was 100 mm / min, and the test was continued until the stroke of the upper gripper reached 40 mm. Immediately after the start of the operation (less than 1 second after the start), the surface of the silicone rubber sheet on which the coating was formed was induced to sink in parallel to the horizontal direction of the silicone rubber sheet (the edge of the center part of the silicone rubber sheet (i.e., the position 7 cm vertically) was grasped to induce the position where the formulation was applied to sink in). The silicone rubber sheet curved with compression (see Figure 1). When the stroke reached 40 mm, the sheet was bent to an irreversible state. The weight change of the coating adhered to the silicone rubber sheet before and after the compression test was measured, and the weight loss rate of the coating was calculated according to formula 1. If the formed coating is weak against bending, i.e., has low adhesion, part or all of the coating peels off from the silicone rubber sheet during compression, resulting in a high weight loss rate. In addition, the weaker the coating is against bending and the lower the adhesion, the more likely it is to peel off even when the stroke is small. When the coating adhered to the silicone rubber sheet and did not peel off at all, the weight loss rate was recorded as 0. The results are summarized in Table 1. Note that, when the topical preparation composition did not solidify when dried and dripped from the silicone rubber sheet, it was recorded as unmeasurable (-). Formula 1: TIFF0007682095000001.tif20169, S 0 represents the weight of the silicon rubber sheet itself, and S1 represents the weight (before compression test) measured after dropping the topical composition onto a silicone rubber sheet and drying it, and S 2 represents the weight measured after the compression test.

[0069] [Table 1]

[0070] The numerical value of each component in Table 1 indicates weight %, and the sum of the "balance" of purified water and the numerical values ​​of the other components is 100 (weight %) (for example, the remaining amount of purified water in Example 1-1 is 80). As shown in Table 1, in the case of the topical preparation composition containing only a polyhydric alcohol having a molecular weight of 100 to 200 (Comparative Example 1-1) and the topical preparation composition containing only a non-polymerizable cationic compound (Comparative Example 1-2, Comparative Example 1-4), the bending strength of the coating was low, and the strength considered to be sufficient for adhesion to the skin was not obtained. Although it is not intended to be bound by any theory, it is believed that this is due to the high crystallinity of the polyhydric alcohol and metal salt, which are solid at room temperature. In addition, the topical preparation composition containing glycerin and chlorohydroxyaluminum (Comparative Example 1-3) did not form a coating, and the topical preparation composition dripped from the silicone rubber sheet. Although it is not intended to be bound by any theory, it is believed that this is due to the fact that glycerin is liquid at room temperature (has a small molecular weight). In Comparative Example 1-1, most of the coating peeled off when the stroke was about 31 mm. In Comparative Example 1-2, most of the coating peeled off when the stroke was about 13 mm. In Comparative Example 1-4, most of the coating peeled off when the stroke was about 28 mm. On the other hand, in the case of the topical preparation composition (Examples 1-1 to 1-10) containing both a polyhydric alcohol having a molecular weight of 100 to 200 and a non-polymerizable cationic compound, even after the silicone rubber sheet was folded, the coating remained adhered to the sheet, and the weight loss rate was 0%. From this, it was confirmed that the combined use of a polyhydric alcohol having a molecular weight of 100 to 200 and a non-polymerizable cationic compound improves the adhesion of the coating (increases the bending strength of the coating), and makes it less likely to peel off even when subjected to physical stimulation.

[0071] <Test Example 2: Astringency Evaluation> The topical agent compositions shown in Table 2 were prepared. Next, 1 ml of each composition was dropped onto the center of a 5 cm x 5 cm artificial leather (Idemitsu Technofine Co., Ltd., product number: PBZ13001, black) placed in a glass petri dish with a diameter of 7 cm, and dried overnight at room temperature without covering. If the composition has astringency, the artificial leather will shrink as the composition dries. After one night, the artificial leather was measured for waviness caused by shrinkage, as shown in Figure 2 (the artificial leather was placed on a transparent petri dish to make it easier to see), and the height from the horizontal plane of the most waviness part (the highest part relative to the horizontal plane) of each artificial leather was measured, and the improvement degree was calculated according to Formula 2 and compared. The higher the degree of improvement in astringency, the more suppressed the astringency. The results are summarized in Table 2. Note that the degree of improvement in astringency was 100% for those without astringency. Here, Examples 2-1 and 2-2 were calculated based on Comparative Example 2-1, and Examples 2-3 to 2-6 were calculated based on Comparative Example 2-2. Formula 2: TIFF0007682095000003.tif20169

[0072] [Table 2]

[0073] In the compositions containing only aluminum chlorohydrate (Comparative Examples 2-1 and 2-2), the artificial leather was significantly wavy and had strong astringency. In contrast, in the compositions further containing a polyhydric alcohol having a molecular weight of 100 to 200 (Examples 2-1 to 2-6), it was confirmed that the waviness was small and the astringency was weak. In other words, by using aluminum chlorohydrate in combination with a polyhydric alcohol having a molecular weight of 100 to 200, it became possible to reduce the astringency of aluminum chlorohydrate. The astringent action of aluminum chlorohydrate, an antiperspirant ingredient, may cause users to complain of skin irritation (such as tightness, tingling, and itching). This astringent action is not correlated with the antiperspirant action, and the antiperspirant action can be obtained without the astringent action. Therefore, it is preferable that the astringent action felt as skin irritation is low. In this experiment, it was unexpectedly confirmed that the astringent action of the antiperspirant ingredient is suppressed by polyhydric alcohols having a molecular weight of 100 to 200. Therefore, according to the present invention, it is possible to reduce the skin irritation caused by the astringent antiperspirant ingredient.

[0074] [Formulation example] Formulation examples of the topical composition of the present invention are shown below (% means % by weight). These can be produced according to the usual method for each form.

[0075] Formulation example 1: Antiperspirant (cream) Benzalkonium chloride 0.07% Isopropyl methylphenol 0.07% Aluminum chlorohydrate 16% Cyclopentasiloxane 25% Alkyl polyacrylate 6% POE / POP dimethicone copolymer 3.5% Concentrated glycerin 7% Isononyl isononanoate 5% l-Menthol 0.5% Erythritol 10% Purified water remainder Total 100%

[0076] Formulation example 2: Antiperspirant (gel) Benzalkonium chloride 0.06% Isopropyl methylphenol 0.05% Aluminum chlorohydrate 8% Magnesium aluminometasilicate 0.5% Dipropylene glycol 10% Polyoxyethylene glycol 0.5% Hydroxypropyl methylcellulose 0.5% Xanthan gum 0.5% Ethanol 10% l-Menthol 0.3% l-Menthyl glyceryl ether 0.3% Peppermint oil 0.3% Fragrance 0.3% Xylitol 15% Purified water remainder Total 100%

[0077] Formulation example 3: Antiperspirant (roll-on) Benzalkonium chloride 0.06% Isopropyl methylphenol 0.06% Zinc paraphenol sulfonate 5% Butylene glycol 5% Talc 3% Nylon powder 0.5% Cetyltrimethylammonium bromide solution 1% Hydrophobized hydroxypropyl methylcellulose 0.1% Absolute ethanol 40% Erythritol 4% Xylitol 4% Purified water remainder Total 100%

[0078] Formulation example 4: Antiperspirant (mist) Benzalkonium chloride 0.05% Isopropyl methylphenol 0.06% Zinc paraphenol sulfonate 1% Butylene glycol 3% Aluminum chlorohydrate 0.05% Sericite Complex 0.2% l-Menthol 0.5% Fragrance 0.05% Absolute ethanol 60% Sorbitol 1% Purified water remainder Total 100%

[0079] Formulation example 5: Antiperspirant (stick) Benzalkonium chloride 0.055% Isopropyl methylphenol 0.05% Aluminum chlorohydrate 5% Polyethylene wax 5% Microcrystalline wax 5% Glyceryl monostearate 3% Octyldodecanol 5% Talc 10% Methylpolysiloxane 5% Decamethylpentasiloxane 35% Silylated anhydrous silica 1% Hydroxyapatite 0.3% Cetyltrimethylammonium bromide solution 0.5% Zinc oxide 0.3% Fragrance 0.1% Cetanol 4% Stearyl alcohol 4% Erythritol 1% Purified water remainder Total 100%

[0080] Formulation Example 6: Antiperspirant (sheet) Aluminum chlorohydrate 1% Polyoxyethylene polyoxypropylene decyl tetradecyl ether 1% Methylsiloxane network copolymer 0.2% Absolute ethanol 25% Paraben 0.1% Erythritol 0.5% Fragrance 0.02% pH adjuster (appropriate amount) Purified water remainder Total 100% [Industrial Applicability]

[0081] According to the present invention, it is possible to realize an external preparation composition that has high adhesion to the skin without using a polymer. In particular, the external preparation composition of the present invention is suitable for use as an antiperspirant by using an antiperspirant component as component (B).

Claims

1. (A) erythritol (excluding erythritol contained on or inside the powder), (B) a non-polymerizable cationic compound, such as an aluminum-based compound and / or a zinc-based compound, and (C) 10% by weight or more of water Contains An external application composition having a form selected from a roll-on, a cream, a stick, a lotion, a gel, a spray, an aerosol, and a powder. (However, the following compositions are excluded. - compositions containing alum and urea; - Deodorant / antiperspirant containing water, aluminum chlorohydrate, steareth-2, cyclopentasiloxane, PPG-15 stearyl, glycerin, steareth-21, xylityl glucoside, anhydrous xylitol, xylitol, grapefruit seed extract, and fragrance; Deodorant / antiperspirant containing water, butylene glycol, sodium stearate, glycerin, alcohol, xylitol, apple fruit water, lemon fruit extract, orange flower water, peppermint extract, tea leaf extract, pearl extract, aloe barbadensis leaf polysaccharide, styrene / alkyl acrylate copolymer, propanediol, ethylhexylglycerin, cholesterol-24, 1,2-hexanediol, caprylyl glycol, 1,2-pentanediol, polyglutamic acid, sodium hyaluronate, octanediol, aluminum chlorohydrate, and fragrance; Deodorant / antiperspirant containing: Water, Cyclomethicone, Aluminum Chlorohydrate, Butylene Glycol, Bis(PEG / PPG-14 / 14) Dimethicone, Xylitol, Hydrogenated Polydecene, Fragrance, PEG / PPG-18 / 18 Dimethicone, Cetyl PEG / PPG-10 / 1 Dimethicone, Nylon-12, Polysorbate 20, Sodium Disodium EDTA, Citronellol, Caprylyl Glycol, Methylisothiazolinone, Geraniol, and Pentaerythrityl Tetra(di-t-butyl hydroxyhydrocinnamate).

2. The topical composition according to claim 1, wherein the concentration of the component (A) is 4 to 20% by weight.

3. The topical composition according to claim 1 or 2, which is an antiperspirant composition.

4. The topical composition according to any one of claims 1 to 3, wherein the total amount of the component (B) is 0.01 to 25 parts by weight when the total amount of the component (A) is 1 part by weight.

5. (A) 4 to 20% by weight of erythritol, and (B) 1 to 15% by weight of at least one selected from the group consisting of zinc paraphenolsulfonate and aluminum chlorohydrate. Contains the total amount of component (B) is in the range of 0.375 to 5 parts by weight when the total amount of component (A) is 1 part by weight, The topical composition according to claim 1 , which is an antiperspirant composition.

6. The topical composition according to any one of claims 1 to 5, which has a film-forming ability.

7. A method for forming a coating that adheres closely to the skin by applying the topical composition according to any one of claims 1 to 6 to the skin.

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