JP2016088925A - External composition for skin - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an external composition for skin which is excellent in skin remaining properties of antimicrobial component.SOLUTION: An external composition for skin is prepared by containing (A) an antimicrobial component, (B) a cyclodextrin compound, (C) a solid wax whose melting point is 40°C or more so that the content of (D) water is 40% by weight or less to the entire composition. The external composition for skin of the invention is excellent in skin remaining properties of (A) the antimicrobial component after an application to the skin, and preferably may be used as a deodorant agent.SELECTED DRAWING: None

Description

  The present invention relates to an external composition for skin. More specifically, the present invention relates to a composition for external use on skin having excellent antimicrobial component skin persistence.

  An external composition for skin containing an antibacterial component is useful for the purpose of treating, preventing and / or improving skin diseases, symptoms and conditions caused by fungi and bacteria.

  For example, the cause of body odor such as odor (also referred to as “Wakiga”) is attributed to the fact that sebum mixed with sweat is decomposed by overgrown bacteria to generate odor. If you are worried about such body odor, you may mask it with perfume, but if you simply use perfume, the body odor and perfume odor may mix and cause an unpleasant odor. . Moreover, simply masking with perfume or the like cannot suppress the overgrown bacteria and cannot solve the root cause of the generation of body odor.

  Therefore, many deodorant preparations for treating, preventing and / or improving body odors such as foul odors have a lot of external compositions containing antibacterial ingredients with the intention of suppressing the growth of bacteria that cause malodors. It is commercially available. In such a composition for external use containing an antibacterial component, it is desired that the composition for external use is applied, sprayed, etc., and then remains on the skin for a long time to exert its antibacterial effect. However, depending on the application site of the skin and the usage situation, the antibacterial component may flow down from the application site and it may be difficult to maintain the antibacterial effect. For example, when an antibacterial ingredient is added to an antiperspirant deodorant intended to be applied to areas that are prone to sweat, the antibacterial ingredient applied to the skin due to sweat that has not been completely suppressed by the antiperspirant ingredient and has overflowed somewhat. There was also concern that the desired antibacterial effect could not be sustained at the application site.

  So far, as an attempt to provide a hypoallergenic deodorant composition having a high antiperspirant effect, a high antibacterial effect, and their durability, and having an excellent deodorizing effect, (A) an antiperspirant component, ( B) It contains two specific types of cationic surfactants, (C) nonionic antibacterial agents, (D) multi-chain nonionic surfactants, and (E) ethanol. It has been proposed that a deodorant composition be prepared so that the mass ratio of is within a specific range (Patent Document 1). However, there is a demand for the development of a further useful new skin external composition that can exhibit a high antibacterial sustained effect.

JP 2014-133724 A

  This invention is made | formed in view of this conventional subject, and it aims at providing the skin external composition excellent in the skin persistence of an antimicrobial component.

  As a result of intensive studies to solve the above-mentioned problems, the present inventors formulated (A) an antibacterial component, (B) a cyclodextrin compound and (C) a solid wax having a melting point of 40 ° C. or more in combination. And (D) an antibacterial component when the external composition is applied to the skin by making the composition for external use such that the water content is 40% by weight or less based on the total composition The inventors have found that the persistence can be improved and have completed the present invention.

That is, the present invention provides the following external composition for skin.
[Item 1] (A) an antibacterial component, (B) a cyclodextrin compound, and (C) a solid wax having a melting point of 40 ° C. or higher, and (D) the content of water relative to the entire composition The composition for external use of skin is 40% by weight or less.
[Item 2] As component (A), isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, cetyltrimethylammonium chloride, cetyltrimethylammonium bromide, triclosan, triclocarban, salicylic acid, paraben, chlorhexidine and salts thereof, lysozyme and its components Salt, acrinol, ethanol, gluconic acid, alkyldiaminoglycine and its salt, popidone iodine, potassium iodide, iodine, cresol, photosensitizer 101, photosensitizer 201, phenoxyethanol, 1,2-pentanediol, piroctone olamine, Item 2. The topical skin composition according to Item 1, comprising at least one selected from the group consisting of halocarban.
[Item 3] The external composition for skin according to Item 1 or 2, comprising as component (B) at least one selected from the group consisting of cyclodextrin, derivatives thereof, and salts thereof.
[Item 4] As component (C), paraffin wax, microcrystalline wax, polyethylene wax, hydrogenated castor oil, polypropylene wax, (stearoxymethicone / dimethicone) copolymer, cetearyl methicone, alkyl (C30-45) cetearyl dimethicone cross Polymer, Carnauba wax, Candelilla wax, Wood wax, Rice bran wax, Hazelou, Urushi wax, Sugar cane wax, Palm wax, Orange peel wax, Orange flower wax, Prunus japonica flower wax, Ginseng flower wax, White yam fruit wax, Sweet acacia flower wax , Tuberose flower wax, beeswax, white beeswax, whale wax, shellac wax, lanolin, montan wax, ozokerite, ceresin wax, cetyl alcohol, stearyl alcohol, and behe Item 4. The external composition for skin according to any one of Items 1 to 3, comprising at least one selected from the group consisting of nil alcohol.
[Item 5] The external composition for skin according to any one of Items 1 to 4, having a hardness at 25 ° C. of 0.05 kgf or more.
[Item 6] The external composition for skin according to any one of Items 1 to 5, which is used as a deodorant agent.
[Item 7] The external composition for skin according to any one of Items 1 to 6, wherein the component (A) is contained in an amount of 0.001% by weight or more based on the entire composition.
[Item 8] The external composition for skin according to any one of Items 1 to 7, wherein the component (B) is contained in an amount of 0.1% by weight or more based on the entire composition.
[Item 9] The external composition for skin according to any one of Items 1 to 8, wherein the component (C) is contained in an amount of 0.01% by weight or more based on the entire composition.

Furthermore, from another viewpoint, the present invention also provides a method for enhancing the skin persistence of the antibacterial component (A) described below.
[Item 10] (A) An antibacterial component, (B) a cyclodextrin compound, and (C) a solid wax having a melting point of 40 ° C. or higher, and (D) the content of water in the entire composition A method for increasing the skin persistence of the component (A) of the external composition, comprising preparing the external composition for skin so as to be 40% by weight or less.

  ADVANTAGE OF THE INVENTION By this invention, the skin external composition excellent in the skin persistence of an antimicrobial component can be provided. In one embodiment, the external composition for skin of the present invention can be suitably used as a deodorant agent or the like, which is often used in skin sites and situations where the applied antibacterial component is easily washed away by sweat or the like.

Hereinafter, the present invention will be described in detail.
It should be understood that the terms used in the present specification are used in the meaning normally used in the art unless otherwise specified.

(1. Composition for external use on skin)
The external composition for skin of the present invention contains (A) an antibacterial component, (B) a cyclodextrin compound, and (C) a solid wax having a melting point of 40 ° C. or higher, and (D) a water content. It is characterized by being 40% by weight or less based on the entire composition.

(A) Antibacterial component:
The composition for external use of the skin of the present invention contains an antibacterial component (hereinafter also simply referred to as component (A)). The antibacterial component used in the present invention refers to any component known in the art that exhibits bactericidal or bacteriostatic action and can suppress the growth of various bacteria (fungi, gram positive bacteria, gram negative bacteria, etc.). . Specifically, as an antibacterial component, oil-soluble antibacterial components such as isopropylmethylphenol, triclosan, triclocarban, salicylic acid, paraben; benzalkonium chloride (also referred to as benzalkonium chloride), benzethonium chloride (also referred to as benzethonium chloride) ), Quaternary ammonium salt type antibacterial components such as cetyltrimethylammonium chloride (also referred to as cetyltrimethylammonium chloride), cetyltrimethylammonium bromide (also referred to as cetyltrimethylammonium bromide), chlorhexidine, lysozyme and salts thereof (for example, Water-soluble antibacterial components such as acrinol, ethanol, gluconic acid, alkyldiaminoglycine and their salts (eg, hydrochloride); popidone Iodine, antibacterial components such as potassium iodide, iodine; cresol, photosensitizer 101, photosensitizer 201, phenoxyethanol, 1,2-pentanediol, piroctone olamine, halocarban and the like. However, it is not limited to these. From the viewpoint that a high effect of improving skin persistence can be easily obtained by the present invention, it is preferable to use an oil-soluble antibacterial component and / or a cationic antibacterial component in the composition for external use of the present invention, more preferably. Is isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, cetyltrimethylammonium chloride, cetyltrimethylammonium bromide, lysozyme chloride (also called lysozyme hydrochloride), chlorhexidine gluconate (also called chlorhexidine gluconate), chlorhexidine hydrochloride (chlorhexidine) Hydrochloride) and / or chlorhexidine acetate (also referred to as chlorhexidine acetate), more preferably isopropylmethylphenol and / or benzalkonium chloride. And it is preferably to use isopropyl methyl phenol.

  In the composition for external use of skin of this invention, only 1 type may be used independently among the said (A) component, and it may be used in combination of 2 or more type.

  The content of the component (A) in the external composition for skin of the present invention can be appropriately set according to the use, the degree of desired effect, and the like. As an example, (A) component is 0.001 weight% or more with respect to the whole composition, Preferably it is 0.01 weight% or more, More preferably, it is good to set it as 0.05 weight% or more. The upper limit of the content of the component (A) is not particularly limited, but as an example, it may be 1% by weight or less, preferably 0.7% by weight or less, more preferably based on the whole composition. May be 0.5% by weight or less. According to the present invention, since the skin persistence of the antibacterial component (A) is improved, a sufficient antibacterial sustained effect can be exhibited even in such a range.

(B) Cyclodextrin compound:
The external composition for skin of the present invention further contains a cyclodextrin compound (hereinafter also simply referred to as component (B)). In the present specification, the cyclodextrin-based compound refers to at least one selected from the group consisting of cyclodextrin, derivatives thereof, and salts thereof.

  Cyclodextrin is a kind of cyclic oligosaccharide having a structure in which glucose is linked cyclically with α-1,4 bonds. Cyclodextrins are α-type (α-cyclodextrin, 6 molecules of glucose), β-type (β-cyclodextrin, 7 molecules of glucose), γ-type (γ-cyclodextrin, 8 molecules of glucose) depending on the number of glucose components. ) Etc. Naturally, it is known that cyclodextrins composed of more molecules of glucose exist. Moreover, the compound which derivatized cyclodextrin is also known until now, You may use such a cyclodextrin derivative in this invention. The cyclodextrin derivative is not particularly limited, and examples thereof include esterified derivatives, etherified derivatives, sulfonylated derivatives, and aminated derivatives. More specifically, alkylated cyclodextrins (such as methylated cyclodextrins) ), Hydroxyalkylated cyclodextrins (such as hydroxypropylated cyclodextrins), sulfoalkylated cyclodextrins (such as sulfobutylated cyclodextrins), aminoalkylated cyclodextrins (such as aminoethylated cyclodextrins), glycosylated cyclodextrins (galactosylcyclo) Dextrin, mannosylcyclodextrin, etc.). The cyclodextrin compound used in the present invention may be a salt of cyclodextrin or a derivative thereof, and any salt that is pharmaceutically or physiologically acceptable can be used. For example, an organic acid salt [eg, monocarboxylate (acetate, trifluoroacetate, butyrate, palmitate, stearate, etc.)]; inorganic acid salt (eg, hydrochloride, sulfate, nitrate, odor) Salts with organic bases (eg, salts with organic amines such as methylamine, triethylamine, triethanolamine, morpholine, piperazine, pyrrolidine, tripyridine, picoline); inorganic bases And the like [for example, ammonium salts; salts with metals such as alkali metals (sodium, potassium, etc.), alkaline earth metals (calcium, magnesium, etc.), aluminum, etc.], but are not limited thereto. In the composition for external use of skin of this invention, only 1 type may be used independently among the said (B) component, and it may be used in combination of 2 or more type.

  In the present invention, any of the above cyclodextrin compounds can be used, but from the viewpoint that the effects of the present invention are more reliably and easily exhibited, preferably cyclodextrin and / or a salt thereof is used. More preferably, cyclodextrin is used, still more preferably α-cyclodextrin, β-cyclodextrin, and γ-cyclodextrin, and particularly preferably β-cyclodextrin.

  The content of the component (B) in the external composition for skin of the present invention can be appropriately set according to the use, the degree of desired effect, and the like. As an example, the component (B) may be 0.1% by weight or more, preferably 1% by weight or more, more preferably 3% by weight or more based on the entire composition. Although the upper limit of content of (B) component is not specifically limited, As an example, it may be 15 weight% or less with respect to the whole composition, Preferably it may be 10 weight% or less, More preferably, 8 What is necessary is just to make it weight% or less.

  Further, in the composition for external use of the skin of the present invention, the ratio of the content of the component (B) to the content of the component (A) is not particularly limited, but the skin persistence of the component (A) is more effectively improved. From the viewpoint that the total amount of the component (A) is preferably 1 part by weight, the content of the component (B) is preferably 0.1 part by weight or more, preferably 1 part by weight or more, more preferably 10 parts by weight. The ratio which becomes the above is illustrated. Although the upper limit of the ratio of the content of the component (B) to the content of the component (A) is not particularly limited, as an example, the content of the component (B) is the total amount per 1 part by weight of the total amount of the component (A). Examples of the ratio are 1000 parts by weight or less, preferably 500 parts by weight or less, and more preferably 100 parts by weight or less.

(C) Solid wax:
The external composition for skin of the present invention further contains a solid wax having a melting point of 40 ° C. or higher (hereinafter also simply referred to as component (C)). The solid wax used in the present invention exhibits waxy physical properties (specifically, water resistance, plasticity, glossiness and / or opacity), has a melting point of 40 ° C. or higher, and at room temperature. Solid thing. The melting point of the solid wax used in the present invention is not particularly limited as long as the effect of the present invention can be obtained as long as it is 40 ° C. or higher, but is usually about 40 to 150 ° C., preferably about 40 to 130 ° C., more preferably 40 to It is about 100 ° C. Specifically, petroleum-derived waxes such as paraffin wax and microcrystalline wax; synthetic waxes such as polyethylene wax, hydrogenated castor oil, polypropylene wax; (stearoxymethicone / dimethicone) copolymer, cetearyl methicone, alkyl (C30-45) ) Silicone waxes such as cetearyl dimethicone cloth polymer; carnauba wax, candelilla wax, wood wax, rice bran wax, hazelau, urushi wax, sugar cane wax, palm wax, orange peel wax, orange blossom wax, large red rose flower wax, yellow rose flower Wax derived from plants such as white bayberry wax, sweet acacia flower wax and tuberose flower wax; wax derived from animals such as beeswax, white beeswax, whale wax, shellac wax, lanolin; (Referred cetanol, also as palmityl alcohol) cetyl alcohol, stearyl alcohol, higher alcohols solid form such as behenyl alcohol; box, ozokerite, waxes derived from mineral such as ceresin wax is like, but not limited to. In the composition for external use of skin of this invention, only 1 type may be used independently among the said (C) component, and it may be used in combination of 2 or more type. Preferably, the effect of the present invention can be further enhanced by using any combination of two or more types of component (C).

  In the present invention, any of the above-described solid waxes having a melting point of 40 ° C. or higher may be used. However, from the viewpoint that the effect of the present invention can be more surely exhibited, preferably a petroleum-derived wax or a synthetic wax. , Silicone waxes, plant-derived waxes, animal-derived waxes, solid higher alcohols, and combinations containing them, more preferably petroleum-derived waxes, synthetic waxes, silicone waxes, solid higher alcohols, and the like. Combinations are used, more preferably petroleum-derived waxes, synthetic waxes, silicone waxes, and combinations comprising them, particularly preferably synthetic waxes, silicone waxes, and combinations comprising them. Specifically, as preferred component (C), paraffin wax, microcrystalline wax, polyethylene wax, hydrogenated castor oil, polypropylene wax, (stearoxymethicone / dimethicone) copolymer, cetearyl methicone, alkyl (C30-45) cetearyl Dimethicone crosspolymer, cetyl alcohol, stearyl alcohol, behenyl alcohol, and combinations containing them, and more preferably paraffin wax, microcrystalline wax, polyethylene wax, hydrogenated castor oil, polypropylene wax, (stearoxymethicone / dimethicone) ) Copolymers, cetearyl methicone, alkyl (C30-45) cetearyl dimethicone crosspolymers, and combinations comprising them More preferred examples include paraffin wax, microcrystalline wax, polyethylene wax, (stearoxymethicone / dimethicone) copolymer, and combinations containing them, and particularly preferred are polyethylene wax, (stearoxymethicone / dimethicone). Mention may be made of copolymers and combinations comprising them.

  The content of the component (C) in the external composition for skin of the present invention can be appropriately set according to the use, the degree of desired effect, and the like. As an example, the component (C) may be 0.01% by weight or more, preferably 0.1% by weight or more, more preferably 1% by weight or more based on the entire composition. Although the upper limit of content of (C) component is not specifically limited, As an example, it may be 60 weight% or less with respect to the whole composition, Preferably it may be 50 weight% or less, More preferably, it is 40. It can be made into weight% or less.

  Furthermore, in the composition for external use of the present invention, the ratio of the content of the component (C) to the content of the component (A) is not particularly limited, but the skin persistence of the component (A) is further effectively improved. From the viewpoint that the total amount of the component (A) is 1 part by weight, the content of the component (C) is preferably 1 part by weight or more, preferably 10 parts by weight or more, more preferably 50 parts by weight or more. The ratio is exemplified. Although the upper limit of the ratio of the content of the component (C) to the content of the component (A) is not particularly limited, as an example, the content of the component (C) is the total amount per 1 part by weight of the total amount of the component (A). Examples of the ratio are 1000 parts by weight or less, preferably 750 parts by weight or less, more preferably 500 parts by weight or less.

  The external composition for skin of the present invention preferably further contains a powder. By blending the powder, a good feeling of smoothness when applied to the skin can be obtained, and the skin remaining property of the antibacterial component according to the present invention can be more effectively enhanced.

  The powder that can be used in the present invention can be any powder that is pharmaceutically or physiologically acceptable. Specifically, silicic anhydride, mica, sericite, talc, kaolin, aluminum oxide, aluminum silicate, magnesium aluminum silicate, magnesium silicate, magnesium oxide, magnesium carbonate, magnesium carbonate, calcium carbonate, zirconium oxide, oxidation Inorganic powders such as cerium, silicon carbide, and boron nitride; organic powders such as cellulose powder, polystyrene powder, nylon powder, polyethylene powder, polypropylene powder, and polystyrene powder; From the viewpoint that the effects of the present invention can be improved more effectively, inorganic powder is preferred, silicic anhydride and talc are more preferred, and silicic anhydride is particularly preferred. In the skin external composition of the present invention, the above powder may be used alone or in combination of two or more.

  When the powder is blended in the composition for external use of the present invention, the content is not particularly limited, but is preferably 0.1 to 30% by weight, more preferably 1 to 20% by weight, based on the whole composition. More preferably, the content is about 5 to 15% by weight.

  In addition, when the powder is blended in the composition for external use of the present invention, the ratio of the content of the powder to the content of the component (A) is not particularly limited, but preferably, the total amount of the component (A) is 1 part by weight. The total content of the powder is about 1 to 1000 parts by weight, more preferably about 10 to 500 parts by weight, and still more preferably about 20 to 200 parts by weight.

  The external composition for skin of the present invention may further contain a liquid oil. The liquid oil refers to an oily component that is liquid at 25 ° C., and may be any liquid oil that is pharmaceutically or physiologically acceptable. Specific examples include silicone oil, fatty acid ester oil, hydrocarbons, liquid higher alcohols and the like, but are not limited thereto. From the viewpoint that the skin persistence effect of the present invention can be exhibited to a higher degree, silicone oil is preferable, and decamethylcyclopentasiloxane, methylpolysiloxane, methylphenylpolysiloxane, polyether-modified is more preferable. Silicone, octamethyltrisiloxane, decamethyltetrasiloxane, octamethylcyclotetrasiloxane, dodecamethylcyclohexasiloxane, methylhydrogen silicone, more preferably decamethylcyclopentasiloxane, methylpolysiloxane, methylphenylpolysiloxane, poly Ether-modified silicone, more preferably decamethylcyclopentasiloxane and methylpolysiloxane. In the composition for external use of the present invention, the above liquid oil may be used alone or in combination of two or more.

  When a liquid oil is blended in the composition for external use of the present invention, the content thereof is not particularly limited, but is preferably 1 to 50% by weight, more preferably 10 to 40% by weight, and still more preferably based on the whole composition. Is preferably about 15 to 35% by weight.

  In addition, when a liquid oil is blended in the composition for external use of the present invention, the ratio of the content of the liquid oil to the content of the component (A) is not particularly limited, but preferably, the total amount of the component (A) is 1 part by weight. The total content of the liquid oil is about 10 to 1000 parts by weight, more preferably 50 to 800 parts by weight, and still more preferably about 100 to 600 parts by weight.

  The external composition for skin of the present invention may further contain a surfactant. By blending the surfactant, the formulation stability of the composition can be enhanced, and the effect of improving the skin persistence of the (A) antibacterial component by the components (B) and (C) of the present invention is more effective. Easily. The surfactant that can be used in the external composition for skin of the present invention can be any liquid oil that is pharmaceutically or physiologically acceptable. Specifically, isostearyl glyceryl ether (monoisostearyl glyceryl ether, diisostearyl glyceryl ether, etc.), myristyl glyceryl ether (monomyristyl glyceryl ether, dimyristyl glyceryl ether, etc.), lauryl glyceryl ether (monolauryl glyceryl ether, disulfide) Glycerin alkyl ethers such as lauryl glyceryl ether; POE-branched alkyl ethers such as polyoxyethylene (hereinafter referred to as POE) -octyldodecyl alcohol and POE-2-decyltetradecyl alcohol; POE-oleyl alcohol ether and POE-cetyl POE-alkyl ethers such as alcohol ethers; sorbitan monooleate, sorbitan monoisostearate and sorbitan monola Sorbitan esters such as rate; POE-sorbitan esters such as POE-sorbitan monooleate, POE-sorbitan monoisostearate, and POE-sorbitan monolaurate; glycerol monooleate, glycerol monostearate, and glycerol monomyristate Such as POE-glycerin monooleate, POE-glycerin monostearate, and POE-glycerin monomyristate; POE-dihydrocholesterol ester, POE-hardened castor oil, and POE- POE-hardened castor oil fatty acid ester such as hydrogenated castor oil isostearate; POE-alkyl aryl ether such as POE-octylphenyl ether; POE-monosteary POE-glycerin alkyl ethers such as glyceryl ether and POE-monomyristyl glyceryl ether; polyglycerin fatty acid esters such as diglyceryl monostearate, decaglyceryl decastearate, decaglyceryl decaisostearate, and diglyceryl diisostearate Non-ionic surfactants of: natural surfactants such as lecithin, hydrogenated lecithin, saponin, surfactin sodium, cholesterol, bile acid, and the like. Preferred are nonionic surfactants, and more preferred are glycerin alkyl ethers. In the external composition for skin of the present invention, the above surfactants may be used alone or in combination of two or more.

  When the surfactant is added to the external composition for skin of the present invention, the content is not particularly limited, but is preferably 0.1 to 10% by weight, more preferably 0.5 to 5%, based on the entire composition. % By weight, more preferably about 1-2% by weight.

  Moreover, when mix | blending surfactant with the composition for skin external use of this invention, the ratio of content of surfactant with respect to content of (A) component is not specifically limited, Preferably, the total amount of (A) component is 1 The total amount of the surfactant per part by weight is 1 to 100 parts by weight, more preferably 3 to 60 parts by weight, and still more preferably about 5 to 40 parts by weight.

  It is envisaged that the composition for external use of the present invention is used under a skin region or situation in which antibacterial components are particularly likely to flow off after application to the skin and sweat easily. Therefore, it is preferable that the composition for external use of the present invention also contains an antiperspirant component. The antiperspirant component can be any pharmaceutically or physiologically acceptable antiperspirant component. Specific examples include, but are not limited to, components having an astringent action such as chlorohydroxyaluminum, zinc paraphenolsulfonate, zinc oxide, aluminum chloride, aluminum sulfate, bromohydroxyaluminum, and aluminum potassium sulfate. From the viewpoint that the (A) antibacterial component (A) antibacterial component can be more effectively improved by the component (B) and component (C) of the present invention, chlorohydroxyaluminum and zinc paraphenolsulfonate are preferably used. More preferably, chlorohydroxyaluminum is used. In the skin external composition of the present invention, the above antiperspirant component may be used alone or in combination of two or more.

  When the antiperspirant component is blended in the external composition for skin of the present invention, the content is not particularly limited, but is preferably 0.1 to 30% by weight, more preferably 0.5 to 25% based on the entire composition. It is good to set it as weight%, More preferably, about 1 to 20 weight%.

  In addition, when the antiperspirant component is blended in the composition for external use of the present invention, the ratio of the content of the antiperspirant component to the content of the component (A) is not particularly limited, but preferably the total amount of the component (A) is 1 The total content of the antiperspirant component per part by weight is 1 to 1000 parts by weight, more preferably 5 to 700 parts by weight, and still more preferably about 10 to 500 parts by weight.

  In addition to the components described above, the composition for external use of the present invention further adds other useful effects, so that a moisturizing component, anti-inflammatory component, sebum adsorbing component, ultraviolet scattering component, ultraviolet absorbing component, DNA damage component A component having a preventive and / or restorative action, a whitening component, a cell activation component, an antioxidant component, an anti-aging component, a keratin softening component, a vitamin, and other various components may be used alone or in combination. . These components are not particularly limited as long as they can be used in the fields of pharmaceuticals, quasi drugs, cosmetics, and the like, and arbitrary components can be appropriately selected and used.

  When other useful components as described above are blended in the composition for external use of the present invention, the content is not particularly limited, but is usually 0.01 to 15% by weight, preferably 0.1 to 10% by weight, More preferably, the content is about 0.3 to 5% by weight.

  The composition for external use of the skin of the present invention can be prepared by appropriately blending components usually used in the fields of pharmaceuticals, quasi drugs, cosmetics, etc., in addition to the above components, depending on the use or dosage form. . The component that can be blended is not particularly limited, but for example, a base or carrier, a fragrance, an antioxidant, a preservative, a pH adjuster, a chelating agent, a stabilizer, an irritation reducer, an antiseptic, a colorant, and a dispersant. Etc. can be mix | blended. In addition, these components can be mix | blended individually by 1 type or in combination of 2 or more types.

  The composition for external use of the skin of the present invention may contain (D) water as a base or carrier, but its content is 40% by weight or less based on the entire composition. When the content of (D) water in the composition for external use of skin of the present invention exceeds 40% by weight, the effect of improving the skin persistence of the (A) antibacterial component by the aforementioned (B) component and (C) component is obtained. It is not preferable because it is not possible. From the viewpoint that a higher effect of the present invention can be easily obtained, the content of the component (A) with respect to the entire composition is preferably 30% by weight or less, more preferably 20% by weight or less, and still more preferably 17% by weight or less. Particularly preferably, the content is 16% by weight or less. The lower limit of the content of (D) water in the external composition for skin of the present invention is not particularly limited. For example, it may not be contained at all, may be 1% by weight or more, and may be 2% by weight or more.

  Examples of the base or carrier other than (D) water that can be used in the external composition for skin of the present invention include dipropylene glycol, 1,3-butylene glycol, glycerin, diglycerin, polyethylene glycol, propylene glycol, and isoprene glycol. Polyhydric alcohol: ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, ethylene glycol monopropyl ether, diethylene glycol monomethyl ether, diethylene glycol monoethyl ether, diethylene glycol monopropyl ether, diethylene glycol monobutyl ether, propylene glycol monoethyl ether, propylene glycol monopropyl ether , Dipropylene glycol monoethyl ether, dipropylene glycol mono Glycol ethers such as propyl ether; cellulose derivatives such as ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose; polyvinylpyrrolidone; carrageenan; polyvinyl butyrate; polyethylene glycol; dioxane; butylene glycol adipic acid polyester; isopropyl myristate, octyldodecyl myristate , Isopropyl palmitate, cetyl palmitate, isononyl isononanoate, pentaerythritol tetra-2-ethylhexanoate, esters such as jojoba oil; polysaccharides such as dextrin, maltodextrin; lower alcohols such as isopropanol; For example, but not limited to.

  Examples of the fragrances include natural fragrances, synthetic fragrances, and blended fragrances. Specific examples include hydrocarbons, esters, ethers, ketones, aldehydes, lactones, phenols, alcohols, and the like, but are not limited thereto.

  Examples of the antioxidant include dibutylhydroxytoluene, butylhydroxyanisole, sorbic acid, sodium sulfite, ascorbic acid, ascorbic acid derivative, tocopherol, tocopherol derivative, erythorbic acid, L-cysteine hydrochloride and the like.

  Examples of pH adjusters include inorganic acids (hydrochloric acid, sulfuric acid, etc.), organic acids (lactic acid, sodium lactate, citric acid, sodium citrate, succinic acid, sodium succinate, etc.), inorganic bases (potassium hydroxide, hydroxide) Sodium), organic bases (triethanolamine, diisopropanolamine, triisopropanolamine, etc.).

  As a chelating agent, for example, as a chelating agent, ethylenediaminetetraacetic acid (edetic acid), ethylenediaminetetraacetic acid salt (sodium salt (sodium edetate: Japanese Pharmacopoeia, EDTA-2Na etc.), potassium salt etc.), phytic acid, Examples include gluconic acid, polyphosphoric acid, and metaphosphoric acid.

Examples of the stabilizer include sodium polyacrylate, dibutylhydroxytoluene, and bitylhydroxyanisole.
Examples of the irritation reducing agent include licorice extract and sodium alginate.

  The above additives can be used singly or in combination of two or more.

  The external composition for skin of the present invention can be prepared in any formulation form known in the field of pharmaceuticals, quasi drugs, cosmetics and the like. Specifically, it is suitable for application to the skin of solid external preparations, ointments (including liniments, pasta, plasters, etc.), creams, gels, emulsions, suspensions, liquids, mists, etc. However, it is not limited to these. Preferably, it is a preparation (also referred to as an emulsion preparation) prepared by a method including an emulsification step. In addition, from the viewpoint that the effect of the present invention can be obtained more reliably, the external composition for skin of the present invention is preferably in the form of a solid to semi-solid preparation at room temperature, solid external preparations, ointments, creams More preferably, it is a solid external preparation and an ointment, and a solid external preparation that is solid at room temperature is particularly preferable. The shape of the solid external preparation is not particularly limited, and may be any shape such as a stick shape (columnar shape, elliptical column shape, prismatic shape, etc.), spherical shape, hemispherical shape, and the like. Such formulation forms can be prepared by any method known to those skilled in the art.

  The hardness of the external composition for skin of the present invention is not particularly limited as long as the effects of the present invention can be achieved. As an example, an approach speed of 2 cm / min using a cylindrical plunger (adapter) with a diameter of 20 mm with a rheometer (RT-2010D / D-CW, manufactured by Rheotech Co., Ltd.) in the same manner as described in the following test example. It means that the hardness (25 ° C.) when entering 1 cm is 0.05 kgf or more, preferably 0.1 kgf or more, more preferably 0.5 kgf or more, further preferably 1 kgf or more, and particularly preferably 2 kgf. That's it.

  The external composition for skin of the present invention can be used in any scene where it is desired to continuously exert an antibacterial action. Specifically, it can be used in applications such as a deodorant agent, but is not limited. According to the present invention, it is expected that the antibacterial component applied to the skin is less likely to flow off due to sweat or the like, and can remain at the site of the applied skin for a long time, so that the antibacterial action can be exhibited for a long time. In view of such a point of view, the composition for external use of the skin of the present invention is easily exposed to a portion of the skin that easily sweats (for example, the armpit or neck), or a situation that is likely to sweat (for example, hot periods such as summer, before and after intense exercise, etc.) It is preferable to be used as a deodorant agent (in particular, an antiperspirant deodorant agent).

The method for using the external composition for skin of the present invention varies depending on the state of the target skin, age, sex, season of use, etc., but in any skin site where it is desired to exert antibacterial action, An appropriate amount (about 0.001 to 0.1 g / cm ² ) is applied by any method known in the art such as coating and spraying. The composition for external use of the skin of the present invention may be used regularly several times a day (for example, about 1 to 5 times per day), or may be used irregularly at a timing when it is desired to exert an antibacterial action. Good. The period of use is not particularly limited, and may be, for example, several days (for example, about 3 days) to about 3 months, preferably about 1 week to about 1 month.

(2. Method to increase skin persistence of antibacterial components)
As described above, (A) an antibacterial component, (B) a cyclodextrin compound, and (C) a solid wax having a melting point of 40 ° C. or higher are used in combination, and (D) the amount of water is in a specific range. It has been confirmed that the skin persistence of the antibacterial component (A) applied to the skin is enhanced by placing it inside.
Accordingly, the present invention, from yet another point of view, comprises (A) an antibacterial component, (B) a cyclodextrin compound, (C) a solid wax having a melting point of 40 ° C. or higher, and (D) water. Also provided is a method for enhancing the skin persistence of the component (A) of the external composition, wherein the external composition is prepared so that the content is 40% by weight or less based on the total composition. . In this method, the order of blending the components (A) to (D) into the external composition is not particularly limited. The method can also be implemented as a cosmetic method not intended for medical treatment.
The types of the components (A) to (D) in the above method and the blending ratio thereof, the types of components that can be blended, the blending ratio, the pharmaceutical form, the method of use and the like are the above-mentioned “(1. Composition for external use on skin)” It is the same as that described in.

EXAMPLES The present invention will be described in detail below based on examples, but the present invention is not limited to these examples.
(Test Example 1: Evaluation of persistence of antibacterial components)
In order to evaluate the persistence of the antimicrobial component at the application site, the following test was performed.
Test preparations shown in Table 1 below were prepared according to a conventional method. Specifically, the test preparation of Example 1 will be described as an example. First, only the oily component is mixed and dissolved by the heat treatment, and only the remaining aqueous component is mixed and similarly heated and dissolved. Each aqueous phase was prepared, emulsified with a homogenizer, and then cooled to room temperature to prepare an external composition for skin. The hardness of the preparation of Example 1 was measured with a rheometer (RT-2010D · D-CW, manufactured by Rheotech Co., Ltd.). First, the measurement upper limit of the rheometer was set to 2 kgf, and a cylindrical plunger (adapter) φ20 mm was installed. A sample obtained by scraping the preparation of Example 1 into a plastic bowl (20 mL) was placed in a rheometer, and the hardness was measured when 1 cm of penetration into the preparation of Example 1 in the plastic bowl at an adapter penetration rate of 2 cm / min. did. As a result, the hardness of the preparation of Example 1 was 2 kgf or more. The preparations of Comparative Examples 1 to 4 were prepared in the same manner as described above.

About each test preparation prepared above, the outflow rate of the antimicrobial component (isopropyl methyl phenol) was evaluated in the following procedures. First, about 25 mg of each test preparation shown in Table 1 was applied to a test site (2.4 cm × 1.5 cm) of NEO cover glass (20 mm × 50 mm, manufactured by Matsunami Glass Industry Co., Ltd.). This was air-dried and then immersed in a centrifuge tube containing 10 ml of purified water, and subjected to ultrasonic treatment (SONIC CLEANER, manufactured by ASONE Co., Ltd.) for about 30 minutes according to the instruction manual of the device. After this ultrasonic treatment, 2 ml of the immersion liquid was sampled, mixed with 2 ml of a methanol / water (7: 3) mixture, filtered, and isopropylmethylphenol in each immersion liquid was quantified by high performance liquid chromatography. . Subsequently, the outflow rate (%) of isopropylmethylphenol was calculated from each quantitative value according to the following formula I.
[Formula I] Outflow rate (%) of isopropylmethylphenol = (Amount of isopropylmethylphenol / Amount of isopropylmethylphenol in each immersion liquid [initial blending amount]) × 100.

  The results are shown in the bottom column of Table 1 above. As apparent from the above results, under the test conditions, (B) cyclodextrin (C) solid wax (paraffin [melting point: 55 ° C.], polyethylene wax [melting point: 75 to 90 ° C.]) having a melting point of 40 ° C. or higher. The test preparation of Comparative Example 3, which does not contain purified microcrystalline wax [melting point: 70 to 85 ° C.] and (stearoxymethicone / dimethicone) copolymer [melting point: 40 to 50 ° C.], has an applied isopropylmethylphenol of about 86. % Will also flow out. And in the test preparations of Comparative Examples 1 and 2 in which only the component (B) or only the component (C) was added to the test preparation of Comparative Example 3, although the outflow rate of isopropylmethylphenol was somewhat suppressed, it was still sufficient. I can't say that. On the other hand, unexpectedly, by combining (A) isopropylmethylphenol with (B) cyclodextrin and (C) a solid wax having a melting point of 40 ° C. or higher, (A) the remaining antimicrobial component It became clear that the rate was highly improved. And when (C) instead of solid wax having a melting point of 40 ° C. or higher, wax that is liquid at room temperature (liquid paraffin) is used, and when (A) an antibacterial component and (B) cyclodextrin are used in combination The high persistence as in the present invention was not recognized (Comparative Example 4).

(Reference Test Example 1: Remaining evaluation of antibacterial components)
In order to further evaluate the persistence of the antimicrobial component at the application site, the following test was conducted.
Test preparations in liquid form shown in Table 2 below were prepared in the same manner as in Test Example 1 above. Subsequently, ultrasonic treatment was performed in the same procedure as in Test Example 1, and isopropylmethylphenol contained in the treated immersion liquid was quantified to calculate an isopropylmethylphenol outflow rate (%).

  The results are shown in the bottom column of Table 2 above. As shown in the above results, when (D) a liquid external composition containing about 60% by weight of water is used, (B) cyclodextrin compound and (C) melting point together with (A) antibacterial component However, even when solid waxes of 40 ° C. or higher were combined and mixed, the isopropylmethylphenol outflow rate was high, and excellent persistence at the coating site as in the present invention was not recognized.

(Test Example 2: Evaluation of remaining antimicrobial components)
In order to further evaluate the persistence of the antimicrobial component at the application site, the following test was conducted.
Test preparations shown in Table 3 below were prepared in the same manner as in Test Example 1 above. About each test preparation of an Example, when hardness (25 degreeC) was measured with the rheometer (RT-2010D * D-CW, the product made from Rheotech Co., Ltd.) on the same measurement conditions as the said Test Example 1, Example 2 was measured. The formulation of Example 3 was 2 kgf or more, the formulation of Example 3 was 2 kgf or more, the formulation of Example 4 was 0.59 kgf, the formulation of Example 5 was 0.14 kgf, and the formulation of Example 6 was 2 kgf or more. Next, ultrasonic treatment is performed in the same procedure as in Test Example 1, and the antibacterial component (isopropylmethylphenol) contained in the immersion liquid after treatment is quantified. Was calculated.

  The results are shown in the bottom column of Table 3 above. As shown in the above results, also in this test example, (A) isopropylmethylphenol, (B) cyclodextrin, and (C) solid wax (paraffin [melting point: 55 ° C.], polyethylene having a melting point of 40 ° C. or higher, polyethylene Wax [melting point: 75-90 ° C.], purified microcrystalline wax [melting point: 70-85 ° C.], (stearoxymethicone / dimethicone) copolymer [melting point: 40-50 ° C.], cetyl alcohol [melting point: 46-55 ° C.] ) And (D) the water content is 40% by weight or less, the (A) isopropylmethylphenol remaining excellent as in the result of Test Example 1 was observed (implementation). Examples 2-6).

(Test Example 3: Antimicrobial component persistence evaluation)
In order to further evaluate the persistence of the antimicrobial component at the application site, the following test was conducted.
A test preparation of Example 7 shown in Table 4 below was prepared in the same manner as in Test Example 1 by a conventional method. When the hardness (25 ° C.) of the preparation of Example 7 was measured using a rheometer (RT-2010D / D-CW, manufactured by Rheotech Co., Ltd.) under the same measurement conditions as in Test Example 1, 2 kgf That was all. The preparations of Comparative Examples 6 to 7 were prepared in the same manner as described above.
Next, in the same manner as in Test Example 1 above, about 25 mg of each test preparation shown in Table 4 below was applied to the test site (2.4 cm × 1.5 cm) of NEO cover glass (24 mm × 50 mm, manufactured by Matsunami Glass Industry Co., Ltd.). Applied. This was air-dried, then immersed in a centrifuge tube containing 10 ml of purified water, and subjected to ultrasonic treatment (SONIC CLEANER, manufactured by ASONE Co., Ltd.) for about 15 minutes according to the instruction manual of the instrument. After this ultrasonic treatment, 2 ml of the immersion liquid was collected, and about 2 ml of an organic solvent was added thereto and shaken for 10 minutes. Next, 2 ml was taken from the mixture after the shaking treatment, mixed with a methanol / water mixture, filtered, and then subjected to benzalkonium chloride (benzalkonium chloride) in each immersion liquid by high performance liquid chromatography. Product) was quantified. Subsequently, the outflow rate (%) of benzalkonium chloride was calculated from each quantitative value according to the following formula II.
[Formula II] Outflow rate (%) of benzalkonium chloride = (amount of benzalkonium chloride / amount of benzalkonium chloride [initial blending amount] in each immersion liquid) × 100.

  The results are shown in the bottom column of Table 4 above. (A) As an antibacterial component, in place of isopropylmethylphenol, when benzalkonium chloride was evaluated for its persistence at the application site, the outflow rate of benzalkonium chloride was (C) a solid wax having a melting point of 40 ° C. or higher. (Paraffin [melting point: 55 ° C.], polyethylene wax [melting point: 75 to 90 ° C.], purified microcrystalline wax [melting point: 70 to 85 ° C.], (stearoxymethicone / dimethicone) copolymer [melting point: 40 to 50 ° C.]) (D) Although the outflow rate was considerably suppressed even when the water content was 40% by weight or less (Comparative Example 6), by further combining (B) cyclodextrin, It was confirmed that the outflow rate of nium can be more effectively suppressed (Example 7). The improvement of the remaining part of the application site by the blending of cyclodextrin has not been known so far, and such an effect of improving the remaining part of the present invention was unexpected.

Examples of the formulation of the present invention are shown below. Formulation Examples 1 to 7 are all solid antiperspirant deodorants having a hardness (25 ° C.) of 2 kgf or more.

Claims (10)

  (A) an antibacterial component, (B) a cyclodextrin-based compound, and (C) a solid wax having a melting point of 40 ° C. or higher, and (D) the water content is 40% by weight with respect to the entire composition. The composition for external use of skin, which is the following.   As component (A), isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, cetyltrimethylammonium chloride, cetyltrimethylammonium bromide, triclosan, triclocarban, salicylic acid, paraben, chlorhexidine and its salt, lysozyme and its salt, acrinol, From ethanol, gluconic acid, alkyldiaminoglycine and its salts, popidone iodine, potassium iodide, iodine, cresol, photosensitizer 101, photosensitizer 201, phenoxyethanol, 1,2-pentanediol, piroctone olamine, and halocarban The composition for external use of skin according to claim 1, comprising at least one selected from the group consisting of:   The external composition for skin according to claim 1 or 2, comprising at least one selected from the group consisting of cyclodextrin, derivatives thereof, and salts thereof as component (B).   As component (C), paraffin wax, microcrystalline wax, polyethylene wax, hydrogenated castor oil, polypropylene wax, (stearoxymethicone / dimethicone) copolymer, cetearyl methicone, alkyl (C30-45) cetearyl dimethicone crosspolymer, carnauba wax, Candelilla wax, wood wax, rice bran wax, hazelou, urushi wax, sugar cane wax, palm wax, orange peel wax, orange flower wax, sorghum flower wax, red rose flower wax, white yam fruit wax, sweet acacia flower wax, tuberose flower wax , Beeswax, honey beeswax, spermaceti, shellac wax, lanolin, montan wax, ozokerite, ceresin wax, cetyl alcohol, stearyl alcohol, and behenyl al Containing at least one selected from the group consisting Lumpur, external composition for skin according to any one of claims 1 to 3.   The external composition for skin according to any one of claims 1 to 4, having a hardness at 25 ° C of 0.05 kgf or more.   The external composition for skin according to any one of claims 1 to 5, which is used as a deodorant agent.   The external composition for skin according to any one of claims 1 to 6, wherein the component (A) is contained in an amount of 0.001% by weight or more based on the total composition.   The external composition for skin according to any one of claims 1 to 7, wherein the component (B) is contained in an amount of 0.1% by weight or more based on the whole composition.   The external composition for skin according to any one of claims 1 to 8, wherein the component (C) is contained in an amount of 0.01% by weight or more based on the whole composition.   (A) an antibacterial component, (B) a cyclodextrin compound, and (C) a solid wax having a melting point of 40 ° C. or higher, and (D) the water content is 40 wt. %. The method for improving the skin persistence of the component (A) of the composition for external use, comprising preparing the composition for external use of skin so as to be not more than%.