External composition containing ascorbic acid and / or its salts

Abstract

To provide an external composition that contains ascorbic acid or a salt thereof, diol with carbon number 3 and water, and in which turbidity by a fragrance material is suppressed even if the content of ethoxydiglycol is less than 20 mass%.SOLUTION: An external composition contains (A) at least one selected from a group consisting of ascorbic acid and a salt of ascorbic acid, (B) diol with carbon number 3, (C) water, (D) fruit-based fragrance material, and (E) alkylene oxide derivative expressed by formula (I), in which the content of ethoxydiglycol is less than 20 mass%.SELECTED DRAWING: Figure 1

Description

[Technical Field]

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

[0002] Ascorbic acid is known to exhibit various effects, including anti-inflammatory effects, acne-improving effects, skin whitening effects, anti-aging effects, antioxidant effects, cell-activating effects by promoting the synthesis of biocomponents such as collagen, and effects that suppress UV-induced cell damage and DNA damage to epidermal keratinocytes. For these reasons, it is widely used as a topical skin preparation.

[0003] Several methods have been investigated for stably solubilizing ascorbic acid in aqueous topical skin preparations (for example, Patent Document 1).

[0004] On the other hand, in the case of solution-type quasi-drugs and cosmetics, highly transparent solutions are sometimes preferred for purposes such as improving the aesthetic appearance of the solution or giving it an appearance that matches the product concept, such as "transparency." [Prior art documents] [Patent Documents]

[0005] [Patent Document 1] WO2018 / 003850 publication [Overview of the project] [Problems that the invention aims to solve]

[0006] The inventors have found that when a solution containing a three-carbon diol and water, and with an ethoxydiglycol content of less than 20% by mass, exhibits excellent stability even when containing ascorbic acid or a salt thereof, however, the addition of fruit-based flavorings tends to cause turbidity and impair the transparency of the solution.

[0007] Therefore, the present invention relates to providing an external composition containing ascorbic acid or a salt thereof, a three-carbon diol, and water, in which turbidity caused by fruit-based fragrances is suppressed even when the ethoxydiglycol content is less than 20% by mass. [Means for solving the problem]

[0008] As a result of diligent research, the inventors of this invention have concluded that We discovered that when (A) at least one selected from the group consisting of ascorbic acid and salts of ascorbic acid, (B) a diol having 3 carbon atoms, (C) water, (D) a fruit-based fragrance, and (E) a specific alkylene oxide derivative are present together, turbidity of the topical composition due to the fruit-based fragrance is suppressed even when the ethoxydiglycol content is less than 20% by mass, leading to the present invention.

[0009] In other words, the present invention provides the following external compositions. Section 1. (A) At least one selected from the group consisting of ascorbic acid and salts of ascorbic acid, (B) A diol with 3 carbon atoms, (C) Water; (D) Fruit flavorings, and (E) Equation (I): R1-O-[(AO) m (EO) n ]-H(wherein, R 1 is a hydrocarbon group having 16 or more carbon atoms, AO is an oxyalkylene group having 3 to 4 carbon atoms, EO is an oxyethylene group, m and n are the average number of moles of oxyalkylene and oxyethylene groups added, respectively, where m≧0 and n≧1, and the oxyalkylene and oxyethylene groups may be added in a block-like or random manner, and the molecular weight of the R1 portion is W. R1 The ratio of n to W R1 Alkylene oxide derivatives represented by (but with a coefficient of 0.088 or less) An external composition containing a substance and having an ethoxydiglycol content of less than 20% by mass. Section 2. The topical composition according to item 1, wherein the content of component (A) is 1 to 30% by mass. Item 3. The external composition according to Item 1 or 2, wherein the content of the component (B) is 1 to 80% by mass. Item 4. The external composition according to any one of Items 1 to 3, wherein the content of the component (C) is 1 to 50% by mass. Item 5. The external composition according to any one of Items 1 to 4, wherein the content of the component (D) is 0.0001 to 2% by mass. Item 6. The external composition according to any one of Items 1 to 5, wherein the content of the component (E) is 0.01 to 3% by mass. Item 7. The external composition according to any one of Items 1 to 6, wherein the AO of the component (E) is an oxypropylene group. Item 8. The external composition according to any one of Items 1 to 7, further containing (F) a lower alcohol. Item 9. The external composition according to any one of Items 1 to 8, wherein the lightness L value in the CIELAB color system is 99.5 or more. Item 10. The external composition according to any one of Items 1 to 9, wherein the pH is 2 to 5.

[0010] In addition, the present invention provides a method for solubilizing the following fruit-based fragrance. Item 11. (A) At least one selected from the group consisting of ascorbic acid and salts of ascorbic acid, (B) A diol having 3 carbon atoms, (C) Water, and (D) A fruit-based fragrance containing, in an external composition wherein the content of ethoxydiglycol is less than 20% by mass, (E) Formula (I): R1 - O - [(AO) m (EO) n -H (wherein R 1The hydrocarbon group has 16 or more carbon atoms, AO is an oxyalkylene group having 3 to 4 carbon atoms, EO is an oxyethylene group, m and n are the average number of moles of addition of an oxyalkylene group having 3 to 4 carbon atoms and an oxyethylene group, respectively, m≧0, n≧1, and the oxyalkylene group and the oxyethylene group may be added in a block form or in a random form. The molecular weight W of the R1 part R1 The ratio n / W of n to R1 is 0.088 or less), and a method for solubilizing a fruit-based fragrance, characterized by coexisting an alkylene oxide derivative represented by [Advantages of the Invention]

[0011] According to the present invention, a highly transparent external composition with suppressed turbidity due to a fruit-based fragrance can be obtained. [Brief Description of the Drawings]

[0012] [Figure 1] It is a photograph of the appearance of Comparative Example 7 and Example 1 after standing at 25°C for 1 day after preparation in Test Example 1. [Embodiments for Carrying Out the Invention]

[0013] In this specification, the unit "mass%" of the content is synonymous with "g / 100g".

[0014] [External Composition] 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, (C) water, (D) a fruit-based fragrance, and (E) a specific alkylene oxide derivative.

[0015] ((A) At least one selected from the group consisting of ascorbic acid and salts of ascorbic acid) As the ascorbic acid used in the present invention, ascorbic acid commercially available as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics can be used, and these generally refer to L-forms, although not limited thereto.

[0016] Salts of ascorbic acid can also be used. Here, a salt of ascorbic acid is a pharmaceutically acceptable salt. While not limited to these, examples include salts with organic bases (e.g., salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, etc., and basic ammonium salts such as arginine), and salts with inorganic bases (e.g., alkali metal salts such as ammonium salt, sodium salt, potassium salt, alkaline earth metal salts such as calcium salt, magnesium salt, aluminum salt, etc.). Preferred salts of ascorbic acid are sodium salt or potassium salt.

[0017] In the present invention, ascorbic acid and its salts can be used individually or in combination of two or more. From the viewpoint of significantly achieving the effects of the present invention, ascorbic acid is preferred.

[0018] Ascorbic acid or its salts may be synthesized or commercially available.

[0019] In the topical composition of the present invention, the total content of component (A) is appropriately set in balance with other components. From the viewpoint of imparting functions such as whitening, anti-inflammatory, anti-aging, and antioxidant, the total content of component (A) is preferably 1% by mass or more, more preferably 5% by mass or more, and even more preferably 10% by mass or more, based on the total amount of the topical composition. Furthermore, from the viewpoint of ensuring good stability of component (A), the total content of component (A) is preferably 30% by mass or less, more preferably 27% by mass or less, and even more preferably 25% by mass or less, based on the total amount of the topical composition.

[0020] In the topical composition of the present invention, the total content of component (A) is preferably 1 to 30% by mass, more preferably 5 to 27% by mass, and even more preferably 10 to 25% by mass, based on the total amount of the topical composition.

[0021] ((B) Diol with 3 carbon atoms) The three-carbon diol used in the present invention is not particularly limited as long as it is used as an ingredient in topical preparations in the fields of pharmaceuticals, quasi-drugs, or cosmetics. In addition, commercially available three-carbon diols can be used as is. While not limited, examples of three-carbon diols include 1,3-propanediol (CAS number: 504-63-2, English name: 1,3-Dihydroxypropane or TrimethyleneGlycol) or propylene glycol (CAS number: 57-55-6, English name: 1,2-Dihydroxypropane, Japanese alternative name: 1,2-propanediol), and one type may be used or a combination may be used as appropriate. It is preferable that component (B) contains at least 1,3-propanediol. For example, from the viewpoint of reducing skin irritation, improving usability, and suppressing discoloration, combining 1,3-propanediol and propylene glycol is one preferred embodiment.

[0022] In the topical composition of the present invention, the total content of component (B) is preferably 1% by mass or more, more preferably 5% by mass or more, even more preferably 10% by mass or more, even more preferably 15% by mass or more, and particularly preferably 20% by mass or more, based on the total amount of the topical composition, from the viewpoint of ensuring good stability of ascorbic acid and its salts. Furthermore, the total content of component (B) is preferably 80% by mass or less, more preferably 75% by mass or less, even more preferably 70% by mass or less, even more preferably 65% ​​by mass or less, and particularly preferably 60% by mass or less, based on the total amount of the topical composition.

[0023] In the topical composition of the present invention, the total content of component (B) is preferably 1 to 80% by mass, more preferably 5 to 75% by mass, even more preferably 10 to 70% by mass, even more preferably 15 to 65% by mass, and particularly preferably 20 to 60% by mass, based on the total amount of the topical composition, from the viewpoint of ensuring good stability of ascorbic acid and its salts.

[0024] (B) The content of 1,3-propanediol in component (B) is preferably 10% by mass or more, more preferably 20% by mass or more, and even more preferably 25% by mass or more, based on the total amount of the topical composition. Furthermore, the content of 1,3-propanediol is preferably 70% by mass or less, more preferably 65% ​​by mass or less, and even more preferably 60% by mass or less, based on the total amount of the topical composition. The content of 1,3-propanediol is preferably 10 to 70% by mass, more preferably 20 to 65% by mass, and even more preferably 25 to 60% by mass, based on the total amount of the topical composition.

[0025] (B) Of the components, the propylene glycol content is preferably 1% by mass or more, more preferably 3% by mass or more, and even more preferably 5% by mass or more, based on the total amount of the topical composition. Furthermore, the propylene glycol content is preferably 20% by mass or less, more preferably 15% by mass or less, and even more preferably 10% by mass or less, based on the total amount of the topical composition. The propylene glycol content is preferably 1 to 20% by mass, more preferably 3 to 15% by mass, and even more preferably 5 to 10% by mass, based on the total amount of the topical composition.

[0026] ((C)Water) The topical skin composition of the present invention contains water. The amount of water relative to the total amount of the topical composition is not particularly limited, but from the viewpoint of ensuring good stability of ascorbic acid and its salts, it is preferably 1 to 50% by mass, more preferably 3 to 40% by mass, and even more preferably 5 to 30% by mass.

[0027] ((D) Fruit-based fragrance) The fruit-based fragrance used in the present invention is not particularly limited as long as it is a fragrance having a fruit-like flavor and is used as an ingredient in topical skin preparations in pharmaceuticals, quasi-drugs, or cosmetics. The fruit-based fragrance may be a natural fragrance or a synthetic fragrance, but it is preferable that it contains essential oils or oil-soluble components.

[0028] Examples of fruit-based flavorings include citrus flavorings, peach flavorings, cherry flavorings, and apple flavorings, but citrus flavorings are preferred among them.

[0029] Citrus fragrances include extracts from citrus plants or fragrances that have the flavor of citrus plants. Citrus plants are plants belonging to the Rutaceae family, Rutiaceae subfamily, and Citrus tribe. Such plants include oranges, lemons, grapefruits, sudachi, limes, yuzu, kabosu, bergamot, tangerines, mandarins, shikwasa, ponkan, pomelo, hassaku, jabara, tankan, and iyokan.

[0030] Citrus fragrances may use extracts of citrus plants in particular, and extracts of the fruit or peel are especially preferred. Such fragrances are not limited to those containing citrus essential oils such as orange oil, lemon oil, grapefruit oil, sudachi oil, lime oil, yuzu oil, kabosu oil, and shikwasa oil.

[0031] Citrus fragrances are preferably manufactured and used by blending at least one oil-soluble component selected from the group consisting of limonene, limonin, nomilin, β-pinene, γ-terpinene, citral, α-pinene, auraptene, nobiletin, linalool, linalyl acetate, ionone, thymol, and perillaldehyde. These components can also be used as salts or derivatives. Here, salts are not particularly limited, but examples include salts with organic bases (e.g., salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt, basic ammonium salts such as arginine), salts with inorganic bases (e.g., alkali metal salts such as ammonium salt, sodium salt, potassium salt, alkaline earth metal salts such as calcium salt, magnesium salt, aluminum salt, etc.). Derivatives include acetic acid derivatives. Particularly preferred salts are sodium salt and potassium salt.

[0032] In the topical composition of the present invention, the total content of component (D) relative to the total amount of the topical composition is appropriately set in balance with other components. From the viewpoint of significantly achieving the effects of the present invention, the total content of component (D) is preferably 0.0001% by mass or more, more preferably 0.001% by mass or more, even more preferably 0.01% by mass or more, even more preferably 0.05% by mass or more, and particularly preferably 0.1% by mass or more, relative to the total amount of the topical composition. Furthermore, from the viewpoint of significantly achieving the effects of the present invention, the total content of component (D) is preferably 2% by mass or less, more preferably 1.5% by mass or less, even more preferably 1% by mass or less, even more preferably 0.8% by mass or less, and particularly preferably 0.6% by mass or less, relative to the total amount of the topical composition.

[0033] In the topical composition of the present invention, the total content of component (D) is preferably 0.0001 to 2% by mass, more preferably 0.001 to 1.5% by mass, even more preferably 0.01 to 1% by mass, even more preferably 0.05 to 0.8% by mass, and particularly preferably 0.1 to 0.6% by mass, based on the total amount of the topical composition, from the viewpoint of significantly exhibiting the effects of the present invention.

[0034] ((E) Alkylene oxide derivatives) The topical composition of the present invention comprises, as component (E), formula (I): R1-O-[(AO) m (EO) n ]-H(wherein, R 1 is a hydrocarbon group having 16 or more carbon atoms, AO is an oxyalkylene group having 3 to 4 carbon atoms, EO is an oxyethylene group, m and n are the average number of moles of oxyalkylene and oxyethylene groups added, respectively, where m≧0 and n≧1, and the oxyalkylene and oxyethylene groups may be added in a block-like or random manner, and the molecular weight of the R1 portion is W. R1 n / W is the ratio of n to the total. R1 It contains an alkylene oxide derivative represented by (0.088 or less). The oxyalkylene derivative of component (E) is preferred in that it solubilizes fruit fragrances while minimizing skin irritation.

[0035] From the viewpoint of significantly achieving the effects of the present invention, the number of carbon atoms in the hydrocarbon group R1 is 16 or more, preferably 18 or more. The number of carbon atoms in the hydrocarbon group R1 may be, for example, 30 or less, 28 or less, 26 or less, or 24 or less. From the viewpoint of significantly achieving the effects of the present invention, a carbon atom count of 18 in the hydrocarbon group R1 is particularly preferred.

[0036] The hydrocarbon group of R1 may include one or more combinations selected from the group consisting of linear or branched aliphatic hydrocarbon groups, alicyclic hydrocarbon groups (such as cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl groups), and aromatic hydrocarbon groups (such as phenyl and naphthyl groups). R1 is preferably composed of a linear or branched aliphatic hydrocarbon group. In this case, it may have double or triple bonds, but the total number of double and triple bonds is preferably 3 or less, more preferably 2 or less, and even more preferably 1 or less.

[0037] (E) Suitable examples of the R1-O- moiety of component (E) include, for example, the R1-OH compounds cetanol (1-hexadecanol), palmitrail alcohol (cis-9-hexadecene-1-ol), 1-heptadecanol, stearyl alcohol (1-octadecanol), isostearyl alcohol (16-methylheptadecene-1-ol), elaidyl alcohol (9E-octadecene-1-ol), oleyl alcohol (cis-9-octadecene-1-ol), linoleyl alcohol (9Z,12Z-octadecadiene-1-ol), elidelinoleyl alcohol (9E,12E-octadecadiene-1-ol), linolenyl alcohol (9Z,12Z,15Z-octadecadiene-1-ol), elidelinolenyl alcohol (9E,12E,15E Examples include the portion obtained by removing the hydrogen atom from the hydroxyl group of (-octadecatriene-1-ol), ricinoleyl alcohol (12-hydroxy-9-octadecene-1-ol), nonadecyl alcohol, arachidyl alcohol (1-eicosanol), heneicosanol, behenyl alcohol (1-docosanol), erucyl alcohol (cis-13-docosen-1-ol), decyltetradecanol (2-decyl-1-tetradecanol), lignoceryl alcohol (1-tetracosanol), ceryl alcohol (1-hexacosanol), 1-heptacosanol, montanyl alcohol (1-octacosanol), 1-nonacosanol, myricyl alcohol (1-triacontanol), 1-dotriacontanol, or gezyl alcohol (1-tetratriacontanol).

[0038] In component (E), the above-mentioned R1 and R1-O- portions may be a single type or a mixture of two or more types.

[0039] The above AO is an oxyalkylene group having 3 to 4 carbon atoms, and examples include an oxypropylene group (abbreviated as PO), an oxybutylene group, an oxyisobutylene group, an oxytrimethylene group, an oxytetramethylene group, and preferably an oxypropylene group and / or an oxybutylene group, and more preferably an oxypropylene group.

[0040] The average number of moles of AO added, m, is 0 or greater, and can be, for example, 1 or greater, 5 or greater, or 10 or greater. Furthermore, m can be, for example, 35 or less, 30 or less, 25 or less, or 20 or less.

[0041] The average number of moles of EO added, n, is 1 or more. Furthermore, from the viewpoint of achieving the effects of the present invention, n is preferably 2 or more, more preferably 5 or more, and even more preferably 10 or more. And n may be, for example, 40 or less, 30 or less, 25 or less, or 24 or less.

[0042] The sum of the average number of added moles of AO and EO, m+n, is preferably 50 or less from the viewpoint of significantly achieving the effects of the present invention, and can be, for example, 45 or less, 40 or less, or 37 or less. In addition, m+n can be, for example, 1 or more, 2 or more, 3 or more, 5 or more, or 10 or more.

[0043] In this specification, the molecular weight of the R1 portion of the above formula (I) is defined as W R1 [(AO) m (EO) n The molecular weight of the portion (which may be referred to as R2 in this specification) is W R2 Let's assume that.

[0044] (E) n / W R1 From the viewpoint of significantly achieving the effects of the present invention, the n / W of component (E) is 0.088 or less, for example, 0.085 or less, 0.08 or less, 0.075 or less, or 0.071 or less. R1 For example, this could be 0.003 or higher, 0.005 or higher, 0.008 or higher, 0.01 or higher, 0.015 or higher, 0.02 or higher, 0.025 or higher, or 0.03 or higher.

[0045] In the topical composition of the present invention, component (E) W R2 / W R1 For example, it could be 4.8 or less, 4.6 or less, 4 or less, 3.8 or less, 3.6 or less, 2.5 or less, or 2 or less. And W R2 / W R1For example, this could be 1 or more, 1.1 or more, 1.2 or more, 1.3 or more, 1.4 or more, 1.5 or more, or 1.6 or more, or 1.7 or more.

[0046] (E) Among the compounds containing PO and / or EO, ​​(m+n) / W R1 This could be, for example, 0.11 or less, 0.1 or less, 0.09 or less, 0.08 or less, 0.05 or less, or 0.04 or less. And (m+n) / W R1 For example, this could be 0.003 or higher, 0.005 or higher, 0.008 or higher, 0.01 or higher, 0.015 or higher, 0.02 or higher, 0.025 or higher, or 0.03 or higher.

[0047] Specific examples of alkylene oxide derivatives of component (E) include, for example, Ceteth-1, Ceteth-2, Ceteth-3, Ceteth-4, Ceteth-5, Ceteth-6, Ceteth-7, Ceteth-8, Ceteth-10, Ceteth-12, Ceteth-13, Ceteth-14, Ceteth-15, Ceteth-16, Ceteth-17, Ceteth-18, Ceteth-20; Isoceteth-5, Isoceteth-7, Isoceteth-10, Isoceteth-12, Isoceteth-15, Isoceteth-20; Oleth-2, Oleth-3, Oleth-4, Oleth-5, Oleth-6, Oleth-7, Oleth-8, Oleth-9, Oleth-10, Oleth-11, Oleth-12, Oleth-13, Oleth-15, Oleth-16, Oleth-20; Steareth-1, Steareth-2, Steareth-3, Steareth-4, Steareth-5, Steareth-6, Steareth-7, Steareth-8, Steareth-9, Steareth-10, Steareth-11, Steareth-12, Steareth-13, Steareth-14, Steareth-15, Steareth-16, Steareth-17, Steareth-18, Steareth-20, Steareth-21; Isosteareth-2, Isosteareth-3, Iso Steareth-5, Isosteareth-8, Isosteareth-10, Isosteareth-12, Isosteareth-15, Isosteareth-16, Isosteareth-20, Isosteareth-22; Octyldodeceth-2, Octyldodeceth-5, Octyldodeceth-10, Octyldodeceth-16, Octyldodeceth-20; Decyltetradeceth-5, Decyltetradeceth-10, Decyltetradeceth-15, Decyltetradeceth-20, Decyltetradeceth-25; Decylpentadeceth-5, Decylpentadeceth-10, Decylpentadeceth-1 5, Decylpentadeceth-20, Decylpentadeceth-25; PPG-1 Ceteth-1, PPG-1 Ceteth-5, PPG-1 Ceteth-10, PPG-2 Ceteth-1, PPG-2 Ceteth-5, PPG-2 Ceteth-10, PPG-2 Ceteth-12, PPG-4 Ceteth-1, PPG-4 Ceteth-5, PPG-4 Ceteth-10, PPG-8 Ceteth-1, PPG-8 Ceteth-2, PPG-8 Ceteth-5, PPG-8 Ceteth-10; PPG-9 Steareth-3, PPG-30 Steareth-4, PPG-34 Steareth-3, PPG-38 Steareth-6;This includes one or more species selected from the group consisting of PPG-6 Decyltetradeceth-12, PPG-6 Decyltetradeceth-20, PPG-20 Decyltetradeceth-10, and PPG-13 Decyltetradeceth-24.

[0048] In the topical composition of the present invention, the total content of component (E) relative to the total amount of the topical composition is appropriately set in balance with other components. From the viewpoint of significantly achieving the effects of the present invention, the total content of component (E) is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, even more preferably 0.1% by mass or more, and even more preferably 0.15% by mass or more, relative to the total amount of the topical composition. Furthermore, from the viewpoint of significantly achieving the effects of the present invention, the total content of component (E) is preferably 3% by mass or less, more preferably 2% by mass or less, even more preferably 1% by mass or less, even more preferably 0.8% by mass or less, and particularly preferably 0.6% by mass or less, relative to the total amount of the topical composition.

[0049] In the topical composition of the present invention, the total content of component (E) is preferably 0.01% to 3% by mass, more preferably 0.05% to 2% by mass, even more preferably 0.1% to 1% by mass, even more preferably 0.15% to 0.8% by mass, and particularly preferably 0.15% to 0.6% by mass, from the viewpoint of significantly exhibiting the effects of the present invention.

[0050] (Ratio of each component) In the external composition of the present invention, the total content of component (B) relative to the total content of component (A) is preferably 0.1 to 30 parts by mass, more preferably 0.3 to 25 parts by mass, and even more preferably 0.7 to 20 parts by mass, from the viewpoint of ensuring good stability of component (A).

[0051] In the external composition of the present invention, the content of propylene glycol per 1 part by mass of the total content of component (A) is preferably 0.1 to 10 parts by mass, more preferably 0.2 to 9 parts by mass, and even more preferably 0.3 to 8.5 parts by mass, from the viewpoint of ensuring good stability of component (A).

[0052] In the external composition of the present invention, the content of component (C) relative to the total content of component (A) is preferably 0.1 to 3.0 parts by mass, more preferably 0.4 to 2.6 parts by mass, and even more preferably 0.7 to 2.2 parts by mass, from the viewpoint of ensuring good stability of component (A).

[0053] In the external composition of the present invention, the total content of component (D) relative to the total content of component (A) is preferably 0.005 to 0.20 parts by mass, more preferably 0.01 to 0.15 parts by mass, and even more preferably 0.013 to 0.10 parts by mass, from the viewpoint of significantly exhibiting the effects of the present invention.

[0054] In the external composition of the present invention, the total content of component (E) relative to the total content of component (A) is preferably 0.005 to 0.45 parts by mass, more preferably 0.01 to 0.40 parts by mass, and even more preferably 0.015 to 0.35 parts by mass, from the viewpoint of significantly exhibiting the effects of the present invention.

[0055] In the external composition of the present invention, the total content of component (E) relative to the total content of component (D) is preferably 0.2 to 12.5 parts by mass, more preferably 0.3 to 11 parts by mass, and even more preferably 0.4 to 10 parts by mass, from the viewpoint of significantly exhibiting the effects of the present invention.

[0056] ((F) Lower alcohol) The topical composition of the present invention may contain lower alcohols in addition to the above-mentioned components (A) to (E), as long as they do not hinder the effects of the present invention, from the viewpoint of improving usability, stability, and promoting transdermal absorption. The lower alcohols used in the present invention are not particularly limited as long as they are used as components of topical skin preparations in the fields of pharmaceuticals, quasi-drugs, or cosmetics. In this specification, "lower alcohol" refers to C1 to C6 alcohols. Of these, C1 to C3 alcohols can be used particularly preferably. As such examples, ethanol is preferred, but methanol, n-propanol, isopropanol, etc. can also be used.

[0057] In the topical composition of the present invention, the total content of lower alcohols, if present, is preferably 0.01% by mass or more, more preferably 0.1% by mass or more, even more preferably 0.5% by mass or more, even more preferably 1% by mass or more, and particularly preferably 3% by mass or more, based on the total amount of the topical composition. Furthermore, the content of lower alcohols is preferably 50% by mass or less, more preferably 45% by mass or less, even more preferably 40% by mass or less, and even more preferably 35% by mass or less, based on the total amount of the topical composition.

[0058] The total content of lower alcohols in the topical composition of the present invention is preferably 0.01 to 50% by mass, more preferably 0.1 to 45% by mass, even more preferably 0.5 to 40% by mass, even more preferably 1 to 35% by mass, and particularly preferably 3 to 35% by mass, based on the total amount of the topical composition.

[0059] (Butylene glycol) In addition to the above components (A) to (F), the topical composition of the present invention may further contain butylene glycol (also called 1,3-butylene glycol or 1,3-butanediol) from the viewpoint of improving usability, stability, and promoting transdermal absorption.

[0060] In the topical composition of the present invention, the content of butylene glycol, when included, is preferably 0.01% by mass or more, more preferably 0.1% by mass or more, and even more preferably 0.3% by mass or more, based on the total amount of the topical composition, from the viewpoint of improving usability, stability, and promoting transdermal absorption. Furthermore, the content of butylene glycol is preferably 40% by mass or less, more preferably 35% by mass or less, and even more preferably 30% by mass or less, based on the total amount of the topical composition.

[0061] The butylene glycol content in the topical composition of the present invention is preferably 0.01 to 40% by mass, more preferably 0.1 to 35% by mass, and even more preferably 0.3 to 30% by mass, based on the total amount of the topical composition.

[0062] (Ethoxydiglycol, polyethylene glycol) In addition to the above components (A) to (F) and butylene glycol, the external composition of the present invention may also contain ethoxydiglycol (diethylene glycol monoethyl ether; CAS number 110-90-0) and / or polyethylene glycol.

[0063] From the viewpoint of suppressing browning caused by component (A), the ethoxydiglycol content is preferably less than 20% by mass of the total amount of the topical composition, more preferably less than 10% by mass, even more preferably 1% by mass or less, and even more preferably 0.1% by mass or less. In some cases, the topical composition may contain substantially no or no ethoxydiglycol, such as 0.01% by mass or less. In some cases, from the viewpoint of stabilizing the oil-soluble components, the ethoxydiglycol content may be 0.1% by mass or more, or 1% by mass or more, of the total amount of the topical composition.

[0064] The polyethylene glycol referred to in this invention is not particularly limited, but for example, it has a degree of polymerization of 4 or higher and is used as a base in pharmaceuticals, quasi-drugs, and cosmetics. Specifically, it is polyethylene glycol with an average molecular weight of about 150 to 1000, and may be polyethylene glycol with an average molecular weight of about 170 to 800. Examples of such polyethylene glycols include polyethylene glycol 200, polyethylene glycol 300, polyethylene glycol 400, polyethylene glycol 500, polyethylene glycol 600, polyethylene glycol 700, polyethylene glycol 800, etc. Commercial products of these exist, so it is also possible to obtain and use these commercial products. Examples of commercial products include polyethylene glycol 200, polyethylene glycol 300, polyethylene glycol 400, polyethylene glycol 600 sold by NOF Corporation, and polyethylene glycol 200, polyethylene glycol 300, polyethylene glycol 400, polyethylene glycol 600 sold by Sanyo Chemical Industries, Ltd.

[0065] Here, the average molecular weight can be determined, for example, in accordance with the average molecular weight test described in the section on polyethylene glycol in the 2006 Standards for Raw Materials of Quasi-Drugs. <Method for measuring the average molecular weight of polyethylene glycol with an average molecular weight of 190-210> Precisely weigh approximately 0.8 g of polyethylene glycol and place it in a 200 mL pressure-resistant stoppered bottle. Add approximately 25 mL of pyridine, heat to dissolve, and allow to cool. Separately, take 42 g of phthalic anhydride and add it to a 1 L light-shielded stoppered bottle containing 300 mL of freshly distilled pyridine, shake vigorously to dissolve, and let stand for at least 16 hours. Precisely weigh 25 mL of this solution and add it to the aforementioned pressure-resistant stoppered bottle. Seal the bottle tightly, wrap it in a sturdy cloth, and place it in a water bath preheated to 98°C ± 2°C. Ensure that the liquid in the bottle is immersed in the water bath. Heat at 98°C ± 2°C for 30 minutes, then allow to cool to room temperature. Next, accurately add 50 mL of 0.5 mol / L sodium hydroxide solution and titrate this solution with 0.5 mol / L sodium hydroxide solution. Use 5 drops of phenolphthalein-pyridine solution (1 → 100) as an indicator. However, the endpoint of the titration is defined as the point when the solution exhibits a pale red color that persists for 15 seconds. A blank test is performed using the same method. The obtained values ​​are applied to the following formula to calculate the average molecular weight. Average molecular weight = [Amount of sample (g) × 4000] / (ab) a: Amount of 0.5 mol / L sodium hydroxide solution consumed in a blank test (mL) b: Amount of 0.5 mol / L sodium hydroxide solution consumed in the sample test (mL)

[0066] Note that even for polyethylene glycols with an average molecular weight other than 190-210, the weighing amount will differ, but otherwise, the test method will be the same as for polyethylene glycols with an average molecular weight of 190-210.

[0067] These polyethylene glycols may be one type or a combination of two or more types.

[0068] In the topical composition of the present invention, the total content of polyethylene glycol is less than 5% by mass, preferably less than 3% by mass, more preferably less than 1% by mass, even more preferably less than 0.5% by mass, and even more preferably 0.1% by mass or less, based on the total amount of the topical composition, from the viewpoint of providing a good odor for the topical composition. In some cases, the topical composition may contain substantially no polyethylene glycol or no polyethylene glycol at all, such as 0.01% by mass or less.

[0069] (pH adjuster) The topical composition of the present invention may also contain a pH adjuster in addition to the above-mentioned components (A) to (F), as long as it does not interfere with the effects of the present invention, from the viewpoint of improving usability, stability, and promoting transdermal absorption.

[0070] As pH adjusting agents used in the present invention, compounds commonly used as components of topical skin preparations in the fields of pharmaceuticals, quasi-drugs, or cosmetics can be used. While not particularly limited, examples include amine-containing pH adjusting agents (e.g., aminoethylsulfonic acid or its salts, monoethanolamine, triethanolamine, diisopropanolamine, triisopropanolamine, L-carnitine, low molecular weight betaine (more preferably trimethylglycine)), organic acid salts (e.g., sodium lactate, 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), 3-O-ethyl ascorbic acid or its salts.

[0071] In the topical composition of the present invention, the total content of the pH adjusting agent is not particularly limited, but is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, relative to the total amount of the topical composition. Furthermore, the total content of the pH adjusting agent is preferably 10% by mass or less, more preferably 5% by mass or less, relative to the total amount of the topical composition. The content of the pH adjusting agent having an amine is preferably 0.01% to 10% by mass, more preferably 0.05% to 5% by mass, relative to the total amount of the topical composition. The total content of 3-O-ethyl ascorbic acid or its salt is preferably 0.005% to 10% by mass, more preferably 0.01% to 5% by mass, even more preferably 0.02% to 3% by mass, and even more preferably 0.1% to 2% by mass, relative to the total amount of the topical composition.

[0072] In the topical composition of the present invention, the ratio of the pH adjusting agent to component (A) is not particularly limited, but is preferably 0.00001 to 20 parts by mass, more preferably 0.0001 to 20 parts by mass, even more preferably 0.0005 to 10 parts by mass, even more preferably 0.005 to 5 parts by mass, and most preferably 0.01 to 1 part by mass, per 1 part by mass of the total content of component (A).

[0073] (Other ingredients) In addition to the above-mentioned components, the topical composition of the present invention may further contain one or more of the following components in combination, for the purpose of enhancing or supplementing the various effects of ascorbic acid, and for the purpose of adding other useful effects: 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 biocomponents such as collagen, blood circulation promoting components, moisturizing components, and anti-aging components.

[0074] In addition to the above components, the topical composition of the present invention may further contain surfactants other than component (E), solubilizing components, oils and fats, sugars, or transdermal absorption-promoting components. In particular, by incorporating surfactants other than component (E), solubilizing components, or oils and fats, the stability, effectiveness, and feel of ascorbic acid in an aqueous solvent can be further improved.

[0075] The topical composition of the present invention may contain, as needed, various components commonly used as components of topical preparations in the pharmaceutical, quasi-drug, or cosmetic fields, within quantitative and qualitative ranges that do not impair the quality such as appearance stability or viscosity, and do not impair the effects of the present invention. These components may be used individually or in combination of two or more as desired.

[0076] (brightness) From the viewpoint of significantly exhibiting the effects of the present invention, the topical composition of the present invention is preferably a highly transparent composition in which a fruit-based fragrance is solubilized. From the viewpoint of providing a highly transparent solution, the topical composition of the present invention is preferably a lightness L value of 99.5 or higher in the CIELAB color system. More specifically, the L value of the topical composition of the present invention is measured by the method described in the examples.

[0077] (pH) The topical composition of the present invention is preferably in the acidic range of pH 2 to 5, from the viewpoint of the stability of component (A), low irritation to the skin and mucous membranes, and good skin feel.

[0078] (form, physical properties) The topical composition of the present invention can be prepared in various desired forms, such as paste, mousse, gel, liquid, emulsion, cream, sheet (substrate-supported), aerosol, and spray. These can be manufactured by conventional methods in the industry. Among these, the topical composition of the present invention is preferred in liquid form, as it exhibits a remarkable aesthetic appearance due to its transparency.

[0079] The topical composition of the present invention can be prepared as a composition having a suitable viscosity, particularly when used as a topical composition applied to the skin. The viscosity of the topical composition of the present invention is not particularly limited, but 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, and most preferably about 1 to 50 mPa·s. The viscosity measurement method is, in more detail, in accordance with the method described in the 16th edition of the Japanese Pharmacopoeia [B] General Test Methods 2. Physical Test Methods Other Physical Test Methods 2.53 Viscosity Measurement Method 2.2 Method Rotational Viscometer Method 2.1.3 Method using a cone-plate rotational viscometer (cone-type viscometer).

[0080] (Application / Container) The topical composition of the present invention can be used, for example, as a whitening agent, anti-inflammatory agent, and anti-aging agent, and may have effects such as acne prevention and treatment, and antioxidant effects. Furthermore, when applied to the skin, it may enhance skin transparency, retain moisture, refine skin texture, and reduce roughness. In addition, it may have effects such as minimizing the appearance of pores and providing skin conditioning and moisturizing, and can also be used for the prevention and treatment of blemishes.

[0081] The external compositions of the present invention can be, for example, basic cosmetics such as serums, lotions, sunscreens, emulsions, creams, oils, and packs; makeup cosmetics such as foundations, lipsticks, lip balms, mascaras, eyeshadows, eyeliners, eyebrow pencils, and nail polishes; cleansing agents such as facial cleansers, makeup removers, and body washes; and various external compositions belonging to the fields of cosmetics, external pharmaceuticals, or external quasi-drugs, such as antiperspirants for underarm odor, athlete's foot treatments, antipruritics, wound healing agents, cleansing agents, anti-inflammatory and analgesic agents, acne treatments, hemorrhoid treatments, antiseptics, disinfectants, whitening agents, and ultraviolet protection agents. Due to its effects on the skin, the present invention is preferably used in products applied to the skin, such as external skin preparations (formulations for the skin).

[0082] The external composition of the present invention can be suitably used in products that are labeled with terms such as "transparent," "translucent," "sheer skin," or "clear skin" (for example, products related to preventing or improving blemishes, skin beautification, whitening, sunscreen, etc.), as the transparency of the composition allows for the association of the labeling concept.

[0083] The topical composition of the present invention can be used in known or commonly used dosages and administration methods, divided into one to several times per day, depending on the application.

[0084] The topical composition of the present invention is provided in any container. The container for containing the topical composition of the present invention is not particularly limited and may be made of glass or plastic, for example, but a transparent container is preferred as it allows the composition inside to be seen, and the aesthetic appeal due to the transparency of the composition is clearly displayed. Here, "transparent container" includes both colorless transparent containers and colored transparent containers.

[0085] (Manufacturing method) The topical composition of the present invention can be prepared by mixing components (A) to (E) above with any of the optional components as needed, further adding other solvents or commonly used topical agent bases as needed, and adjusting the pH as needed. For example, as described in the examples, the composition may be prepared by separating it into an aqueous phase containing components (A) to (C) and optionally (F), butylene glycol, ethoxydiglycol, polyethylene glycol, etc., and an oil phase containing (D) and (E), and then mixing the aqueous and oil phases.

[0086] [Method for solubilizing fruit-based fragrances] The present invention encompasses the following methods. Here, "solubilization of fragrance" refers to a state in which there is no or almost no turbidity of the fragrance, for example, that the lightness L value of the external composition in the CIELAB color system is 99.5 or higher. In an external composition containing (A) at least one selected from the group consisting of ascorbic acid and salts of ascorbic acid, (B) a diol having 3 carbon atoms, (C) water, and (D) a fruit-based fragrance, the ethoxydiglycol content is less than 20% by mass, (E) Equation (I): R1-O-[(AO) m (EO) n ]-H(wherein, R 1 is a hydrocarbon group having 16 or more carbon atoms, AO is an oxyalkylene group having 3 to 4 carbon atoms, EO is an oxyethylene group, m and n are the average number of moles of oxyalkylene and oxyethylene groups added, respectively, where m≧0 and n≧1, and the oxyalkylene and oxyethylene groups may be added in a block-like or random manner, and the molecular weight of the R1 portion is W. R1 The ratio of n to W R1 A method for solubilizing fruit-based fragrances, characterized by the coexistence of an alkylene oxide derivative (which is 0.088 or less).

[0087] The specific forms of components (A) to (E) and other permissible components in the above method shall be in accordance with the description in [Topical Composition] above. [Examples]

[0088] Next, the present invention will be specifically described with reference to examples and test cases, but the present invention is not limited to the following examples and test cases. Unless otherwise specified, the units of the amounts of each component in the table are in mass percent.

[0089] [Measurement method] (Measurement of turbidity) The turbidity of the topical composition due to fragrance was evaluated by measuring the lightness L value in the CIELAB color system using a spectrophotometer CM-5 (manufactured by Konica Minolta, Inc.). 40 mL of the prepared sample was placed in a 50 mL screw-cap bottle (manufactured by Nippon Denki Rika Glass, SV-50) and left to stand at 25°C for 1 day. For spectrophotometer measurements, 27 mL of the test solution was placed in a glass cell (CM-A99, 20 mm thick), and the L, a, and b values ​​in the CIELAB color system were measured at 25°C. The measured values ​​used were the L, a, and b values ​​obtained with purified water as a blank. Calibration and measurement of the instrument were performed according to the manual provided with the instrument. As shown in Comparative Example 7 in Figure 1 (L value: 99.11), when the obtained L value was less than 99.5, significant turbidity was observed visually. Therefore, an L value of 99.5 or higher was judged as no turbidity (○), and an L value less than 99.5 was judged as turbidity (×).

[0090] [Test Example 1. Test to suppress turbidity using fruit-based fragrances] In the formulations shown in Tables 1 and 2 below, the oil phase components were stirred with a magnetic stirrer while the aqueous phase components were added to solubilize the external composition. The resulting composition was placed in a transparent vial and allowed to stand at 25°C for one day. The lightness L values ​​obtained after standing and the results of the turbidity assessment due to the fragrance are shown in the same table.

[0091] In the examples using alkylene oxide derivatives having the structure of formula (I) above, compounds with R1 having 16 carbon atoms (Examples 3 and 5), 18 carbon atoms (Examples 1, 2, 7, and 8), and 24 carbon atoms (Examples 4 and 6) did not show any turbidity due to fruit-based fragrances.

[0092] On the other hand, topical compositions using alkylene oxide derivatives with R1 having 12 carbon atoms (Comparative Example 1) or 10 carbon atoms (Comparative Example 2) were found to be cloudy due to fragrance. Furthermore, topical compositions using surfactants that do not have the structure of formula (I), such as fatty acid esters in which R1 constitutes the fatty acid portion (Comparative Examples 3-6), or hydrogenated castor oil or coconut oil without the long-chain hydrocarbon portion of R1 (Comparative Examples 7-10), were found to be cloudy due to fruity fragrance.

[0093] Furthermore, none of the topical compositions in the examples shown in Tables 1 and 2 showed any precipitation or discoloration of ascorbic acid.

[0094] [Table 1]

[0095] [Table 2]

[0096] The topical compositions in Example 1 and Comparative Example 7, in which the fruit fragrance was replaced with water, showed no visible turbidity. Furthermore, the topical compositions in Example 1 and Comparative Example 7, in which the surfactant (oleth-10 or PEG-40 hydrogenated castor oil) was replaced with water, showed separation of the aqueous and oil phases. Moreover, the topical compositions in Example 1 and Comparative Example 7, in which both the fruit fragrance and the surfactant were replaced with water, also showed no visible turbidity. From these results, it is shown that (1) in compositions containing ascorbic acid, 1,3-propanediol, and water with ethoxydiglycol at less than 20% by mass, the addition of a fruit fragrance causes significant separation of the oil phase due to the fragrance, and (2) the surfactant (alkylene oxide derivative) in the examples suppresses the separation of the oil phase and turbidity of the solution caused by the fruit fragrance.

[0097] [Examples of formulations] The topical compositions of the present invention were prepared according to conventional methods based on the formulations shown in Tables 3 to 6 below.

[0098] [Table 3]

[0099] [Table 4]

[0100] [Table 5]

[0101] [Table 6] [Industrial applicability]

[0102] Because the external composition of the present invention is highly transparent, it is useful, for example, as a solution-type quasi-drug or cosmetic. The external composition of the present invention can be used particularly effectively for quasi-drugs or cosmetics contained in transparent containers in which the solution is visible.

Claims

1. (A) At least one selected from the group consisting of ascorbic acid and salts of ascorbic acid, (B) A diol with 3 carbon atoms, (C) water; (D) Fruit flavors, and (E) Formula (I): R １ -O-[(AO) ｍ (EO) ｎ ]-H (wherein R1 is a hydrocarbon group having 16 or more carbon atoms, AO is an oxyalkylene group having 3 to 4 carbon atoms, EO is an oxyethylene group, m and n are the average number of moles of oxyalkylene and oxyethylene groups having 3 to 4 carbon atoms, respectively, where m≧0 and n≧1, and the oxyalkylene and oxyethylene groups may be added in a block-like manner or randomly, R １ Molecular weight of part W Ｒ１ The ratio of n to n / W Ｒ１ A topical composition containing an alkylene oxide derivative represented by (0.003 to 0.088), wherein the ethoxydiglycol content is 1% by mass or less.

2. The topical composition according to claim 1, wherein the content of component (A) is 1 to 30% by mass.

3. The topical composition according to claim 1 or 2, wherein the content of component (B) is 1 to 80% by mass.

4. The topical composition according to any one of claims 1 to 3, wherein the content of component (C) is 1 to 50% by mass.

5. The topical composition according to any one of claims 1 to 4, wherein the content of component (D) is 0.0001 to 2% by mass.

6. The topical composition according to any one of claims 1 to 5, wherein the content of component (E) is 0.01 to 3% by mass.

7. The topical composition according to any one of claims 1 to 6, wherein the AO of component (E) is an oxypropylene group.

8. Furthermore, the external composition according to any one of claims 1 to 7, further comprising (F) a lower alcohol.

9. The external composition according to any one of claims 1 to 8, wherein the lightness L value in the CIELAB color system is 99.5 or higher.

10. The topical composition according to any one of claims 1 to 9, wherein the pH is 2 to 5.

11. (A) At least one selected from the group consisting of ascorbic acid and salts of ascorbic acid, (B) A diol with 3 carbon atoms, (C) Water, and (D) Fruit-based fragrance A topical composition containing, and having an ethoxydiglycol content of 1% by mass or less, (E) Formula (I): R １ -O-[(AO) ｍ (EO) ｎ -H (wherein, R １ is 16 carbon atoms The above hydrocarbon groups, AO is an oxyalkylene group having 3 to 4 carbon atoms, EO is an oxyethylene group, m and n are the average number of moles of oxyalkylene and oxyethylene groups having 3 to 4 carbon atoms, respectively, where m ≥ 0 and n ≥ 1, and the oxyalkylene and oxyethylene groups may be added in a block-like manner or randomly, R １ Molecular weight of part W Ｒ１ The ratio of n to n / W Ｒ１ A method for solubilizing fruit-based fragrances, characterized by the presence of an alkylene oxide derivative represented by (but having a value of 0.003 or more and 0.088 or less).

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