Composition for external application containing ascorbic acid and / or salt thereof

A composition with specific ratios of ascorbic acid, diol, water, and ethoxydiglycol, along with a controlled pH, addresses stability and absorption issues, enhancing the effectiveness of ascorbic acid in skin preparations.

JP2025108661AInactive Publication Date: 2025-07-23ROHTO PHARM CO LTD
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Patent Information

Application Number
JP2025069388
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2018-03-30
Filing Date
2025-04-21
Publication Date
2025-07-23
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Existing compositions containing ascorbic acid face issues such as coloring, precipitation during low-temperature storage, and percutaneous absorption problems, which affect their stability and efficacy in skin preparations.

Method used

The composition is formulated with ascorbic acid or its salts at 10% by mass or less, a diol with 3 carbon atoms at 30% by mass or more, water at 20% by mass or less, and ethoxydiglycol at less than 30% by mass, with a pH of 4.5 or less, or within the range of 10 to 25% by mass for ascorbic acid, 30 to 90% by mass for the diol, and a pH of 2.0 to 6.0, to enhance stability and percutaneous absorption.

Benefits of technology

The formulation suppresses coloring and precipitation, ensuring stability and improved skin permeability of ascorbic acid, making it suitable for various skin preparations.

✦ Generated by Eureka AI based on patent content.

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Abstract

To provide a composition for external application which has excellent stability and feeling of use.SOLUTION: According to the present invention, a composition for external application is prepared to contain (A) 10 mass% or less of at least one that is selected from the group consisting of ascorbic acid and salts of ascorbic acid, (B) 30 mass% or more of a diol having three carbon atoms, and (C) 20 mass% or less of water, while having an ethoxydiglycol content of less than 30 mass% and a pH of 4.5 or less. Alternatively, a composition for external application according to the present invention is prepared to contain (A) 10-25 weight% of at least one that is selected from the group consisting of ascorbic acid and salts of ascorbic acid, (B) a diol having three carbon atoms in an amount of 30-90 mass% in components other than (A) and (C), and (C) water, while having an ethoxydiglycol content of less than 30 mass% and a pH of 2.0 to 6.0 and satisfying (C) / (A)=0.2-5.SELECTED DRAWING: Figure 1
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Description

[Technical field]

[0001] The present invention relates to a composition for external use containing ascorbic acid and / or a salt thereof. [Background technology]

[0002] Ascorbic acid has anti-inflammatory, acne-fighting, whitening, anti-aging, and antioxidant effects. As a result, it has a cell activation effect by promoting the synthesis of biocomponents such as collagen, and an effect of activating epidermal keratinocytes by ultraviolet rays. It is known that it exerts various effects such as suppressing cell damage and DNA damage caused by It is widely used as an external skin preparation in the hope of achieving these effects.

[0003] There are several methods for stably solubilizing ascorbic acid in aqueous skin preparations. It has been studied (for example, Patent Document 1: WO02 / 19972, Patent Document 2: WO 00 / 78283, Patent Document 3: JP 2002-348228 A, Patent Document 4 (JP 2005-225865 A). [Prior art documents] [Patent documents]

[0004] [Patent Document 1] WO02 / 19972 publication [Patent Document 2] WO00 / 78283 publication [Patent Document 3] JP 2002-348228 A [Patent Document 4] JP 2005-225865 A Summary of the Invention [Problem to be solved by the invention]

[0005] An object of the present invention is to provide an ascorbic acid-containing external composition having good properties. To do so.

Means for Solving the Problems

[0006] Provided is an external composition containing ascorbic acid and / or a salt thereof.

[0007] According to the study by the present inventors, when ascorbic acid and / or a salt thereof is blended, there are some cases where coloring is observed during production, or coloring may be observed after a certain period of time. It was also found that there may be problems such as precipitation of ascorbic acid during low-temperature storage and problems with percutaneous absorption. Furthermore, it was found that there may be cases where there are problems such as precipitation of ascorbic acid during low-temperature storage and problems with percutaneous absorption. It was found that there may be cases where there are problems such as precipitation of ascorbic acid during low-temperature storage and problems with percutaneous absorption.

[0008] As a result of intensive studies to solve this problem, the present inventors have found that (A) at least one selected from the group consisting of ascorbic acid and salts of ascorbic acid is 10% by mass or less, (B) 30% by mass or more of a diol having 3 carbon atoms, (C) 20% by mass or less of water, and further the content of ethoxydiglycol is less than 30% by mass, and the pH is 4.5 or less. Alternatively, (A) at least one selected from the group consisting of ascorbic acid and salts of ascorbic acid is 10 to 25% by mass, (B) a diol having 3 carbon atoms is 30 to 90% by mass in the components excluding (A) and (C), (C) water, and further the content of ethoxydiglycol is Less than 30% by mass, (C) / (A)=0.2 to 5, and by setting the pH to 2.0 to 6.0, The coloring of ascorbic acid is suppressed, and an external composition excellent in the percutaneous absorption property (skin permeability) of ascorbic acid is obtained, and the present invention has been completed. At least one selected from the group consisting of ascorbic acid and salts of ascorbic acid is 10 to 25% by mass, (B) a diol having 3 carbon atoms is 30 to 90% by mass in the components excluding (A) and (C), (C) water, and further the content of ethoxydiglycol is Less than 30% by mass, (C) / (A)=0.2 to 5, and by setting the pH to 2.0 to 6.0, Less than 30% by mass, (C) / (A)=0.2 to 5, and by setting the pH to 2.0 to 6.0, The coloring of ascorbic acid is suppressed, and an external composition excellent in the percutaneous absorption property (skin permeability) of ascorbic acid is obtained. The inventors have found that an external composition excellent in the percutaneous absorption property (skin permeability) of ascorbic acid can be obtained, and have completed the present invention.

[0009] That is, the present invention provides an external composition described below. Item 1. (A) At least 1 selected from the group consisting of ascorbic acid and salts of ascorbic acid is 10% by mass or less; (B) A diol having 3 carbon atoms is 30% by mass or more; and (C) Water is contained in an amount of 20% by mass or less, the content of ethoxydiglycol is less than 30% by mass and the pH is 4.5 or less: an external composition Item 2. The external composition according to Item 1, wherein the content of the component (B) is 40% by mass or more: Item 3. The external composition according to Item 1 or 2, wherein the content of the ascorbic acid or its salt is 3 to 10% by mass: Item 4. (C) The external composition according to any one of Items 1 to 3, wherein the content of water is 10% by mass or less : Item 5. (A) At least 1 selected from the group consisting of ascorbic acid and salts of ascorbic acid is 10 to 25% by mass (B) A diol having 3 carbon atoms is 30 to 90% by mass in components other than (A) and (C); and (C) Water is contained, the content of ethoxydiglycol is less than 30% by mass, (C) / (A)=0.2 to 5 and the pH is 2.0 to 6.0: an external composition Item 6. Furthermore, the external composition according to any one of Items 1 to 5, which contains butylene glycol and / or a lower alcohol : Item 7. The external composition according to any one of Items 1 to 6, wherein the component (B) is 1,3-propanediol and / or propylene glycol : Item 8. The external composition according to any one of Items 1 to 7, wherein the component (B) contains at least 1,3-propanediol : Item 9. ​The content of ethoxydiglycol is 10% by mass or less, and the external composition according to any one of items 1 to 8: Item 10. The external composition according to any one of items 1 to 9, wherein the external composition is a solubilized external composition having a transmittance of 85 to 100% at a wavelength of 700 nm: Item 11. The external composition according to any one of items 1 to 10, wherein the external composition is for promoting the percutaneous absorption of ascorbic acid: Item 12. At least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid is 10% by mass or less; (B) a diol having 3 carbon atoms is 30% by mass or more; and (C) water is 20% by mass or less, and the content of ethoxydiglycol is less than 30% by mass, and the pH is 4.5 or less, thereby preventing coloring and / or precipitation of crystals of the external composition containing at least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid. Item 13. (A) At least one selected from the group consisting of ascorbic acid and salts of ascorbic acid is 10 to 25% by mass (B) a diol having 3 carbon atoms is 30 to 90% by mass in components other than (A) and (C); and (C) water is contained, the content of ethoxydiglycol is less than 30% by mass, (C) / (A) = 0.2 to 5, and the pH is 2.0 to 6.0, thereby preventing coloring and / or precipitation of crystals of the external composition containing at least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid. Item 14.

Advantages of the Invention

[0010] ​​​​​​​​​The present invention can provide an external composition excellent in stability.

Brief Description of Drawings

[0011]

Figure 1

Modes for Carrying Out the Invention

[0012] In this specification, the unit of content “mass %” is synonymous with “g / 100 g”.

[0013] The first aspect of the present invention is first when at least one selected from the group consisting of ascorbic acid and salts of ascorbic acid is 10% by mass or less (hereinafter also referred to as the first invention). The external composition of the first invention is as follows. The external composition of the first invention (A) At least one selected from the group consisting of ascorbic acid and salts of ascorbic acid is 10% by mass or less; (B) A diol having 3 carbon atoms is 30% by mass or more; and (C) Water is 20% by mass or less, the content of ethoxydiglycol (diethylene glycol monoethyl ether) is less than 30% by mass, and the pH is 4.5 or less. (C) Water is 20% by mass or less, the content of ethoxydiglycol (diethylene glycol monoethyl ether) is less than 30% by mass, and the pH is 4.5 or less. is an external composition. is an external composition.

[0014] The external composition of the first invention is stable in a relatively low concentration range of at least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid, and has excellent percutaneous absorbability. The external composition of the first invention is stable in a relatively low concentration range of at least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid, and has excellent percutaneous absorbability. is excellent.

[0015] [(A) At least one selected from the group consisting of ascorbic acid and salts of ascorbic acid] In the present invention, as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics ​Commercially available ascorbic acid can be used, and these usually refer to the L-form ones.

[0016] Salts of ascorbic acid can also be used. Here, the salts of ascorbic acid are pharmaceutically acceptable salts. Without limitation, for example, salts with organic bases (such as salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, etc., basic ammonium salts such as arginine salt, etc.), salts with inorganic bases (such as ammonium salt, sodium salt, potassium salt and other alkali metal salts, calcium salt, magnesium salt and other alkaline earth metal salts, aluminum salt, etc.). Salts of ascorbic acid include, but are not limited to, salts with organic bases (such as salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, etc., basic ammonium salts such as arginine salt, etc.), salts with inorganic bases (such as ammonium salt, sodium salt, potassium salt and other alkali metal salts, calcium salt, magnesium salt and other alkaline earth metal salts, aluminum salt, etc.). Particularly preferred salts of ascorbic acid are sodium salt and potassium salt. Specifically, Salts of ascorbic acid include, but are not limited to, salts with organic bases (such as salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, etc., basic ammonium salts such as arginine salt, etc.), salts with inorganic bases (such as ammonium salt, sodium salt, potassium salt and other alkali metal salts, calcium salt, magnesium salt and other alkaline earth metal salts, aluminum salt, etc.). Particularly preferred salts of ascorbic acid are sodium salt and potassium salt. Specifically, Salts of ascorbic acid include, but are not limited to, salts with organic bases (such as salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, etc., basic ammonium salts such as arginine salt, etc.), salts with inorganic bases (such as ammonium salt, sodium salt, potassium salt and other alkali metal salts, calcium salt, magnesium salt and other alkaline earth metal salts, aluminum salt, etc.). Particularly preferred salts of ascorbic acid are sodium salt and potassium salt. Specifically, Salts of ascorbic acid include, but are not limited to, salts with organic bases (such as salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, etc., basic ammonium salts such as arginine salt, etc.), salts with inorganic bases (such as ammonium salt, sodium salt, potassium salt and other alkali metal salts, calcium salt, magnesium salt and other alkaline earth metal salts, aluminum salt, etc.). Particularly preferred salts of ascorbic acid are sodium salt and potassium salt. Specifically, Salts of ascorbic acid include, but are not limited to, salts with organic bases (such as salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, etc., basic ammonium salts such as arginine salt, etc.), salts with inorganic bases (such as ammonium salt, sodium salt, potassium salt and other alkali metal salts, calcium salt, magnesium salt and other alkaline earth metal salts, aluminum salt, etc.). Particularly preferred salts of ascorbic acid are sodium salt and potassium salt. Specifically, Salts of ascorbic acid include, but are not limited to, salts with organic bases (such as salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, etc., basic ammonium salts such as arginine salt, etc.), salts with inorganic bases (such as ammonium salt, sodium salt, potassium salt and other alkali metal salts, calcium salt, magnesium salt and other alkaline earth metal salts, aluminum salt, etc.). Particularly preferred salts of ascorbic acid are sodium salt and potassium salt. Specifically, Salts of ascorbic acid include, but are not limited to, salts with organic bases (such as salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, etc., basic ammonium salts such as arginine salt, etc.), salts with inorganic bases (such as ammonium salt, sodium salt, potassium salt and other alkali metal salts, calcium salt, magnesium salt and other alkaline earth metal salts, aluminum salt, etc.). Particularly preferred salts of ascorbic acid are sodium salt and potassium salt. Specifically, Salts of ascorbic acid include, but are not limited to, salts with organic bases (such as salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, etc., basic ammonium salts such as arginine salt, etc.), salts with inorganic bases (such as ammonium salt, sodium salt, potassium salt and other alkali metal salts, calcium salt, magnesium salt and other alkaline earth metal salts, aluminum salt, etc.). Particularly preferred salts of ascorbic acid are sodium salt and potassium salt. Specifically, Salts of ascorbic acid include, but are not limited to, salts with organic bases (such as salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, etc., basic ammonium salts such as arginine salt, etc.), salts with inorganic bases (such as ammonium salt, sodium salt, potassium salt and other alkali metal salts, calcium salt, magnesium salt and other alkaline earth metal salts, aluminum salt, etc.). Particularly preferred salts of ascorbic acid are sodium salt and potassium salt. Specifically,

[0017] In the present invention, ascorbic acid or its salts can be used alone or in combination of two or more. In the present invention, ascorbic acid or its salts can be used alone or in combination of two or more.

[0018] In the external composition of the first invention, the total content of component (A) relative to the total amount of the external composition is appropriately set according to the balance with other components. Relative to the total amount of the external composition, the total content of component (A) is not particularly limited as long as it is 10% by mass or less, but preferably 1% by mass or more, more preferably 2% by mass or more, still more preferably 3% by mass or more. Relative to the total amount of the external composition, the total content of component (A) is 10% by mass or less, preferably 9% by mass In the external composition of the first invention, the total content of component (A) relative to the total amount of the external composition is appropriately set according to the balance with other components. Relative to the total amount of the external composition, the total content of component (A) is not particularly limited as long as it is 10% by mass or less, but preferably 1% by mass or more, more preferably 2% by mass or more, still more preferably 3% by mass or more. Relative to the total amount of the external composition, the total content of component (A) is 10% by mass or less, preferably 9% by mass In the external composition of the first invention, the total content of component (A) relative to the total amount of the external composition is appropriately set according to the balance with other components. Relative to the total amount of the external composition, the total content of component (A) is not particularly limited as long as it is 10% by mass or less, but preferably 1% by mass or more, more preferably 2% by mass or more, still more preferably 3% by mass or more. Relative to the total amount of the external composition, the total content of component (A) is 10% by mass or less, preferably 9% by mass In the external composition of the first invention, the total content of component (A) relative to the total amount of the external composition is appropriately set according to the balance with other components. Relative to the total amount of the external composition, the total content of component (A) is not particularly limited as long as it is 10% by mass or less, but preferably 1% by mass or more, more preferably 2% by mass or more, still more preferably 3% by mass or more. Relative to the total amount of the external composition, the total content of component (A) is 10% by mass or less, preferably 9% by mass In the external composition of the first invention, the total content of component (A) relative to the total amount of the external composition is appropriately set according to the balance with other components. Relative to the total amount of the external composition, the total content of component (A) is not particularly limited as long as it is 10% by mass or less, but preferably 1% by mass or more, more preferably 2% by mass or more, still more preferably 3% by mass or more. Relative to the total amount of the external composition, the total content of component (A) is 10% by mass or less, preferably 9% by mass % Hereinafter, it is more preferably 8% by mass or less. With respect to the total amount of the external composition, the total content of component (A) is preferably 1% by mass to 10% by mass, more preferably 2% by mass to 10% by mass, and still more preferably 3% by mass to 8% by mass.

[0019] [(B) 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. The diol having 3 carbon atoms is not limited, but is preferably 1,3-propanediol (CAS number: 504-63-2, English name: 1,3-Dihydroxypropane or Trim ethyleneGlycol) or propylene glycol (CAS number: 57-55- 6, English name: 1,2-Dihydroxypropane, Japanese alias: 1,2-propanedi ol). For example, it is possible to use either one or both of 1,3-propanediol or propylene glycol as component (B). Such a diol having 3 carbon atoms can also be used as a commercially available product as it is. From the viewpoints of alleviating irritation to the skin, improving the feeling of use, and suppressing coloring, it is preferable to combine 1,3-propanediol and propylene glycol. In the external composition of the first invention, the total content of component (B) with respect to the total amount of the external composition is 30% by mass or more, preferably 35% by mass or more, more preferably 40% by mass or more, and still more preferably 45% by mass or more.

[0020] The total content of component (B) with respect to the total amount of the external composition is preferably 90% by mass or less. ​​​​​Preferably, it is 85% by mass or less, more preferably 80% by mass or less.

[0021] The total content of component (B) with respect to the total amount of the external composition of the first invention is preferably 35 to 90% by mass, more preferably 40 to 85% by mass, still more preferably 45 to 80% by mass .

[0022] In the external composition of the first invention, the ratio of the content of component (B) to component (A) is not particularly limited, but is preferably 3 to 300 parts by mass, more preferably 3 to 30 parts by mass, still more preferably 5 to 25 parts by mass with respect to 1 part by mass of the total content of component (A).

[0023] [(C) Water] The external composition of the first invention is a liquid composition containing water. The proportion of water is not limited, but is preferably 0.1% by mass or more, more preferably 1% by mass or more, most preferably more than 1% by mass with respect to the external composition. More than 1% by mass is not particularly limited, but can be, for example, a value such as 1.01% by mass or more or 1.1% by mass or more. The proportion of water is 20% by mass or less with respect to the external composition. Preferably, it is 15% by mass or less, more preferably 10% by mass or less.

[0024] The total content of component (C) with respect to the total amount of the external composition of the first invention is preferably 1 part by mass % to 15% by mass, more preferably more than 1% by mass to 10% by mass, still more preferably 2 to 10 % by mass.

[0025] In the external composition of the first invention, the ratio of the content of component (C) to component (A) is not particularly limited, but is preferably 0.1 to 10 parts by mass with respect to 1 part by mass of the total content of component (A). The amount is 0.125 to 8 parts by mass, more preferably 0.2 to 5 parts by mass. There is.

[0026] In the present invention, thus, precipitation of ascorbic acid or its salt can be suppressed even in a composition containing a small amount of water. Furthermore, an external composition excellent in stability can be obtained. However, from the viewpoint of suppressing precipitation of ascorbic acid at low temperature, it is preferable to blend it even in a small amount. It is preferable.

[0027] [Ethoxydiglycol (diethylene glycol monoethyl ether)] In the present invention, mainly from the viewpoint of improving stability, ethoxydiglycol is not contained or, if contained, is less than 30% by mass. The ethoxydiglycol contained in the external composition in an amount less than 30% by mass 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.

[0028] In the external composition of the first invention, the content of ethoxydiglycol with respect to the total amount of the external composition is less than 30% by mass, preferably 20% by mass or less, more preferably 10% by mass or less, still more preferably 5% by mass or less, and ethoxydiglycol may not be contained in the external composition. The total content of ethoxydiglycol is 0 or more and less than 30% by mass, preferably 0 to 20% by mass, more preferably 0 to 10% by mass, still more preferably about 0 to 5% by mass.

[0029] In the external composition of the first invention, the ratio of the content of the ethoxydiglycol component to the (A) component is preferably 0 to 10 parts by mass with respect to 1 part by mass of the total content of the (A) component, 0 ~5 parts by mass are more preferable. In some cases, it can also be 0.001~10 parts by mass, or 0.0 ~5 parts by mass.

[0030] [pH] From the viewpoints of the stability of the component (A), low irritation to the skin and mucous membranes, and good skin feel in terms of skin use, the first external composition of the present invention preferably has a pH of 1.5~4.5, more preferably a p H of 2~4, and is desirably in an acidic range.

[0031] The external composition of the first invention contains a predetermined amount of the component (A), the component (B), and the component (C), specifies the content of ethoxydiglycol, and further sets the pH to 4.5 or less, thereby obtaining a stable external composition with good properties.

[0032] [Glycol ether] In the present invention, mainly from the viewpoint of improving stability, glycol ether other than ethoxydiglycol is not contained, or even if it is contained, the total amount of glycol ether in combination with ethoxydiglycol is preferably less than 40% by mass. Here, glycol ether other than ethoxydiglycol 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. It may be any one that can be dissolved in an amount of 10 g or more per 100 g of water. Examples include those having a polymerization degree of 2 or less. Specifically, diethylene glycol monomethyl ether, diethylene glycol monopropyl ether, di ethylene glycol monobutyl ether, diethylene glycol monoisobutyl ether , diethylene glycol dimethyl ether, ethylene glycol monobutyl ether, ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, triethylene glycol, etc. Chilene glycol monobutyl ether, tetraethylene glycol monobutyl ether, propylene glycol monomethyl ether, propylene glycol monoethyl ether, propylene glycol monopropyl ether, dipropylene glycol monomethyl ether l, dipropylene glycol monoethyl ether, dipropylene glycol monopropyl ether, etc. can be exemplified. Furthermore, diethylene glycol monomethyl ether, dieth ylene glycol monopropyl ether, diethylene glycol monobutyl ether, die thylene glycol monoisobutyl ether, diethylene glycol dimethyl ether, e thylene glycol monobutyl ether, ethylene glycol monomethyl ether, ethyle ne glycol monoethyl ether, triethylene glycol monobutyl ether, tetra ethylene glycol monobutyl ether, propylene glycol monomethyl ether, p ropylene glycol monoethyl ether, propylene glycol monopropyl ether, dipropylene glycol monomethyl ether, dipropylene glycol monoethyl ether l, dipropylene glycol monopropyl ether are typical examples. In particular, die thylene glycol monomethyl ether, diethylene glycol monopropyl ether, e thylene glycol monobutyl ether, triethylene glycol monobutyl ether, te traethylene glycol monobutyl ether, propylene glycol monomethyl ether l, propylene glycol monoethyl ether, propylene glycol monopropyl ether l, dipropylene glycol monomethyl ether, dipropylene glycol monoethyl e ther, dipropylene glycol monopropyl ether are typical examples.

[0033] These glycol ethers can also be used alone or in combination of two or more kinds. .

[0034] In the external composition of the first invention, the total content of glycol ethers including ethoxydiglycol with respect to the total amount of the external composition is preferably less than 40% by mass, more preferably 30% by mass or less, still more preferably less than 10% by mass, and even more preferably 10% by mass or less. The glycol ether may not be contained in the external composition.

[0035] The total content of glycol ethers including ethoxydiglycol is preferably 0 or more and less than 40% by mass, more preferably 0 or more and less than 30% by mass, still more preferably about 0 or more and 1 0% by mass.

[0036] In the external composition of the first invention, the ratio of the content of the glycol ether component to the (A) component is preferably 0 to 20 parts by mass, more preferably 0 to 10 parts by mass with respect to 1 part by mass of the total content of the (A) component. Also, in some cases, it can be 0.001 to 20 parts by mass, or 0.01 to 10 parts by mass.

[0037] The external composition of the first invention contains a predetermined amount of the (A) component, the (B) component, and the (C) component, defines the content of the whole glycol ether, and sets the pH to 4.5 or less, thereby it is also possible to obtain an external composition with better stability.

[0038] [Lower alcohol] From the viewpoints of improving the usability, stability, and promoting percutaneous absorption, the external composition of the first invention The above components (A), (B), and (C), and components therein, may be used in any manner that does not impede the effects of the invention. In this case, in addition to glycol ethers such as ethoxydiglycol, lower alcohols should be used. The lower alcohol used in the present invention may be a pharmaceutical or medical product. There are no particular limitations as long as it is used as an ingredient in topical skin preparations in the field of topical or cosmetic products. In this specification, the term "lower alcohol" refers to a C1-C6 alcohol. Among these, C1-C3 alcohols are particularly preferred. Other examples of such alcohols include ethanol, methanol, n-propanol, and isopropanol. Examples include ru.

[0039] In the topical composition of the first invention, the content of the lower alcohol relative to the total amount of the topical composition When contained, it is preferably 0.01% by mass or more, more preferably 0.1% by mass or more. More preferably, the content is 0.25% by mass or more, even more preferably, 1% by mass or more, The content of ethanol is preferably 3% by mass or more. The content of ethanol is preferably 45% by mass or less. More preferably, it is 40% by mass or less, even more preferably, it is 35% by mass or less, and even more preferably It is preferably 20% by mass or less.

[0040] The content of the lower alcohol in the topical composition of the first invention is preferably 0.01 to 45% by mass, more preferably 0.1 to 40% by mass, and even more preferably 0.25 to 35% by mass. % by mass, even more preferably 1 to 20% by mass, and most preferably 3 to 20% by mass.

[0041] [Butylene glycol] The composition for external use of the present invention is characterized in that it has the following properties: Unless it interferes with the effects, in the above (A) component, (B) component, and (C) component, and in the case where they are included, in addition to glycol ethers such as ethoxydiglycol, butylene glycol ( 1,3-butylene glycol) may also be included.

[0042] In the external composition of the first invention, the content of butylene glycol relative to the total amount of the external composition, when included, is preferably 0.01% by mass or more, more preferably 0.1% by mass or more, still more preferably 0.25% by mass or more. The content of butylene glycol is preferably 55% by mass or less, more preferably 50% by mass or less, still more preferably 45% by mass or less.

[0043] The content of butylene glycol in the external composition of the first invention is preferably 0.01 to 55% by mass, more preferably 0.1 to 50% by mass, still more preferably 0.25 to 45 % by mass.

[0044] [pH adjuster] From the viewpoints of improving the usability, stability, and promoting percutaneous absorption, the external composition of the first invention, unless it interferes with the effects of the first invention, in the above (A) component, (B) component, and (C) component, and when included, in addition to glycol ethers such as ethoxydiglycol, a pH adjuster may also be included.

[0045] As the pH adjuster used in the first invention, compounds usually used as components of external skin preparations in the fields of pharmaceuticals, quasi-drugs, or cosmetics can be used. Although not particularly limited, pH adjusters having amines (for example, aspartic acid or its salts, ε-amino Caproic acid or its salt, glutamic acid or its salt, aminoethylsulfonic acid or its salt , monoethanolamine, triethanolamine, diisopropanolamine, triiso propanolamine, arginine, lysine, L-carnitine, low molecular weight betaine, preferably low molecular weight betaine, more preferably trimethylglycine), organic acid salts (e.g., sodium lactate lithium, sodium acetate, sodium citrate, sodium succinate, sodium oxalate calcium gluconate, sodium pyrrolidonecarboxylate, etc.), inorganic acid salts (e.g., sodium metabisulfite, potassium metabisulfite, sodium phosphate, potassium nitrate, sodium borate sodium, preferably sodium metabisulfite), basic amino acids and their salts (argin nine, lysine, or histidine and their salts), 3-O-ethylascorbic acid or its salt, etc. are exemplified.

[0046] In the external composition of the first invention, the total content of the pH adjuster with respect to the total amount of the external composition is not particularly limited, but is preferably 0.01% by mass or more, more preferably 0.05% by mass or more. With respect to the total amount of the external composition, the total content of the pH adjuster is preferably 1 0% by mass or less, more preferably 5.0% by mass or less. With respect to the total amount of the external composition, the content of the amine or the pH adjuster having an amino group is preferably 0.01% by mass to 10 % by mass, more preferably 0.05% by mass to 5.0% by mass.

[0047] In the external composition of the first invention, the ratio of the content of the pH adjuster to the component (A) is not particularly limited, but is 0.00001 to 20 parts by mass with respect to 1 part by mass of the total content of the component (A) parts are preferred, more preferably 0.0001 to 20 parts by mass, and 0.0005 to 10 parts by mass are even more preferred, 0.005 to 5 parts by mass are still more preferred, and 0.01 to 1 part by mass is most preferred .

[0048] [Other components] In the external composition of the present invention, in addition to the above components (A), (B), and (C), and when included, in addition to less than a certain amount of ethoxydiglycol, further, for the purpose of enhancing or supplementing various actions that ascorbic acid has, and for adding other useful actions, whitening components, anti-inflammatory components, antibacterial components, cell-activating components, astringent components, antioxidant components, acne-improving components, anti-aging components, components that promote the synthesis of biological components such as collagen, blood circulation-promoting components, moisturizing components, anti-aging preventive components, etc., can be blended by combining one or more of various components. Preferably one or more of whitening components, anti-inflammatory components, antibacterial components, cell-activating components, astringent components, antioxidant components, anti-aging components, or moisturizing components. Particularly preferred combinations of these components include combinations with whitening components, combinations of whitening components and antioxidant components , combinations with antioxidant components, combinations with anti-aging components, and combinations of whitening components and anti-aging components . Examples of these components include those conventionally used and those that will be used in the future as components of external skin preparations in the fields of pharmaceuticals, quasi-drugs , or cosmetics. There is no particular limitation as long as they are those that can be used, and any ones can be appropriately selected and used. In addition to the above components, the external composition of the present invention can further contain a surfactant, solubilizing component, oils and fats , saccharides, or percutaneous absorption-promoting components. In particular, surfactants, solubilizing components, or

[0049] The external composition of the present invention can also contain a surfactant, solubilizing component, oils and fats , saccharides, or percutaneous absorption-promoting components. In particular, surfactants, solubilizing components, or By blending fats and oils, the stability, effectiveness, and usability of ascorbic acid in an aqueous solvent can be further improved.

[0050] In the external composition of the present invention, within an amount and quality range that do not impair the quality such as appearance stability and viscosity, and also do not impair the effects of the present invention, various components generally used as components of external preparations in the fields of pharmaceuticals, quasi-drugs, or cosmetics, for example, amino acids, irritation reducers , thickeners, preservatives, ultraviolet protectants, coloring agents, dispersants, additional pH adjusters, fragrances, etc. can be blended as needed. These components can be used alone or in any combination of two or more. , thickeners, preservatives, ultraviolet protectants, coloring agents, dispersants, additional pH adjusters, fragrances, etc. can be blended. In addition, these components can be blended singly or in any combination of two or more.

[0051] The external composition of the first invention contains at least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid in an amount of 10% by mass or less, (B) a diol having 3 carbon atoms in an amount of 30% by mass or more, and (C) water in an amount of 20% by mass or less, the content of ethoxydiglycol being less than 30% by mass, and the pH being 4.5 or less. If necessary, the above-mentioned optional components are blended and mixed, and further, if necessary, other solvents, bases of external preparations commonly used, etc. are blended, and thus can be prepared into various desired forms such as paste, mousse, gel, liquid, emulsion, cream, sheet (substrate-supported), aerosol, spray, etc. These can be produced by ordinary methods in the industry.

[0052] The external composition of the present invention is particularly preferably a transparent to semi-transparent composition in which ascorbic acid and / or its salt is solubilized. Here, "solubilized" is defined as follows. That is, for example, by ultraviolet-visible absorbance measurement method, using a spectrophotometer or a photoelectric​​​ Using a spectrophotometer UV-2450 (manufactured by Shimadzu Corporation), the transmittance at a wavelength of 700 nm is the transmittance is in the range of 80 to 100%, preferably 85 to 100%, more preferably 90 to 100% Here, the transmittance of water is taken as 100%. The solubilized composition of the present invention is transparent or semi-transparent in appearance. The method for measuring transmittance is, more specifically, the 16th revised Japanese Pharmacopoeia [B] General Test Methods 2. Physical Test Methods Spectrophotometric Methods 2.24 Ultraviolet-Visible Absorbance Measurement method as described in the method.

[0053] [Viscosity] The external composition of the present invention can be prepared as a composition having an appropriate viscosity desired when used for application to the skin, particularly. The external composition of the present invention Although the viscosity is not particularly limited, for example, when measured at 25 ° C using an E-type viscometer, the viscosity is usually about 1 to 300 mPa·s, preferably about 1 to 200 mPa·s, more preferably about 1 to 100 mPa·s, most preferably about 1 to 50 mPa·s. The method for measuring viscosity is, more specifically, the 16th revised Japanese Pharmacopoeia [B] General Test Methods 2. Physical Test Methods Other Physical Test Methods 2.53 Viscosity Measurement Method 2. Second Method Rotational Viscometer Method 2.1.3 Conical-plate type rotational viscometer (cone-plate type viscometer) as described in the method. shall conform to the method described.

[0054] [Use] The external composition of the present invention is particularly effective as a whitening agent, an anti-inflammatory agent, and an anti-aging agent. For example it has the action of preventing and treating acne and antioxidation. Furthermore, by applying to the skin, the transparency of the skin is enhanced, moisture is retained, texture is improved, and the effect of suppressing roughness is exhibited in some cases In addition, it may have effects such as making pores less noticeable and conditioning and moisturizing the skin. It can also be used to prevent and treat spots.

[0055] The composition for external use of the present invention can be, for example, a beauty essence, a lotion, a sunscreen cream, a milky lotion, a cream, or the like. Basic cosmetics such as creams, lotions, oils and packs; foundations, lipsticks, lip Make-up such as creams, mascara, eyeshadow, eyeliner, eyebrow pencil, and nail polish Cosmetics; face washes, cleansers, body washes, and other cleansing products; underarm odor prevention agents, athlete's foot treatment agents, soothing agents Itching agent, wound healing agent, cleaning agent, cleansing agent, anti-inflammatory analgesic, acne treatment, hemorrhoid treatment, disinfectant , whitening agents, UV protection agents, etc., belong to the fields of cosmetics, topical medicines, and topical quasi-drugs. The present invention can be applied to various external compositions. It is preferably used in products that are applied to the outer skin, such as skin preparations.

[0056] [Stabilization method] The present invention also relates to a compound (A) selected from the group consisting of ascorbic acid and salts of ascorbic acid. In the present invention, the stabilization of ascorbic acid is carried out by at least one method. According to the synthesis method, (A) a compound selected from the group consisting of ascorbic acid and salts of ascorbic acid is (B) at least one diol having 3 carbon atoms in an amount of 10 mass% or less; and (C) using 20% by mass or less of water and limiting the content of ethoxydiglycol to less than 30% by mass. By adjusting the pH to 4.5 or less, a stable product containing ascorbic acid can be obtained. That is, the present invention relates to a composition comprising (A) ascorbic acid and (B) at least one selected from the group consisting of a salt of an acid having 3 carbon atoms, Using 30% by mass or more of a diol and 20% by mass or less of (C) water in combination, with the content of ethoxydiglycol being less than 30% by mass and the pH being 4.5 or less, a method for imparting stability to an external composition containing at least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid. Here, stabilization means, but is not limited to, for example, being stable even at high temperatures or low temperatures. Specifically, it means that precipitation of ascorbic acid or its salt is suppressed even when the external composition is stored at 4°C for one week, or that appearance changes such as coloring are suppressed even after storage at 50°C or after storage at 40°C for a certain period of time. In the method of the present invention, at least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid, (B) a diol having 3 carbon atoms, (C) water, and the content and ratio of ethoxydiglycol are the same as those used in the above external composition. Furthermore, the product obtained by this method can be used once to several times a day according to the use, etc., at known or commonly used dosages. The second aspect of the present invention is when at least one selected from the group consisting of ascorbic acid and salts of ascorbic acid is 10 to 25% by mass (hereinafter also referred to as the second invention). The external composition of the second invention comprises: (A) at least one selected from the group consisting of ascorbic acid and salts of ascorbic acid, 10 to 25% by mass (B) a diol having 3 carbon atoms, 30 to 90% by mass in the components other than (A) and (C); and (C) water

[0057] The external composition according to the present invention contains: (A) at least one selected from the group consisting of ascorbic acid and salts of ascorbic acid, (B) a diol having 3 carbon atoms in an amount of 30% by mass or more, and (C) water in an amount of 20% by mass or less, with the content of ethoxydiglycol being less than 30% by mass and the pH being 4.5 or less, to impart stability to the external composition. Here, stabilization means, but is not limited to, for example, being stable even at high temperatures or low temperatures. Specifically, it means that precipitation of ascorbic acid or its salt is suppressed even when the external composition is stored at 4°C for one week, or that appearance changes such as coloring are suppressed even after storage at 50°C or after storage at 40°C for a certain period of time.

[0058] The external composition of the present invention contains: (A) at least one selected from the group consisting of ascorbic acid and salts of ascorbic acid, (B) a diol having 3 carbon atoms in an amount of 30% by mass or more, and (C) water in an amount of 20% by mass or less, with the content of ethoxydiglycol being less than 30% by mass and the pH being 4.5 or less, to impart stability to the external composition. Here, stabilization means, but is not limited to, for example, being stable even at high temperatures or low temperatures. Specifically, it means that precipitation of ascorbic acid or its salt is suppressed even when the external composition is stored at 4°C for one week, or that appearance changes such as coloring are suppressed even after storage at 50°C or after storage at 40°C for a certain period of time. (B) a diol having 3 carbon atoms, 30 to 90% by mass in the components other than (A) and (C); and (C) water ​containing less than 30% by mass of ethoxydiglycol, (C) / (A) = 0.2 to 5, and having a pH of 2.0 to 6.0.

[0059] The topical composition of the second invention is stable in at least one relatively high concentration range selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid, and has excellent percutaneous absorbability. It is excellent.

[0060] [at least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid] In the present invention, commercially available ascorbic acid can be used as a component of a topical skin preparation in the fields of pharmaceuticals, quasi-drugs, or cosmetics, and these usually refer to the L-form. Salts of ascorbic acid can also be used. Here, the salts of ascorbic acid are the same as those defined in the case of the first invention. Although not limited, for example, salts with organic bases (e.g., salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, etc., salts with basic ammonium such as arginine salt, etc.), salts with inorganic bases (e.g., ammonium salt, alkali metal salts such as sodium salt, potassium salt, etc., alkaline earth metal salts such as calcium salt, magnesium salt, etc., aluminum salt, etc.). Particularly preferred salts of ascorbic acid are sodium salt and potassium salt. Specifically, sodium ascorbate, sodium ascorbyl monophosphate, sodium ascorbyl diphosphate, sodium ascorbyl triphosphate, sodium ascorbyl-2-sulfate, etc. can be mentioned.

[0061] For example, salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, etc., salts with basic ammonium such as arginine salt, etc. Salts with inorganic bases (e.g., ammonium salt, alkali metal salts such as sodium salt, potassium salt, etc., alkaline earth metal salts such as calcium salt, magnesium salt, etc., aluminum salt, etc.). Particularly preferred salts of ascorbic acid are sodium salt and potassium salt. Specifically, sodium ascorbate, sodium ascorbyl monophosphate, sodium ascorbyl diphosphate, sodium ascorbyl triphosphate, sodium ascorbyl-2-sulfate, etc. can be mentioned. ​​​​​​​​​

[0062] In the present invention, ascorbic acid or its salt can be used alone or in combination of two or more kinds. It is possible.

[0063] In the external composition of the second invention, the total content of component (A) with respect to the total amount of the external composition is , appropriately set according to the balance with other components. With respect to the total amount of the external composition, the total content of component (A) is not particularly limited as long as it is 10 to 25% by mass.

[0064] [(B) Diol having 3 carbon atoms] The diol having 3 carbon atoms used in the external composition of the second 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. It is the same as that defined in the case of the first invention. The diol having 3 carbon atoms is not limited, but is preferably 1,3-propanediol or propylene glycol. For example, either one or both of 1,3-propanediol or propylene glycol can be used as component (B). Such a diol having 3 carbon atoms can also be used as a commercially available product as it is. From the viewpoints of alleviating irritation to the skin, improving the feeling of use, and suppressing coloring, it is preferable to combine 1,3-propanediol and propylene glycol. In the external composition of the second invention, the total content of component (B) with respect to the total amount of the external composition is not particularly limited as long as it is 10% by mass or more, preferably 15% by mass or more, more preferably 20% by mass or more, and still more preferably 25% by mass or more. The total content of component (B) with respect to the total amount of the external composition is preferably 90% by mass or less. For example, either one or both of 1,3-propanediol or propylene glycol can be used as component (B). Such a diol having 3 carbon atoms can also be used as a commercially available product as it is. From the viewpoints of alleviating irritation to the skin, improving the feeling of use, and suppressing coloring, it is preferable to combine 1,3-propanediol and propylene glycol. One or both of them can be used as component (B). Such a diol having 3 carbon atoms can also be used as a commercially available product as it is. From the viewpoints of alleviating irritation to the skin, improving the feeling of use, and suppressing coloring, it is preferable to combine 1,3-propanediol and propylene glycol. For example, either one or both of 1,3-propanediol or propylene glycol can be used as component (B). Such a diol having 3 carbon atoms can also be used as a commercially available product as it is. From the viewpoints of alleviating irritation to the skin, improving the feeling of use, and suppressing coloring, it is preferable to combine 1,3-propanediol and propylene glycol. For example, either one or both of 1,3-propanediol or propylene glycol can be used as component (B). Such a diol having 3 carbon atoms can also be used as a commercially available product as it is. From the viewpoints of alleviating irritation to the skin, improving the feeling of use, and suppressing coloring, it is preferable to combine 1,3-propanediol and propylene glycol.

[0065] In the external composition of the second invention, the total content of component (B) with respect to the total amount of the external composition is 10% by mass or more, preferably 15% by mass or more, more preferably 20% by mass or more, and still more preferably 25% by mass or more. For example, either one or both of 1,3-propanediol or propylene glycol can be used as component (B). Such a diol having 3 carbon atoms can also be used as a commercially available product as it is. From the viewpoints of alleviating irritation to the skin, improving the feeling of use, and suppressing coloring, it is preferable to combine 1,3-propanediol and propylene glycol. The total content of component (B) with respect to the total amount of the external composition is preferably 90% by mass or less. Preferably, it is 85% by mass or less, more preferably 80% by mass or less, still more preferably 70% by mass or less.

[0066] The total content of component (B) relative to the total amount of the external composition is preferably 10 to 90% by mass, more preferably 15 to 85% by mass, still more preferably 20 to 80% by mass, and even more preferably 25% by mass to 70% by mass.

[0067] In the external composition of the second invention, the ratio of the content of component (B) to component (A) is not particularly limited, but is preferably 0.5 to 10 parts by mass, more preferably 0.75 to 8 parts by mass, and still more preferably 1 to 7 parts by mass with respect to 1 part by mass of the total content of component (A).

[0068] In the external composition of the second invention, the content of component (B) relative to components other than component (A) and the following component (C) is preferably 30 to 95% by mass, more preferably 40 to 90% by mass and even more preferably 50 to 85% by mass. %

[0069] [(C) Water] The external composition of the second invention is a liquid composition containing water. The proportion of water is not limited, but is preferably 0.01% by mass to 60% by mass, more preferably 1% by mass to 50% by mass, even more preferably 3% by mass to 40% by mass and particularly preferably 5% by mass to 30% by mass with respect to the external composition.

[0070] In the external composition of the second invention, the ratio of the content of component (C) to component (A) is not particularly limited, but is preferably 0.2 to 5 parts by mass The amount is 0.5 to 2 parts by mass, more preferably 0.6 to 1.8 parts by mass. It is.

[0071] [Ethoxydiglycol (diethylene glycol monoethyl ether)] In the second invention, from the viewpoint of mainly improving stability, ethoxydiglycol is not contained or, if contained, is less than 30% by mass. Ethoxydiglycol contained in the external composition in an amount of less than 30% by mass 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. It 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.

[0072] In the external composition of the second invention, the content of ethoxydiglycol relative to the total amount of the external composition is less than 30% by mass, preferably 20% by mass or less, more preferably 10% by mass or less, and even more preferably 5% by mass or less. Ethoxydiglycol may not be contained in the external composition. The total content of ethoxydiglycol is 0 or more and less than 30% by mass, preferably 0 to 20% by mass by mass, more preferably 0 to 10% by mass, and even more preferably about 0 to 5% by mass.

[0073] In the external composition of the second invention, the ratio of the content of the ethoxydiglycol component to the (A) component is preferably 0 to 10 parts by mass, and 0 to 5 parts by mass is more preferable, with respect to 1 part by mass of the total content of the (A) component. Also, in some cases, it can be 0.001 to 10 parts by mass, or 0.0 1 to 5 parts by mass.

[0074] [pH] The external composition of the present invention usually only needs to have a liquid property of pH 1 to 8. However, from the viewpoints of the stability of ascorbic acid , low irritation to the skin and mucous membranes, and good skin feel, it is preferable Preferably, the pH is 2 to 7, more preferably 2 to 6, even more preferably 2 to 5, and particularly preferably The pH is preferably in the acidic range of 2 to 4.5.

[0075] [Glycol Ether] In the present invention, mainly from the viewpoint of improving stability, a glycoconjugate other than ethoxydiglycol is used. It does not contain glycol ethers, or if it does, it does not contain glycol ethers in combination with ethoxydiglycol. The total amount of ethers is preferably less than 40% by mass. Glycol ethers other than those recalled are not intended to be used for the treatment of skin irritation or skin problems in the fields of pharmaceuticals, quasi-drugs, or cosmetics. There is no particular restriction as long as it is used as an ingredient in external preparations. Anything that dissolves at a temperature of 100° C. or more is acceptable. Examples of such things include those with a degree of polymerization of 2 or less. Diethylene glycol monomethyl ether, diethylene glycol monopropyl ether, di Ethylene glycol monobutyl ether, diethylene glycol monoisobutyl ether , diethylene glycol dimethyl ether, ethylene glycol monobutyl ether, Ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, triethylene glycol ethylene glycol monobutyl ether, tetraethylene glycol monobutyl ether, Propylene glycol monomethyl ether, propylene glycol monoethyl ether, Propylene glycol monopropyl ether, dipropylene glycol monomethyl ether Dipropylene glycol monoethyl ether, dipropylene glycol monopropyl Further, diethylene glycol monomethyl ether, diethylene Diethylene glycol monopropyl ether, diethylene glycol monobutyl ether, Thylene glycol monoisobutyl ether, diethylene glycol dimethyl ether, e thylene glycol monobutyl ether, ethylene glycol monomethyl ether, ethyle ne glycol monoethyl ether, triethylene glycol monobutyl ether, tetra ethylene glycol monobutyl ether, propylene glycol monomethyl ether, p ropylene glycol monoethyl ether, propylene glycol monopropyl ether, dipropylene glycol monomethyl ether, dipropylene glycol monoethyl ether l, dipropylene glycol monopropyl ether are typical examples. In particular, die thylene glycol monomethyl ether, diethylene glycol monopropyl ether, e thylene glycol monobutyl ether, triethylene glycol monobutyl ether, te traethylene glycol monobutyl ether, propylene glycol monomethyl ether l, propylene glycol monoethyl ether, propylene glycol monopropyl ether l, dipropylene glycol monomethyl ether, dipropylene glycol monoethyl ether l, dipropylene glycol monopropyl ether are typical examples.

[0076] These glycol ethers can also be used alone or in combination of two or more.

[0077] In the external composition of the second invention, the total content of glycol ethers including ethoxydiglycol with respect to the total amount of the external composition is preferably less than 40% by mass, more preferably 30% by mass or less, still more preferably less than 10% by mass, and even more preferably 10% by mass or less, and the glycol ether may not be included in the external composition. ​​

[0078] The total content of glycol ethers including ethoxydiglycol is preferably 0 or more and less than 40% by mass, more preferably 0 or more and less than 30% by mass, still more preferably about 0 or more and 1 0% by mass.

[0079] In the external composition of the second invention, the content of the glycol ether component relative to the component (A) is preferably 0 to 20 parts by mass, more preferably 0 to 10 parts by mass, based on 1 part by mass of the total content of the component (A). In some cases, it can also be 0.001 to 20 parts by mass, or 0.01 to 10 parts by mass.

[0080] The external composition of the second invention contains predetermined amounts of the component (A), the component (B), and the component (C), defines the total content of the entire glycol ether, and by setting the pH to 1.5 to 4.5 or lower, more preferably pH 2 to 4.5 or lower, a more stable external composition can also be obtained.

[0081] [Lower alcohol] From the viewpoints of improving the usability, stability, and promoting percutaneous absorption, the external composition of the second invention may contain, as long as it does not interfere with the effects of the present invention, the above-mentioned component (A), component (B), and component (C), and when included in addition to glycol ethers such as ethoxydiglycol, 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. In the present specification, when referring to "lower alcohol", it refers to an alcohol having 1 to 6 carbon atoms . Among them, in particular, an alcohol having 1 to 3 carbon atoms can be preferably used. As an example, in addition to ethanol, methanol, n-propanol, isopropanol, etc. may be mentioned. and the like.

[0082] In the external composition of the second invention, the content of the lower alcohol relative to the total amount of the external composition , if contained, is preferably 0.01% by mass or more, more preferably 0.1% by mass or more , still more preferably 0.25% by mass or more, even more preferably 1% by mass or more, most preferably 3% by mass or more. The ethanol content is preferably 45% by mass or less , more preferably 40% by mass or less, still more preferably 35% by mass or less, even more preferably 20% by mass or less.

[0083] The content of the lower alcohol contained in the external composition of the second invention is preferably 0.01 to 45% by mass, more preferably 0.1 to 40% by mass, still more preferably 0.25 to 35% by mass , even more preferably 1 to 20% by mass, and most preferably 3 to 20% by mass.

[0084] [Butylene glycol] From the viewpoints of improving the usability, stability, and promoting percutaneous absorption, the external composition of the present invention , as long as it does not interfere with the effects of the present invention, the above components (A), (B), and (C), and when contained , in addition to glycol ethers such as ethoxydiglycol, butylene glycol ( 1,3-butylene glycol) may also be included.

[0085] In the external composition of the second invention, the content of butylene glycol relative to the total amount of the external composition , if contained, is preferably 0.01% by mass or more, more preferably 0.1% by mass % or more, still more preferably 0.25% by mass or more. The content of butylene glycol , preferably 40% by mass or less, more preferably 35% by mass or less, and even more preferably The content is 30% by mass or less.

[0086] The content of butylene glycol in the topical composition of the second invention is preferably 0.01 0.1 to 35% by mass, and more preferably 0.25 to 30% by mass. Mass %.

[0087] [pH adjuster] The composition for external use according to the second invention has the following features from the viewpoints of improving the feeling of use, stability, and promotion of percutaneous absorption: As long as it does not interfere with the effects of the invention in 2, the above components (A), (B), and (C), and If the product is to be used in a liquid environment, in addition to glycol ethers such as ethoxydiglycol, a pH adjuster should also be used. It may include.

[0088] The pH adjuster used in the second invention is a pH adjuster that is used in the fields of medicines, quasi-drugs, and cosmetics. Compounds that are commonly used as ingredients in skin external preparations can be used. However, pH adjusters having amines (e.g., aspartic acid or its salts, ε-amines) Nocaproic acid or its salt, glutamic acid or its salt, aminoethylsulfonic acid or its salt , monoethanolamine, triethanolamine, diisopropanolamine, triiso Propanolamine, arginine, lysine, L-carnitine, low molecular weight betaine, preferably is a low molecular weight betaine, more preferably trimethylglycine), an organic acid salt (e.g., sodium lactate Sodium, Sodium Acetate, Sodium Citrate, Sodium Succinate, Sodium Oxalate calcium gluconate, sodium pyrrolidone carboxylate, etc.), inorganic acid salts (e.g. , sodium pyrosulfite, potassium pyrosulfite, sodium phosphate, potassium nitrate, sodium borate (preferably sodium pyrosulfite), basic amino acids and their salts (argi nine, lysine, or histidine and their salts), 3-O-ethyl ascorbic acid or its salts, etc. are exemplified.

[0089] In the external composition of the second invention, the total content of the pH adjuster with respect to the total amount of the external composition is not particularly limited, but is preferably 0.01% by mass or more, more preferably 0.05% by mass or more. With respect to the total amount of the external composition, the total content of the pH adjuster is preferably 20% by mass or less, more preferably 10% by mass or less. With respect to the total amount of the external composition, the content of the amine or the pH adjuster having an amino group is preferably 0.01% by mass to 20% by mass,

[0090] In the external composition of the second invention, the ratio of the content of the pH adjuster to the component (A) is not particularly limited, but with respect to 1 part by mass of the total content of the component (A), 0.00001 to 20 parts by mass is preferred, 0.0001 to 20 parts by mass is more preferred, 0.0005 to 10 parts by mass is even more preferred, 0.005 to 5 parts by mass is still more preferred, and 0.01 to 1 part by mass is most preferred.

[0091] [Other components] In the external composition of the second invention, in addition to the component (A), component (B), and component (C) described above, and when included, less than a certain amount of ethoxydiglycol, further, for the purpose of enhancing or supplementing various actions that ascorbic acid has, and for adding other useful actions, beauty White component, anti-inflammatory component, antibacterial component, cell-activating component, astringent component, antioxidant component, acne-improving component , anti-aging component, component for promoting synthesis of biological components such as collagen, blood circulation promoting component, moisturizing component, various components such as anti-aging component, etc. can be blended by combining one or more of them. Preferably it is one or more components of whitening component, anti-inflammatory component, antibacterial component, cell-activating component, astringent component, antioxidant component, anti-aging component or moisturizing component. As combinations of these components Particularly preferred ones include combinations with whitening components, combinations of whitening components and antioxidant components , combinations with antioxidant components, combinations with anti-aging components, and combinations of whitening components and anti-aging components. As each of these components , those conventionally used as components of external preparations for skin in the fields of pharmaceuticals, quasi-drugs, or cosmetics, and those that will be used in the future are not particularly limited, and any ones can be appropriately selected and used . In addition to the above components, the external composition of the present invention can further contain a surfactant, solubilizing component, oils and fats , saccharides or percutaneous absorption promoting components. In particular, by blending a surfactant, solubilizing component or oils and fats , the stability, effectiveness, and usability of ascorbic acid in an aqueous solvent can be further improved . In the external composition of the present invention, within an amount and quality range that do not impair the quality such as appearance stability and viscosity, and also do not impair the effects of the present invention

[0092] , various components generally used as components of external preparations in the fields of pharmaceuticals, quasi-drugs or cosmetics as needed, for example, amino acids, irritation reducing agents , thickeners, preservatives, ultraviolet ray protectants, coloring agents, dispersants, additional pH adjusters, fragrances, etc. can be blended .

[0093] ​​​​​It is possible. These components can be used alone or in any combination of two or more. It is possible.

[0094] The external composition of the second invention comprises at least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid in an amount of 10 to 25% by mass; (B) a diol having 3 carbon atoms in an amount of 30 to 90% by mass in components other than (A) and (C); and (C) water, with the content of ethoxydiglycol being less than 30% by mass, (C) / (A) = 0.2 to 5, and the pH being 2.0 to 6.0. Optionally, the above-mentioned optional components are blended and mixed, and further, if necessary, other solvents, bases of externally applied agents commonly used, etc. are blended, so that it can be prepared into various desired forms such as paste, mousse, gel, liquid, emulsion, cream, sheet (substrate supported), aerosol, spray, etc. These can be manufactured by the usual methods in the industry. The external composition of the present invention is particularly preferably a transparent to semi-transparent composition in which ascorbic acid and / or its salt is solubilized. Here, "solubilized" is defined as follows. That is, for example, by the ultraviolet-visible absorbance measurement method, using a spectrophotometer or a photoelectric spectrophotometer UV-2450 (manufactured by Shimadzu Corporation), as the transmittance at a wavelength of 700 nm, the transmittance is in the range of 80 to 100%, preferably 85 to 100%, more preferably 90 to 100%.

[0095] Here, the transmittance of water is taken as 100%. The solubilized composition of the present invention exhibits a transparent to semi-transparent appearance. The method for measuring the transmittance is, in more detail, the 16th revised Japanese Pharmacopoeia [B] General Test Methods 2. Physical Test Methods Spectrophotometric Methods 2.24 Ultraviolet-Visible Absorbance Measurement measurement. measurement. measurement. measurement. measurement. measurement. measurement. It conforms to the method described in the law.

[0096] [Viscosity] When the external composition of the present invention is used, especially when used for application to the skin, it can be prepared as a composition having an appropriate viscosity as desired. The external composition of the present invention The viscosity is not particularly limited. For example, when measured at 25 °C using an E-type viscometer, the vis cosity is usually about 1 to 300 mPa·s, preferably about 1 to 200 mPa·s, more preferably about 1 to 100 mPa·s, and most preferably about 1 to 50 mPa·s. The method for measuring viscosity is more specifically described in the 16th revised Japanese Pharmacopoeia [B] General Test Methods 2. Physical Test Methods Other Physical Test Methods 2.53 Viscosity Measurement Method 2. Method 2 Rotational Viscometer Method 2.1.3 It conforms to the method described in the conical - plate type rotational viscometer (cone - plate type viscometer).

[0097] [Use] The external composition of the present invention is particularly effective as a whitening agent, anti - inflammatory agent, and anti - aging agent. For example, it has the effects of preventing and treating acne and antioxidation. Furthermore, when applied to the skin, it can enhance the transparency of the skin, retain moisture, improve texture, and suppress roughness. In some cases it can also have effects such as making pores less noticeable and skin conditioning and moisturizing. In addition, it can also be used for the prevention and treatment of stains.

[0098] The external composition of the present invention includes, for example, basic cosmetics such as skin - care lotions, lotions, sunscreens, emulsions, creams, lotions, oils, and packs; makeup cosmetics such as foundations, lipsticks, lip creams, mascaras, eyeshadows, eyeliners, eyebrow pencils, and nail cosmetics; cosmetics for cleansing such as facial cleansers, cleansing agents, and body washes; antiperspirants, athlete's foot treatments, and sedatives ​ Itching agents, wound healing agents, wiping agents, cleaning agents, anti-inflammatory and analgesic agents, acne treatment agents, agents for hemorrhoids, bactericidal and disinfectant agents and belong to the fields of cosmetics, external pharmaceuticals or quasi-drugs, such as whitening agents, ultraviolet protectants, etc. They can be made into various external compositions. From the perspective of the effects on the skin, the present invention is preferably used in products applied to the outer skin such as skin external agents (preparations for external skin use).

[0099] [Stabilization method] Furthermore, the present invention also includes at least one stabilization method selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid. In the present invention, according to the stabilization method of ascorbic acid, at least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid is 10 to 25% by mass; (B) a diol having 3 carbon atoms is 30 to 90% by mass in components other than (A) and ( C); and (C) water is contained, the content of ethoxydiglycol is less than 30% by mass, (C) / (A) = 0.2 to 5, and the pH is 2.0 to 6.0. By doing so, a stable preparation can be obtained while containing ascorbic acid. That is, the present invention provides a method for imparting stability to an external composition containing at least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid, wherein at least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid is 10 to 25% by mass; (B) a diol having 3 carbon atoms is 30 to 90% by mass in components other than (A) and (C ); and (C) water is contained, the content of ethoxydiglycol is less than 30% by mass, (C) / (A) = 0.2 to 5, and the pH is 2.0 to 6.0. By doing so, stability is imparted to an external composition containing at least one selected from the group consisting of (A) ascorbic acid and salts of ascorbic acid. Here, stabilization means, but is not limited to, for example, ensuring stability even at high temperatures or low temperatures. Specifically, the composition for external use is preserved at least for one week at 4°C. The precipitation of ascorbic acid or its salts is inhibited, or the product is stored at 50°C or at 40°C. This refers to the fact that changes in appearance, such as discoloration, are suppressed even after a certain period of storage.

[0100] In the method of the present invention, (A) a compound selected from the group consisting of ascorbic acid and salts of ascorbic acid (B) at least one selected from the group consisting of a diol having 3 carbon atoms, and (C) water and an ethoxylated isopropanol. The content and ratio of cyclodextrin are the same as those used in the above-mentioned topical composition. Furthermore, the material obtained by this method can be divided into one or several times a day depending on the purpose. and can be used in known or customary dosages and administration. EXAMPLES

[0101] The present invention will now be described in detail 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 %.

[0102] The topical compositions shown in Tables 1 to 6 were prepared in a conventional manner. These compositions were then subjected to testing.

[0103] [Ascorbic acid color inhibition confirmation test] After storage at 40° C. or 50° C. of topical compositions according to some examples and comparative examples of the present invention The coloring of the product was suppressed by visual inspection and a color difference meter. Ascorbic acid was added to the mixed solution of each component according to the formula (mass%), and the mixture was heated at 60°C for 10 The composition was prepared by heating and mixing for 10 minutes to dissolve the components. Filled and left standing in each thermo-hygrostat at 40 °C or 50 °C for 1 week (denoted as 1W) or 4 weeks (denoted as 4W). The container was taken out of the thermo-hygrostat every measurement period, equilibrated at 25 °C, and then evaluated. The presence or absence and degree of coloring of each test solution were determined by visual observation and measurement with a color difference meter.

[0104] For the measurement with a color difference meter, 1 mL of the test solution was placed in a glass cell (CM-A97, thickness 2 mm), and the b value was measured with a spectrophotometer CM-5 (manufactured by Konica Minolta Inc.). The measured value used Δb* when purified water was used as a blank. The change in color difference was calculated by the following formula. (Change in color difference (Δb value)) = (Measured value of the test solution after heat preservation (b value after accelerated test)) - (Measured value of the test solution before heat preservation (b value before accelerated test)) The b value is used as an index indicating transparency. Therefore, the smaller the Δb value, the less coloring. Also, if the ratio of Δb between the two is 1.4 or less, the difference in coloring is not felt so much. On the other hand, when it exceeds 1.4, the difference in coloring can be clearly seen visually, and it was found that it may cause inconvenience to the quality. Therefore, the presence or absence of coloring was determined by whether the ratio was 1.4 or less when the Δb value of the sample with no change in coloring was set to 1.

[0105] [Ascorbic acid precipitation inhibition confirmation test] The presence or absence of ascorbic acid precipitation was visually evaluated for the external compositions according to some examples and comparative examples of the present invention when the preparations were stored at low temperature. Specifically, according to the formulations (mass %) described in various formulation tables, ascorbic acid was added to a mixed solution of various components, heated and mixed at 60 °C for 10 minutes to dissolve, and the composition was prepared. The prepared composition was filled into a transparent glass bottle. The test solutions were then stored in a dark place at 4℃ for one or four weeks, after which they were visually observed. The presence or absence of crystal precipitation was judged.

[0106] <Evaluation criteria> ◯: No precipitate was visible to the naked eye. ×: Precipitates were visible to the naked eye.

[0107] [Ascorbic acid percutaneous absorption test] The transdermal absorbability of the topical compositions according to some examples of the present invention and comparative examples was examined. The improved absorption allows ascorbic acid to penetrate deep into the skin, This is expected to have a greater anti-aging effect. It is possible for ascorbic acid to exert its effects up to

[0108] The percutaneous absorption of ascorbic acid from the topical compositions prepared in the Examples and Comparative Examples was evaluated using a corneal swabs. This was confirmed by measuring it by layer stripping evaluation.

[0109] Specifically, first, the aspartate complex of the component that penetrated into the skin of the upper arm and forearm of a healthy human was examined in the stratum corneum. Corbic acid levels were confirmed by tape stripping. The subjects were two healthy male subjects with a 1.5 cm x 1. A cotton pad soaked with 750 μL of the topical composition of the Example or Comparative Example was applied to the area 5 cm away from the skin. After removing the cotton, the remaining sample on the skin surface was removed with a new cotton pad. The sample was then left to stand for 30 minutes. This time was the sample penetration time. Using a tape strip (manufactured by Sumitomo 3M), tape strips were performed 7 times consecutively from the application site to measure keratinocytes. The entire layer of the tape was used as a sample for measurement. Through preliminary tests, it was set to ensure that the required amount of keratinocytes was peeled off for each tape strip and that no inflammation or pain occurred after the tape stripping.

[0110] The obtained measurement specimens were extracted with 1 mL of an extraction solvent which was a mixed solution of Tritonx-100 (manufactured by MP Biomedicals), mercaptoethanol (manufactured by Wako Pure Chemical Industries, Ltd.) and purified water (1:1:1000). The penetration amount (μg / cm ) of ascorbic acid was measured by HPLC from the extraction solution from which foreign matters were removed using a 0.45 μm syringe filter (manufactured by GL Sciences Inc.). 2 ) It was measured by HPLC. The HPLC manufactured by Agilent equipped with a reversed-phase column (CAPCELL PAK C18 SG120, manufactured by Shiseido Co., Ltd.) (mobile phase: acetonitrile / 0.02 M phosphoric acid solution (pH 3.0) (1:9), detection wavelength of absorbance: 270 nm) was used to measure the amount of L-ascorbic acid contained in the solution. The results were compared as the penetration amount (μg / cm ) by averaging the measured values of the measurement specimens collected from three locations on each arm of two subjects. 2 )

[0111] In addition, the detection of ascorbic acid by HPLC was performed using an ultraviolet absorption photometer at a wavelength of 270 nm using a reversed-phase column (CAPCELL PAK C18 SG120, manufactured by Shiseido Co., Ltd.), and the content was calculated from the calibration curve.

[0112] (Examples 1-1 to 1-6, Comparative Examples 1-1 to 1-3) External compositions of the examples and comparative examples having the compositions shown in Table 1 were prepared according to a conventional method. Among the evaluation items, for the ratio of Δb, taking the color difference value of the external composition in Example 1-1 as the reference (1), the comparison It describes the ratio of the value. That is, the stability ratio represents the ratio of Δb.

[0113] The results of the ascorbic acid coloring inhibition confirmation tests of the compositions of the examples and comparative examples are shown together in Table 1 and Table 2.

[0114]

Table 1

[0115]

Table 2

[0116] The composition of the example had an effect of inhibiting coloring even when stored under high temperature conditions, and showed excellent stability over a long period. On the other hand, coloring was observed in the composition of the comparative example under the storage conditions of the test.

[0117] (Examples 2-1 to 2-2, Comparative Example 2-1) External compositions of the examples and comparative examples having the compositions shown in Table 3 were prepared according to a conventional method. Among the evaluation items, for the ratio of Δb, taking the color difference value of the external composition in Example 2-1 as the reference (1), the ratio of the comparative value is described. That is, the stability ratio represents the ratio when the value of Δb in Example 2-1 is set to 1.

[0118] The results of the ascorbic acid coloring inhibition confirmation test and the results of the ascorbic acid precipitation inhibition confirmation test of the compositions of the examples and comparative examples are shown together in Table 3.

[0119]

Table 3

[0120] That is, the composition shown in the example has the effects of inhibiting the precipitation of ascorbic acid and inhibiting the coloring of the composition. It can be seen that the compatibility of both properties has been achieved.

[0121] (Examples 3-1 to 3-3, Comparative Examples 3-1 to 3-2) External compositions of the examples and comparative examples having the compositions shown in Table 4 were prepared according to a conventional method.

[0122] The results of the ascorbic acid coloring inhibition confirmation test and the ascorbic acid precipitation inhibition confirmation test of the compositions of the examples and comparative examples are shown together in Table 4.

[0123]

Table 4

[0124] (Examples 4-1 to 4-3, Comparative Examples 4-1 to 4-2) External compositions of the examples and comparative examples having the compositions shown in Table 5 were prepared according to a conventional method.

[0125] The results of the ascorbic acid coloring inhibition confirmation test and the ascorbic acid precipitation inhibition confirmation test of the compositions of the examples and comparative examples are shown together in Table 4. Among the evaluation items, the ratio of Δb is described as the ratio of the comparative value with the color difference value of the external composition in Example 4-1 as the reference (1). That is, the stability ratio represents the ratio when the Δb value of Example 4-1 is set to 1.

[0126]

Table 5

[0127] It was found that the compositions shown in the examples achieved the compatibility of both the inhibition of ascorbic acid precipitation at low temperatures and the inhibition of coloring of the composition. For example, when ethoxydiglycol was at a high concentration of 4 0 mass% or more, precipitation was observed particularly at low temperatures with a lower pH. When the pH was slightly ​In the enhanced formulation, no precipitation was observed at low temperatures even at high concentrations of ethoxydiglycol. However, when the concentration was 30% by mass or more, it was found that the degree of coloring was clearly high. From this, it is preferable that the content of ethoxydiglycol is less than 30% by mass even if it is blended.

[0128] Furthermore, Table 6 shows the results of the ascorbic acid coloring suppression confirmation test, the ascorbic acid precipitation suppression confirmation test, and the percutaneous absorption test for the compositions of another example and comparative example. Among the evaluation items, the ratio of Δb is described as the ratio of the comparative value with the color difference value of the external composition in Example 5-1 as the reference (1). That is, the stability ratio represents the ratio when the Δb value of Example 5-1 is set to 1.

[0129]

Table 6

[0130] The composition of the example can suppress the precipitation of ascorbic acid even under low-temperature storage, and it was found that both properties of suppressing the coloring of the composition during storage were achieved. Furthermore, it was found that the composition of the present invention is also excellent in percutaneous absorbability.

[0131] The results of the percutaneous absorbability of the compositions of Examples 5-1 to 5-2 and Comparative Examples 5-1 to 5-2 are shown in FIG. 1.

[0132] Next, external compositions having the compositions shown in Tables 7 to 9 were prepared according to a conventional method. Then, these compositions were subjected to tests according to each test item.

[0133] [Ascorbic acid coloring suppression confirmation test] The presence or absence of suppression of coloring after storage at 40 ° C or 50 ° C of the external compositions having the compositions shown in Tables 7 to 9​​​​​​​​​ The evaluation was carried out visually and with a color difference meter. Specifically, the method was the same as that used in Examples 1 to 5 and Comparative Examples 1 to 5. The confirmation test was carried out in exactly the same way.

[0134] [Ascorbic acid precipitation inhibition confirmation test] The presence or absence of ascorbic acid precipitation was visually evaluated when the external composition with the composition shown in Tables 7 to 9 was stored at low temperature. Specifically, the method was the same as that used in Examples 1 to 5 and Comparative Examples 1 to 5. and the confirmation test was carried out in exactly the same way.

[0135] [Ascorbic acid percutaneous absorption test] The percutaneous absorption of the external composition according to some examples and comparative examples of the second invention was verified. By improving percutaneous absorption, ascorbic acid penetrates into the skin, and a higher anti-aging effect is expected as a composition. That is, in some cases, it becomes possible to exert the effect of ascorbic acid deep into the stratum corneum.

[0136] The percutaneous absorption of ascorbic acid in the external compositions prepared in the examples and comparative examples was confirmed by measuring it by evaluation using stratum corneum stripping. Specifically, the confirmation test was carried out in exactly the same way as the method used in Examples 1 to 5 and Comparative Examples 1 to 5.

[0137] (Examples 6-1 to 8-1, Comparative Examples 6-2 to 8-3) The external compositions of the examples and comparative examples with the composition shown in Table 7 were prepared according to a conventional method. Among the evaluation items in the same table, the ratio of Δb is described as the ratio of the comparison value with the color difference value of the external composition in Example 1 as the reference (1). That is, the ratio of stability is represented by the ratio of Δb. Also, the ratio described in the column of the percutaneous absorption test results of the external compositions of the examples and comparative examples is 1,3-butylene glycol. ​​​The percutaneous absorption amount of Comparative Example 5-1 (Formulation 40) formulated based on recall is taken as 1, and the value is obtained by ratio. It is a value obtained by ratio. Ratio = (Percutaneous absorption amount (μg / cm 2 ) of the composition of any one of the Examples and Comparative Examples) / (Percutaneous absorption amount (μg / cm ) of the composition of Comparative Example 5- 2 1)

[0138] The results of each test of the compositions of the Examples and Comparative Examples are shown in Tables 7 to 9 together.

[0139]

Table 7

[0140]

Table 8

[0141]

Table 9

[0142] The composition of the Example had an effect of suppressing coloring even when stored under high temperature conditions, and showed excellent stability over a long period. On the other hand, coloring was observed in the composition of the Comparative Example under the storage conditions of the test. Also, the precipitation at low temperature of the composition of the Example was suppressed as compared with the composition of the Comparative Example.

[0143] [Formulation Example] Formulation Examples are shown in Tables 10 to 12 below. All of the Formulation Examples can be suitably used for lotions, skin conditioners, etc. The contents in the Formulation Examples are all in mass%.

[0144]

Table 10

[0145]

Table 11

[0146]

Table 12

Claims

【Claim 1】 The invention described in the specification.

Citation Information

Patent Citations

  • Ascorbic acid-containing composition for outer skin

    JP2002348228A

  • Skin care preparation for external use

    JP2005225865A

  • Stable l-ascorbic acid composition

    WO2000078283A1

  • Stabilized ascorbic acid solutions

    WO2002019972A2