CN115697294A

CN115697294A - Skin external composition containing ascorbic acid and/or its salt

Info

Publication number: CN115697294A
Application number: CN202180042513.7A
Authority: CN
Inventors: 安藤达也; 桝本爱; 中田大贵
Original assignee: Rohto Pharmaceutical Co Ltd
Current assignee: Rohto Pharmaceutical Co Ltd
Priority date: 2020-06-19
Filing date: 2021-06-18
Publication date: 2023-02-03
Also published as: JPWO2021256566A1; TW202203895A; WO2021256566A1

Abstract

The invention provides a skin external composition with excellent use feeling and appearance. The purpose of the present invention is to provide a composition for external application to the skin, which has a good feeling in use, that is, which has good lubrication and is inhibited from coloring. The present invention prepares a composition for external application to the skin, comprising: 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) 1 to 50% by mass of a diol having 3 carbon atoms.

Description

Skin external composition containing ascorbic acid and/or its salt

Technical Field

The present invention relates to a composition for external application to the skin, which contains ascorbic acid and/or a salt thereof.

Background

Ascorbic acid is known to exhibit various effects such as an anti-inflammatory effect, an acne improvement effect, a whitening effect, an anti-aging effect, an antioxidant effect, a cell activation effect by promoting the synthesis of a biological component such as collagen, and an effect of inhibiting cell damage or DNA damage of epidermal keratinocytes due to ultraviolet rays, and is expected to be used as an external preparation for skin. A technique for improving the stability of ascorbic acid has been proposed (for example, patent document 1).

Documents of the prior art

Patent document

Patent document 1: japanese patent laid-open No. 2005-225865

Disclosure of Invention

The invention aims to provide an ascorbic acid-containing composition for external application to the skin, which has a good feel in use and a good appearance.

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

The present inventors have conducted extensive studies to solve the problem, and as a result, have found that a composition for external application to the skin excellent in feeling of use and appearance can be obtained by containing (a) at least one selected from ascorbic acid and a salt of ascorbic acid, (B) at least one selected from 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, and have completed the present invention.

Namely, the present invention provides the following disclosed compositions for external application to the skin.

An external composition for skin comprising: at least one selected from ascorbic acid and a salt of ascorbic acid, (B) at least one selected from 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.

The composition for external application to skin according to item 1, wherein the concentration of the component (A) is 1 to 10% by mass.

The composition for external application to skin according to item 1 or 2, wherein the concentration of the component (B) is 0.001 to 2% by mass.

The composition for external skin application according to any one of claims 1 to 3, further comprising (D) water in an amount of 1 to 15% by mass.

The composition for external application to skin according to any one of claims 1 to 4, further comprising (E) a lower alcohol in an amount of 1 to 20% by mass.

The composition for external skin application according to any one of claims 1 to 5, wherein the pH is from 2 to 5.

Further, the present invention provides a method for the following composition for external application to the skin.

Item 7. A method for suppressing coloring of a composition for external application to skin, comprising (a) at least one member selected from the group consisting of ascorbic acid and a salt of ascorbic acid, wherein the coloring of the composition for external application to skin is suppressed by blending (a) at least one member selected from the group consisting of ascorbic acid and a salt of ascorbic acid, (B) at least one member 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 coloring inhibitor for a composition containing (a) at least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid, comprising: (B) At least one selected from 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.

Item 9. A method for imparting a feeling of use to a composition for external application to skin containing (a) at least one member selected from the group consisting of ascorbic acid and a salt of ascorbic acid, the composition for external application to skin being imparted with a feeling of use by using (a) at least one member selected from the group consisting of ascorbic acid and a salt of ascorbic acid, (B) at least one member 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.

An agent for improving sensation in use comprising (a) at least one member selected from the group consisting of ascorbic acid and salts of ascorbic acid, comprising: (B) At least one selected from 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.

According to the present invention, a composition for external application to the skin, which is excellent in feeling of use and appearance, can be provided.

Detailed Description

In the present specification, the unit of the content "% by mass" is the same as the meaning of "g/100 g".

[ composition for external application to the skin ]

The composition for external application to the skin of the present invention comprises:

(A) At least one selected from ascorbic acid and salts of ascorbic acid,

(B) At least one selected from 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) at least one selected from ascorbic acid and salts of ascorbic acid)

As the ascorbic acid used in the present invention, there can be used commercially available ascorbic acid as a component of a skin external preparation in the fields of pharmaceuticals, quasi drugs, and cosmetics, and these are not limited, and refer to L-form ascorbic acid in general.

Salts of ascorbic acid may also be used. Here, the salt of ascorbic acid means a pharmaceutically acceptable salt. Examples of the salt include, but are not limited to, salts with organic bases (for example, salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, and pyridine salt, basic ammonium salts such as arginine salt), salts with inorganic bases (for example, alkali metal salts such as ammonium salt, sodium salt, and potassium salt, alkaline earth metal salts such as calcium salt and magnesium salt, and aluminum salt). Preferred salts of ascorbic acid are sodium and potassium salts.

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

In the composition for external application to skin of the present invention, the total content of the component (a) relative to the total amount of the composition for external application to skin can be appropriately set in accordance with the balance with other components.

The total content of the component (a) is preferably 20% by mass or less, more preferably 10% by mass or less, further preferably 7% by mass or less, and further more preferably 5% by mass or less, relative to the total amount of the composition for external application to the skin. The total content of the component (a) is preferably 0.5% by mass or more, more preferably 1% by mass or more, further preferably 2% by mass or more, and further more preferably 3% by mass or more, relative to the total amount of the composition for external application to the skin. The total content of component (a) is preferably 0.5 to 20% by mass, more preferably 1 to 10% by mass, even more preferably 2 to 9% by mass, and even more preferably 3 to 5% by mass, based on the total amount of the composition for external application to the skin.

(B) at least one member selected from the group consisting of salicylic acid, a salt of salicylic acid and a derivative of salicylic acid)

The salicylic acid or salicylic acid derivative used in the present invention is not particularly limited as long as it is used as a component for external skin preparations in the fields of pharmaceuticals, quasi drugs, and cosmetics.

Salts of salicylic acid may also be used. Here, the salt of salicylic acid means a pharmaceutically acceptable salt. Examples of the salt include, but are not limited to, alkali metal salts, alkaline earth metal salts, and salts with organic bases. Examples of the salicylate include at least one selected from 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 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 salicylic acid derivative may be used as the component (B). Examples of such salicylic acid derivatives include, but are not limited to, ethylene glycol salicylate, phenyl salicylate, methyl salicylate, 2-ethylhexyl salicylate, dipropylene glycol salicylate, and titanium salicylate. (B) Salicylic acid, a salt of salicylic acid, or a derivative of salicylic acid may be used as synthesized, or a commercially available product may be used.

In the composition for external application to skin of the present invention, the total content of the component (B) is not limited, but is preferably 0.001% by mass or more, more preferably 0.005% by mass or more, further preferably 0.01% by mass or more, and further more preferably 0.05% by mass or more, relative to the total amount of the composition for external application to skin.

The total content of the component (B) is not limited, but is preferably 5% by mass or less, more preferably 2% by mass or less, further preferably 1% by mass or less, and further more preferably 0.5% by mass or less, relative to the total amount of the composition for external application to the skin.

The total content of the component (B) is preferably 0.001 to 5% by mass, more preferably 0.005 to 2% by mass, even more preferably 0.01 to 1% by mass, and even more preferably 0.05 to 0.5% by mass, based on the total amount of the composition for external application to the skin. In addition, the amount may be 0.001 to 5 mass%, 0.01 to 4 mass%, 0.1 to 3 mass%, 0.5 to 2 mass%, or the like, based on the use for acne medication.

The ratio of the component (B) to the amount of the component (a) to be blended in the composition for external application to the skin of the present invention is not particularly limited, and is preferably 0.0002 to 10 parts by mass, more preferably 0.001 to 1 part by mass, further preferably 0.005 to 0.25 parts by mass, and further more preferably 0.01 to 0.2 parts by mass, based on 1 part by mass of the total content of the component (a).

((C) 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 a component used as an external skin preparation in the fields of pharmaceuticals, quasi drugs, and cosmetics. In addition, such a diol having 3 carbon atoms may be used as it is as a commercially available product. Examples of the diol having 3 carbon atoms include, but are not limited to, 1, 3-propanediol (CAS number: 504-63-2, english name: 1, 3-Dihydroxypropionane or TrimethyleneGlycol) and propylene glycol (CAS number: 57-55-6, english name: 1, 2-Dihydroxypropionane, chinese name: 1, 2-propanediol), and one of them may be used or a combination of them may be used as appropriate. From the viewpoint of reducing irritation to the skin, improving the feeling of use, and suppressing coloring, it is also one of preferable embodiments to combine 1, 3-propanediol and propylene glycol, and it is more preferable to contain at least 1, 3-propanediol as the component (C).

In the composition for external application to skin of the present invention, the total content of the component (C) is 1% by mass or more, preferably 5% by mass or more, and more preferably 10% by mass or more, relative to the total amount of the composition for external application to skin.

The total content of component (C) is 50% by mass or less, preferably 40% by mass or less, and more preferably 30% by mass or less, relative to the total amount of the composition for external application to the skin.

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

In the composition for external application to the skin of the present invention, the ratio of the component (C) to the amount of the component (a) is not particularly limited, but is preferably 0.05 to 100 parts by mass, more preferably 0.5 to 40 parts by mass, and still more preferably 1 to 15 parts by mass, based on 1 part by mass of the total content of the component (a).

(C) The amount of propylene glycol in the component (a) is 0.1% by mass or more, preferably 0.5% by mass or more, more preferably 1% by mass or more, further preferably 5% by mass or more, and further more preferably 10% by mass or more, based on the total amount of the composition for external application to the skin. The amount of propylene glycol to be blended is preferably 50% by mass or less and 40% by mass or less, more preferably 30% by mass or less, still more preferably 20% by mass or less, and still more preferably 10% by mass or less.

The total content of propylene glycol 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 10 to 20% by mass, based on the total amount of the composition for external application to the skin.

In the composition for external application to the skin of the present invention, the ratio of the amount of propylene glycol blended with respect to the component (a) is not particularly limited, but is preferably 0.05 to 80 parts by mass, more preferably 0.5 to 30 parts by mass, and still more preferably 1 to 10 parts by mass, based on 1 part by mass of the total content of the component (a).

(C) The amount of 1, 3-propanediol to be incorporated in the component (a) is 0.1% by mass or more, preferably 0.5% by mass or more, more preferably 1% by mass or more, more preferably 5% by mass or more, and still more preferably 10% by mass or more, based on the total amount of the composition for external application to the skin. The amount of 1, 3-propanediol to be blended is 50 mass% or less, 40 mass% or less, 30 mass% or less, more preferably 25 mass% or less, still more preferably 20 mass% or less, and still more preferably 15 mass% or less.

The total content of 1, 3-propanediol is 0.1 to 50% by mass, 0.5 to 40% by mass, 1 to 30% by mass, preferably 5 to 20% by mass, and more preferably 10 to 15% by mass, based on the total amount of the composition for external application to the skin.

In the composition for external application to the skin of the present invention, the ratio of the amount of 1, 3-propanediol blended with component (a) is not particularly limited, but is preferably 0.05 to 60 parts by mass, more preferably 0.5 to 20 parts by mass, and still more preferably 1 to 7.5 parts by mass, based on 1 part by mass of the total content of component (a).

In the composition for external application to the skin of the present invention, as the component (C), propylene glycol and 1, 3-propanediol may be blended. In this case, the total amount of propylene glycol and 1, 3-propanediol may be 10 mass% or more, 15 mass% or more, 20 mass% or more, 25 mass% or more, or 30 mass% or more, and may be 50 mass% or less, 45 mass% or less, 40 mass% or less, or 35 mass% or less.

The total amount of propylene glycol and 1, 3-propanediol may be 10 to 50 mass%, 15 to 45 mass%, 20 to 40 mass%, or 25 to 35 mass% based on the total amount of the composition for external application to the skin.

When propylene glycol and 1, 3-propanediol are both blended, they may be 5 to 25% by mass, 5 to 20% by mass, 5 to 15% by mass, 10 to 25% by mass, 10 to 20% by mass, 10 to 15% by mass, 15 to 25% by mass, 15 to 20% by mass, or the like, respectively.

The composition for external skin application of the present invention may contain (D) water and/or (E) a lower alcohol in addition to the above-mentioned component (a), (B) and (C) as long as the effects of the present invention are not impaired.

((D) Water)

The composition for external application to the skin of the present invention may be a composition containing water. The water content is not limited, and the water content is preferably 0.1 to 30% by mass, more preferably 1 to 20% by mass, and still more preferably 2 to 15% by mass, based on the total amount of the composition for external application to the skin.

In the composition for external application to the skin of the present invention, the ratio of the component (D) to the component (a) is preferably 0.005 to 60 parts by mass, more preferably 0.1 to 20 parts by mass, and still more preferably 0.2 to 7.5 parts by mass, based on 1 part by mass of the total content of the component (a).

((E) lower alcohol)

The composition for external application to the skin of the present invention may also contain a lower alcohol. The lower alcohol used in the present invention is not particularly limited as long as it is a component used as an external preparation for skin in the fields of pharmaceuticals, quasi drugs, and cosmetics. In this specification, reference to "lower alcohol" means a C1-C6 alcohol. Among them, C1-C3 alcohols are particularly preferably used. Examples of such a solvent include methanol, ethanol, n-propanol, and isopropanol, and among these, ethanol is preferred.

When the composition for external application to the skin of the present invention contains the component (E), the total content of the component (E) is preferably 0.1 to 40% by mass, more preferably 0.5 to 10% by mass, and still more preferably 1 to 7% by mass, based on the total amount of the composition for external application to the skin.

In the composition for external application to skin of the present invention, the amount of ethanol is typically preferably 1 to 40% by mass, more preferably 2 to 30% by mass, and still more preferably 3 to 20% by mass, based on the total amount of the composition for external application to skin.

In the composition for external application to the skin of the present invention, the ratio of the amount of component (E) to component (a) is preferably 0.005 to 80 parts by mass, more preferably 0.05 to 10 parts by mass, and still more preferably 0.1 to 3.5 parts by mass, based on 1 part by mass of the total content of component (a).

(polyhydric alcohol)

The composition for external application to 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 a component used as an external skin preparation in the fields of pharmaceuticals, quasi drugs, and cosmetics. The polyhydric alcohol is not limited, but may be added for the purpose of moisture retention or as a solubilizer. Specific examples thereof include glycerin, diglycerin, dipropylene glycol, 1, 3-butanediol, and 3-methyl-1, 3-butanediol.

When the polyol other than component (C) is contained, the total content of the polyol other than component (C) is preferably from 0.1 to 60% by mass, more preferably from 1 to 50% by mass, and still more preferably from 10 to 45% by mass, based on the total amount of the composition for external skin application of the present invention.

(vitamin E)

The composition for external application to the skin of the present invention may contain tocopherol, a tocopherol salt, a tocopherol derivative, and other vitamin E compounds in addition to the component (a), (B), and (C) as described above, as long as the effects of the present invention are not impaired. As the tocopherol, the salt of the tocopherol, the derivative of the tocopherol, and the like used in the present invention, a compound generally used as a component of a skin external preparation in the fields of pharmaceuticals, quasi drugs, or cosmetics can be used, and may be any of d-, l-, or dl-isomer, or may be any of α, β, γ, or δ structures. Examples of the tocopherol include d- α -tocopherol, d- β -tocopherol, d- γ -tocopherol, d- δ -tocopherol, l- α -tocopherol, l- β -tocopherol, l- γ -tocopherol, l- δ -tocopherol, dl- α -tocopherol, dl- β -tocopherol, dl- γ -tocopherol, and dl- δ -tocopherol, which are mixtures thereof. The derivative of tocopherol is not limited, but is preferably an ester of tocopherol. In addition, as the tocopherol derivative, in particular, one selected from tocopherol acetate, tocopherol nicotinate or a salt thereof, tocopherol succinate or a salt thereof, tocopherol linolenate, tocopherol phosphate or a salt thereof, tocopherol (linolenic acid/oleic acid) ester, and tocotrienol, and the like can be exemplified.

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

(ascorbic acid derivative)

The composition for external application to skin of the present invention may contain an ascorbic acid derivative in addition to the above-mentioned component (a), (B) and (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-ethyl ascorbic acid, L-ascorbic acid 2-glucoside, dehydroascorbic acid, sodium ascorbyl phosphate, magnesium ascorbyl phosphate, sodium ascorbyl monophosphate, sodium ascorbyl diphosphate, sodium ascorbyl triphosphate, sodium ascorbyl-2-sulfate, and salts thereof.

Salt refers to pharmaceutically acceptable salts. Examples of the salt include, but are not limited to, salts with organic bases (for example, salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, and pyridine salt, and basic ammonium salts such as arginine), salts with inorganic bases (for example, alkali metal salts such as ammonium salt, sodium salt, and potassium salt, alkaline earth metal salts such as calcium salt and magnesium salt, and aluminum salt). Particularly preferred salts of 3-O-ethyl ascorbic acid are sodium salts and potassium salts.

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

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

(surfactant)

The composition for external application to the skin of the present invention may contain a surfactant as long as the effect of the present invention is not impaired. When the surfactant is contained, although not limited thereto, a nonionic surfactant is preferable, for example, polyoxyethylene hydrogenated castor oil 40, polyoxyethylene hydrogenated castor oil 60, polyoxyethylene hydrogenated castor oil 80, polyoxyethylene polyoxypropylene decyltetradecyl ether, polyoxyethylene (20) polyoxypropylene (4) cetyl ether, polyoxyethylene (10) polyoxypropylene (4) cetyl ether, polyoxyethylene (10) oleyl ether, polyoxyethylene stearyl ether, polyoxyethylene isopropyl ether, PEG-8 glyceryl isostearate, polyoxyethylene sorbitan monolaurate (20E.O.), polyoxyethylene sorbitan isostearate (20E.O.), polyoxyethylene sorbitan stearate (20E.O.), coconut oil fatty acid polyglycerin-10 ester, coconut oil polyglycerin-3 ester, coconut oil fatty acid PEG-7 glyceride, polyglycerin-10 dioleate, polyglycerin-10 diisostearate, triisostearic acid PEG-40 glyceride, isostearic acid PEG-40 glyceride, polyglycerin-10 trioleate, polyglycerin-10 triglyceride, polyglycerin myristate, caprylic acid triglyceride, polyoxyethylene caprylic acid monoglyceride, polyoxyethylene lauryl ether, etc., particularly preferred are polyoxyethylene polyoxypropylene decyltetradecyl ether, polyoxyethylene hydrogenated castor oil 40, polyoxyethylene hydrogenated castor oil 60, polyoxyethylene hydrogenated castor oil 80, polyoxyethylene sorbitan isostearate (20E.O.), polyoxyethylene sorbitan monolaurate (20E.O.), polyglycerol laurate.

In the composition for external application to skin of the present invention, the total content of the surfactant relative to the total amount of the composition for external application to skin is appropriately set in accordance with the balance with other ingredients. The total content of the surfactant is preferably 0.001 to 10% by mass, more preferably 0.005 to 7% by mass, and still more preferably 0.01 to 5% by mass, based on the total amount of the composition for external application to the skin.

(other Components)

The composition for external application to the skin of the present invention may further comprise, in addition to the above-mentioned component (a), (B) and (C), one or two or more of various components such as a whitening component, an anti-inflammatory component, an antibacterial component, a cell-activating component, an astringent component, an antioxidant component, an acne-improving component, an anti-aging component, a biological component synthesis-promoting component such as collagen, a blood circulation-promoting component, a moisturizing component, an anti-aging component and the like, or a combination thereof, in order to enhance or supplement various actions of ascorbic acid and to add other useful actions. Preferably one or more of whitening component, antiinflammatory component, antibacterial component, cell activating component, astringent component, antioxidant component, antiaging component or moisturizing component. As a particularly preferable combination of these components, a combination with a whitening component and an antioxidant component, a combination with each antioxidant component, a combination with an anti-aging component, and a combination with each whitening component and anti-aging component can be given. The components are not particularly limited as long as they are conventionally used as components for external skin preparations in the fields of pharmaceuticals, quasi drugs, and cosmetics, or they are used in the future, and any component can be appropriately selected and used. Among these, isopropyl methylphenol as a bactericidal ingredient and/or dipotassium glycyrrhizinate as an anti-inflammatory ingredient can be particularly preferably used.

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

The composition for external application to the skin of the present invention may contain, as necessary, various components that are generally used as components for external application in the fields of pharmaceuticals, quasi drugs, and cosmetics, such as amino acids, irritation reducing agents, thickening agents, preservatives, ultraviolet ray protective agents, coloring agents, dispersants, additional pH adjusting agents, and perfumes, in such an amount and quality that the stability of appearance, the viscosity, and other qualities are not impaired, and the effects of the present invention are not impaired. These components may be blended singly or in any combination of two or more.

(form)

The composition for external application to the skin of the present invention can be prepared in various desired forms such as a paste, mousse, gel, liquid, emulsion, cream, sheet (substrate-supported), aerosol, spray, and the like by blending and mixing the component (a), the component (B), the component (C), and optionally the above-mentioned optional components, and further optionally blending other solvents, bases for external preparations, and the like. These can be produced by a method generally used in the art.

The composition for external application to the skin of the present invention is particularly preferably a transparent or translucent composition in which ascorbic acid and/or a salt thereof has been solubilized. Here, "solubilization" is as defined. That is, for example, the transmittance is in the range of 80% to 100%, preferably 85% to 100%, more preferably 90% to 100% in terms of transmittance at a wavelength of 700nm by an ultraviolet-visible absorbance measurement method using a spectrophotometer UV-2450 (manufactured by Shimadzu corporation) or a photoelectric photometer. The water permeability is defined herein as 100%. The solubilizing compositions of the present invention have a transparent or translucent appearance. More specifically, the method for measuring the transmittance is based on the method described in the 16 th revision of the general test method 2 of the Japanese pharmacopoeia [ B ], the spectroscopic measurement method by physical test method 2.24, the ultraviolet-visible absorbance measurement method.

(viscosity)

The composition for external application to the skin of the present invention can be prepared to have a suitable viscosity which is desirable for use of the composition for external application to the skin. The viscosity of the composition for external application to the skin of the present invention is not particularly limited, and for example, the viscosity when measured at 25 ℃ with an E-type viscometer is usually about 1 to 300mPa · s, preferably about 1 to 200mPa · s, more preferably about 1 to 100mPa · s, and most preferably about 1 to 50mPa · s. More specifically, the method of measuring the viscosity is based on the method described in the 16 th revised Japanese pharmacopoeia [ B ] general test method 2, physical test method, other physical test method 2.53 method of measuring the viscosity 2, second method rotational viscometer method 2.1.3 cone-plate rotational viscometer (cone-plate viscometer).

(pH)

The composition for external application to the skin of the present invention may generally have a liquid property of pH1 to pH8, but from the viewpoint of stability of ascorbic acid, low irritation to the skin or mucous membrane, and good feeling of use on the skin, it is preferably pH2 to pH7, more preferably pH2 to pH6, even more preferably pH2 to pH5.0, and most preferably pH2 to pH4.5. Preferably an acidic region.

(use)

The composition for external application to the skin of the present invention is effective particularly as a whitening agent, an anti-inflammatory agent, and an anti-aging agent, and has, for example, an anti-acne or anti-oxidation effect. Further, depending on the application to the skin, the effects of improving the skin transparency, keeping moisture, adjusting the skin texture, and suppressing roughness may be exhibited. Furthermore, the skin may have effects of moisturizing skin concerned with acne scars or pores, making pores inconspicuous, smoothing skin, and moisturizing skin, and may be used for preventing or treating spots.

The composition for external application to the skin of the present invention can be prepared into various compositions for external application to the skin, which are in the fields of cosmetics, external pharmaceuticals for external use or quasi drugs for external use, such as basic cosmetic materials for beauty lotion, astringent, sunscreen cream, milky lotion, cream, lotion, oil and pack, color cosmetic materials for foundation, lipstick, mascara, eye shadow, eyeliner, eyebrow and nail polish, cleansing agents for cleansing milk, makeup remover, body cleansing agents, and the like, and anti-bromhidrosis agents, beriberi remedies, antipruritic agents, wound healing agents, cleansing agents, anti-inflammatory analgesics, acne remedies, hemorrhoid remedies, bactericidal disinfectants, whitening agents, ultraviolet ray preventives, and the like. The present invention is preferably used for products to be applied to the outer skin, such as skin external preparations (preparations for outer skin) from the viewpoint of the action and effect on the skin. The composition of the present invention can be used in a known or customary manner and amount of the composition, depending on the intended use and the like, once to several times a day.

[ method of inhibiting coloring ]

In addition, the present invention also includes a method for inhibiting coloration of a composition for external application to the skin, which contains (a) at least one member selected from the group consisting of ascorbic acid and a salt of ascorbic acid. According to the method for suppressing coloring of the present invention, a stable preparation in which coloring is suppressed while containing ascorbic acid can be obtained by containing (a) at least one selected from ascorbic acid and a salt of ascorbic acid, (B) at least one selected from 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. That is, the present invention relates to a method for suppressing coloring of a composition for external application to skin, which contains (a) at least one selected from ascorbic acid and a salt of ascorbic acid, wherein the coloring of the composition for external application to skin is suppressed by containing (a) at least one selected from ascorbic acid and a salt of ascorbic acid, (B) at least one selected from 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. The term "suppression of coloring" as used herein is not limited, and means, for example, suppression of coloring (including improvement of transparency) by ascorbic acid during storage. By such suppression of coloring, the composition for external application to skin of the present invention has a good appearance. Further, the good appearance due to such suppression of coloring includes, for example, that the composition does not stick to clothes or the like.

The coloring suppression of the present invention is similar to that used in the skin external composition, for example, in that the composition contains (a) at least one selected from ascorbic acid and a salt of ascorbic acid, (B) at least one selected from salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C) 1 to 50 mass% of a glycol having 3 carbon atoms.

[ coloration inhibitor ]

The present invention also comprises a coloring inhibitor for a skin external composition containing (a) at least one selected from ascorbic acid and a salt of ascorbic acid. The coloring inhibitor of the present invention is a coloring inhibitor for a skin external composition containing (a) at least one selected from ascorbic acid and a salt of ascorbic acid, comprising: (B) At least one selected from 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.

The coloring inhibitor of the present invention is prepared into a composition for external application to the skin containing (a) at least one selected from ascorbic acid and a salt of ascorbic acid, (B) at least one selected from 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, or the content thereof, and the like, as in the composition for external application to the skin.

[ method for improving feeling in use ]

The present invention also encompasses a method for improving the feeling of use of a composition for external application to the skin, which contains (a) at least one member selected from the group consisting of ascorbic acid and a salt of ascorbic acid. According to the method for improving a feeling of use of the present invention, a favorable feeling of use can be obtained by containing (a) at least one selected from ascorbic acid and a salt of ascorbic acid, (B) at least one selected from 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. That is, the present invention relates to a method for imparting a good feeling of use to a composition for external application to skin containing (a) at least one member selected from the group consisting of ascorbic acid and a salt of ascorbic acid, wherein the composition for external application to skin contains (a) at least one member selected from the group consisting of ascorbic acid and a salt of ascorbic acid, (B) at least one member selected from the group consisting of salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C) 1 to 50 mass% of a glycol having 3 carbon atoms. Here, the feeling of use is not limited, but means, for example, less friction, smooth feeling of application, and the like.

In the method for improving a feeling of use of the present invention, the skin external composition containing (a) at least one selected from ascorbic acid and a salt of ascorbic acid, (B) at least one selected from salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C) 1 to 50% by mass of a glycol having 3 carbon atoms, or the content thereof, is prepared in the same manner as in the above-mentioned skin external composition.

[ feeling-of-use improver ]

The present invention also comprises a feeling-of-use enhancer for a skin external composition containing (a) at least one selected from ascorbic acid and a salt of ascorbic acid. The use feeling improving agent of the present invention is a use feeling improving agent of a skin external composition containing (a) at least one selected from ascorbic acid and a salt of ascorbic acid, and contains: (B) At least one selected from 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.

The feeling of use enhancing agent of the present invention is prepared as in the case of the composition for external application to the skin containing (a) at least one selected from ascorbic acid and a salt of ascorbic acid, (B) at least one selected from salicylic acid, a salt of salicylic acid, and a derivative of salicylic acid, and (C) 1 to 50% by mass of a glycol having 3 carbon atoms, or the content thereof.

Examples

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

Skin external compositions having the compositions shown in tables 1 to 4 were prepared according to a conventional method.

[ test example 1: ascorbic acid coloration inhibition confirmation test

The compositions of the reference examples, comparative examples and examples were evaluated for the presence or absence of coloration after storage at 60 ℃ by visual observation and a color difference meter. Specifically, the compositions were prepared by mixing and dissolving the respective ingredients according to the formulations described in the tables. 10mL of the prepared composition was filled in a 20mL screw bottle and allowed to stand in a thermostat at 60 ℃ for 5 days. After 5 days in the measurement period, the screw bottle was taken out from the thermostat, and the temperature was maintained at 25 ℃ for evaluation. Each composition was subjected to measurement to determine the presence or absence and degree of coloring.

Measurement the L value, a value and b value of the CIELAB color system were measured at 25 ℃ by using a spectrocolorimeter CM-5 (manufactured by Konikameonta corporation) and 2.5mL of the test solution in a glass cuvette (CM-A97, thickness: 2 mm). The measurement value used was Δ L Δ a Δ b when the purified water was set as a blank.

The L value (Δ L) is a value related to luminance, a value (Δ a) is a value related to the bidirectional relationship between red and green, and b value (Δ b) is a value related to the bidirectional relationship between yellow and blue.

Δ E ab is represented by the following formula, and is an index showing the overall coloring degree of the compositions of examples and comparative examples.

ΔE*ab＝{(ΔL*) ² +(Δa*) ² +(Δb*) ² } ^1/2

The Δ L increase rate was obtained by the following equation.

Δ L increase = Δ L (D65) (post-storage)/Δ L (D65) (pre-storage)

The Δ a increase rate is obtained by the following equation.

Δ a increase rate = Δ a (D65) (after storage)/Δ a (D65) (before storage)

The Δ b increase rate was obtained by the following equation.

Δ b increase rate = Δ b (D65) (after storage)/Δ b (D65) (before storage)

The Δ E ab increase rate was obtained by the following equation. In the formula, (D65) represents that a D65 light source is used.

Δ Ε ab (D65) increase = Δ Ε ab (D65) (post-storage)/Δ Ε ab (D65) (pre-storage)

[ Table 1]

Here, the improvement rate (%) of Δ a (D65) in example 1-1 is represented by { (increase rate of Δ a (D65) in reference example 1-increase rate of Δ a (D65) in example 1-1)/(increase rate of Δ a (D65) in reference example 1-1) } × 100.

The improvement rate (%) of Δ a (D65) in comparative example 1-1 is represented by { (increase rate of Δ a (D65) in reference example 1-2-increase rate of Δ a (D65) in comparative example 1-1)/(increase rate of Δ a (D65) in reference example 1-2) } × 100.

The improvement rate (%) of Δ b (D65) in example 1-1 is represented by { (increase rate of Δ b (D65) in reference example 1-increase rate of Δ b (D65) in example 1-1)/(increase rate of Δ b (D65) in reference example 1-1) } × 100.

The improvement rate (%) of Δ b (D65) in comparative example 1-1 is represented by { (increase rate of Δ b (D65) in reference example 1-2-increase rate of Δ b (D65) in comparative example 1-1)/(increase rate of Δ b (D65) in reference example 1-2) } × 100.

Regarding the Δ a value, the composition of example 1-1 in which 1, 3-propanediol was 30 mass% had a color tone close to that of water by adding salicylic acid as compared with that of reference example 1-1. On the other hand, in a system containing 60% by mass of 1, 3-propanediol, the color tone of water was deviated from that of reference example 1-2 by adding salicylic acid. Regarding the Δ b value, the coloring-suppressing effect by salicylic acid was observed in the composition of example 1-1 in which 1, 3-propanediol was 30 mass%. On the other hand, the composition of comparative example 1-1, in which 1, 3-propanediol was 60 mass%, exhibited no coloration-inhibiting effect and was poor. The composition of example 1-1 was further inhibited from coloring by the addition of salicylic acid. In addition, the composition of comparative example 1-1 was significantly deteriorated in all the indexes evaluated as compared with the composition of example 1-1.

[ Table 2]

[ Table 3]

Here, the improvement rate (%) of Δ L (D65) in each example is represented by { (increase rate of Δ L (D65) in each reference example — increase rate of Δ L (D65) in each example)/increase rate of Δ L (D65) in each reference example } × 100.

The improvement rate (%) of Δ L (D65) in the comparative example is represented by { (increase rate of Δ L (D65) in the reference example-increase rate of Δ L (D65) in the comparative example)/increase rate of Δ L (D65) in the reference example } × 100.

The improvement rate (%) of Δ E × ab (D65) is represented by { (increase rate of Δ E × ab (D65) in each reference example — increase rate of Δ E × ab (D65) in each example)/increase rate of Δ E × ab (D65) in each reference example } × 100.

The improvement rate (%) of Δ E ab (D65) in the comparative example is represented by { (increase rate of Δ E ab (D65) in the reference example — increase rate of Δ E abD 65) in the comparative example)/increase rate of Δ E ab (D65) in the reference example } × 100.

Each reference example is a composition in which salicylic acid was removed from the composition of each example or comparative example, and in tables 2 and 3, the composition on the left of each example or comparative example is referred to.

The effect of improving the brightness by salicylic acid was observed in the composition of the example containing 30% by mass of propylene glycol. On the other hand, this effect was not observed in the composition containing 60% by mass of propylene glycol. The same applies to compositions containing propylene glycol. The same applies to the case where a base other than propylene glycol is used.

The effect of improving the brightness by salicylic acid was observed in the composition containing 30% by mass of propylene glycol. On the other hand, this effect was not observed in the composition of 60% by mass. The same applies to propylene glycol. The same applies to the case where a base other than propylene glycol is used.

These effects were also observed in the compositions of examples in which 1, 3-propanediol was used in combination with propylene glycol, and the effects were also observed in the compositions of examples in which the total content of 1, 3-propanediol and propylene glycol was 15 mass%. The effect was also confirmed in the case of using polyethylene glycol as a base or in the case of reducing the amount of salicylic acid to be blended.

When the compositions of examples were compared with those of the reference examples or comparative examples, coloration was suppressed, the overall hue was suppressed, and transparency was high.

[ test example 2: confirmation test for improvement in Friction

(coefficient of static Friction)

Artificial leather (supare PBZ13001 (precision optical technology corporation)) was attached to a moving stage of a friction-sensing tester, and 1mL of each composition was spread over the artificial leather so as to spread over the contact. Next, a 50g weight was attached to the measuring unit. The contact was attached to a measuring unit, and measurement was performed 1000 times every 1 second for 20 seconds. The average value of the friction coefficients obtained from the measurement results at the start of the operation was calculated as the friction coefficient (μ k) of the formulation. As a contact of a friction sensing tester (Tribomaster TL201Ts, manufactured by Trinity Labo corporation), "a touch contact which imitates a fingerprint pattern" is used.

The measurement conditions were hammer: 50g, measurement time: 20 seconds, travel distance: 10cm, moving speed: 5mm/s, measured every 1 msec.

[ Table 4]

[ Table 5]

[ Table 6]

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. Each reference example is a composition obtained by removing salicylic acid from the composition of each example or comparative example, and tables 4 to 6 show the composition on the left of each example or comparative example.

If salicylic acid is added to 30 mass% of 1, 3-propanediol, the friction becomes small. When the 1, 3-propanediol content is 60% by mass, no improvement is observed, and the friction increases. In addition, the friction coefficient of example 3-1 was lower than that of either the reference example or the comparative example, and it was confirmed that the composition was smooth at the start of application when applied to the skin.

These effects were also observed in the compositions of examples in which 1, 3-propanediol was used in combination with propylene glycol, and the effects were also observed in the compositions of examples in which the total content of 1, 3-propanediol and propylene glycol was 15 mass%. The effect was also confirmed when polyethylene glycol was used as a base or when the amount of salicylic acid added was reduced.

(coefficient of dynamic Friction)

The artificial leather was attached to the moving stage of the friction sensing tester, and 1mL of the test formulation was spread over the artificial leather so as to be spread over the contact piece. Subsequently, a 50g hammer was attached to the measuring unit. The contact was attached to a measuring unit, and measurement was performed 1000 times per 1 second for 20 seconds. The average value of the friction coefficients obtained from the measurement results 5 to 15 seconds after the start of the measurement was calculated as the friction coefficient (μ k) of the formulation. Note that as the contact of the friction sensing tester (Tribomaster TL201Ts, manufactured by Trinity Labo corporation), "a tactile contact imitating a fingerprint pattern" is used.

[ Table 7]

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. Each reference example is a composition in which salicylic acid was removed from the composition of each example or comparative example, and the composition on the left of each example or comparative example is referred to in table 7.

If salicylic acid is added to 30 mass% of 1, 3-propanediol, the friction becomes small. When the 1, 3-propanediol content is 60% by mass, no improvement is observed, and the friction increases. In addition, the friction coefficient of example 4-1 was lower than that of either the reference example or the comparative example, and it was confirmed that the composition was smooth when applied to the skin.

[ formulation examples ]

The formulations are exemplified in tables 8 and 9 below. The formulation examples are all beauty lotion, and the contents in the formulation examples are all mass percent.

[ Table 8]

[ Table 9]

Claims

1. A composition for external application to the skin comprising: at least one selected from ascorbic acid and a salt of ascorbic acid, (B) at least one selected from 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.

2. The composition for external application to skin according to claim 1, wherein the concentration of the component (A) is 1 to 10% by mass.

3. The composition for external application to skin according to claim 1 or 2, wherein the concentration of the component (B) is 0.001 to 2% by mass.

4. The composition for external skin application according to any one of claims 1 to 3, further comprising (D) water in an amount of 1 to 15% by mass.

5. The composition for external application to skin according to any one of claims 1 to 4, further comprising (E) a lower alcohol in an amount of 1 to 20% by mass.

6. The composition for external skin application according to any one of claims 1 to 5, wherein the pH is 2 to 5.

7. A method for suppressing coloring of a composition for external application to the skin, which contains (A) at least one member selected from the group consisting of ascorbic acid and a salt of ascorbic acid, wherein the coloring of the composition for external application to the skin is suppressed by blending (A) at least one member selected from the group consisting of ascorbic acid and a salt of ascorbic acid, (B) at least one member 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.

8. A coloring inhibitor for a skin external composition containing (A) at least one selected from ascorbic acid and a salt of ascorbic acid, comprising: (B) At least one selected from 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.

9. A method for imparting a feeling of use to a composition for external application to the skin, which contains (A) at least one member selected from the group consisting of ascorbic acid and a salt of ascorbic acid, wherein the feeling of use is imparted to the composition for external application to the skin by using (A) at least one member selected from the group consisting of ascorbic acid and a salt of ascorbic acid, (B) at least one member 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.

10. A feeling-of-use enhancer for a composition containing (A) at least one member selected from the group consisting of ascorbic acid and a salt of ascorbic acid, comprising: (B) At least one selected from 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.