RESIDENTIAL PRODUCTS

Abstract

The invention relates to a localized composition exhibiting superior adhesion to the skin. This localized composition consists of (A) at least one polyhydric alcohol with a molecular weight between 100 and 200, and (B) at least one non-polymerizable cationic compound. Composition (B) may be a metal-containing compound with a divalent or higher valence in aqueous solution, a basic amino acid, an alkanol amine, or an alkyl amine, and composition (A) may be glucose, sorbitol, fructose, xylitol, or erytritol.

Description

External preparation composition

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

[0002] Antiperspirants are applied 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 of the formulation peeling off from the application site due to friction, and therefore there is a need to develop a formulation that adheres better to the application site.

[0003] Patent Document 1 discloses an antiperspirant composition that spreads smoothly upon application, and the resin adheres to the skin even after application, providing a sustained, dry feel. 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 formulation 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 underarm darkening. 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.

[0005] JP 2004-059501 A JP 2018-203683 A

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

[0007] As a result of extensive investigations to solve the above-mentioned problems, the present inventors discovered that a topical preparation composition having excellent adhesion to the skin can be provided by using a polyhydric alcohol having a specific molecular weight in combination with a cationic non-polymerizable compound, and thus completed the present invention.

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

[0009] [2] In the composition of the above [1], 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 at least one selected from the group consisting of a compound containing a metal that becomes a divalent or higher cation in an aqueous solution, a basic amino acid, an alkanolamine, and an alkylamine.

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

[0012] [5] In the compositions [1] to [4] above, the component (B) is preferably one or more selected from the group consisting of zinc paraphenolsulfonate, aluminum chlorohydrate, alum, arginine, and lysine.

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

[0014] [7] The topical compositions of [1] to [6] above are suitable for use as antiperspirant compositions.

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

[0016] [9] A preferred embodiment of the composition of [1] above is an antiperspirant composition containing: (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 p-phenolsulfonate, aluminum chlorohydrate, and alum.

[0017]

[10] A more preferred embodiment of the composition of [1] above is an antiperspirant composition containing: (A) 1 to 15 wt % of erythritol; and (B) 1 to 20 wt % of at least one non-polymerizable cationic compound selected from the group consisting of zinc p-phenolsulfonate and aluminum chlorohydrate; wherein the total amount of component (B) is in the range of 1 to 3 parts by weight when the total amount of component (A) is 1 part by weight.

[0018]

[11] The compositions according to any one of [1] to

[10] above are characterized by having 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 form a coating that adheres to the skin. Preferred examples, concentrations, parts by weight, combinations, and applications of the components (A) and (B) in this use are as described in [2] to

[10] above.

[0020] According to the present invention, an external preparation composition having excellent adhesion to the skin can be provided.

[0021] Fig. 1 is a photograph showing the apparatus and test method used in the adhesion (coating strength) evaluation test of Test Example 1. Fig. 2 is a photograph explaining the test method of the astringency evaluation test of Test Example 2.

[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, by blending both component (A) and component (B), a preparation exhibiting high adhesion to skin can be obtained. Although the mechanism by which the composition of the present invention exhibits excellent skin adhesion is not clear, it is thought that the interaction between the hydroxy groups generated from component (A) and the cations of component (B) may cause components (A) and (B) to form a film on the skin, thereby adhering to the skin.

[0023] Typically, 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 rather contains a polyhydric alcohol (A) and a cationic compound (non-polymer) (B). Both components (A) and (B) are low molecular weight compounds that can form a film on the skin, thereby exhibiting high adhesion to the skin.

[0024] The component (A) used in the topical preparation composition of the present invention is a polyhydric alcohol having a molecular weight in the range of 100 to 200 (i.e., 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. The number of hydroxy groups is more preferably 3 to 6, and particularly preferably 4 to 5. The component (A) used in the topical preparation composition of the present invention is preferably a polyhydric alcohol having a linear carbon chain. Although the mechanism is unclear, this is because a linear chain makes it easier to form a coating. From the viewpoint of further enhancing the effects of the present invention, preferred components of the present invention include saccharides having hydroxy groups and a molecular weight of 100 to 200, with monosaccharides or monosaccharide alcohols being particularly preferred. Preferred examples of component (A) include glucose (molecular weight: approximately 180), sorbitol (molecular weight: approximately 182), fructose (molecular weight: approximately 180), xylitol (molecular weight: approximately 152), erythritol (also known as erythritol) (molecular weight: approximately 122), 1,6-hexanediol (molecular weight: approximately 118), 1,8-octanediol (molecular weight: approximately 146), 1,9-nonanediol (molecular weight: approximately 160), 1,10-decanediol (molecular weight: approximately 174), 1,11-undecanediol (molecular weight: approximately 188), and 1,2-decanediol (molecular weight: approximately 174). Particularly preferred components (A) are erythritol, xylitol, and sorbitol, more preferably erythritol and xylitol, and most preferably erythritol. The component (A) of the present invention is generally commercially available and therefore easily available.

[0025] The molecular weight of 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 of less than 100 are not preferred because many of them are liquid at room temperature, making it difficult to form a film. Polyhydric alcohols with a molecular weight of more than 200 are not preferred because the film they form has poor adhesion to the skin, perhaps due to their excessively high crystallinity. It is preferred that component (A) used in the topical composition of the present invention is solid at room temperature (e.g., 15 to 25°C).

[0026] In the topical preparation composition of the present invention, the above-mentioned component (A) may be used alone or in combination of two or more. 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, it is preferably 0.01 to 25 wt% (w / w%), more preferably 1 to 20 wt%, even more preferably 3 to 15 wt%, particularly preferably 5 to 12 wt%, and most preferably 7 to 10 wt%, 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. Furthermore, the "non-polymerizable" compound of the present invention is not a monomer that polymerizes 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. Note that, when the component (B) is a hydrate, the molecular weight refers to the molecular weight excluding HO. Specific examples of the component (B) include compounds containing metals that become divalent or higher cations in 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 compounds (i.e., trivalent cations [Al 3+]), and zinc compounds such as zinc paraphenolsulfonate (i.e., divalent cations [Zn 2+ ]) are exemplified. All of the above compounds have antiperspirant properties 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. In other words, 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 basic amino acids in component (B) include arginine, lysine, histidine, tryptophan, and ornithine, which are known to have antibacterial properties and are therefore preferred.

[0030] Examples of alkanolamines used as component (B) 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 used as 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 antibacterial activity as component (B), component (B) having antibacterial activity 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 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.

[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)·12H0) are more preferred, aluminum chlorohydrate and zinc paraphenolsulfonate are particularly preferred, and aluminum chlorohydrate is even more preferred.

[0034] In the topical preparation composition of the present invention, the above-mentioned component (B) may be used alone or in combination of two or more. 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, it is preferably 0.1 to 20 wt % (w / w %), more preferably 0.3 to 15 wt %, even more preferably 1 to 12 wt %, and particularly preferably 5 to 10 wt %, based on the total weight of the composition.

[0035] In the topical preparation 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 that requires 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 an external preparation composition to the desired skin area, and can also be used to maintain long-term adhesion. By improving adhesion, an external preparation composition that is resistant to friction can be provided. In particular, by adhering an antibacterial component to the external preparation composition, the application area can be kept clean and body odor can be suppressed. Therefore, the external preparation composition of the present invention may be used to keep the application area clean or to suppress odor at the application area.

[0038] The topical composition of the present invention may further contain a cooling agent in addition to the components (A) and (B). The cooling agent is not particularly limited, but examples thereof include menthol, menthyl glyceryl ether, menthyl lactate, peppermint oil, camphor, and icilin, with menthol being preferred. The cooling agent may be used alone or in combination of two or more.

[0039] When a cooling agent is blended in the topical composition of the present invention, the content thereof 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 components (A) and (B). The surfactant is not particularly limited, but examples thereof include glycerin alkyl ethers such as isostearyl glyceryl ether (monoisostearyl 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.); polyoxyethylene (hereinafter sometimes referred to as POE)-octyldodecyl alcohol; POE-branched alkyl ethers such as POE-2-decyltetradecyl 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, Glycerin fatty acid esters such as glycerin monostearate and glycerin monomyristate; POE-glycerin fatty acid esters such as POE-glycerin monooleate, POE-glycerin monostearate, and POE-glycerin 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-monosulfan POE-glycerin alkyl ethers such as tearyl 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 sometimes 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 polyglycerin fatty acid esters, such as diglyceryl monostearate, decaglyceryl decastearate, decaglyceryl decaisostearate, diglyceryl diisostearate, and polyglyceryl monolaurate. Other examples include naturally occurring surfactants such as lecithin, hydrogenated lecithin, saponin, sodium surfactin, cholesterol, and bile acids. 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 into the topical preparation 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 0.1 to 20 wt %, more preferably 0.5 to 10 wt %, and even more preferably 1 to 5 wt %, 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, "lower alcohol" refers to a monohydric alcohol having 1 to 6 carbon atoms. The lower alcohol is not particularly limited as long as it is pharmaceutically 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 more effectively achieving the effects of the present invention, ethanol, propanol, isopropanol, n-butyl alcohol, s-butyl alcohol, t-butyl alcohol, and isobutyl alcohol are preferred, ethanol and isopropanol are more preferred, and ethanol is even more preferred. In the topical composition of the present invention, the above lower alcohols may be used alone or in combination of two or more.

[0043] When a lower alcohol is blended into 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 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 weight of the 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, cocoa 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 candelilla wax, rice bran wax, cotton wax, carnauba wax, lanolin, isopropyl lanolinate, POE lanolin alcohol ether, POE lanolin alcohol acetate, polyethylene glycol lanolinate, 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 adipate, 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, glycerin di-2-heptylundecanoate, tri-2-ethylhexyl trimellitate, tritridecyl trimellitate, trimethylolpropane tri-2-ethylhexylate, trimethylolpropane triisostearate, pentaerythritol tetra-2-ethylhexanoate, glycerin tri-2-ethylhexanoate, trimethylolpropane triisostearate, Cetyl 2-ethylhexanoate, glycerin trimyristate, caprylic / capric triglyceride, caprylic / capric / myristic / stearic triglyceride, 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 eicosanedioate / tetradecanedioate, ethyl acetate, butyl acetate, amyl acetate, triethyl citrate, phytosteryl / isostearyl / cetyl / stearyl / behenyl dimer dilinoleate, polyglyceryl-2 triisostearate, dimer dilinoleyl dimer dilinoleate, dipentaerythrityl tripolyhydroxystearate Examples of ester oils include erythrityl, glyceryl tri(behenate / isostearate / eicosanedioate), polyglyceryl-10 (eicosanedioate / tetradecanedioate), 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 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. 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 into the topical preparation 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 thereof is, for example, 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 composition of the present invention may further contain various components, such as moisturizing components, bactericidal components, anti-inflammatory components, sebum-adsorbing components, UV-scattering components, UV-absorbing components, components having the effect of preventing and / or repairing DNA damage, whitening components, cell-activating components, antioxidant components, anti-aging components, keratin-softening components, and vitamins, either alone or in combination to impart other useful effects. These components are not particularly limited as long as they can be used in the fields of pharmaceuticals, quasi-drugs, cosmetics, etc., 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 thereof include vitamin A such as retinol derivatives such as retinol, retinol acetate, retinol palmitate, retinol propionate, and retinol linoleate, hydrogenated retinol, retinal, retinoic acid, methyl retinoate, ethyl retinoate, retinol retinoate, 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 compounds 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 compounds 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 compounds 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 compounds such as methylhesperidin, ergocalciferol, and cholecalciferol; Vitamin K compounds such as phylloquinone and farnoquinone. Vitamin B1s such as thiamine and its salts (e.g., dibenzoylthiamine hydrochloride, thiamine hydrochloride, and thiamine diphosphate); Vitamin B6s such as pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, 5'-pyridoxal phosphate, and pyridoxamine hydrochloride; Vitamin B12s such as cyanocobalamin, hydroxocobalamin, and deoxyadenosylcobalamin; folates such as folic acid and pteroylglutamic acid; pantothenic acid, calcium pantothenate, pantothenyl a Examples of suitable anti-inflammatory agents include pantothenic acids such as alcohol (panthenol), D-pantetheine, D-pantethine, coenzyme A, pantothenyl ethyl ether, and calcium pantetheine sulfonate; biotins such as biocytin; and vitamin-like factors such as carnitine, ferulic acid, α-lipoic acid, orotic acid, orotic acid, γ-oryzanol, pyrroloquinoline quinone, hesperidin, glucosyl herperidin, glucurolactone, glucuronic acid amide, ubiquinone, and salts thereof.

[0055] In addition to the above-mentioned components, the topical composition of the present invention can be prepared by appropriately blending components commonly used in the fields of pharmaceuticals, quasi-drugs, cosmetics, etc., depending on the intended use or dosage form. The components that can be blended are not particularly limited, and examples of additives that can be blended include bases or carriers, fragrances, antioxidants, preservatives, pH adjusters, chelating agents, stabilizers, irritation-reducing agents, antiseptics, colorants, and dispersants. These components can be blended singly 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 is formulated with water, the content of water is not particularly limited, but from the viewpoint of further enhancing the effects of the present invention, the content is preferably 0.001 to 85 wt %, more preferably 10 to 55 wt %, 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 known in the fields of pharmaceuticals, quasi-drugs, cosmetics, etc. Specific examples of formulations suitable for application to the skin include, but are not limited to, roll-on, sheet (referring to wipe-off type sheets, not patches), cream (preferably W / O type), stick, lotion, gel, spray (e.g., aerosol), spray (mist), powder, etc. From the viewpoint of achieving the effects of the present invention more reliably, the topical composition of the present invention is more preferably in the form of a roll-on, sheet, cream, or stick. Such formulations can be prepared by any method known to those skilled in the art.

[0059] A preferred embodiment of the topical composition of the present invention is an antiperspirant composition (particularly preferably an antiperspirant composition in the form of a roll-on, sheet, cream, or stick) containing: (A) 1 to 20 wt % (more preferably 3 to 15 wt %, particularly preferably 5 to 12 wt %, and even more preferably 7 to 10 wt %) 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 wt % (more preferably 1 to 15 wt %, particularly preferably 1 to 12 wt %, and even more preferably 5 to 10 wt %) 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). In the antiperspirant composition, when the total amount of component (A) is taken as 1 part by weight, the total amount of 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 known as benzalkonium chloride) and / or isopropylmethylphenol in amounts of 0.01 to 0.2% by weight (more preferably 0.03 to 0.1% by weight). The antiperspirant composition preferably further contains water (purified water) and / or ethanol (e.g., absolute ethanol).

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

[0061] The method of use of the topical composition of the present invention may vary depending on the skin condition, age, sex, season, and other factors of the subject. Generally, an appropriate amount (about 0.001 to 0.1 g / cm) is applied to any area of ​​the skin where antiperspirant and antibacterial effects are desired (preferably the face, behind the ears, neck, décolleté, back, armpits, hands, feet, etc.). 2 A dose of the composition (about 1000 mg / day) is applied by any method known in the art, such as application of a topical application. The topical application 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 when it is desired to exert the antiperspirant and antibacterial effects. The period of use is not particularly limited, and may be, for example, from several days (for example, about 3 days) to about 3 months, preferably from about 1 week to about 1 month.

[0062] The pH of the topical preparation composition of the present invention can be appropriately set depending on the types of component (A) and component (B), the types and contents of other blended components, the formulation, the method of use, etc. There are no limitations as long as it is within a physiologically or pharmaceutically 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 for filling the topical preparation composition of the present invention is not particularly limited. It may be any container used for topical pharmaceutical preparations, quasi-drugs, or cosmetics. Examples of such containers include containers in which a part or all, preferably all, of the surface that comes into contact with the topical preparation 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.

[0064] From the viewpoint of ease of handling, preferred materials for the container filling the topical composition of the present invention 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); polypropylene (PP) (including isotactic polypropylene, syndiotactic polypropylene, and atactic polypropylene); 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, 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. Furthermore, the numerical ranges of the above-mentioned concentrations, pH, parts by weight, etc. can also be arbitrarily combined, and when multiple numerical ranges are described, the upper and lower limits of each numerical range can also be arbitrarily combined.

[0066] The composition of the present invention will be explained 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 composition of the present invention was prepared, applied to one side of a flexible sheet, and dried to form a coating on the sheet. The sheet with the coating formed on its surface was then gradually curved, and the amount of coating that peeled off from the sheet was measured to evaluate the adhesion of the coating (i.e., the less coating that peeled off from the sheet, the higher the adhesion of the coating). A more detailed evaluation method is described below.

[0068] The topical formulation compositions (aqueous solutions) shown in Table 1 were prepared. 1 mL of this aqueous solution was dropped onto the center (7 cm x 3.5 cm) of a rectangular silicone rubber sheet measuring 0.1 mm thick, 14 cm long, and 7 cm wide, and then dried at 25°C and 50±5% humidity for two days. The upper and lower ends of the silicone rubber sheet were then vertically fixed to an AUTOGRAPH AGS-X 5kN (Shimadzu Corporation) equipped with a screw-flat type gripper. The top and bottom of the silicone rubber sheet were fixed so that the upper surfaces of the gripping teeth of the upper gripper were aligned with the upper end of the silicone rubber sheet, and the lower surfaces of the gripping teeth of the lower gripper were aligned with the lower end of the silicone rubber sheet. The left and right sides of the silicone rubber sheet were fixed so that the centers of the gripping teeth and the center of the silicone rubber sheet were aligned. The compression test was then initiated (i.e., the upper gripper was moved closer 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 coated surface of the silicone rubber sheet was induced to concave parallel to the horizontal direction of the silicone rubber sheet (by gripping the edge of the central portion of the silicone rubber sheet (i.e., the vertical position 7 cm) so that the applied position of the formulation was concave). As the silicone rubber sheet was compressed, it curved (see Figure 1). At the stroke of 40 mm, the sheet was bent to the point where it could not be restored. The change in weight 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 Equation 1. If the formed coating was weak to bending, i.e., had poor adhesion, part or all of the coating would peel off from the silicone rubber sheet during compression, resulting in a high weight loss rate. Furthermore, coatings that were weak to bending and had poor adhesion were more likely to peel off even at small strokes. 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 topical composition that did not solidify when dried and dripped from the silicone rubber sheet was recorded as unmeasurable (-). Formula 1: In the formula, S0 represents the weight of the silicone rubber sheet itself, S1 represents the weight measured after dropping the topical composition onto the silicone rubber sheet and drying it (before the compression test), and S2 represents the weight measured after the compression test.

[0069]

[0070] The numerical values ​​for each component in Table 1 indicate weight percent, and the sum of the "remaining amount" of purified water and the numerical values ​​of other components equals 100 (weight percent) (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 compositions containing only a non-polymerizable cationic compound (Comparative Examples 1-2 and 1-4), the bending strength of the coating was low, and strength sufficient for adhesion to the skin was not obtained. While not intending to be bound by any theory, this is thought to be due to the high crystallinity of the polyhydric alcohol and metal salt, which are solid at room temperature. Furthermore, the topical preparation composition containing glycerin and chlorohydroxyaluminum (Comparative Example 1-3) did not form a coating, and the topical preparation composition drooped from the silicone rubber sheet. While not intending to be bound by any theory, this is thought to be due to the fact that glycerin is a liquid at room temperature (its molecular weight is small). 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 compositions (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, the coating remained adhered to the sheet even after the silicone rubber sheet was folded, and the weight loss rate was 0%. This confirmed that the combined use of a polyhydric alcohol having a molecular weight of 100 to 200 and a non-polymerizable cationic compound improved the adhesion of the coating (increased the coating's bending strength) and made it less likely to peel off even when subjected to physical stimuli.

[0071] Test Example 2: Astringency Evaluation The topical compositions shown in Table 2 were prepared. Subsequently, 1 ml of each composition was dropped onto the center of a 5 cm x 5 cm piece of artificial leather (Idemitsu Technofine Co., Ltd., product number: PBZ13001, black) placed in a 7 cm diameter glass petri dish, and the dish was dried overnight at room temperature without a lid. If the composition has astringency, the artificial leather will shrink as the composition dries. After one night, the artificial leather was examined for waviness caused by shrinkage. As shown in Figure 2 (photographed with the artificial leather placed on a transparent petri dish for ease of viewing), the height of the most waviness-intensive part (the highest part relative to the horizontal plane) of each artificial leather was measured from the horizontal plane, and the degree of improvement was calculated according to Equation 2 and compared. The higher the degree of astringency improvement, the more suppressed the astringency. The results are summarized in Table 2. A sample with no astringency was considered to have a degree of astringency improvement of 100%. Here, the calculations for Examples 2-1 and 2-2 were performed for Comparative Example 2-1, and the calculations for Examples 2-3 to 2-6 were performed for Comparative Example 2-2.

[0072]

[0073] In the compositions containing only aluminum chlorohydrate (Comparative Examples 2-1 and 2-2), the artificial leather exhibited significant waviness and 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), the waviness was small and the astringency was weak. That is, 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. Aluminum chlorohydrate, an antiperspirant ingredient, can cause users to complain of skin irritation (such as tightness, tingling, and itching) due to its astringent effect. This astringent effect is not correlated with antiperspirant activity, and antiperspirant activity can be achieved even without astringent activity. Therefore, it is preferable that the astringent effect, which is perceived as skin irritation, is low. Unexpectedly, this experiment confirmed that the astringent action of antiperspirant ingredients is suppressed by polyhydric alcohols having a molecular weight of 100 to 200. Therefore, according to the present invention, it is possible to reduce skin irritation caused by astringent antiperspirant ingredients.

[0074] [Formulation Examples] 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 the form.

[0075] Formulation example 1: Antiperspirant (cream) Benzalkonium chloride 0.07% Isopropylmethylphenol 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 Rest Total 100%

[0076] Formulation Example 2: Antiperspirant (Gel) Benzalkonium chloride 0.06% Isopropylmethylphenol 0.05% Aluminum chlorohydrate 8% Magnesium aluminometasilicate 0.5% Dipropylene glycol 10% Polyoxyethylene glycol 0.5% Hydroxypropylmethylcellulose 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 Balance Total 100%

[0077] Formulation Example 3: Antiperspirant (roll-on) Benzalkonium chloride 0.06%, isopropylmethylphenol 0.06%, zinc paraphenolsulfonate 5%, butylene glycol 5%, talc 3%, nylon powder 0.5%, cetyltrimethylammonium bromide solution 1%, hydrophobized hydroxypropylmethylcellulose 0.1%, absolute ethanol 40%, erythritol 4%, xylitol 4%, purified water, balance, total 100%

[0078] Formulation Example 4: Antiperspirant (mist) Benzalkonium chloride 0.05% Isopropylmethylphenol 0.06% Zinc paraphenolsulfonate 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 Rest Total 100%

[0079] Formulation Example 5: Antiperspirant (Stick) Benzalkonium chloride 0.055%, Isopropylmethylphenol 0.05%, Aluminum chlorohydrate 5%, Polyethylene wax 5%, Microcrystalline wax 5%, Glyceryl monostearate 3%, Octyldodecanol 5%, Talc 10%, Methylpolysiloxane 5%, Decamethylpentasiloxane 35%, Silylated anhydrous silicic acid 1%, Hydroxyapatite 0.3%, Cetyltrimethylammonium bromide solution 0.5%, Zinc oxide 0.3%, Fragrance 0.1%, Cetyl alcohol 4%, Stearyl alcohol 4%, Erythritol 1%, Purified water, Balance 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 Rest Total 100%

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

Claims

1. An external preparation composition containing (A) at least one polyhydric alcohol having a molecular weight of 100 to 200, and (B) at least one non-polymerizable cationic compound.

2. The composition according to claim 1, wherein the number of hydroxy groups of the component (A) is 4 or more.

3. The external preparation composition according to claim 1 or 2, wherein the component (B) is at least one selected from the group consisting of a compound containing a metal that becomes a divalent or higher cation in an aqueous solution, a basic amino acid, an alkanolamine, and an alkylamine.

4. The external preparation composition according to any one of claims 1 to 3, wherein the component (A) is at least one selected from the group consisting of glucose, sorbitol, fructose, xylitol, and erythritol.

5. The external preparation composition according to any one of claims 1 to 4, wherein the component (B) is at least one selected from the group consisting of zinc parahydroxybenzenesulfonate, chlorohydroxyaluminum, alum, arginine, and lysine.

6. The external preparation composition according to any one of claims 1 to 5, wherein the concentration of the component (A) is 4 to 20% by weight.

7. The external preparation composition according to any one of claims 1 to 6, which is an antiperspirant composition.

8. The external preparation composition according to any one of claims 1 to 7, wherein when the total amount of the component (A) is 1 part by weight, the total amount of the component (B) is 0.01 to 25 parts by weight.

9. An external preparation composition according to claim 1, which is an antiperspirant composition containing (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 parahydroxybenzenesulfonate, chlorohydroxyaluminum, and alum.

10. (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 parahydroxybenzenesulfonate and chloroaluminum hydroxide; The external preparation composition according to claim 1, which is an antiperspirant composition, wherein when the total amount of the component (A) is 1 part by weight, the total amount of the component (B) is in the range of 1 to 3 parts by weight.

11. The external preparation composition according to any one of claims 1 to 10, which has film-forming ability.

12. 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 form a film that adheres to the skin.