JP6888064B2 - Topical skin composition - Google Patents

Description

The present invention relates to a composition for external use on the skin. More specifically, the present invention relates to a composition for external use on the skin, which is an antibacterial component having excellent residual skin.

The external composition for skin containing an antibacterial ingredient is useful for the purpose of treating, preventing and / or ameliorating a skin disease, symptom, or condition caused by fungi, bacteria, or the like.

For example, one of the major causes of body odor such as axillary odor (also called armpit odor) is that sebum mixed with sweat is decomposed by overgrown germs to generate odor. If you are concerned about such body odor, you may mask it with perfume, etc., but if you simply use perfume, etc., the body odor and perfume odor may mix and cause an unpleasant odor. .. In addition, masking with perfume or the like cannot suppress overgrown germs, and does not solve the root cause of the generation of body odor.

Therefore, in deodorant agents for treating, preventing and / or ameliorating anxious body odors such as axillary odors, there are many external composition for skin containing antibacterial components with the intention of suppressing the growth of germs that cause bad odors. It is commercially available. In such an external composition for skin containing an antibacterial component, it is desired that the external composition remains on the skin for a long period of time and exerts its antibacterial effect after being applied by application, spraying or the like. However, depending on the application site and usage conditions of the skin, 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 where sweat is likely to occur, the antibacterial ingredient applied to the skin due to the sweat that overflows to some extent cannot be completely suppressed by the antiperspirant ingredient. Was washed away, and there was concern that the desired antibacterial effect could not be maintained at the application site.

As an attempt to provide a hypoallergenic deodorant composition having a high antiperspirant effect, a high antibacterial effect, and their persistence, and having an excellent deodorant effect, (A) an antiperspirant component and ( B) Contains two specific cationic surfactants, (C) nonionic antibacterial agent, (D) multi-chain nonionic surfactant, and (E) ethanol, among the specific components. It has been proposed to prepare a deodorant composition so that the mass ratio of the deodorant is within a specific range (Patent Document 1). However, there is a need for the development of a new and more useful external composition for skin capable of exerting a high antibacterial lasting effect.

Japanese Unexamined Patent Publication No. 2014-133724

The present invention has been made in view of such conventional problems, and an object of the present invention is to provide a composition for external use on the skin, which has excellent skin persistence of an antibacterial component.

As a result of diligent studies to solve the above problems, the present inventors have combined (A) an antibacterial component, (B) a cyclodextrin-based compound, and (C) a solid wax having a melting point of 40 ° C. or higher. In addition, by making the composition for external use on the skin such that the content of water (D) is 40% by weight or less with respect to the entire composition, the antibacterial component (A) when the external composition is applied to the skin. We have found that the survivability is enhanced, and have completed the present invention.

That is, the present invention provides the following external composition for skin.
[Item 1] The composition 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) the content of water is relative to the entire composition. A composition for external use on the skin, which is 40% by weight or less.
[Item 2] As the component (A), isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, cetyltrimethylammonium chloride, cetyltrimethylammonium bromide, triclosan, triclocarban, salicylic acid, paraben, chlorhexidine and its salt, lysoteam and its salt. Salt, acrinol, ethanol, gluconic acid, alkyldiaminoglycine and its salts, popidone iodine, potassium iodide, iodine, cresol, photosensitizer 101, photosensitizer 201, phenoxyethanol, 1,2-pentanediol, pyrocton olamine, Item 2. The external composition for skin according to Item 1, which comprises at least one selected from the group consisting of halocarbin and halocarban.
Item 3. The external composition for skin according to Item 1 or 2, which contains at least one selected from the group consisting of cyclodextrin, a derivative thereof, and a salt thereof as the component (B).
[Item 4] As the component (C), paraffin wax, microcrystallin wax, polyethylene wax, hardened beeswax, polypropylene wax, (stealoxymethicone / dimethicone) copolymer, cetearylmethicone, alkyl (C30-45) cetearyldimethicone cloth. Polymer, carnauba wax, candelilla wax, wood wax, rice bran wax, hazerou, urshiro, sugar cane wax, palm wax, orange peel wax, orange flower wax, sardine wax, beeswax wax, white beeswax fruit wax, sweet acacia wax Item 1 containing at least one selected from the group consisting of tuberous flower wax, beeswax, sardine wax, whale wax, cellac wax, lanolin, montan wax, ozokerite, ceresin wax, cetyl alcohol, stearyl alcohol, and behenyl alcohol. The composition for external use on the skin according to any one of 3 to 3.
[Item 5] The composition for external use on the skin according to any one of Items 1 to 4, wherein the hardness at 25 ° C. is 0.05 kgf or more.
[Item 6] The composition for external use on the skin according to any one of Items 1 to 5, which is used as a deodorant agent.
Item 7. The composition for external use on the 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 composition for external use on the 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.

Further, from another viewpoint, the present invention also provides a method for enhancing the skin persistence of the (A) antibacterial component listed below.
[Item 10] (A) An antibacterial component, (B) a cyclodextrin-based compound, and (C) a solid wax having a melting point of 40 ° C. or higher are blended, and (D) the content of water is contained in the entire composition. A method for enhancing the skin persistence of the component (A) of the external composition, which comprises preparing the composition for external use on the skin so as to have a content of 40% by weight or less.

INDUSTRIAL APPLICABILITY According to the present invention, it is possible to provide a composition for external use on the skin, which is an antibacterial component having excellent residual skin. 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 generally used in a skin portion or situation 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 herein are used in the meaning commonly used in the art unless otherwise specified.

(1. Topical skin composition)
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) contains water. It is characterized in that it is 40% by weight or less based on the whole composition.

(A) Antibacterial component:
The external composition for 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 can exert a bactericidal or bacteriostatic action to suppress the growth of various bacteria (fungi, gram-positive bacteria, gram-negative bacteria, etc.). .. Specifically, as antibacterial components, oil-soluble antibacterial components such as isopropylmethylphenol, triclosan, triclocarban, salicylic acid, and paraben; benzalkonium chloride (also referred to as benzalkonium chloride) and benzethonium chloride (also referred to as benzethonium chloride). ), Cetyltrimethylammonium chloride (also referred to as cetyltrimethylammonium chloride), quaternary ammonium salt-type antibacterial components such as cetyltrimethylammonium bromide (also referred to as cetyltrimethylammonium bromide), chlorhexidine, lysozyme and salts thereof (for example, Cationic antibacterial components such as hydrochloride, acetate, gluconate); water-soluble antibacterial components such as acrinol, ethanol, gluconic acid, alkyldiaminoglycine and salts thereof (eg, hydrochloride); popidone iodo, iodide Iodo-based antibacterial components such as potassium and iodine; cresol, photosensitizer No. 101, photosensitizer No. 201, phenoxyethanol, 1,2-pentanediol, pyrocton olamine, halocarban and the like can be mentioned, but are not limited thereto. .. 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 external composition for skin of the present invention, which is more preferable. Is isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, cetyltrimethylammonium chloride, cetyltrimethylammonium bromide, lysoteam chloride (also called lysoteam hydrochloride), chlorhexidine gluconate (also called chlorhexidine gluconate), chlorhexidine hydrochloride (chlorhexidine). Chlorhexidine acetate (also referred to as chlorhexidine acetate) and / or chlorhexidine acetate (also referred to as chlorhexidine acetate) are preferably used, more preferably isopropylmethylphenol and / or benzalkonium chloride, and particularly preferably isopropylmethyl. It is better to use phenol.

In the external composition for skin of the present invention, only one of the above components (A) may be used alone, or two or more thereof may be used in combination.

The content of the component (A) in the external composition for skin of the present invention can be appropriately set according to the intended use, the degree of desired effect, and the like. As an example, the content of the component (A) is preferably 0.001% by weight or more, preferably 0.01% by weight or more, and more preferably 0.05% by weight or more with respect to the entire composition. 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 entire composition. May be 0.5% by weight or less. According to the present invention, since the skin persistence of the (A) antibacterial component is improved, a sufficient antibacterial lasting 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-based compound (hereinafter, also simply referred to as component (B)). As used herein, the cyclodextrin-based compound refers to at least one selected from the group consisting of cyclodextrin, its derivatives, and salts thereof.

Cyclodextrin is a kind of cyclic oligosaccharide having a structure in which glucose is cyclically linked by α-1,4 bonds. Cyclodextrin is α-type (α-cyclodextrin, 6 glucose molecules), β-type (β-cyclodextrin, 7 glucose molecules), γ-type (γ-cyclodextrin, 8 glucose molecules), depending on the number of glucose constituting. ) Etc. It is known that cyclodextrin, which is composed of more molecules of glucose, also exists in nature. Further, a compound obtained by derivatizing cyclodextrin is also known so far, and such a cyclodextrin derivative may be used in the present invention. The cyclodextrin derivative is not particularly limited, and examples thereof include an esterified derivative, an etherified derivative, a sulfonylated derivative, and an amination derivative. More specifically, an alkylated cyclodextrin (methylated cyclodextrin and the like) can be mentioned. ), Hydroxyalkylated cyclodextrin (hydroxypropylated cyclodextrin, etc.), sulfoalkylated cyclodextrin (sulfobutylated cyclodextrin, etc.), aminoalkylated cyclodextrin (aminoethylated cyclodextrin, etc.), glycosylated cyclodextrin (galactosylcyclo) Dextrin, mannosylcyclodextrin, etc.) and the like can be mentioned. The cyclodextrin-based 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, organic acid salts [eg, monocarboxylates (acetate, trifluoroacetate, butyrate, palmitate, stearate, etc.)]; inorganic acid salts (eg, hydrochloride, sulfate, nitrate, odor). Hydrochloride, phosphate, etc.); Salts with organic bases (eg, salts with organic amines such as methylamine, triethylamine, triethanolamine, morpholin, piperazine, pyrrolidine, tripyridine, picolin, etc.); with inorganic bases Salts [for example, ammonium salts; alkali metals (sodium, potassium, etc.), alkaline earth metals (calcium, magnesium, etc.), salts with metals such as aluminum, etc.]; and the like, but are not limited thereto. In the external composition for skin of the present invention, only one of the above components (B) may be used alone, or two or more thereof may be used in combination.

Any of the above cyclodextrin-based compounds can be used in the present invention, but cyclodextrin and / or a salt thereof is preferably used from the viewpoint of being more surely high and easily exerting the effect of the present invention. More preferably, cyclodextrin is used, more preferably α-cyclodextrin, β-cyclodextrin, γ-cyclodextrin is used, and particularly preferably β-cyclodextrin is used.

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

Further, in the external composition for 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 more effectively improves the skin persistence of the component (A). From the viewpoint that the total amount of the component (A) is preferably 0.1 part by weight or more, preferably 1 part by weight or more, and more preferably 10 parts by weight, the total content of the component (B) is 0.1 part by weight or more. The above ratio is exemplified. The upper limit of the ratio of the content of the component (B) to the content of the component (A) is not particularly limited, but 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). It can be exemplified that the ratio is 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, etc.), has a melting point of 40 ° C. or higher, and is at room temperature. A solid one. The melting point of the solid wax used in the present invention is not particularly limited as long as it is 40 ° C. or higher as long as the effects of the present invention can be obtained, but it 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 microcrystallin wax; synthetic waxes such as polyethylene wax, hardened castor oil, and polypropylene wax; (stealoxymethicone / dimethicone) copolymer, cetearylmethicone, and alkyl (C30-45). ) Silicone wax such as cetearyl dimethicone crosspolymer; carnauba wax, candelilla wax, wood wax, rice bran wax, hazerou, urshiro, sugar cane wax, palm wax, orange peel wax, orange flower wax, sardine wax, kuchibenisuisen flower wax , Plant-derived waxes such as white peach fruit wax, sweet acacia flower wax, tuberose flower wax; animal-derived waxes such as beeswax, sardine wax, whale wax, cellac wax, and lanolin; Wax; solid higher alcohol such as cetyl alcohol (also referred to as cetanol, palmityl alcohol, etc.), stearyl alcohol, behenyl alcohol; and the like; but are not limited thereto. In the external composition for skin of the present invention, only one of the above components (C) may be used alone, or two or more thereof may be used in combination. Preferably, by using two or more kinds of the component (C) in any combination, a higher effect of the present invention can be expected.

In the present invention, any of the above solid waxes having a melting point of 40 ° C. or higher may be used, but from the viewpoint that the effect of the present invention is more reliably exhibited, petroleum-derived wax and synthetic wax are preferable. , Silicone wax, plant-derived wax, animal-derived wax, solid higher alcohol, and combinations containing them are used, more preferably petroleum-derived wax, synthetic wax, silicone wax, solid higher alcohol, and a combination thereof. Combinations are used, more preferably petroleum-derived waxes, synthetic waxes, silicone waxes, and combinations containing them, and particularly preferably synthetic waxes, silicone waxes, and combinations containing them. Specifically, as the preferred component (C), paraffin wax, microcrystalline wax, polyethylene wax, hardened castor oil, polypropylene wax, (stealoxymethicone / dimethicone) copolymer, cetearylmethicone, alkyl (C30-45) cetearyl. Dimethicone crosspolymers, cetyl alcohols, stearyl alcohols, behenyl alcohols, and combinations containing them can be mentioned, more preferably paraffin wax, microcrystalline wax, polyethylene wax, hardened castor oil, polypropylene wax, (stealoxymethicone / dimethicone). ) Copolymers, cetearylmethicone, alkyl (C30-45) cetearyldimethicone crosspolymers, and combinations containing them, more preferably paraffin wax, microcrystalline wax, polyethylene wax, (stealoxymethicone / dimethicone). ) Polymers, and combinations containing them, and particularly preferably polyethylene wax, (stearoxymethicone / dimethicone) copolymers, and combinations containing them.

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

Further, in the external composition for skin 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 more effectively improves the skin persistence of the component (A). From the viewpoint that the total amount of the component (A) is preferably 1 part by weight or more, the content of the component (C) is preferably 1 part by weight or more, preferably 10 parts by weight or more, and more preferably 50 parts by weight or more. The ratio is illustrated. The upper limit of the ratio of the content of the component (C) to the content of the component (A) is not particularly limited, but 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). It can be exemplified that the ratio is 1000 parts by weight or less, preferably 750 parts by weight or less, and 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 smooth and good feeling of use can be obtained when applied to the skin, and the skin persistence of the antibacterial component according to the present invention can be further 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, aluminum magnesium silicate, magnesium silicate, magnesium oxide, magnesium carbonate, magnesium carbonate, calcium carbonate, zirconium oxide, oxidation. Inorganic powders such as cerium, silicon carbide, and boron nitride; and organic powders such as cellulose powder, polystyrene powder, nylon powder, polyethylene powder, polypropylene powder, and polystyrene powder; are not limited thereto. From the viewpoint that the effect of the present invention can be improved more effectively, an inorganic powder is preferable, silicic acid anhydride and talc are more preferable, and silicic acid anhydride is particularly preferable. In the external composition for skin 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 external composition for skin of the present invention, the content thereof is not particularly limited, but is preferably 0.1 to 30% by weight, more preferably 1 to 20% by weight, based on the entire composition. More preferably, it is about 5 to 15% by weight.

Further, when the powder is blended in the external composition for skin 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 1 part by weight of the total amount of the component (A). The total content of the powder is preferably 1 to 1000 parts by weight, more preferably 10 to 500 parts by weight, and further preferably about 20 to 200 parts by weight.

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

When the liquid oil content is blended in the external composition for skin 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, still more preferably, based on the entire composition. Is preferably about 15 to 35% by weight.

When the liquid oil content is added to the external composition for skin of the present invention, the ratio of the liquid oil content to the content of the component (A) is not particularly limited, but preferably 1 part by weight of the total amount of the component (A). The total content of the liquid oil is preferably 10 to 1000 parts by weight, more preferably 50 to 800 parts by weight, and further preferably about 100 to 600 parts by weight.

The external composition for skin of the present invention may further contain a surfactant. By blending a surfactant, the pharmaceutical stability of the composition can be enhanced, and the effect of the components (B) and (C) of the present invention on improving the skin persistence of the (A) antibacterial component is more effective. It becomes easier to exert the effect. The surfactant that can be used in the external composition for skin of the present invention may 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, di). Glycerin alkyl ether such as lauryl glyceryl ether); POE-branched alkyl ether such as polyoxyethylene (hereinafter referred to as POE) -octyldodecyl alcohol or POE-2-decyltetradecyl alcohol; POE-oleyl alcohol ether or POE-cetyl POE-alkyl ethers such as alcohol ethers; sorbitan esters such as sorbitan monooleate, sorbitan monoisostearate and sorbitan monolaurate; POE-sorbitan monooleate, POE-sorbitan monoisostearate, and POE-sorbitan monolaurate. POE-sorbitan esters such as rates; glycerin monooleate, glycerin monostearate, and glycerin fatty acid esters such as glycerin monomillistate; POE-glycerin monooleate, POE-glycerin monostearate, and POE-glycerin monomillistate. POE-glycerin fatty acid esters such as POE-dihydrocholesterol ester, POE-hardened castor oil, and POE-hardened castor oil fatty acid esters such as POE-hardened castor oil isostearate; POE-alkylaryl such as POE-octylphenyl ether. Ether; POE-glycerin alkyl ether such as POE-monostearyl glyceryl ether, POE-monomyristyl glyceryl ether; diglyceryl monostearate, decaglyceryl decasterate, decaglyceryl decaisostearate, diglyceryl diisostearate, etc. Various non-ionic surfactants such as polyglycerin fatty acid ester: Or naturally derived surfactants such as lecithin, hydrogenated lecithin, saponin, sodium surfactinate, cholesterol and bile acid can be exemplified. A nonionic surfactant is preferable, and a glycerin alkyl ether is more preferable. In the external composition for skin of the present invention, the above-mentioned surfactant may be used alone or in combination of two or more.

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

Further, when the surfactant is blended in the external composition for skin of the present invention, the ratio of the content of the surfactant 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 surfactant per part by weight is preferably 1 to 100 parts by weight, more preferably 3 to 60 parts by weight, and further preferably about 5 to 40 parts by weight.

It is assumed that the external composition for skin of the present invention is used in a skin portion or condition where the antibacterial component is particularly liable to run off after application to the skin and is liable to sweat. Therefore, it is preferable that the external composition for skin of the present invention also contains an antiperspirant component. The antiperspirant component can be any pharmaceutically or physiologically acceptable antiperspirant component. Specific examples thereof include, but are not limited to, astringent components such as chlorohydroxyaluminum, zinc paraphenolsulfonate, zinc oxide, aluminum chloride, aluminum sulfate, bromohydroxyaluminum, and potassium aluminum sulfate. Chlorhydroxyaluminum and zinc paraphenolsulfonate are preferably used from the viewpoint of more effectively exerting the skin residual improving effect of the (A) antibacterial component by the components (B) and (C) of the present invention. Chlorhydroxyaluminum is more preferably used. In the external composition for skin of the present invention, the above antiperspirant components 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, its content is not particularly limited, but is preferably 0.1 to 30% by weight, more preferably 0.5 to 25% by weight, based on the entire composition. It is preferably about 1 to 20% by weight, more preferably about 1 to 20% by weight.

When the antiperspirant component is added to the external composition for skin 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 preferably 1 to 1000 parts by weight, more preferably 5 to 700 parts by weight, and further preferably about 10 to 500 parts by weight.

The external composition for skin of the present invention further adds other useful actions in addition to the above-mentioned components, so that it has a moisturizing component, an anti-inflammatory component, a sebum adsorbing component, an ultraviolet scattering component, an ultraviolet absorbing component, and DNA damage. Various components such as a preventive and / or repair component, a whitening component, a cell activating component, an antioxidant component, an antiaging component, a keratin softening component, and vitamins may be blended in one or a combination of two or more. .. The respective components are not particularly limited as long as they can be used in the fields of pharmaceuticals, quasi-drugs, cosmetics, etc., and any one can be appropriately selected and used.

When the above-mentioned other useful ingredients are added to the external composition for skin of the present invention, the content thereof is not particularly limited, but is usually 0.01 to 15% by weight, preferably 0.1 to 10% by weight. More preferably, it is about 0.3 to 5% by weight.

Further, the external composition for skin of the present invention can be prepared by appropriately blending in addition to the above-mentioned components, components usually used in fields such as pharmaceuticals, quasi-drugs, and cosmetics, depending on the intended use or dosage form. .. The components that can be blended are not particularly limited, but are, for example, bases or carriers, fragrances, antioxidants, preservatives, pH adjusters, chelating agents, stabilizers, irritation reducing agents, preservatives, coloring agents, and dispersants. Additives such as can be blended. In addition, these components can be blended individually by 1 type or in any combination of 2 or more types.

The external composition for skin of the present invention may contain (D) water as a base or a carrier, but the content thereof is 40% by weight or less based on the whole composition. When the content of (D) water in the external composition for skin of the present invention exceeds 40% by weight, the effect of improving the skin persistence of the (A) antibacterial component due to the above-mentioned components (B) and (C) is obtained. It is not preferable because it will not be possible. From the viewpoint that even higher effects 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, still more preferably 17% by weight or less. It is preferable that the content is 16% by weight or less, particularly preferably 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, but may be, for example, not contained at all, may be 1% by weight or more, and may be further 2% by weight or more.

Examples of the base or carrier other than water (D) 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, isoprene glycol and the like. Polyhydric alcohols; 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. , Glycol ethers such as dipropylene glycol monoethyl ether, dipropylene glycol monopropyl ether; cellulose derivatives such as ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose; polyvinylpyrrolidone; carrageenan; polyvinylbutyrate; polyethylene glycol; dioxane; butylene Polyethylene glycol adipate polyester; isopropyl myristate, octyldodecyl myristate, isopropyl palmitate, cetyl palmitate, isononyl isononanoate, pentaerythlit tetra2-ethylhexanoate, esters such as jojoba oil; like dextrin, maltodextrin Polysaccharides; lower alcohols such as isopropanol; and the like; but not limited to these.

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

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 the pH adjuster include inorganic acids (hydrochloric acid, sulfuric acid, etc.), organic acids (lactic acid, sodium lactate, citric acid, sodium citrate, succinate, sodium succinate, etc.), and inorganic bases (potassium hydroxide, hydroxide). (Sodium, etc.), organic bases (triethanolamine, diisopropanolamine, triisopropanolamine, etc.) and the like.

Examples of the chelating agent include ethylenediaminetetraacetic acid (edetic acid), ethylenediaminetetraacetic acid salt (sodium salt (Japanese Pharmacopoeia, EDTA-2Na, etc.), potassium salt, etc.), phytic acid, and the like. Examples thereof include gluconic acid, polyphosphoric acid and metaphosphoric acid.

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

As the above-mentioned additives, one type can be used alone, or two or more types can be used in combination.

The external composition for skin of the present invention can be prepared in any pharmaceutical form known in the fields such as pharmaceuticals, quasi-drugs, and cosmetics. Specifically, it is suitable for application of solid external preparations, ointments (including liniments, pasta, plasters, etc.), creams, gels, emulsions, suspensions, liquids, mists, etc. to the skin. Examples of the formulation form can be mentioned, but the present invention is not limited to these. Preferably, it is a preparation (also referred to as an emulsified preparation) prepared by a method including an emulsification step. Further, from the viewpoint that a higher 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 formulation at room temperature, and is a solid external preparation, an ointment, or a cream. It is more preferably an agent, more preferably a solid external preparation or an ointment, and particularly preferably a solid external preparation which is solid at room temperature. The shape of the solid external preparation is not particularly limited, and may be any shape such as stick-shaped (cylindrical, elliptical, prismatic, etc.), spherical, hemispherical, and the like. Such a pharmaceutical form can be prepared by any method well 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 exhibited. As an example, the approach speed is 2 cm / min using a cylindrical plunger (adapter) with a diameter of 20 mm using a rheometer (RT-2010D / D-CW, manufactured by Leotech Co., Ltd., etc.) in the same manner as in the test example described later. It is said that the hardness (25 ° C.) at the time of entering 1 cm is 0.05 kgf or more, preferably 0.1 kgf or more, more preferably 0.5 kgf or more, still more preferably 1 kgf or more, and particularly preferably 2 kgf. That is all.

The external composition for skin of the present invention can be used in any situation where it is desired to continuously exert an antibacterial action. Specifically, it can be used as a deodorant agent or the like, but is not limited. According to the present invention, it can be expected that the antibacterial component applied to the skin is less likely to run off due to sweat or the like, can stay in the applied skin part for a long time, and can exert its antibacterial action for a long period of time. From this point of view, the external composition for skin of the present invention can be applied to sweaty skin areas (for example, under the armpits and neck muscles) and sweaty situations (for example, hot seasons such as summer, before and after strenuous exercise, etc.). ), It is preferable to use it as a deodorant (especially an antiperspirant deodorant).

The method of using the external composition for skin of the present invention varies depending on the condition, age, gender, season of use, etc. of the skin to be used, but it can be applied to any part of the skin where antibacterial action is desired. 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 external composition for skin of the present invention may be used regularly several times a day (for example, about 1 to 5 times a day), or may be used irregularly at a timing when it is desired to exert an antibacterial effect. 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 1 month.

(2. Method of increasing skin persistence of antibacterial component)
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 to be blended is in a specific range. It has been confirmed that the skin persistence of the (A) antibacterial component applied to the skin is enhanced by putting it inside.
Therefore, from yet another point of view, the present invention comprises (A) an antibacterial component, (B) a cyclodextrin-based 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, which comprises preparing the external composition for skin so that the content is 40% by weight or less based on the total content of the 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 performed as a cosmetological method unintended for medical treatment.
The types of the components (A) to (D) and their blending ratios in the above method, the types of other components that can be blended and their blending ratios, the formulation form, the method of use, etc. are described in the above "(1. External composition for skin)". It is the same as that described in.

Hereinafter, the present invention will be described in detail based on examples, but the present invention is not limited to these examples.
(Test Example 1: Evaluation of residual antibacterial component)
The following tests were conducted to evaluate the persistence of the antibacterial component at the application site.
The test products 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 heat treatment, and only the remaining aqueous component is mixed and similarly heated and dissolved. Each of the aqueous phases was prepared, emulsified with a homogenizer, and then cooled to room temperature to prepare an external composition for skin. The hardness of the pharmaceutical product of Example 1 was measured with a rheometer (RT-2010D / D-CW, manufactured by Leotech Co., Ltd.). First, the upper limit of measurement of the rheometer was set to 2 kgf, and a cylindrical plunger (adapter) φ20 mm was installed. A plastic jar (20 mL) rubbed with the formulation of Example 1 was placed in a rheometer, and the adapter penetration speed was set to 2 cm / min, and the hardness when the formulation of Example 1 was penetrated into the plastic jar by 1 cm was measured. did. As a result, the hardness of the formulation of Example 1 was 2 kgf or more. The formulations of Comparative Examples 1 to 4 were also prepared in the same manner as described above.

For each test product prepared above, the outflow rate of the antibacterial component (isopropylmethylphenol) was evaluated by the following procedure. First, about 25 mg of each test preparation shown in Table 1 above was applied to a test site (2.4 cm × 1.5 cm) of a NEO cover glass (20 mm × 50 mm, manufactured by Matsunami Glass Ind. Co., Ltd.). After air-drying this, it was immersed in a centrifuge tube containing 10 ml of purified water, and ultrasonic treatment (SONIC CLEANER, manufactured by AS ONE Corporation) was performed for about 30 minutes according to the instruction manual of the device. After this sonication, 2 ml of the immersion liquid was collected, 2 ml of a methanol / water (7: 3) mixed solution was added, mixed, filtered, and then isopropylmethylphenol in each immersion liquid was quantified by high performance liquid chromatography. .. Then, 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 in each immersion liquid / amount of isopropylmethylphenol [initial blending amount]) × 100

The results are shown in the bottom column of Table 1 above. As is clear from the above results, under the present test conditions, (B) cyclodextrin also has (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.]) was not included in the test preparation of Comparative Example 3 in which the applied isopropylmethylphenol was about 86. % Will be leaked. In the test products of Comparative Examples 1 and 2 in which only the component (B) or only the component (C) was added to the test product of Comparative Example 3, the outflow rate of isopropylmethylphenol was slightly suppressed, but it was still sufficient. I can't say. On the other hand, quite unexpectedly, by blending (A) isopropylmethylphenol with (B) cyclodextrin and (C) solid wax having a melting point of 40 ° C. or higher, (A) residual antibacterial component remains. It became clear that the rate was highly improved. When (C) a wax (liquid paraffin) liquid at room temperature is used instead of the solid wax having a melting point of 40 ° C. or higher, and (A) an antibacterial component and (B) cyclodextrin are used in combination. , High residual property as in the present invention was not observed (Comparative Example 4).

(Reference test example 1: Evaluation of residual antibacterial component)
The following tests were conducted to further evaluate the persistence of the antibacterial component at the application site.
The test product in the liquid form shown in Table 2 below was prepared by a conventional method in the same manner as in Test Example 1 above. Next, ultrasonic treatment was performed in the same procedure as in Test Example 1 above, and isopropylmethylphenol contained in the treated immersion liquid was quantified to calculate the 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 for skin containing about 60% by weight of water is prepared, (A) an antibacterial component, (B) a cyclodextrin compound and (C) a melting point are obtained. Even when a solid wax having a temperature of 40 ° C. or higher was blended in combination, the outflow rate of isopropylmethylphenol was high, and excellent residual property at the coating site as in the present invention was not observed.

(Test Example 2: Evaluation of residual antibacterial component)
The following tests were conducted to further evaluate the persistence of the antibacterial component at the application site.
The test products shown in Table 3 below were prepared by a conventional method in the same manner as in Test Example 1 above. When the hardness (25 ° C.) of each test product of Example was measured with a rheometer (RT-2010D / D-CW, manufactured by Leotech Co., Ltd.) under the same measurement conditions as in Test Example 1, Example 2 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, the antibacterial component (isopropylmethylphenol) contained in the treated immersion liquid is quantified, and the isopropylmethylphenol outflow rate (%) is calculated by the above formula I. 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 having a melting point of 40 ° C. or higher (paraffin [melting point: 55 ° C.], polyethylene). Wax [melting point: 75-90 ° C], purified microcrystalline wax [melting point: 70-85 ° C], (stealoxymethicone / dimethicone) copolymer [melting point: 40-50 ° C], cetyl alcohol [melting point: 46-55 ° C] ) Are combined and the content of (D) water is 40% by weight or less, so that excellent (A) isopropylmethylphenol persistence is observed as in the result of Test Example 1 above (implementation). Examples 2-6).

(Test Example 3: Evaluation of residual antibacterial component)
The following tests were conducted to further evaluate the persistence of the antibacterial component at the application site.
The test product of Example 7 shown in Table 4 below was prepared by a conventional method in the same manner as in Test Example 1 above. When the hardness (25 ° C.) of the pharmaceutical product of Example 7 was measured using a rheometer (RT-2010D / D-CW, manufactured by Leotech Co., Ltd.) under the same measurement conditions as in Test Example 1, 2 kgf. That was all. The formulations of Comparative Examples 6 to 7 were also 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 placed on the test site (2.4 cm × 1.5 cm) of the NEO cover glass (24 mm × 50 mm, manufactured by Matsunami Glass Ind. Co., Ltd.). It was applied. After air-drying this, it was immersed in a centrifuge tube containing 10 ml of purified water, and ultrasonic treatment (SONIC CLEANER, manufactured by AS ONE Corporation) was performed for about 15 minutes according to the instruction manual of the device. After this ultrasonic treatment, 2 ml of the immersion liquid was collected, about 2 ml of an organic solvent was added thereto, and the mixture was shaken for 10 minutes. Next, 2 ml was collected from the mixed solution after the shaking treatment, methanol / water mixed solution was added, mixed, filtered, and then benzalkonium chloride (benzalkonium chloride) in each immersion solution was subjected to high performance liquid chromatography. The thing) was quantified. Next, the outflow rate (%) of benzalkonium chloride was calculated from each quantitative value according to the following formula II.

[Formula II] Benzalkonium chloride outflow rate (%) = (Amount of benzalkonium chloride / Amount of benzalkonium chloride in each immersion liquid [Initial compounding amount]) × 100

The results are shown in the bottom column of Table 4 above. (A) As an antibacterial component, benzalkonium chloride was evaluated for residual properties at the coating site instead of isopropylmethylphenol. As a result, 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: 75-90 ° C], purified microcrystalin wax [melting point: 70-85 ° C], (stearoxymethicone / dimethicone) copolymer [melting point: 40-50 ° C]) Although the outflow rate was considerably suppressed by combining (D) and reducing the water content to 40% by weight or less (Comparative Example 6), benzalkonium chloride was further combined with (B) cyclodextrin. It was confirmed that the outflow rate of nium could be suppressed even more effectively (Example 7). The improvement of the residual property at the application site by blending cyclodextrin has not been known so far, and such an effect of improving the residual property of the present invention was unexpected.

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

Claims (13)

At least one antibacterial component selected from the group consisting of (A) isopropylmethylphenol and a quaternary ammonium salt type antibacterial component, (B) a cyclodextrin compound, and ( C) 20 to 60 weights based on the entire composition. containing% solid wax scan melting point of 40 ° C. or more, and (E) 15 to 50 wt% of the liquid oil component of the total composition, and, relative to the total content of the composition of (D) water der 20 wt% or less Te Ri, (a) the content of component (C) to component 1 part by weight is 1 to 1,000 parts by weight, external skin perspiration deodorant composition. The composition for external sweat-resistant deodorant for external use according to claim 1, which contains the component (D) in an amount of 1% by weight or more based on the entire composition. The composition for external sweat-resistant deodorant for skin according to claim 1 or 2, which contains at least one selected from the group consisting of cyclodextrin, a derivative thereof, and a salt thereof as a component (B). (C) Contains at least one selected from the group consisting of petroleum-derived wax, synthetic wax, silicone wax, plant-derived wax, animal-derived wax, mineral-derived wax, and solid higher alcohol. The composition for external sweat-resistant deodorant for skin according to any one of claims 1 to 3. The composition for external sweat-resistant deodorant for external use according to any one of claims 1 to 4, which has a hardness of 0.05 kgf or more at 25 ° C. The composition for external sweat-resistant deodorant for external use according to any one of claims 1 to 5, wherein the component (A) is contained in an amount of 0.001% by weight or more based on the entire composition. The composition for external sweat-resistant deodorant for external use according to any one of claims 1 to 6, wherein the component (B) is contained in an amount of 0.1% by weight or more based on the entire composition. The composition for external sweat-resistant deodorant for external use according to any one of claims 1 to 7 , which contains 0.1 to 1000 parts by weight of the component (B) with respect to 1 part by weight of the component (A). The composition for external sweat-resistant deodorant for skin according to any one of claims 1 to 8, which contains 10 to 1000 parts by weight of the component (E) with respect to 1 part by weight of the component (A). In the composition for external deodorant for skin, at least one antibacterial component selected from the group consisting of (A) isopropylmethylphenol and a quaternary ammonium salt type antibacterial component, (B) cyclodextrin compound, and (C) composition. Solid wax having a melting point of 20 to 60% by weight based on the whole product at 40 ° C. or higher, (D) water having a melting point of 20% by weight or less based on the whole composition (including the case where the component (D) is not present). And (E) for improving the skin persistence of the component (A) to sweat in this composition for external deodorant for skin, which comprises coexisting with 15 to 50% by weight of liquid oil with respect to the entire composition. Method. The method according to claim 10, wherein the content of the component (C) with respect to 1 part by weight of the component (A) in the composition for external deodorant for skin is set to 1 to 1000 parts by weight. The method according to claim 10 or 11, wherein the content of the component (D) in the composition for external deodorant for skin is 1% by weight or more based on the whole composition. At least one antibacterial ingredient selected from the group consisting of (A) isopropylmethylphenol and a quaternary ammonium salt type antibacterial ingredient, (B) a cyclodextrin-based compound, and (C) 20 to 60 weights based on the entire composition. % Is a solid wax having a melting point of 40 ° C. or higher, and (E) a liquid oil content of 15 to 50% by weight based on the whole composition, and (D) a water content of 20% by weight based on the whole composition. The component (B), the component (C), the component (E), and the component (D) in the state of being present in the composition for external deodorant for skin which is% or less (however, the component (D) may not be present. ), In the composition for external deodorant for skin, for improving the skin persistence of the component (A) to sweat.