External components
By combining polyoxyalkylene (poly)glyceryl ether and a nonionic surfactant with ascorbic acid derivatives, the composition stabilizes ascorbic acid in topical formulations, preventing discoloration and enhancing moisturization.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- KOBAYASHI PHARMA CO LTD
- Filing Date
- 2024-12-20
- Publication Date
- 2026-07-02
AI Technical Summary
Ascorbic acid discolors in water-based formulations, limiting their stability and compatibility with moisturizing ingredients, which are essential for effective skin whitening compositions.
Incorporating polyoxyalkylene (poly)glyceryl ether and a nonionic surfactant with an HLB of 14.5 or less into topical compositions containing ascorbic acid derivatives, along with water, to suppress discoloration and enhance moisturizing effects.
The composition effectively prevents discoloration while maintaining moisturizing properties and skin compatibility, allowing for a wider range of formulation options.
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Abstract
Description
Technical Field
[0001] The present disclosure relates to an external composition that contains ascorbic acids and is suppressed from discoloring.
Background Art
[0002] Ascorbic acids are known as so-called whitening components that suppress melanin production and / or dilute produced melanin, and are formulated and used in skin external compositions for the purpose of obtaining an effect of suppressing skin pigmentation (Patent Documents 1 to 3).
[0003] However, since ascorbic acid discolors yellow in water, there is a problem in its stable formulation in cosmetics and the like. For the purpose of stabilizing ascorbic acid, a technique has been proposed in which methylpyrrolidone and polyhydric alcohol are formulated together with ascorbic acid in a skin external preparation, and the amount of water is set to 10% by mass or less (Patent Document 4).
Prior Art Documents
Patent Documents
[0004]
Patent Document 1
Patent Document 2
Patent Document 3
Patent Document 4
Summary of the Invention
Problems to be Solved by the Invention
[0005] The technique of combining ascorbic acid with methylpyrrolidone and polyhydric alcohols, while keeping the water content to 10% by mass or less, severely limits the applicable formulation forms due to the need to keep the water content to a minimum. Furthermore, since skin is less susceptible to UV damage when well-moisturized, it is desirable that the topical composition also contains moisturizing ingredients to facilitate the whitening effect of ascorbic acid. Therefore, even when a topical composition containing ascorbic acid contains moisturizing ingredients, a new formulation that can suppress discoloration due to storage is desired.
[0006] Therefore, the object of this disclosure is to provide a topical composition that contains ascorbic acid derivatives but in which discoloration is suppressed. [Means for solving the problem]
[0007] The inventors of the present invention conducted diligent studies to solve the aforementioned problems and found that by selecting polyoxyalkylene (poly)glyceryl ether as a moisturizing ingredient to be incorporated into an external composition containing ascorbic acid, and by incorporating a nonionic surfactant with an HLB of 14.5 or less, discoloration due to storage can be suppressed. This disclosure was completed by further studies based on this finding.
[0008] In other words, this disclosure provides external compositions in the following embodiments. Item 1. A topical composition comprising (A) ascorbic acid and / or a derivative thereof, (B) polyoxyalkylene (poly)glyceryl ether, (C) a nonionic surfactant with an HLB of 14.5 or less, and (D) water. Item 2. The topical composition according to Item 1, wherein component (C) is from the group consisting of polyoxyethylene hydrogenated castor oil and / or polyoxyalkylene alkyl ethers. Item 3. The topical composition according to item 1 or 2, wherein the content of component (B) per 1 part by weight of component (A) is 0.003 to 10 parts by weight. Item 4. The topical composition according to any one of items 1 to 3, wherein the content of component (C) is 0.001 to 10% by weight. Item 5. The topical composition according to any one of items 1 to 4, wherein the content of component (D) is 15 to 98% by weight. [Effects of the Invention]
[0009] According to this disclosure, a topical composition is provided that contains ascorbic acid derivatives while suppressing discoloration. [Modes for carrying out the invention]
[0010] The topical composition disclosed herein is characterized by comprising (A) ascorbic acid and / or its derivatives (hereinafter also referred to as "component (A)" or "ascorbic acids"), (B) polyoxyalkylene (poly)glyceryl ether (hereinafter also referred to as "component (B)"), (C) a nonionic surfactant with an HLB of 14.5 or less (hereinafter also referred to as "component (C)" or "a specified nonionic surfactant"), and (D) water (hereinafter also referred to as "component (D)"). The topical composition disclosed herein is resistant to discoloration (specifically yellowing) due to storage. A preferred embodiment of the topical composition disclosed herein is excellent in moisturizing effect, skin compatibility, and / or non-stickiness. The topical composition disclosed herein is described in detail below. In this disclosure, the numerical range "X~Y" refers to a range of X or more and Y or less.
[0011] (A) Ascorbic acids The topical compositions disclosed herein contain ascorbic acid and / or its derivatives as component (A). Conventionally, aqueous topical compositions containing ascorbic acid compounds discolor upon storage, but the topical compositions disclosed herein exhibit suppressed discoloration upon storage.
[0012] Ascorbic acid derivatives are known components with whitening and antioxidant properties. Specifically, the ascorbic acid and its derivatives used in this disclosure are ascorbic acid, ascorbic acid esters, ascorbyl ethers, ascorbic acid glycosides, and salts thereof.
[0013] Ascorbic acid esters are not particularly limited to the extent that they are pharmaceutically or cosmetically acceptable, but examples include ascorbic acid phosphate esters (ascorbic acid monophosphate, ascorbic acid diphosphate, ascorbic acid triphosphate), ascorbic acid sulfate esters (ascorbic acid monosulfate, ascorbic acid disulfate, ascorbic acid trisulfate), ascorbic acid alkyl esters (ascorbic acid monoalkyl esters such as ascorbic acid monostearate, ascorbic acid monopalmitate, ascorbic acid monooleate; ascorbic acid dialkyl esters such as ascorbic acid distearate, ascorbic acid dipalmitate, ascorbic acid dioleate; trialkyl esters such as ascorbic acid tristearate, ascorbic acid tripalmitate, ascorbic acid trioleate), and tetra-2-hexyldecanoate ascorbyl.
[0014] Ascorbyl ethers are not particularly limited to those that are pharmaceutically or cosmetically acceptable, but examples include ethyl ascorbic acid (2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid), 3-glyceryl ascorbic acid, bisglyceryl ascorbic acid, alkylglyceryl ascorbyl, etc.
[0015] Ascorbic acid glycosides are not particularly limited, as long as they are pharmaceutically or cosmetically acceptable, but examples include ascorbic acid glucoside.
[0016] When ascorbic acid is in the form of an acid salt, the type of salt is not particularly limited as long as it is pharmaceutically or cosmetically acceptable, but examples include sodium salt, potassium salt, magnesium salt, calcium salt, barium salt, ammonium salt, monoethanolamine salt, diethanolamine salt, triethanolamine salt, monoisopropanolamine salt, triisopropanolamine salt, noyl-ascorbic acid, etc.
[0017] These ascorbic acids may be either the L-form or the D-form, with the L-form being preferred.
[0018] These ascorbic acids may be used alone or in combination of two or more.
[0019] Among these ascorbic acids, preferably, ascorbic acid, ascorbate, and ascorbic acid glycoside are mentioned. Furthermore, although ascorbic acid or its salts are inherently prone to discoloration, when the external composition of the present disclosure contains ascorbic acid or its salts, the discoloration can be particularly significantly suppressed. From this perspective, preferred examples of ascorbic acids include ascorbic acid or its salts.
[0020] Regarding the content of the component (A) in the external composition for skin of the present disclosure, it may be appropriately set according to the required degree of the action of the component (A), etc. For example, 0.01 to 10% by weight, preferably 0.1 to 8% by weight, more preferably 1 to 6% by weight, and still more preferably 2 to 4% by weight can be mentioned.
[0021] (B) Polyoxyalkylene (poly)glyceryl ether The external composition of the present disclosure contains polyoxyalkylene (poly) glyceryl ether as the component (B). Conventionally, an aqueous external composition containing ascorbic acids and a predetermined nonionic surfactant undergoes discoloration during storage. However, by using polyoxyalkylene (poly) glyceryl ether in combination with ascorbic acids and a predetermined nonionic surfactant in the aqueous external composition, discoloration during storage can be suppressed. Also, in a preferred embodiment of the external composition of the present disclosure, by using polyoxyalkylene (poly) glyceryl ether in combination with ascorbic acids and a predetermined nonionic surfactant, the moisturizing feeling can be improved.
[0022] In the present disclosure, (poly) glyceryl ether means glyceryl ether or polyglyceryl ether. Similarly, (poly) glycerin means glycerin or polyglycerin.
[0023] Polyoxyalkylene (poly)glyceryl ethers are compounds in which an alkylene oxide is added to the hydroxyl group of (poly)glycerol.
[0024] The degree of polymerization of (poly)glycerin constituting polyoxyalkylene (poly)glyceryl ether is not particularly limited, and examples include 1 to 4. From the viewpoint of suppressing discoloration during storage and / or improving moisturizing effects, preferred degrees of polymerization of (poly)glycerin are 1 to 3, more preferably 1 (glycerin) and 2 (diglycerin). Furthermore, from the viewpoint of further enhancing the moisturizing effect, a more preferred degree of polymerization of (poly)glycerin is 1 (glycerin).
[0025] Examples of alkylene oxides constituting polyoxyalkylene (poly)glyceryl ethers include ethylene oxide, propylene oxide, 1,2-butylene oxide, and 2,3-butylene oxide. Among these alkylene oxides, ethylene oxide and / or propylene oxide are preferred from the viewpoint of suppressing discoloration during storage and / or improving moisturizing properties. Furthermore, the molar ratio of ethylene oxide to total alkylene oxide is not particularly limited and can be selected from 0 to 100%, but from the viewpoint of improving moisturizing properties, it is preferably 40% or more, more preferably 45% or more, and even more preferably 50% or more.
[0026] There are no particular limitations on the number of alkylene oxides added to polyoxyalkylene (poly)glyceryl ether, but examples include 3 to 70. From the viewpoint of suppressing discoloration during storage and / or improving moisturizing effects, preferred numbers of alkylene oxides added include 7 to 65, more preferably 14 to 60. Furthermore, from the viewpoint of further enhancing effects such as improved moisturizing effects, even more preferred numbers of alkylene oxides added include 24 to 50.
[0027] Examples of polyoxyalkylene (poly)glyceryl ethers include polyoxyethylene glyceryl ether (POE glyceryl ether), polyoxypropylene glyceryl ether (POP glyceryl ether), polyoxyethylene polyoxypropylene glyceryl ether (POE·POP glyceryl ether), and polyoxybutylene polyoxyethylene polyoxypropylene glyceryl ether (POB·POE·POP glyceryl ether). Specific examples of POE glyceryl ether include POE(3) glyceryl ether, POE(7) glyceryl ether, POE(8) glyceryl ether, POE(12) glyceryl ether, POE(18) glyceryl ether, POE(20) glyceryl ether, POE(26) glyceryl ether, and POE(31) glyceryl ether. Specific examples of POP glyceryl ethers include POP(8) glyceryl ether, POP(10) glyceryl ether, POP(16) glyceryl ether, POP(50) glyceryl ether, and POP(70) glyceryl ether. Specific examples of POE·POP glyceryl ethers include POE(24)POP(24) glyceryl ether and POE(22)POP(25) glyceryl ether. Specific examples of POB·POE·POP glyceryl ethers include POB(3)POE(8)POP(5) glyceryl ether. Note that "POE" is an abbreviation for polyoxyethylene, "POP" is an abbreviation for polyoxypropylene, and "POB" is an abbreviation for polyoxybutylene, and the number in parentheses after POE, POP, or POB indicates the number of moles added.
[0028] Among polyoxyalkylene (poly)glyceryl ethers, an example of polyoxyalkylene polyglyceryl ether is polyoxyalkylene diglyceryl ether. Examples of polyoxyalkylene diglyceryl ethers include polyoxyethylene diglyceryl ether (POE diglyceryl ether), polyoxypropylene diglyceryl ether (POP diglyceryl ether), and polyoxyethylene polyoxypropylene diglyceryl ether (POE·POP diglyceryl ether). Specific examples of POE diglyceryl ether include POE(4) diglyceryl ether, POE(13) diglyceryl ether, POE(20) diglyceryl ether, POE(30) diglyceryl ether, and POE(60) diglyceryl ether. Specific examples of POP diglyceryl ether include POP(9) diglyceryl ether, POP(14) diglyceryl ether, and POP(24) diglyceryl ether. Specific examples of POE·POP diglyceryl ethers include POE(2)POP(14) diglyceryl ether. "POE" is an abbreviation for polyoxyethylene, "POP" for polyoxypropylene, and "POB" for polyoxybutylene. The numbers in parentheses after POE, POP, or POB indicate the number of moles added.
[0029] These polyoxyalkylene (poly)glyceryl ethers may be used individually or in combination of two or more types.
[0030] The content of component (B) in the topical skin composition of this disclosure is not particularly limited and may be set appropriately according to the desired degree of suppression of discoloration due to storage and / or improvement of moisturizing sensation, for example, 0.01 to 30% by weight. From the viewpoint of enhancing the effects of suppressing discoloration due to storage and / or improving moisturizing sensation, a preferred content of component (B) is 0.05 to 20% by weight, more preferably 0.1 to 15% by weight, and even more preferably 0.3 to 10% by weight. From the viewpoint of achieving both moisturizing sensation and non-stickiness, a more preferred content of component (B) is 1 to 9% by weight, even more preferably 2.5 to 8% by weight, particularly preferably 2.8 to 7% by weight, or 3.5 to 6% by weight.
[0031] In the topical skin composition of this disclosure, the ratio of component (A) to component (B) is determined according to the content of each component, but for example, the content of component (B) per 1 part by weight of component (A) is 0.003 to 10 parts by weight. From the viewpoint of enhancing effects such as suppressing discoloration due to storage and / or improving moisturizing sensation, a preferred content of component (B) per 1 part by weight of component (A) is 0.015 to 6.5 parts by weight, more preferably 0.03 to 5 parts by weight, and even more preferably 0.1 to 3.5 parts by weight. From the viewpoint of achieving both moisturizing sensation and non-stickiness, a more preferred content of component (B) per 1 part by weight of component (A) is 0.3 to 3 parts by weight, even more preferably 0.8 to 2.5 parts by weight, particularly preferably 0.9 to 2.3 parts by weight, or 1.2 to 3 parts by weight.
[0032] (C) Specified nonionic surfactant The topical composition disclosed herein contains a nonionic surfactant with an HLB of 14.5 or less as component (C). Conventionally, aqueous topical compositions containing ascorbic acid derivatives and polyoxyalkylene (poly)glyceryl ethers discolor upon storage, but discoloration upon storage can be suppressed by using a predetermined nonionic surfactant in combination with ascorbic acid derivatives and polyoxyalkylene (poly)glyceryl ethers in the aqueous topical composition. Furthermore, in a preferred embodiment of the topical composition disclosed herein, skin compatibility can be improved by using a predetermined nonionic surfactant in combination with ascorbic acid derivatives and polyoxyalkylene (poly)glyceryl ethers.
[0033] The HLB of a nonionic surfactant is not particularly limited as long as it is 14.5 or less, and may be 14.0 or less, 13.5 or less, 13.0 or less, or 12.5 or less. From the viewpoint of further enhancing the effect of suppressing discoloration due to storage, a preferred HLB of the nonionic surfactant is 12.2 or less. Furthermore, the HLB of the nonionic surfactant is not particularly limited even at its lower limit, but specific ranges of HLB include, for example, 2.0 to 14.5, 4.0 to 14.0, 5.0 to 13.5, 6.0 to 13.0, or 7.0 to 12.5, preferably 8.0 to 12.2.
[0034] The HLB (Hydrophile-Lypophile Balance) value is a value that indicates the affinity of a nonionic surfactant for water and oil. In this disclosure, the HLB value of the nonionic surfactant is a value obtained by a measurement method that conforms to the actual measurement of HLB values by emulsification method described on pages 854-855 of "Handbook - Cosmetics and Pharmaceutical Raw Materials - Revised Edition," Nikko Chemicals Co., Ltd., revised edition published February 1, 1977. Specifically, the nonionic surfactant to be measured for HLB value is combined with polyoxyethylene sorbitan monostearate (NIKKOL TS-10, HLB 14.9) as a standard substance, and the total amount of these two emulsifiers is kept constant, while only the ratio is changed to emulsify liquid paraffin (HLB 10.1), which is the substance to be emulsified. After standing for 24 hours, the optimal ratio of surfactant at which stability is determined from the amount of creaming, turbidity, and water separation of the lower layer, and the HLB value x of the surfactant is calculated using the following formula (1). y=(x×Amount used (mass%)+z×Amount used (mass%)) / 100...Formula (1) In equation (1) above, x represents the HLB value of the nonionic surfactant (the substance being measured), y represents the HLB value of the liquid paraffin, and z represents the HLB value of polyoxyethylene sorbitan monostearate (the standard substance). The HLB value of the liquid paraffin can be determined in a similar manner by combining sorbitan monostearate (NIKKOL SS-10, HLB 4.7) and polyoxyethylene sorbitan monostearate (NIKKOL TS-10, HLB 14.9).
[0035] The types of nonionic surfactants are not particularly limited, but examples include polyoxyalkylene alkyl ethers, polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid esters, polyglycerin fatty acid esters, polyoxyethylene glycerin fatty acid esters, glycerin fatty acid esters, polyoxyethylene sorbitan fatty acid esters, sorbitan fatty acid esters, polyoxyethylene alkyl ethers, polyethylene glycol fatty acid esters, and the like.
[0036] These nonionic surfactants may be used individually or in combination of two or more. Among these nonionic surfactants, polyoxyalkylene alkyl ethers and polyoxyethylene hydrogenated castor oil are preferred, and polyoxyalkylene alkyl ethers are more preferred, from the viewpoint of further enhancing effects such as suppressing discoloration during storage.
[0037] Examples of polyoxyalkylene alkyl ethers include polyoxyethylene alkyl ethers (POE alkyl ethers), polyoxypropylene alkyl ethers (POP alkyl ethers), and polyoxyethylene polyoxypropylene alkyl ethers (POE·POP alkyl ethers). Examples of POE alkyl ethers include POE ethylene lauryl ether, POE cetyl ether, POE oleyl ether, POE stearyl ether, POE alkyl (C12-14) ether, POE tridecyl ether, POE myristyl ether, POE isostearyl ether, and POE behenyl ether. Examples of POP alkyl ethers include POP butyl ether, POP myristyl ether, POP cetyl ether, POP stearyl ether, and POP lanolin alcohol ether. Examples of POE·POP alkyl ethers include POE·POP butyl ether, POE·POP lauryl ether, POE·POP cetyl ether, POE·POP stearyl ether, and POE·POP decyltetradecyl ether. Examples of POE·POP decyltetradecyl ethers include POE(12)POP(6) decyltetradecyl ether, POE(20)POP(6) decyltetradecyl ether, POE(30)POP(6) decyltetradecyl ether, POE(24)POP(13) decyltetradecyl ether, and POE(10)POP(20) decyltetradecyl ether. "POE" is an abbreviation for polyoxyethylene, and "POP" is an abbreviation for polyoxypropylene. The number in parentheses after POE or POP indicates the number of moles added. These polyoxyalkylene alkyl ethers may be used individually or in combination of two or more. Among these polyoxyalkylene alkyl ethers, POE·POP alkyl ethers are preferred, and POE·POP decyltetradecyl ethers are more preferred, from the viewpoint of further enhancing the effect of suppressing discoloration during storage.
[0038] Examples of polyoxyethylene hydrogenated castor oil include POE hydrogenated castor oil 2, POE hydrogenated castor oil 5, POE hydrogenated castor oil 6, POE hydrogenated castor oil 7, POE hydrogenated castor oil 8, POE hydrogenated castor oil 10, POE hydrogenated castor oil 20, POE hydrogenated castor oil 25, POE hydrogenated castor oil 30, POE hydrogenated castor oil 35, POE hydrogenated castor oil 40, POE hydrogenated castor oil 45, POE hydrogenated castor oil 50, POE hydrogenated castor oil 55, and POE hydrogenated castor oil 60. "POE" is an abbreviation for polyoxyethylene, and "POP" is an abbreviation for polyoxypropylene. The numbers at the end indicate the number of moles added. These polyoxyethylene hydrogenated castor oils may be used individually or in combination of two or more types.
[0039] In the topical compositions of this disclosure, the content of component (C) is not particularly limited and can be set appropriately according to the desired degree of improved suppression of discoloration during storage, improved skin compatibility, and / or lack of stickiness, for example, 0.001 to 10% by weight. From the viewpoint of enhancing the effects of improved suppression of discoloration during storage, improved skin compatibility, and / or lack of stickiness, preferred content of component (C) is 0.003 to 5% by weight, more preferably 0.005 to 1% by weight, even more preferably 0.01 to 0.5% by weight, particularly preferably 0.07 to 0.42% by weight, 0.25 to 0.32% by weight, or 0.09 to 0.15% by weight.
[0040] In the topical skin composition of this disclosure, the ratio of component (A) to component (C) is determined according to the content of each component, but for example, the content of component (C) per 1 part by weight of component (A) is 0.0003 to 3 parts by weight. From the viewpoint of improving the suppression of discoloration due to storage, improving skin compatibility, and / or the absence of stickiness, a preferred content of component (B) per 1 part by weight of component (A) is 0.001 to 1.6 parts by weight, more preferably 0.0016 to 0.3 parts by weight, even more preferably 0.003 to 0.16 parts by weight, particularly preferably 0.02 to 0.14 parts by weight, 0.08 to 0.12 parts by weight, or 0.03 to 0.05 parts by weight.
[0041] (D)Water The topical composition disclosed herein contains water as component (D). Conventionally, topical compositions containing ascorbic acid derivatives together with water discolor upon storage, but the topical composition disclosed herein has suppressed discoloration upon storage.
[0042] The content of component (D) in the topical composition of this disclosure may be set appropriately depending on the formulation form, etc., and can be selected from, for example, 1 to 99% by weight. The topical composition of this disclosure is a topical composition that contains ascorbic acid derivatives together with water, yet exhibits excellent discoloration suppression effects, and can effectively suppress discoloration even if it contains a relatively large amount of water. From this viewpoint, preferred content of component (D) in the topical composition of this disclosure includes 15 to 98% by weight, 40 to 96% by weight, 60 to 94% by weight, 70 to 92% by weight, or 75 to 90% by weight.
[0043] Other ingredients The topical compositions of this disclosure may or may not contain, in addition to the components described above, pharmaceutically acceptable bases and / or additives as needed. Examples of such bases and additives, whether present or absent, include surfactants, oily bases (mineral oil, higher (6-34 carbon) monohydric alcohols, fatty acid alkyl esters, vegetable oils, animal oils, cholesterol, higher fatty acids with 12-34 carbon atoms, silicone oil, etc.), monohydric lower (1-5 carbon atoms, preferably 2-3 carbon atoms) alcohols, polyhydric alcohols (ethylene glycol, 1,3-butylene glycol, isoprene glycol, dipropylene glycol, and other dihydric and trihydric alcohols, etc.), thickeners, chelating agents, pH adjusters, buffers, preservatives, antioxidants, stabilizers, fragrances, colorants, etc. When these additives are included in the topical compositions of this disclosure, their content may be appropriately determined depending on the type of base and / or additive used.
[0044] If the topical composition of this disclosure contains surfactants among the other components (i.e., surfactants other than components (B) and (C)), the content of such surfactants (surfactants other than components (B) and (C)) may be greater than 0% by weight and 5% by weight or less, greater than 0% by weight and 3% by weight or less, greater than 0% by weight and 1% by weight or less, or greater than 0% by weight and 0.5% by weight or less. In preferred embodiments of the topical composition of this disclosure, surfactants other than components (B) and (C) are not included.
[0045] Furthermore, the topical compositions disclosed herein may contain pharmacological components in addition to the components described above. Examples of such pharmacological components include antihistamines, local anesthetics, moisturizers, anti-inflammatory agents, antiseptics, antipruritics, skin protectants, blood circulation promoting components, and vitamins. These pharmacological components may be used individually or in combination of two or more. When these pharmacological components are included in the topical compositions disclosed herein, their concentrations may be appropriately set according to the type of pharmacological component used, the expected effect, etc.
[0046] pH The pH of the topical composition disclosed herein can be selected without particular limitation from the pH generally applied to topical compositions, but examples include 5.0 to 7.5, preferably 5.5 to 7.0, and more preferably 5.7 to 6.5. It is known that among ascorbic acid derivatives, ascorbic acid, ascorbic acid esters, ascorbic acid glycosides, and their salts inherently discolor (yellowing) more strongly as the pH decreases. Because the topical composition disclosed herein has an excellent discoloration-inhibiting effect, it can effectively suppress discoloration even at relatively low pH levels where these ascorbic acid derivatives are inherently prone to discoloration. From this viewpoint, preferred pH values for the topical composition disclosed herein include 5.0 to 7.0, 5.0 to 6.5, 5.0 to 6.3, or 5.0 to 6.1. In this disclosure, the pH of the topical composition is a value measured under a temperature condition of 25°C.
[0047] Formulation form / dosage type The dosage form of the topical composition disclosed herein is not particularly limited as long as it can be applied topically, and may be liquid, solid, semi-solid (cream, gel, ointment, paste), solid, etc., but preferably liquid or semi-solid, and more preferably liquid. Furthermore, the topical composition disclosed herein may be a non-emulsified formulation such as an aqueous formulation or an oily formulation, or an emulsified formulation such as an oil-in-water emulsion formulation or a water-in-oil emulsion formulation. Among these dosage forms, aqueous formulations are preferred.
[0048] The formulation of the topical composition disclosed herein is not particularly limited as long as it is suitable for topical use, and may be any formulation such as a topical pharmaceutical, a topical quasi-drug, a cosmetic, or a cleanser. Among these formulations, topical pharmaceuticals, topical quasi-drugs, and cosmetics are preferred, more preferably topical quasi-drugs and cosmetics, and even more preferably cosmetics. Furthermore, the cosmetic may be either a leave-on cosmetic or a leave-off cosmetic, but a leave-on cosmetic is preferred.
[0049] More specific formulations of the topical compositions disclosed herein include liquid preparations (including lotions, sprays, aerosols, emulsions, and oils), water-soluble ointments, oily ointments, creams, foams, gels, and patches; cosmetics such as ointments, creams, emulsions, lotions, beauty oils, packs, and gels; and skin cleansing products such as body shampoos and hair shampoos. Among these formulations, liquid preparations (more preferably lotions) and lotions are preferred. These formulations can be prepared by compounding them using bases and / or additives appropriate to the formulation, in accordance with known methods described in the General Provisions for Formulations of the Sixteenth Revised Japanese Pharmacopoeia, etc. [Examples]
[0050] The present disclosure will be explained in more detail below with reference to examples, but the present disclosure is not limited to these examples.
[0051] Test Example 1 [1] Preparation of topical compositions External compositions (lotions) were prepared by mixing the ingredients shown in Tables 1-4 in the indicated amounts. In Tables 1-4, for the ingredients listed as (B), Glycereth-26 is POE(2)POP(14) diglyceryl ether, PPG-24 Glycereth-24 is POE(24)POP(24) glyceryl ether, and PPG-14 polyglyceryl-2 ether is POP(14) diglyceryl ether. Furthermore, regarding the components listed as component (C), PPG-6 Decyltetradeceth-12 is POE(12)POP(6) Decyltetradecyl ether, PPG-13 Decyltetradeceth-24 is POE(24)POP(13) Decyltetradecyl ether, PPG-6 Decyltetradeceth-30 is POE(30)POP(6) Decyltetradecyl ether, PEG-30 Hydrogenated Castor Oil is POE Hydrogenated Castor Oil 30, PEG-40 Hydrogenated Castor Oil is POE Hydrogenated Castor Oil 40, PEG-50 Hydrogenated Castor Oil is POE Hydrogenated Castor Oil 50, and PEG-60 Hydrogenated Castor Oil is POE Hydrogenated Castor Oil 60.
[0052] [2] Evaluation of topical compositions [2-1] Stability evaluation The prepared topical compositions were stored at 50°C for one week. After storage, the temperature was returned to 25°C, and the YI value (yellowness) was measured using a spectrophotometer. The obtained YI values were stratified based on the following criteria to derive a discoloration score from -7 to +3. A lower discoloration score indicates a better discoloration (yellowing) suppression effect. The results are shown in Tables 1 to 4. YI value less than 1.00: Discoloration score -7 YI value between 1.00 and 1.50: Discoloration score -6 YI value between 1.50 and 2.00: Discoloration score -5 YI value between 2.00 and 2.50: Discoloration score -4 YI value between 2.50 and 3.00: Discoloration score -3 YI value between 3.00 and 3.50: Discoloration score -2 YI value between 3.50 and 4.00: Discoloration score -1 YI value between 4.00 and 4.50: Discoloration score +1 YI value between 4.50 and 5.00: Discoloration score +2 YI value 5.00 or higher: Discoloration score +3
[0053] [2-2] User experience evaluation Ten cosmetic evaluation panelists assessed the usability of the topical compositions immediately after preparation. Specifically, they applied the topical compositions to their faces and scored each evaluation item—moisture retention, skin absorption, and non-stickiness—based on the following criteria.
[0054] <Moisturizing effect> 4 points: Very moisturizing. 3 points: Moisturizing 2 points: Slightly moisturizing. 1 point: Does not feel moisturizing.
[0055] <Skin compatibility> 4 points: Very good on the skin 3 points: Blends well with the skin 2 points: Doesn't blend well with the skin. 1 point: Does not blend well with the skin.
[0056] <Non-sticky> 4 points: No stickiness. 3 points: Slightly sticky feeling. 2 points: Feels sticky 1 point: I feel a very strong stickiness.
[0057] Based on the total score obtained, each evaluation item was judged according to the following criteria. The results are shown in Tables 1-4. ◎: 35 points or more ○: 30 points or more, less than 35 points △: 25 points or more, less than 30 points ×: Less than 25 points
[0058] [Table 1]
[0059] [Table 2]
[0060] [Table 3]
[0061] [Table 4]
[0062] As shown in Tables 1-4, compared to the topical compositions containing components (A) and (B) (Comparative Examples 1 and 2), and the topical compositions containing components (A) and (C) (Comparative Examples 3-5), the topical compositions containing components (A), (B), and (C) (Examples 1-14) showed significantly suppressed discoloration (yellowing). Furthermore, in the topical compositions containing components (A), (B), and (C), when component (B) was replaced with glycerin (Comparative Example 6), and when component (C) was replaced with a nonionic surfactant with an HLB value exceeding 14.5 (Comparative Example 7), the discoloration was more pronounced than in Comparative Examples 1-5.
[0063] Furthermore, as shown in Tables 1-4, the topical compositions containing components (A) and (B) (Comparative Examples 1 and 2) had poor skin compatibility, and the topical compositions containing components (A) and (C) (Comparative Examples 3-5) had poor moisturizing properties. However, the topical compositions containing components (A), (B), and (C) (Examples 1-14) were excellent in both moisturizing properties and skin compatibility. In addition, the topical compositions containing components (A), (B), and (C) (Examples 1-14) were also excellent in terms of non-stickiness.
[0064] Prescription examples Topical compositions (lotions) with the formulations shown in Table 5 were prepared. All of the obtained topical compositions showed suppressed discoloration (yellowing) and excellent moisturizing properties, skin compatibility, and non-greasy feel.
[0065] [Table 5]
Claims
1. A topical composition comprising (A) ascorbic acid and / or its derivatives, (B) polyoxyalkylene (poly)glyceryl ether, (C) a nonionic surfactant with an HLB of 14.5 or less, and (D) water.
2. The topical composition according to claim 1, wherein component (C) is selected from the group consisting of polyoxyethylene hydrogenated castor oil and / or polyoxyalkylene alkyl ethers.
3. The topical composition according to claim 1 or 2, wherein the content of component (B) per 1 part by weight of component (A) is 0.003 to 10 parts by weight.
4. The topical composition according to claim 1 or 2, wherein the content of component (C) is 0.001 to 10% by weight.
5. The topical composition according to claim 1 or 2, wherein the content of component (D) is 15 to 98% by weight.