WO2021256566A1

WO2021256566A1 - Composition for external use on skin containing ascorbic acid and/or salt thereof

Info

Publication number: WO2021256566A1
Application number: PCT/JP2021/023237
Authority: WO
Inventors: 達也安藤; 愛桝本; 大貴中田
Original assignee: ロート製薬株式会社
Priority date: 2020-06-19
Filing date: 2021-06-18
Publication date: 2021-12-23
Also published as: JPWO2021256566A1; TW202203895A; CN115697294A

Abstract

Provided is a composition for external use on the skin which is excellent in terms of use feeling and appearance.　The purpose of the present invention is to provide a composition for external use on the skin which has satisfactory use feeling, that is, good slipperiness, and is reduced in coloration. The composition for external use on the skin comprises (A) at least one compound selected from the group consisting of ascorbic acid and salts of ascorbic acid, (B) at least one compound selected from the group consisting of salicylic acid, salts of salicylic acid, and derivatives of salicylic acid, and (C) a diol having three carbon atoms, the content of which is 1-50 mass%.

Description

External skin composition containing ascorbic acid and / or a salt thereof

The present invention relates to an external composition for skin containing ascorbic acid and / or a salt thereof.

Ascorbic acid has anti-inflammatory effect, acne improving effect, whitening effect, anti-aging effect, antioxidant effect, cell activation effect by promoting synthesis of biological components such as collagen, and suppresses cell damage and DNA damage caused by ultraviolet rays of epidermal keratinocytes. It is known to exert various effects such as the effect of collagen, and it is used as an external preparation for skin in anticipation of these effects. A technique for improving the stability of such ascorbic acid has been proposed (for example, Patent Document 1).

Japanese Unexamined Patent Publication No. 2005-225856

An object of the present invention is to provide an ascorbic acid-containing external composition for skin that has a good usability and appearance.

According to the studies by the present inventors, it has been found that when a composition containing ascorbic acid and / or a salt thereof is used as a skin external preparation, it may be difficult to have both a good feeling of use and a good appearance. did.

As a result of diligent studies to solve this problem, the present inventors have obtained at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid, (B) salicylic acid, a salt of salicylic acid, and the like. By containing at least one selected from the group consisting of a derivative of salicylic acid and 1 to 50% by mass of (C) a diol having 3 carbon atoms, a composition for external use on the skin having excellent usability and appearance can be obtained. We found that and came to complete the present invention.

That is, the present invention provides the composition for external use on the skin listed below.
Item 1.
At least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid, (B) at least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C). A composition for external use on the skin containing 1 to 50% by mass of a diol having 3 carbon atoms.
Item 2.
Item 2. The external composition for skin according to Item 1, wherein the concentration of the component (A) is 1 to 10% by mass.
Item 3.
Item 2. The composition for external use on the skin according to Item 1 or 2, wherein the concentration of the component (B) is 0.001 to 2% by mass.
Item 4.
The composition for external use on the skin according to any one of Items 1 to 3, further comprising (D) 1 to 15% by mass of water.
Item 5.
The composition for external use on the skin according to any one of Items 1 to 4, further comprising (E) 1 to 20% by mass of a lower alcohol.
Item 6.
Item 6. The composition for external use on the skin according to any one of Items 1 to 5, wherein the pH is 2 to 5.

Furthermore, the present invention provides the following methods for external skin compositions.
Item 7.
At least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid, (B) at least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C). A method for suppressing coloration of an external composition for skin containing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid by blending 1 to 50% by mass of a diol having 3 carbon atoms.
Item 8.
(B) at least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C) ascorbic acid and (A) ascorbic acid containing 1 to 50% by mass of a diol having 3 carbon atoms. A color inhibitor for a composition comprising at least one selected from the group consisting of salts of ascorbic acid.
Item 9.
At least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid, (B) at least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C). Improving the usability of the composition for external use on the skin containing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid by using 1 to 50% by mass of a diol having 3 carbon atoms. how to.
Item 10.
(B) at least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C) ascorbic acid and (A) ascorbic acid containing 1 to 50% by mass of a diol having 3 carbon atoms. A usability-enhancing agent for a composition containing at least one selected from the group consisting of salts of ascorbic acid.

INDUSTRIAL APPLICABILITY According to the present invention, it is possible to provide a composition for external use on the skin, which is excellent in usability and appearance.

In the present specification, the unit of content "mass%" is synonymous with "g / 100g".

[External skin composition]
The external composition for skin of the present invention is
(A) At least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid;
(B) At least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid; and (C) an external composition for skin containing 1 to 50% by mass of a diol having 3 carbon atoms.

(At least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid)
As the ascorbic acid used in the present invention, ascorbic acid commercially available as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics can be used, and these are usually L-forms, though not limited. Refers to things.

Ascorbic acid salt can also be used. Here, the salt of ascorbic acid is a pharmaceutically acceptable salt. Although not limited, for example, a salt with an organic base (for example, a salt with a tertiary amine such as a trimethylamine salt, a triethylamine salt, a monoethanolamine salt, a triethanolamine salt, a pyridine salt, a basic ammonium salt such as arginine). Etc.), salts with inorganic bases (eg, alkali metal salts such as ammonium salt, sodium salt, potassium salt, alkaline earth metal salt such as calcium salt, magnesium salt, aluminum salt, etc.) and the like are exemplified. Preferred ascorbic acid salts are sodium and potassium salts.

In the present invention, ascorbic acid or a salt thereof can be used alone or in combination of two or more. Ascorbic acid is preferable from the viewpoint of remarkably exerting the effect of the present invention. (A) Ascorbic acid or a salt thereof may be synthesized and used, or a commercially available product may be used.

In the external composition for skin of the present invention, the total content of the component (A) with respect to the total amount of the external composition for skin is appropriately set according to the balance with other components.

The total content of the component (A) with respect to the total amount of the external composition for skin is preferably 20% by mass or less, more preferably 10% by mass or less, still more preferably 7% by mass or less, still more preferably 5% by mass. % Or less. The total content of the component (A) with respect to the total amount of the external composition for skin is preferably 0.5% by mass or more, more preferably 1% by mass or more, still more preferably 2% by mass or more. , Even more preferably 3% by mass or more. The total content of the component (A) with respect to the total amount of the external composition for skin is preferably 0.5 to 20% by mass, more preferably 1 to 10% by mass, still more preferably 2 to 9% by mass, and even more. It is preferably 3 to 5% by mass.

((B) At least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid)
The salicylic acid or the derivative of salicylic acid used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics.

Salicylic acid salt can also be used. Here, the salt of salicylic acid is a pharmaceutically acceptable salt. Examples thereof include, but are not limited to, alkali metal salts, alkaline earth metal salts, salts with organic bases, and the like. Examples of the salicylate include at least one selected from the group consisting of sodium salicylate, calcium salicylate, magnesium salicylate and potassium salicylate.

From the viewpoint of remarkably exerting the effect of the present invention, at least one selected from the group consisting of salicylic acid, sodium salicylate, calcium salicylate, magnesium salicylate and potassium salicylate is preferable, and salicylic acid and / or sodium salicylate is more preferable. In another embodiment, a derivative of salicylic acid can be used as the component (B). Such derivatives of salicylic acid include, but are not limited to, ethylene glycol salicylate, phenyl salicylate, methyl salicylate, 2-ethylhexyl salicylate, dipropylene glycol salicylate, Ti salicylate and the like. (B) Salicylic acid, a salt of salicylic acid, or a derivative of salicylic acid may be synthesized and used, or a commercially available product may be used.

In the external composition for skin of the present invention, the total content of the component (B) with respect to the total amount of the external composition for skin is not limited, but is preferably 0.001% by mass or more, more preferably 0.005% by mass. % Or more, more preferably 0.01% by mass or more, still more preferably 0.05% by mass or more.
The total content of the component (B) with respect to the total amount of the external composition for skin is not limited, but is preferably 5% by mass or less, more preferably 2% by mass or less, still more preferably 1% by mass or less. , Even more preferably 0.5% by mass or less.

The total content of the component (B) with respect to the total amount of the external composition for skin is preferably 0.001 to 5% by mass, preferably 0.005 to 2% by mass, and more preferably 0.01 to 1% by mass. More preferably, it is 0.05 to 0.5% by mass. Further, it may be 0.001 to 5% by mass, 0.01 to 4% by mass, 0.1 to 3% by mass, 0.5 to 2% by mass, etc., considering the case where it is used for acne medicine. ..

In the external composition for skin of the present invention, the ratio of the blending amount of the component (B) to the component (A) is not particularly limited, but 0.0002 to 10 mass with respect to 1 part by mass of the total content of the component (A). Parts are preferable, 0.001 to 1 part by mass is more preferable, 0.005 to 0.25 parts by mass is more preferable, and 0.01 to 0.2 parts by mass is even more preferable.

((C) A diol having 3 carbon atoms)
The diol having 3 carbon atoms used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics. Further, as such a diol having 3 carbon atoms, a commercially available product can be used as it is. The diol having 3 carbon atoms is not limited, but is, for example, 1,3-propanediol (CAS number: 504-63-2, English name: 1,3-Dihydroxypropane or TrimethyleneGlycol) or propylene glycol (CAS number: 57). -55-6, English name: 1,2-Dihydroxypropane, Japanese name alias: 1,2-propanediol) can be exemplified, and one type may be used or may be used in combination as appropriate. From the viewpoint of alleviating irritation to the skin, improving the feeling of use, and suppressing coloration, it is also one of the preferable embodiments to combine 1,3-propanediol and propylene glycol, and at least 1,3-propanediol as the component (C). It is more preferable to include.

In the external composition for skin of the present invention, the total content of the component (C) with respect to the total amount of the external composition for skin is 1% by mass or more, preferably 5% by mass or more, more preferably 10% by mass or more. be.
The total content of the component (C) with respect to the total amount of the external composition for skin is 50% by mass or less, preferably 40% by mass or less, and more preferably 30% by mass or less.

The total content of the component (C) with respect to the total amount of the external composition for skin is 1 to 50% by mass, preferably 5 to 40% by mass, and more preferably 10 to 30% by mass.

In the external composition for skin of the present invention, the ratio of the blending amount of the component (C) to the component (A) is not particularly limited, but is 0.05 to 100 mass with respect to 1 part by mass of the total content of the component (A). Parts are preferable, 0.5 to 40 parts by mass is more preferable, and 1 to 15 parts by mass is further preferable.

Among the components (C), the blending amount of propylene glycol is 0.1% by mass or more, preferably 0.5% by mass or more, more preferably 1% by mass or more, and further, with respect to the total amount of the external composition for skin. It is preferably 5% by mass or more, and even more preferably 10% by mass or more. The blending amount of propylene glycol is preferably 50% by mass or less, 40% by mass or less, more preferably 30% by mass or less, still more preferably 20% by mass or less, still more preferably 10% by mass or less.
The total content of propylene glycol with respect to the total amount of the external composition for skin is 0.1 to 50% by mass, 0.5 to 40% by mass, 1 to 40% by mass, preferably 5 to 30% by mass, and more preferably 5 to 30% by mass. It is 10 to 20% by mass.

In the composition for external use on the skin of the present invention, the ratio of the blending amount of propylene glycol to the component (A) is not particularly limited, but 0.05 to 80 parts by mass is based on 1 part by mass of the total content of the component (A). Preferably, 0.5 to 30 parts by mass is more preferable, and 1 to 10 parts by mass is further preferable.

Of the components (C), the blending amount of 1,3-propanediol is 0.1% by mass or more, preferably 0.5% by mass or more, more preferably 1% by mass, based on the total amount of the external composition for skin. % Or more, more preferably 5% by mass or more, still more preferably 10% by mass or more. The blending amount of 1,3-propanediol is 50% by mass or less, 40% by mass or less, 30% by mass or less, more preferably 25% by mass or less, still more preferably 20% by mass or less, still more preferably 15% by mass or less. be.

The total content of 1,3-propanediol with respect to the total amount of the external composition for skin is 0.1 to 50% by mass, 0.5 to 40% by mass, 1 to 30% by mass, preferably 5 to 20% by mass. More preferably, it is 10 to 15% by mass.

In the external composition for skin of the present invention, the ratio of the blending amount of 1,3-propanediol to the component (A) is not particularly limited, but is 0.05 to 0.05 with respect to 1 part by mass of the total content of the component (A). 60 parts by mass is preferable, 0.5 to 20 parts by mass is more preferable, and 1 to 7.5 parts by mass is further preferable.

In the composition for external use on the skin of the present invention, the component (C) may be a mixture of propylene glycol and 1,3-propanediol. In this case, the total amount of propylene glycol and 1,3-propanediol may be 10% by mass or more, 15% by mass or more, 20% by mass or more, 25% by mass or more, 30% by mass or more, and 50% by mass. % Or less, 45% by mass or less, 40% by mass or less, 35% by mass or less.
The total amount of propylene glycol and 1,3-propanediol to be added to the total amount of the external composition for skin was 10% by mass to 50% by mass, 15 to 45% by mass, 20 to 40% by mass, and 25 to 35% by mass. May be.
When both propylene glycol and 1,3-propanediol are blended, 5 to 25% by mass, 5 to 20% by mass, 5 to 15% by mass, 10 to 25% by mass, and 10 to 20% by mass, respectively. It may be 10 to 15% by mass, 15 to 25% by mass, 15 to 20% by mass, or the like.

In addition to the above components (A), (B), and (C), the composition for external use on the skin of the present invention comprises (D) water and / or (E) lower grade as long as it does not interfere with the effects of the present invention. It may contain alcohol.

((D) water)
The external composition for skin of the present invention may be a composition containing water. The proportion of water is not limited, but the content of water with respect to the total amount of the external composition for skin is preferably 0.1 to 30% by mass, more preferably 1 to 20% by mass, still more preferably 2 to 15. It is mass%.

In the external composition for skin of the present invention, the ratio of the component (D) to the component (A) is preferably 0.005 to 60 parts by mass with respect to 1 part by mass of the total content of the component (A), preferably 0.1. Up to 20 parts by mass is more preferable, and 0.2 to 7.5 parts by mass is even more preferable.

((E) Lower alcohol)
The external composition for skin of the present invention may contain a lower alcohol. The lower alcohol used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics. As used herein, the term "lower alcohol" refers to the alcohol of C1-C6. Of these, C1-C3 alcohols can be particularly preferably used. Examples of such examples include methanol, ethanol, n-propanol, isopropanol and the like, with ethanol being preferred.

In the external composition for skin of the present invention, the total content of the component (E) with respect to the total amount of the external composition for skin is preferably 0.1 to 40% by mass, more preferably 0.5 to 10% by mass when it is contained. %, More preferably 1 to 7% by mass.

In addition, although not limited, typically, in the external composition for skin of the present invention, the amount of ethanol with respect to the total amount of the external composition for skin is preferably 1 to 40% by mass, more preferably 2 to 30% by mass. , More preferably 3 to 20% by mass.

In the external composition for skin of the present invention, the ratio of the blending amount of the component (E) to the component (A) is preferably 0.005 to 80 parts by mass with respect to 1 part by mass of the total content of the component (A). 0.05 to 10 parts by mass is more preferable, and 0.1 to 3.5 parts by mass is further preferable.

(Multivalent alcohol)
The composition for external use on the skin of the present invention may contain a polyhydric alcohol in addition to the above-mentioned component (A), component (B), and component (C) as long as the effect of the present invention is not impaired.

The polyhydric alcohol used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics. Polyhydric alcohols may be added, but not limited to, for moisturizing or as a solubilizer. Specific examples thereof include glycerin, diglycerin, dipropylene glycol, 1,3-butylene glycol, 3-methyl-1,3-butanediol and the like.

The total content of the polyhydric alcohol other than the component (C) with respect to the total amount of the external composition for skin of the present invention, when contained, is preferably 0.1 to 60% by mass, more preferably 1 to 50% by mass. More preferably, it is about 10 to 45% by mass.

(Vitamin E)
The composition for external use on the skin of the present invention contains tocopherol, a salt of tocopherol, a derivative of tocopherol, and the like, in addition to the above components (A), (B), and (C), as long as the effects of the present invention are not impaired. It may contain vitamin Es. As the tocopherol, the salt of tocopherol, the derivative of tocopherol and the like used in the present invention, a compound usually used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics can be used. It may be either a body or a dl body, and may have any of α, β, γ, and δ structures. Examples of tocopherols include d-α-tocopherol, d-β-tocopherol, d-γ-tocopherol and d-δ-tocopherol, l-α-tocopherol, l-β-tocopherol, l-γ-tocopherol, l-. Examples thereof include δ-tocopherol, dl-α-tocopherol, dl-β-tocopherol, dl-γ-tocopherol, dl-δ-tocopherol and the like, which are mixtures thereof. The derivative of tocopherol is not limited, but an ester of tocopherol is preferable. In particular, as derivatives of tocopherol, tocopherol acetate, tocopherol nicotinic acid ester or a salt thereof, tocopherol succinic acid ester or a salt thereof, tocopherol linolenic acid ester, tocopherol phosphate or a salt thereof, (linoleic acid / oleic acid) tocopherol , And one selected from the group consisting of tocotolinole, and the like are exemplified.

In the external composition for skin of the present invention, the total content of vitamin E with respect to the total amount of the external composition for skin is not particularly limited, but is preferably 0.00001 to 10% by mass, more preferably 0.0001 to 5% by mass. %.

(Ascorbic acid derivative)
The composition for external use on the skin of the present invention may contain an ascorbic acid derivative in addition to the above-mentioned component (A), component (B), and component (C) as long as the effect of the present invention is not impaired. Examples of the ascorbic acid derivative used in the present invention include 3-O-ethylascorbic acid, L-ascorbic acid 2-glucoside, dehydroascorbic acid, sodium ascorbic acid phosphate, magnesium ascorbic acid phosphate, and ascorbic acid monophosphate. Examples thereof include sodium, sodium ascorbic acid diphosphate ester, sodium ascorbic acid triphosphate ester, sodium ascorbic acid-2-sulfate ester, and salts thereof.

Salt is a pharmaceutically acceptable salt. Examples of the salt include, but are not limited to, salts with organic bases (eg, salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, arginine and the like. Examples thereof include salts with inorganic bases (eg, alkali metal salts such as ammonium salts, sodium salts and potassium salts, alkaline earth metal salts such as calcium salts and magnesium salts, aluminum salts, etc.). To. Particularly preferable salts of 3-O-ethylascorbic acid are sodium salt and potassium salt.

In the present invention, these ascorbic acid derivatives may be used alone or in combination of two or more.

In the external composition for skin of the present invention, the total content of the ascorbic acid derivative with respect to the total amount of the external composition for skin is preferably 0.005 to 10% by mass, more preferably 0.01 to 5% by mass, still more preferably. , 0.02 to 3% by mass, and even more preferably 0.05 to 2% by mass.

(Surfactant)
The external composition for skin of the present invention may contain a surfactant as long as it does not interfere with the effects of the present invention. When a surfactant is contained, a nonionic surfactant is preferable, and for example, polyoxyethylene hydrogenated castor oil 40, polyoxyethylene hydrogenated castor oil 60, polyoxyethylene hydrogenated castor oil 80, and polyoxy Ethylene polyoxypropylene decyltetradecyl ether, polyoxyethylene (20) polyoxypropylene (4) cetyl ether, polyoxyethylene (10) cetyl ether, polyoxyethylene (10) polyoxypropylene (4) cetyl ether, polyoxy Ethylene (10) oleyl ether, polyoxyethylene stearyl ether, polyoxyethylene isoalcohol ether, PEG-8 glyceryl isostearate, polyoxyethylene sorbitan monolaurate (20EO), polyoxyethylene sorbitan isostearate (20EO) ), Polyoxyethylene sorbitan stearate (20EO), palm oil fatty acid polyglyceryl-10, palm oil fatty acid polyglyceryl-3, palm oil fatty acid PEG-7 glyceryl, polyglyceryl dioleate-10, polyglyceryl diisostearate-10, PEG-40 glyceryl triisostearate, PEG-40 glyceryl isostearate, polyglyceryl-10 trilaurate, hexaglyceryl tricaprylate, polyglyceryl laurate, polyglyceryl myristate, polyoxyethylene lauryl ether and the like can be used, especially polyoxyethylene. Polyoxypropylene decyltetradecyl ether, polyoxyethylene hydrogenated castor oil 40, polyoxyethylene hydrogenated castor oil 60, polyoxyethylene hydrogenated castor oil 80, polyoxyethylene sorbitan isostearate (20EO), polyoxyethylene monolaurate Sorbitane (20EO) and polyglyceryl laurate are preferred.

In the external composition for skin of the present invention, the total content of the surfactant with respect to the total amount of the external composition for skin is appropriately set depending on the balance with other components. The total content of the surfactant with respect to the total amount of the external composition for skin is preferably 0.001 to 10% by mass, more preferably 0.005 to 7% by mass, still more preferably 0.01 to 5% by mass. Is.

(Other ingredients)
In addition to the above-mentioned components (A), (B), and (C), the external composition for skin of the present invention is further used for the purpose of enhancing or supplementing various actions of ascorbic acid, and other components. To add useful effects, whitening component, anti-inflammatory component, antibacterial component, cell activation component, astringent component, antioxidant component, acne improving component, anti-aging component, biological component synthesis promoting component such as collagen, blood circulation promoting component , Moisturizing component, anti-aging component and other various components can be blended in one type or in combination of two or more. It is preferably one or more components of a whitening component, an anti-inflammatory component, an antibacterial component, a cell activating component, an astringent component, an antioxidant component, an antiaging component or a moisturizing component. Particularly preferable combinations of these components are a combination with a whitening component, a combination of a whitening component and an antioxidant component, each combination with an antioxidant component, a combination with an anti-aging component, and a whitening component and an anti-aging component. Each combination of can be mentioned. Each of these ingredients is not particularly limited as long as it is conventionally used as an ingredient of a skin external preparation in the fields of pharmaceuticals, quasi-drugs, or cosmetics, and is not particularly limited as long as it is used in the future. Can be used. Of these, isopropylmethylphenol, which is a bactericidal component, and / or dipotassium glycyrrhizinate, which is an anti-inflammatory component, are particularly preferably used.

The composition for external use on the skin of the present invention may further contain a solubilizing component, oils and fats, saccharides, or a transdermal absorption promoting component in addition to each of the above components. In particular, by blending a solubilizing component or oils and fats, the stability, effectiveness and usability of ascorbic acid in an aqueous solvent can be further improved.

The composition for external use on the skin of the present invention is, if necessary, a pharmaceutical product, a quasi-drug, or a pharmaceutical product, within a quantitative and qualitative range that does not impair the quality such as appearance stability and viscosity, and does not impair the effect of the present invention. Various components commonly used as components of external agents in the cosmetic field, such as amino acids, irritation reducing agents, thickeners, preservatives, UV protection agents, coloring agents, dispersants, additional pH regulators, fragrances, etc. Can be blended. It should be noted that these components may be used alone or in combination of two or more.

(form)
The external composition for skin of the present invention contains (A), (B), and (C) components, and if necessary, each of the above optional components is blended and mixed, and if necessary, other solvents and commonly used external applications are added. By blending the base of the agent, various desired forms such as paste, mousse, gel, liquid, milky, cream, sheet (supporting a base material), aerosol, and spray are prepared. be able to. These can be manufactured by conventional methods in the art.

The composition for external use on the skin of the present invention is particularly preferably a transparent or translucent composition in which ascorbic acid and / or a salt thereof is solubilized. Here, "solubilization" is defined as follows. That is, for example, the transmittance is 80 to 100%, preferably 85 to 100, as the transmittance at a wavelength of 700 nm using a spectrophotometer or a photoelectric photometer UV-2450 (manufactured by Shimadzu Corporation) by an ultraviolet-visible absorbance measurement method. %, More preferably in the range of 90 to 100%. Here, the transmittance of water is 100%. The solubilized composition of the present invention has a transparent or translucent appearance. For more details, the permeability measurement method is the 16th revised Japanese Pharmacopoeia [B] general test method. Physical test method Spectroscopic measurement method 2.24 Follow the method described in the ultraviolet-visible absorbance measurement method.

(viscosity)
The external composition for skin of the present invention can be prepared as a composition having an appropriate viscosity desired especially when using the external composition for skin used for application to the skin. The viscosity of the external composition for skin of the present invention is not particularly limited, but for example, the viscosity when measured at 25 ° C. using an E-type viscometer is usually about 1 to 300 mPa · s, preferably 1 to 200 mPa · s. The degree, more preferably about 1 to 100 mPa · s, and most preferably about 1 to 50 mPa · s. More specifically, the viscosity measurement method is the 16th revised Japanese Pharmacopoeia [B] general test method. Physical test method Other physical test methods 2.53 Viscosity measurement method 2. Second method Rotational viscometer method 2.1.3 Follow the method described in the cone-plate type rotational viscometer (cone plate type viscometer).

(PH)
The composition for external use on the skin of the present invention may usually have a liquid property of pH 1 to 8, but is preferable from the viewpoints of stability of ascorbic acid, hypoallergenicity to the skin and mucous membranes, and good skin usability. The pH is 2 to 7, more preferably pH 2 to 6, still more preferably pH 2 to 5.0, and most preferably pH 2 to 4.5. It is desirable that it is in an acidic region.

(Use)
The external composition for skin of the present invention is particularly effective as a whitening agent, an anti-inflammatory agent, and an anti-aging agent, and has, for example, acne prevention, treatment, and antioxidative effects. Further, when applied to the skin, the transparency of the skin is enhanced, the moisture is maintained, the texture is smoothed, and the effect of suppressing roughness may be exhibited. In addition, it may have effects such as moisturizing the skin where acne scars and pores are anxious, making the pores inconspicuous, leading to smooth skin, moisturizing the skin, and for preventing and treating stains. It can also be used.

The external composition for skin of the present invention is, for example, basic cosmetics such as beauty liquids, lotions, sunscreen creams, milky lotions, creams, lotions, oils and packs; foundations, lipsticks, lip creams, mascara, eye shadows, eye liners. , Makeup cosmetics such as eyebrows and beautiful nails; Cleaning agents such as facial cleansers, cleansers, and body cleaning agents; It can be used as various external skin compositions belonging to the fields of cosmetics, external medicines or external pharmaceutical products such as acne therapeutic agents, hemorrhagic agents, sterilizing and disinfecting agents, whitening agents, ultraviolet protective agents and the like. From the viewpoint of the effect on the skin, the present invention is preferably used for products applied to the integument such as an external skin preparation (formulation for the integument). The composition of the present invention can be used once or several times a day according to the intended use and the like, in a known or commonly used dosage and administration.

[Coloring suppression method]
The present invention also includes a method for suppressing coloration of an external composition for skin containing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid. According to the coloring suppressing method of the present invention, at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid; (B) selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid. By containing 1 to 50% by mass of (C) a diol having 3 carbon atoms, it is possible to obtain a stable preparation in which coloring is suppressed while containing ascorbic acid. That is, the present invention is at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid; (B) at least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid. Species; and (C) an external skin composition containing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid by containing 1 to 50% by mass of a diol having 3 carbon atoms. The present invention relates to a method for suppressing coloration of an object. Here, the term "coloring suppression" refers to, but is not limited to,, for example, the suppression of coloring caused by ascorbic acid (including the improvement of transparency) when stored. Due to such color suppression, the external composition for skin of the present invention exhibits a good appearance. Further, the good appearance due to such color suppression also includes, for example, the fact that the pharmaceutical product does not color when it adheres to clothing or the like.

In the color suppression of the present invention, at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid; (B) at least selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid. The composition for external use on the skin containing 1 to 50% by mass of (C) a diol having 3 carbon atoms and the content thereof are the same as those used in the composition for external use on the skin.

[Color inhibitor]
The present invention also includes a color inhibitor of an external composition for skin containing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid. The color inhibitor of the present invention contains (B) at least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C) 1 to 50% by mass of a diol having 3 carbon atoms. , (A) A color inhibitor of an external composition for skin containing at least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid.

In the color inhibitor of the present invention, at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid; (B) selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid. At least one type; and (C) a composition for external use on the skin containing 1 to 50% by mass of a diol having 3 carbon atoms, and the content thereof are the same as those used in the above-mentioned external composition for skin. ..

[How to improve usability]
The present invention also includes a method for improving the usability of an external composition for skin containing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid. According to the method for improving usability of the present invention, at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid; (B) from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid. A good usability can be obtained by containing at least one selected; and (C) 1 to 50% by mass of a diol having 3 carbon atoms. That is, the present invention is at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid; (B) at least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid. Species; and (C) External skin composition containing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid by containing 1 to 50% by mass of a diol having 3 carbon atoms. It relates to a method of giving a good feeling of use to an object. Here, the usability is not limited, but refers to, for example, less friction and smooth application.

In the method for improving usability of the present invention, at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid; (B) selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid. (C) The composition for external use on the skin containing 1 to 50% by mass of the diol having 3 carbon atoms and the content thereof are the same as those used in the above-mentioned composition for external use on the skin. be.

[Usage improver]
The present invention also includes a usability-enhancing agent for an external skin composition containing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid. The usability improving agent of the present invention contains at least one selected from the group consisting of (B) salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C) 1 to 50% by mass of a diol having 3 carbon atoms. (A) A usability-enhancing agent for an external composition for skin containing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid.

In the usability improving agent of the present invention, at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid; (B) selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid. (C) The composition for external use on the skin containing 1 to 50% by mass of the diol having 3 carbon atoms and the content thereof are the same as those used in the above-mentioned composition for external use on the skin. be.

Next, the present invention will be specifically described with reference to Examples, but the present invention is not limited to the following Examples. The unit of each component amount in the table is mass% unless otherwise specified in the table.

The external composition for skin having the compositions shown in Tables 1 to 4 was prepared according to a conventional method.

[Test Example 1: Ascorbic acid coloring suppression confirmation test]
For the compositions of the standard example, the comparative example, and the example, the presence or absence of suppression of coloring after storage at 60 ° C. was evaluated visually and by a color difference meter. Specifically, various components were mixed and dissolved according to the formulations shown in the table to prepare a composition. 10 mL of the prepared composition was filled in a 20 mL screw cap bottle, and the mixture was allowed to stand in a thermostat at 60 ° C. for 5 days. After 5 days of the measurement period had elapsed, the screw cap bottle was taken out from the thermostat and evaluated after constant temperature at 25 ° C. Each composition was subjected to measurement, and the presence or absence and degree of coloring were determined.
For measurement, use a spectrophotometer CM-5 (manufactured by Konica Minolta Co., Ltd.), put 2.5 mL of the test solution into a glass cell (CM-A97, thickness 2 mm), and set the L value in the CIELAB color system at 25 ° C. , A value, and b value were measured. As the measured value, ΔL * Δa * Δb * when purified water was used as a blank was used.

The L * value (ΔL *) is a value related to lightness, the a * value (Δa *) is a value related to bidirectionality between red and green, and the b * value (Δb *) is a value related to bidirectionality between yellow and blue. be.

ΔE * ab is expressed by the following formula and is an index showing the degree of overall coloring of the composition of the example or the comparative example.

The rate of increase of ΔL was calculated by the following formula.
ΔL increase rate = ΔL (D65) (after storage) / ΔL (D65) (before storage)

The rate of increase in Δa was calculated by the following formula.
Δa increase rate = Δa (D65) (after storage) / Δa (D65) (before storage)

The rate of increase of Δb was calculated by the following formula.
Δb increase rate = Δb (D65) (after storage) / Δb (D65) (before storage)

The rate of increase in ΔE * ab was calculated by the following formula. In the formula (D65), it is shown that the D65 light source was used.
ΔE * ab (D65) increase rate = ΔE * ab (D65) (after storage) / ΔE * ab (D65) (before storage)

Here, the improvement rate (%) of Δa * (D65) in Example 1-1 is {(increase rate of Δa * (D65) in Reference Example 1-1-Δa * (D65) in Example 1-1). (Increase rate of Δa * (D65) in Reference Example 1-1)} × 100.
The improvement rate (%) of Δa * (D65) in Comparative Example 1-1 is {(increase rate of Δa * (D65) in Reference Example 1-2-increase rate of Δa * (D65) in Comparative Example 1-1). ) / (Increase rate of Δa * (D65) in Reference Example 1-2)} × 100.
The improvement rate (%) of Δb * (D65) in Example 1-1 is {(increase rate of Δb * (D65) in Reference Example 1-1-increase rate of Δb * (D65) in Example 1-1). ) / (Increase rate of Δb * (D65) in Reference Example 1-1)} × 100.
The improvement rate (%) of Δb * (D65) in Comparative Example 1-1 is {(increase rate of Δb * (D65) in Reference Example 1-2-increase rate of Δb * (D65) in Comparative Example 1-1). ) / (Increase rate of Δb * (D65) in Reference Example 1-2)} × 100.

In the composition of Example 1-1 in which 1,3-propanediol was 30% by mass in relation to the Δa value, the addition of salicylic acid resulted in a color closer to water as compared with Reference Example 1-1. became. On the other hand, in the system in which 1,3-propanediol was 60% by mass, the color of water was different from that of Reference Example 1-2 by adding salicylic acid. In the composition of Example 1-1 in which 1,3-propanediol was 30% by mass in relation to the Δb value, the effect of suppressing coloration by salicylic acid was observed. On the other hand, in the composition of Comparative Example 1-1 in which 60% by mass of 1,3-propanediol was not observed, the coloring was deteriorated. The addition of salicylic acid further suppressed the coloration of the composition of Example 1-1. In addition, the composition of Comparative Example 1-1 was significantly inferior to the composition of Example 1-1 in all the indexes evaluated.

Here, the improvement rate (%) of ΔL * (D65) in each example is {(increase rate of ΔL * (D65) in each reference example-increase rate of ΔL * (D65) in each reference example) / each. The rate of increase of ΔL * (D65) in the reference example} × 100.
The improvement rate (%) of ΔL * (D65) in the comparative example is {(increase rate of ΔL * (D65) in the reference example-increase rate of ΔL * (D65) in the comparative example) / ΔL * (D65) in the reference example. ) Increase rate} × 100.
The improvement rate (%) of ΔE * ab (D65) is {(increase rate of ΔE * ab (D65) in each reference example-increase rate of ΔE * ab (D65) in each reference example) / ΔE in each reference example. * Increase rate of ab (D65)} × 100.
The improvement rate (%) of ΔE * ab (D65) in the comparative example is {(increase rate of ΔE * ab (D65) in the reference example-increase rate of ΔE * abD65 in the comparative example) / ΔE * ab in the reference example. (D65) increase rate} × 100.
Each reference example is a composition obtained by removing salicylic acid from the composition of each Example or Comparative Example, and refers to the composition to the left of each Example or Comparative Example in Tables 2 and 3.

In the composition of the example in which propylene glycol was 30% by mass, the effect of improving the brightness by salicylic acid was observed. On the other hand, the effect was not observed in the composition containing 60% by mass of propylene glycol. The same was true for the composition containing propanediol. The same was true even if the bases other than propylene glycol were changed.
In the composition containing 30% by mass of propylene glycol, the effect of improving the brightness by salicylic acid was observed. On the other hand, the effect was not observed in the composition of 60% by mass. The same was true for propanediol. The same was true even if the bases other than propylene glycol were changed.

Further, these effects were also observed in the composition of the example in which 1,3-propanediol and propylene glycol were mixed and used, and the total content of 1,3-propanediol and propylene glycol was 15% by mass. The effect was also confirmed in the example composition. The effect was confirmed even when polyethylene glycol was used as the base or when the amount of salicylic acid was reduced.

In each of the compositions of the examples, when compared with the standard example or the comparative example, the coloring was suppressed, the overall color taste was suppressed, and the transparency was high.

[Test Example 2: Friction improvement confirmation test]
(Coefficient of static friction)
Artificial leather (Suprale PBZ13001 (Idemitsu Technofine Co., Ltd.)) was attached to a moving table of a friction tester, and 1 mL of each composition was spread on the artificial leather so as to be sufficiently distributed under the contact. Next, a 50 g weight was attached to the measuring unit. The contactor was attached to the measuring unit, and measurement was performed 1000 times per second for 20 seconds. The average value of the friction coefficient obtained from the measurement result at the start of movement was calculated and used as the friction coefficient (μk) of the pharmaceutical product. As the contact of the friction tester (Tribomaster TL201Ts, manufactured by Trinity Lab), a "tactile contactor imitating a fingerprint pattern" was used.
Measurement conditions Weight: 50g, measurement time: 20 seconds, movement distance: 10cm, movement speed: 5mm / s, value is measured every 1msec.

Here, the friction improvement rate (%) of each Example or Comparative Example is represented by {(friction coefficient of each reference example-friction coefficient of each example or comparative example) / friction coefficient of each reference example} × 100. Ru. Each reference example is a composition obtained by removing salicylic acid from the composition of each Example or Comparative Example, and refers to the composition to the left of each Example or Comparative Example in Tables 4 to 6.

Friction was reduced by adding salicylic acid to 30% by mass of 1,3-propanediol. At 60% by mass of 1,3-propanediol, no improvement was observed and the friction increased. In addition, the coefficient of friction of Example 3-1 was lower than that of any of the standard examples or comparative examples, and it was confirmed that the composition was smooth at the beginning of application when applied to the skin.

(Dynamic friction coefficient)
The artificial leather was attached to the moving table of the friction tester, and 1 mL of the test preparation was spread on the artificial leather so as to be sufficiently distributed under the contact. Next, a 50 g weight was attached to the measuring unit. The contactor was attached to the measuring unit, and the measurement was performed 100 times per second for 20 seconds. The average value of the friction coefficient obtained from the measurement results 5 to 15 seconds after the start of measurement was calculated and used as the friction coefficient (μk) of the pharmaceutical product. As the contact of the friction tester (Tribomaster TL201Ts, manufactured by Trinity Lab), a "tactile contactor imitating a fingerprint pattern" was used.
Measurement conditions Weight: 50g, measurement time: 20 seconds, movement distance: 10cm, movement speed: 5mm / s, value is measured every 1msec.

Here, the friction improvement rate (%) of each example or comparative example is represented by {(friction coefficient of each reference example-friction coefficient of each example or comparative example) / friction coefficient of each reference example)} × 100. Will be done. Each reference example is a composition obtained by removing salicylic acid from the composition of each Example or Comparative Example, and refers to the composition to the left of each Example or Comparative Example in Table 7.

Friction was reduced by adding salicylic acid to 30% by mass of 1,3-propanediol. At 60% by mass of 1,3-propanediol, no improvement was observed and the friction increased. In addition, the coefficient of friction of Example 4-1 was lower than that of any of the standard examples or comparative examples, and it was confirmed that the composition was smooth when applied to the skin.

[Prescription example]
Examples of prescriptions are shown in Tables 8 and 9 below. The prescription examples are all beauty essences, and the content in each of the prescription examples is mass%.

Claims

At least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid, (B) at least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C). A composition for external use on the skin containing 1 to 50% by mass of a diol having 3 carbon atoms.
The composition for external use on the skin according to claim 1, wherein the concentration of the component (A) is 1 to 10% by mass.
The composition for external use on the skin according to claim 1 or 2, wherein the concentration of the component (B) is 0.001 to 2% by mass.
The composition for external use on the skin according to any one of claims 1 to 3, further comprising (D) 1 to 15% by mass of water.
The composition for external use on the skin according to any one of claims 1 to 4, further comprising (E) 1 to 20% by mass of a lower alcohol.
The composition for external use on the skin according to any one of claims 1 to 5, which has a pH of 2 to 5.
At least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid, (B) at least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C). A method for suppressing coloration of an external composition for skin containing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid by blending 1 to 50% by mass of a diol having 3 carbon atoms.
(B) at least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C) ascorbic acid and (A) ascorbic acid containing 1 to 50% by mass of a diol having 3 carbon atoms. A color inhibitor for an external skin composition containing at least one selected from the group consisting of salts of ascorbic acid.
At least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid, (B) at least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C). Improving the usability of the composition for external use on the skin containing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid by using 1 to 50% by mass of a diol having 3 carbon atoms. how to.
(B) at least one selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C) ascorbic acid and (A) ascorbic acid containing 1 to 50% by mass of a diol having 3 carbon atoms. A usability-enhancing agent for a composition containing at least one selected from the group consisting of salts of ascorbic acid.