Cosmetic or external preparation for skin

Abstract

To suppress the yellow discoloration of tranexamic acid that is caused by the incorporation of a non-reducing sugar and a sugar alcohol into a composition containing tranexamic acid.SOLUTION: The present invention provides a cosmetic or an external preparation for skin containing the following components (A) to (D): (A) tranexamic acid, (B) a non-reducing sugar, (C) a sugar alcohol, and (D) an organic acid, a salt thereof, or a derivative thereof.SELECTED DRAWING: None

Description

[Technical field]

[0001] The present invention relates to an agent for inhibiting yellowing of cosmetics, topical skin preparations, and compositions containing tranexamic acid, a non-reducing sugar, and a sugar alcohol. [Background technology]

[0002] Tranexamic acid has been conventionally blended into cosmetics and topical skin preparations (hereinafter referred to as cosmetics, etc.) to impart whitening and anti-inflammatory effects, etc. (see, for example, Patent Documents 1 and 2). However, tranexamic acid has problems with stability over time, such as coloration under conditions such as high temperatures, and in order to solve this problem, a technique has been proposed in which saponin or a polymeric compound having a quaternary amino group is used in combination with tranexamic acid (see, for example, Patent Documents 3 and 4).

[0003] On the other hand, many saccharides have excellent hydrophilicity, moisturizing properties, etc., and are therefore widely used in cosmetics and the like for the purposes of moisturizing, hydrating, skin conditioning, etc. However, cosmetic compositions containing tranexamic acid and saccharides have a problem of coloration, and in order to solve this problem, a technique of using inorganic acids, organic acids, vitamins, etc. in combination has been proposed (see, for example, Patent Document 5). [Prior art documents] [Patent documents]

[0004] [Patent Document 1] JP2001-031580A [Patent Document 2] JP 2008-100933 A [Patent Document 3] Japanese Patent Application Publication No. 03-279317 [Patent Document 4] JP 2006-045079 A [Patent Document 5] JP 2014-62077 A Summary of the Invention [Problem to be solved by the invention]

[0005] A technique for using a specific compound in combination with tranexamic acid and a sugar to suppress discoloration of a cosmetic composition has been known, but it is limited to some sugars and is technically insufficient. In addition, among sugars, trehalose, which is a non-reducing sugar, is widely used to impart a moisturizing effect to cosmetics and the like due to its high water retention compared to glucose, which is a reducing sugar, but it was not known at all that the combination of tranexamic acid with a non-reducing sugar and other sugars would cause significant discoloration. The present inventors have confirmed that yellowing is significantly accelerated in cosmetics that contain both a non-reducing sugar and a sugar alcohol, compared to cosmetics that contain either a non-reducing sugar or a sugar alcohol in addition to tranexamic acid. Furthermore, they have confirmed that the addition of a sorbitan surfactant further accelerates yellowing.

[0006] Therefore, an object of the present invention is to provide a cosmetic preparation, etc. that can suppress the significant yellowing that occurs when a non-reducing sugar and a sugar alcohol are added to a cosmetic preparation, etc. that contains tranexamic acid. [Means for solving the problem]

[0007] In order to achieve the above object, the present invention has the following configuration. 1. The following components (A) to (D); (A) Tranexamic acid (B) Non-reducing sugars (C) Sugar alcohol (D) Organic acids, their salts, or their derivatives A cosmetic or topical skin preparation comprising the compound. 2. The cosmetic or topical skin preparation according to 1, wherein the component (D) is nicotinamide. 3. A cosmetic or topical skin preparation according to 1. or 2., wherein the component (B) is trehalose. 4. A cosmetic or topical skin preparation according to 1. or 2., wherein the component (C) is sorbitol. 5. A cosmetic or topical skin preparation according to 1. or 2., further comprising component (E) a sorbitan surfactant. 6. The following ingredients (A) to (C) each containing an organic acid, its salt, or its derivative as an active ingredient; (A) Tranexamic acid (B) Non-reducing sugars (C) Sugar alcohol An agent for inhibiting yellowing of a composition containing the compound. 7. The following components (A) to (C) are used, which include an organic acid, its salt, or its derivative; (A) Tranexamic acid (B) Non-reducing sugars (C) Sugar alcohol A method for inhibiting yellowing of a composition comprising: Effect of the Invention

[0008] According to the present invention, it is possible to inhibit yellowing of cosmetics and the like containing tranexamic acid, a non-reducing sugar, and a sugar alcohol under high-temperature storage conditions. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0009] The present invention will be described in detail below. In this specification, the symbol "to" means a range including the numerical values ​​before and after it.

[0010] Tranexamic acid, the component (A) used in the present invention, is a type of amino acid with the chemical name trans-4-(aminomethyl)cyclohexane-1-carboxylic acid. As mentioned above, it is known as an ingredient that has whitening and anti-inflammatory effects on the skin, and is also sometimes used as a hemostatic agent.

[0011] In the cosmetic or topical skin preparation of the present invention, the content of component (A) tranexamic acid is not particularly limited, but is preferably 0.1% by mass (hereinafter, "% by mass" will be abbreviated simply as "%") or more, more preferably 1% or more, and even more preferably 2% or more. It is also preferably 10% or less, more preferably 7% or less, and even more preferably 5% or less. It is also preferably 0.1 to 10%, more preferably 1 to 7%, and even more preferably 2 to 5%. Within this range, the efficacy of tranexamic acid is excellent, and the stability of the preparation is also excellent.

[0012] The non-reducing sugar of component (B) used in the present invention is a sugar that does not exhibit reducing properties, and is not particularly limited as long as it is used in cosmetics, etc., but specific examples include trehalose, sucrose, etc. Among these, trehalose is preferred from the viewpoint of sensory properties when incorporated into a preparation.

[0013] In the cosmetic or topical skin preparation of the present invention, the content of the non-reducing sugar (B) is not particularly limited, but is preferably 0.001% or more, more preferably 0.1% or more, and even more preferably 1% or more. It is also preferably 20% or less, more preferably 10% or less, and even more preferably 6% or less. It is also preferably 0.001 to 20%, more preferably 0.1 to 10%, and even more preferably 1 to 6%. Within this range, the moisturizing effect is excellent, and the stability of the preparation and the yellowing suppression effect are also excellent.

[0014] The sugar alcohol of component (C) used in the present invention is a carbohydrate in which hydrogen has been added to the carbonyl group of the carbohydrate, and is not particularly limited as long as it is used in cosmetics, etc., but specific examples include sorbitol and xylitol, which are reduced monosaccharides, maltitol and lactitol, which are reduced disaccharides, reduced starch syrup, etc. Among these, sorbitol or maltitol is preferred, and sorbitol is more preferred, from the viewpoint of yellowing inhibition effect and sensory properties when incorporated into a preparation.

[0015] In the cosmetic or skin topical preparation of the present invention, the content of the sugar alcohol component (C) is not particularly limited, but is preferably 0.001% or more, more preferably 0.1% or more, and even more preferably 1% or more. It is also preferably 20% or less, more preferably 10% or less, and even more preferably 6% or less. It is also preferably 0.001 to 20%, more preferably 0.1 to 10%, and even more preferably 1 to 6%. Within this range, the moisturizing effect is excellent, and the stability of the preparation and the yellowing suppression effect are also excellent.

[0016] The organic acid, its salt, or its derivative of component (D) used in the present invention is an organic compound having a carboxyl group, its salt, or its derivative, and is not particularly limited as long as it is used in cosmetics, etc., but specific examples include organic acids such as lactic acid, citric acid, tartaric acid, malic acid, succinic acid, pyrrolidone carboxylic acid, etc.; vitamin B group such as nicotinic acid, pantothenic acid, folic acid, etc.; aliphatic organic acids such as 2-ethylhexanoic acid, caprylic acid, capric acid, etc.; and / or derivatives thereof. The salt of the organic acid is not particularly limited, and examples include inorganic salts such as sodium, potassium, calcium, magnesium, aluminum, zinc, etc., or organic salts of organic amines such as ammonia, monoethanolamine, diethanolamine, triethanolamine, etc., and basic amino acids such as arginine, lysine, etc., and one or more of these can be used in combination. The "derivative" of the present invention, unless otherwise specified, includes esters, amides, or glycosides and refers to those that are acceptable as ingredients of cosmetics and the like. They may be water-soluble or oil-soluble, but are preferably water-soluble from the viewpoint of incorporation into formulations. Among these, from the viewpoint of the efficacy of the formulation on the skin, B vitamins such as nicotinic acid, pantothenic acid, and folic acid and / or derivatives thereof are preferred, nicotinic acid and / or derivatives thereof are more preferred, and nicotinamide is particularly preferred.

[0017] Nicotinamide is an amide compound of nicotinic acid (also called vitamin B3 or niacin), and is a derivative of nicotinic acid, also called nicotinamide or niacinamide. Nicotinamide is a water-soluble vitamin and a known substance that is one of the vitamin B group, and can be obtained by extraction from natural products (such as rice bran) or synthesis by known methods. Specifically, those listed in the 15th revised Japanese Pharmacopoeia 2008 can be used.

[0018] In the cosmetic or skin topical preparation of the present invention, the content of the component (D) organic acid, its salt, or its derivative is not particularly limited, but is preferably 0.001% or more, more preferably 0.002% or more, even more preferably 0.005% or more, and particularly preferably 0.01% or more. It is also preferably 30% or less, more preferably 20% or less, and even more preferably 10% or less. It is also preferably 0.001 to 30%, more preferably 0.002 to 20%, and even more preferably 0.005 to 10%. Within this range, the stability of the preparation is excellent and the yellowing suppression effect is also excellent.

[0019] When component (D) is nicotinic acid amide, the content mass ratio of components (A), (B), (C), and (D) (A):{(B)+(C)}:(D) is not particularly limited, but is preferably 1:0.1-10:0.1-10, more preferably 1:0.5-5:0.2-5, and particularly preferably 1:1-3:0.3-3.5. Within this range, the yellowing inhibition effect is more excellent.

[0020] The cosmetic or topical skin preparation of the present invention may further contain component (E), a sorbitan surfactant. The sorbitan surfactant of component (E) is a sorbitan fatty acid ester or a polyoxyethylene sorbitan fatty acid ester (also called a polysorbate) in which a polyoxyethylene chain has been added to a sorbitan fatty acid ester. There is no particular limitation as long as it is used in cosmetics and the like, and examples thereof include sorbitan fatty acid esters such as sorbitan oleate, sorbitan stearate, sorbitan sesquioleate, and sorbitan palmitate; polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan laurate (20 E.O.) (polysorbate 20), polyoxyethylene sorbitan monostearate (20 E.O.) (polysorbate 60), polyoxyethylene sorbitan tristearate (20 E.O.) (polysorbate 65), polyoxyethylene sorbitan monooleate, (20 E.O.) (polysorbate 80), and polyoxyethylene sorbitan trioleate (20 E.O.) (polysorbate 85); and the like. When component (E) is combined with a cosmetic or the like containing components (A) to (C), yellowing of the cosmetic or the like is promoted, but yellowing can be suppressed by component (D). Among the above-mentioned components (E), from the viewpoint of the effect of suppressing yellowing of cosmetics or the like, polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan laurate (20E.O.) (polysorbate 20), polyoxyethylene sorbitan monostearate (20E.O.) (polysorbate 60), polyoxyethylene sorbitan tristearate (20E.O.) (polysorbate 65), polyoxyethylene sorbitan monooleate (20E.O.) (polysorbate 80), and polyoxyethylene sorbitan trioleate (20E.O.) (polysorbate 85) are preferred, with polyoxyethylene sorbitan monooleate (20E.O.) (polysorbate 80) being more preferred.

[0021] In the cosmetic or topical skin preparation of the present invention, the content of the sorbitan surfactant (E) is not particularly limited, but is preferably 0.0001% or more, more preferably 0.001% or more, and even more preferably 0.01% or more. It is also preferably 10% or less, more preferably 5% or less, and even more preferably 1% or less. It is also preferably 0.0001 to 10%, more preferably 0.001 to 5%, and even more preferably 0.01 to 1%. Within this range, the stability of the preparation is excellent, and the yellowing suppression effect by the component (D) is also excellent.

[0022] In addition to the above-mentioned components (A) to (E), the cosmetic preparation or topical skin preparation of the present invention may contain, as necessary, components used in cosmetic preparations or topical skin preparations, i.e., aqueous components, oily components, surfactants, metal soaps, gelling agents, powders, water-soluble polymers, film-forming agents, resins, UV protection agents, inclusion compounds, antibacterial agents, preservatives, fragrances, deodorants, salts, pH adjusters, antioxidants, cooling agents, animal or microbial extracts, plant extracts, blood circulation promoters, astringents, antiseborrheic agents, skin-whitening agents, anti-inflammatory agents, active oxygen scavengers, cell activators, moisturizers, chelating agents, keratolytic agents, enzymes, hormones, and the like, within the scope of the invention.

[0023] The aqueous component used in the cosmetic or topical skin preparation of the present invention is not particularly limited, but examples thereof include lower alcohols such as ethyl alcohol and isopropyl alcohol, glycols such as propylene glycol, 1,3-butylene glycol, dipropylene glycol, pentanediol, hexanediol, and polyethylene glycol, glycerols such as glycerin, diglycerin, and polyglycerin, and so-called water, such as deionized water, distilled water, purified water, hot spring water, and steam-distilled water derived from plants such as rose water and lavender water, etc. The content of the aqueous component in the cosmetic or topical skin preparation of the present invention is not particularly limited, but is preferably 60 to 99%.

[0024] The surfactant is not particularly limited, but examples thereof include anionic surfactants, cationic surfactants, amphoteric surfactants, and nonionic surfactants other than component (E).

[0025] The oily components are not particularly limited, but include hydrocarbons, fats and oils, waxes, hardened oils, ester oils, fatty acids, higher alcohols, silicone oils, fluorine-based oils, lanolin derivatives, oily gelling agents, and the like, regardless of their origin (such as animal oil, vegetable oil, synthetic oil, etc.) and their properties (such as solid oil, semi-solid oil, liquid oil, volatile oil, etc.).

[0026] Examples of moisturizing agents include proteins, mucopolysaccharides, collagen, elastin, keratin, polyhydric alcohols, etc.; examples of antioxidants include tocopherol, ascorbic acid, etc.; and examples of preservatives include paraoxybenzoic acid esters, phenoxyethanol, etc.

[0027] The cosmetic preparation of the present invention can be in various forms such as liquid, gel, cream, solid, mousse, etc., and may be stored in a container capable of spraying in mist form and sprayed in mist form for use. The formulation of the product of the present invention is not particularly limited and may be a solubilized type, oil-in-water type, water-in-oil type, oil-based type, water-in-oil-in-water type, oil-in-water-in-oil type, multi-layer type, etc.

[0028] The method for producing the cosmetic composition of the present invention is not particularly limited, and the cosmetic composition can be prepared by a conventional method, for example, by mixing the above-mentioned components (A) to (E) and, if necessary, the above-mentioned optional components.

[0029] The use of the present invention as a cosmetic product is not particularly limited, and the present invention can be used as a cosmetic product or an external skin preparation.

[0030] Examples of the cosmetic of the present invention are not particularly limited, and may be in any form, for example, skin care cosmetics such as milky lotion, cream, lotion, beauty serum, and pack; makeup cosmetics such as foundation, blusher, lipstick, eye color, mascara, eyeliner, and nail polish; hair cosmetics such as hair care products, hair tonic, shampoo, rinse, and hair wax; cleansing products such as facial cleanser, and the like.

[0031] Examples of the external skin preparation of the present invention are not particularly limited, and may be in any form, such as external gel, cream, ointment, liquid, liniment, poultice, sheet, etc.

[0032] The present invention also provides the following components (A) to (C), each of which contains the organic acid, a salt thereof, or a derivative thereof as an active ingredient: (A) Tranexamic acid (B) Non-reducing sugars (C) Sugar alcohol The agent for inhibiting yellowing of the composition containing the compound can be obtained by a known method. The agent for inhibiting yellowing or the method for inhibiting yellowing of the present invention can be used in cosmetics; topical skin preparations such as quasi-drugs and pharmaceuticals; oral preparations, injectable preparations, etc., and is particularly suitable for use in cosmetics or topical skin preparations that are applied to the skin. In addition, examples of forms in which the agent for suppressing yellowing of the present invention is blended include cosmetics, quasi-drugs, and skin external preparations such as medicines. When the agent for suppressing yellowing of the present invention is blended in these forms, it may contain an appropriate acceptable ingredient. In addition, the agent for suppressing yellowing of the present invention may be blended when these are produced.

[0033] The present invention can also employ the following configuration. <1> The following components: (A) to (D); (A) Tranexamic acid (B) Non-reducing sugars (C) Sugar alcohol (D) Organic acids, their salts, or their derivatives The cosmetic or topical skin preparation contains the compound. <2> The component (D) is nicotinamide. <1> The cosmetic or topical skin preparation according to claim 1, <3> The component (B) is trehalose. <1> or <2> The cosmetic or topical skin preparation according to claim 1, <4> The component (C) is sorbitol. <1> ~ <3> The cosmetic or topical skin preparation according to any one of the above items. <5> The above-mentioned, further containing component (E) a sorbitan-based surfactant. <1> ~ <4> The cosmetic or topical skin preparation according to any one of the above items. <6> The following ingredients (A) to (C) each contain an organic acid, its salt, or its derivative as an active ingredient: (A) Tranexamic acid (B) Non-reducing sugars (C) Sugar alcohol It is an agent for suppressing yellowing of the composition containing the compound. <7> The following components (A) to (C) use an organic acid, its salt, or its derivative; (A) Tranexamic acid (B) Non-reducing sugars (C) Sugar alcohol A method for inhibiting yellowing of a composition containing the compound. EXAMPLES

[0034] The present invention will be described in more detail below with reference to examples, but the present invention is not limited thereto.

[0035] <Tests for confirming yellowing and inhibiting yellowing of cosmetics containing tranexamic acid, non-reducing sugars, and sugar alcohols>

[0036] Example 1: Verification of the yellowing concentration of tranexamic acid when non-reducing sugar and sugar alcohol are contained and verification of the yellowing suppression effect of component (D)

[0037] The present inventors have found that the combination of tranexamic acid, a non-reducing sugar, and a sugar alcohol promotes yellowing of cosmetics, and further that the yellowing can be suppressed by nicotinamide. The results are shown in Table 1.

[0038] Components 1 to 5 were dissolved uniformly at room temperature according to the composition shown in Table 1 to prepare each sample solution. The solution was then transferred to a standard bottle (No. 5 standard bottle, Kawaguchi Pharmaceutical Chemicals) and stored under high temperature conditions (50°C) for 28 days.

[0039] [Table 1]

[0040] The degree of yellowing in each sample solution was observed by measuring absorbance. 200 μL was dispensed into a 96-well plate (Falcon), and measurements were performed at room temperature using a microplate reader (Biotech).

[0041] The degree of yellowing in each sample solution was measured by measuring the absorbance at 450 nm, and the degree of yellowing at the blended concentration of tranexamic acid and the degree of yellowing due to the combined use of non-reducing sugar and sugar alcohol were confirmed. In addition, a comparison was made between systems containing component (D) and systems not containing component (D).

[0042] The yellowing inhibition rate was calculated by measuring the absorbance at 450 nm of each sample solution and using the following formula (1). Yellowing inhibition rate (%) = ((BA) / B) × 100 (1) A = absorbance of the example B = absorbance of Comparative Example 1-4

[0043] The yellowing inhibition effect was evaluated as follows. (Yellowing inhibition rate) (Evaluation) 50% or more A 30% or more, less than 50% B 5% or more, less than 30% C Less than 5% D

[0044] From the results in Table 1, it was confirmed that yellowing was more accelerated in Comparative Examples 1-1 to 1-4, which contained tranexamic acid, than in Reference Example 1, which contained only non-reducing sugar and sugar alcohol without tranexamic acid. It was also confirmed that yellowing was more accelerated in Comparative Example 1-4, which used a combination of a non-reducing sugar and a sugar alcohol, than in Reference Examples 2 and 3, which contained tranexamic acid in combination with either a non-reducing sugar or a sugar alcohol. On the other hand, in Example 1, in which tranexamic acid was combined with a non-reducing sugar, sugar alcohol, and nicotinamide, the degree of yellowing was reduced compared to Comparative Example 1-4, which did not contain nicotinamide, and the yellowing inhibition effect was excellent.

[0045] <Test on the yellowing inhibition effect of nicotinamide when containing tranexamic acid, non-reducing sugar, and sugar alcohol>

[0046] Example 2: Concentration verification of the yellowing inhibition effect of nicotinamide (Component (D))

[0047] The present inventors have found that the yellowing of cosmetics is accelerated by combining tranexamic acid, non-reducing sugar and sugar alcohol, and that the yellowing can be inhibited by nicotinamide. The inhibiting effect was confirmed when the concentration of nicotinamide was in the range of 0.5 to 10%. The results are shown in Table 2.

[0048] Components 1 to 5 were dissolved uniformly at room temperature to prepare sample solutions according to the compositions shown in Table 2. The solutions were then transferred to standard bottles (No. 5 standard bottles, Kawaguchi Pharmaceutical Chemicals) and stored under high temperature conditions (50°C) for 28 days.

[0049] [Table 2]

[0050] The degree of yellowing in each sample solution was observed by measuring absorbance. 200 μL was dispensed into a 96-well plate (Falcon), and measurements were performed at room temperature using a microplate reader (Biotech).

[0051] The degree of yellowing in each sample solution was measured by measuring the absorbance at 450 nm, and the concentration of component (D) was compared.

[0052] The yellowing inhibition rate was calculated by measuring the absorbance of each sample solution at 450 nm and calculating the following formula (1). The calculation was carried out using Yellowing inhibition rate (%) = ((BA) / B) × 100 (1) A = absorbance of each example B = absorbance of Comparative Example 2-1

[0053] The yellowing inhibition effect was evaluated as follows. (Yellowing inhibition rate) (Evaluation) 50% or more A 30% or more, less than 50% B 5% or more, less than 30% C Less than 5% D

[0054] The results in Table 2 show that Examples 2-1 to 2-4, which contained nicotinamide, had a lower degree of yellowing than Comparative Example 2-1, which did not contain nicotinamide, and thus had an excellent yellowing inhibition effect.

[0055] <Test on the yellowing prevention effect of cosmetics containing tranexamic acid, non-reducing sugar, and sugar alcohol>

[0056] Example 3: Study of component (D)

[0057] The present inventors have found that the combination of tranexamic acid, a non-reducing sugar, and a sugar alcohol promotes yellowing of cosmetics, and further that the yellowing can be suppressed by either nicotinamide or sodium citrate. The results are shown in Table 3.

[0058] Components 1 to 7 were dissolved uniformly at room temperature according to the composition shown in Table 3 to prepare each sample solution. The solution was then transferred to a standard bottle (No. 5 standard bottle, Kawaguchi Pharmaceutical Chemicals) and stored under high temperature conditions (50°C) for 28 days.

[0059] [Table 3]

[0060] The degree of yellowing in each sample solution was observed by measuring absorbance. 200 μL was dispensed into a 96-well plate (Falcon), and measurements were performed at room temperature using a microplate reader (Biotech).

[0061] The degree of yellowing in each sample solution was measured by measuring the absorbance at 450 nm, and a comparison was made between a system containing component (D) and a system not containing component (D).

[0062] The yellowing inhibition rate was calculated by measuring the absorbance of each sample solution at 450 nm and calculating the following formula (1). The calculation was carried out using Yellowing inhibition rate (%) = ((BA) / B) × 100 (1) A = absorbance of each example B = absorbance of Comparative Example 3-1 (in the case of Example 3-2) B = absorbance of Comparative Example 3-2 (Examples 3-3 to 3-4)

[0063] The yellowing inhibition effect was evaluated as follows. (Yellowing inhibition rate) (Evaluation) 50% or more A 30% or more, less than 50% B 5% or more, less than 30% C Less than 5% D

[0064] The results in Table 3 confirm that yellowing is more accelerated in Comparative Examples 3-1 and 3-2, which contain non-reducing sugars and sugar alcohols, than in Reference Example 3, which contains only tranexamic acid but does not contain non-reducing sugars or sugar alcohols. On the other hand, in Example 3-3 in which tranexamic acid was combined with a non-reducing sugar, sugar alcohol, and nicotinamide, the degree of yellowing was reduced compared to the system not containing nicotinamide, demonstrating an excellent yellowing inhibition effect. Similarly, in Examples 3-2 and 3-4, in which tranexamic acid was combined with a non-reducing sugar, sugar alcohol, and sodium citrate, the degree of yellowing was reduced compared to the system not containing sodium citrate, demonstrating excellent yellowing inhibition effects.

[0065] <Test on the yellowing inhibition effect of cosmetics containing sorbitan surfactants in addition to tranexamic acid, non-reducing sugars and sugar alcohols>

[0066] Example 4: Experiment to confirm yellowing of tranexamic acid, non-reducing sugar, and sugar alcohol when component (E) is contained, and verification of the yellowing suppression effect of each component (D)

[0067] The present inventors have found that the yellowing of cosmetics is accelerated by combining sorbitan surfactants in addition to tranexamic acid, non-reducing sugars and sugar alcohols, and that the yellowing can be suppressed by either nicotinamide or sodium citrate. The results are shown in Table 4.

[0068] Components 1 to 8 were dissolved uniformly at room temperature according to the composition shown in Table 4 to prepare each sample solution. The solution was then transferred to a standard bottle (No. 5 standard bottle, Kawaguchi Pharmaceutical Chemicals) and stored under high temperature conditions (50°C) for 28 days.

[0069] [Table 4]

[0070] The degree of yellowing in each sample solution was observed by measuring absorbance. 200 μL was dispensed into a 96-well plate (Falcon), and measurements were performed at room temperature using a microplate reader (Biotech).

[0071] The degree of yellowing in each sample solution was measured by measuring the absorbance at 450 nm, and a comparison was made between a system containing component (D) and a system not containing component (D).

[0072] The yellowing inhibition rate was calculated by measuring the absorbance of each sample solution at 450 nm and calculating the following formula (1). The calculation was carried out using Yellowing inhibition rate (%) = ((BA) / B) × 100 (1) A = absorbance of each example B = absorbance of Comparative Example 4-1 (Examples 4-1 to 4-2) B = absorbance of Comparative Example 4-2 (Examples 4-3 to 4)

[0073] The yellowing inhibition effect was evaluated as follows. (Yellowing inhibition rate) (Evaluation) 50% or more A 30% or more, less than 50% B 5% or more, less than 30% C Less than 5% D

[0074] The results in Table 4 confirm that yellowing is more accelerated in Comparative Examples 4-1 and 4-2, which contain non-reducing sugars, sugar alcohols, and sorbitan-based surfactants, than in Reference Example 4, which contains only tranexamic acid without non-reducing sugars or sugar alcohols. On the other hand, in Examples 4-1 and 4-3, in which tranexamic acid was combined with a non-reducing sugar, a sugar alcohol, a sorbitan surfactant, and nicotinamide, the degree of yellowing was reduced compared to the system not containing nicotinamide, and the yellowing inhibition effect was excellent. Similarly, in Examples 4-2 and 4-4, in which tranexamic acid was combined with a non-reducing sugar, a sugar alcohol, a sorbitan surfactant, and sodium citrate, the degree of yellowing was reduced compared to the system not containing sodium citrate, demonstrating excellent yellowing inhibition effects.

[0075] Example 5 [Lotion] (Component) (%) 1. Ethanol 4.88 2. PEG-50 hydrogenated castor oil isostearate 0.3 3. Methylparaben 0.1 4. 1,3-butylene glycol 0.5 5. Citric acid 0.02 6. Sodium citrate 0.02 7. Purified water remaining amount 8. Tranexamic acid 1.0 9. Trehalose 1.0 10. Sorbitol 1.0

[0076] (Manufacturing method) A: Mix components (1) to (3). B: Mix components (4) to (10). A was added to B and stirred to obtain a lotion.

[0077] The lotion of Example 5 had an A rating for yellowing inhibition effect, and was excellent in inhibiting the yellowing of tranexamic acid, non-reducing sugars, and sugar alcohols.

[0078] Example 6 [Emulsion] (Component) (%) 1. Polyoxyethylene (20 mol) sorbitan monostearate 1.0 2. Polyoxyethylene (20 mol) sorbitan trioleate 0.5 3. Glyceryl Monostearate 1.0 4. Stearic acid 0.5 5. Behenyl alcohol 0.5 6. Squalane 4.0 7. Carboxyvinyl polymer 0.1 8. Methyl parahydroxybenzoate 0.1 9. Sodium hydroxide 0.05 10. Tranexamic acid 1.0 11. Nicotinamide 1.5 12. Trehalose 1.0 13. Maltitol 1.0 14. Purified water remaining amount 15. Ethanol 5.0 16.Fragrance 0.05

[0079] (Manufacturing method) A: Mix ingredients (1) to (6) uniformly at 70°C. B: Components (7) to (14) are mixed uniformly at 70°C. C: Add A to B, emulsify and cool to room temperature. D: (15) to (16) were added to C and mixed uniformly to obtain an emulsion.

[0080] The emulsion of Example 6 was rated C for its yellowing inhibition effect, and was excellent in inhibiting the yellowing of tranexamic acid, non-reducing sugar, and sugar alcohol.

[0081] Example 7 [Cream] (Component) (%) 1. Hydrogenated soy lysophospholipid 1.0 2. Cholesterol-complexed hydrogenated soy phospholipid 1.0 3. Squalane 5.0 4. Heavy Liquid Isoparaffin 2.0 5. Neopentyl glycol dicaprate 5.0 6. Glyceryl triethylhexanoate 5.0 7. Phytosteryl Oleate 1.0 8. Shea butter 1.0 9. Ceramide-2 0.01 10. Cetostearyl alcohol 3.0 11. Behenyl alcohol 2.0 12. Dipropylene glycol 20.0 13. Polyoxyethylene sorbitan monooleate (20E.O.) 0.5 14. Sorbitan Sesquioleate 0.5 15. Polyoxypropylene (10P.O.) methyl glucoside 5.0 16. Sodium pyrosulfite 0.01 17. Sodium monohydrogen phosphate 0.1 18. Sodium dihydrogen phosphate 0.1 19. Phenoxyethanol 0.2 20. Acrylic Acid / Sodium Acrolydimethyltaurate Copolymer 1.0 21. Hydroxypropyl methylcellulose 0.1 22. Nicotinamide 6.0 23. Tranexamic acid 3.0 24. Trehalose 10.0 25. Sorbitol 10.0 26. Remaining purified water

[0082] (Manufacturing method) A: Dissolve components (1) to (14) by heating at 70°C. B: Heat component (26) to 70°C, add to A and emulsify. C: B was cooled, and ingredients (15) to (25) were added and mixed to obtain a cream.

[0083] The cream of Example 7 was rated C for its yellowing inhibition effect, and was excellent in inhibiting the yellowing of tranexamic acid, non-reducing sugar, and sugar alcohol.

[0084] Example 8 [Sunscreen cosmetic (water-in-oil cream type)] (Component) (%) 1. Polyoxyethylene (20 mol) sorbitan monolaurate 0.2 2. Polyoxyethylene (60 mol) hydrogenated castor oil 0.1 3. Purified water remaining amount 4. Dipropylene glycol 10.0 5. Magnesium sulfate 0.5 6. Sodium citrate 0.05 7. Tranexamic acid 1.0 8. Trehalose 2.0 9. Maltitol 2.0 10. Decamethylcyclopentasiloxane 20.0 11. Isotridecyl isononanoate 5.0 12. 2-Ethylhexyl p-methoxycinnamate 8.0 13. Dimethicone 3.0 14. Dimethylstearylammonium Hectorite 1.2

[0085] (Manufacturing method) A: Uniformly disperse components (1) to (9). B: Uniformly disperse components (10) to (14). C: While stirring B, gradually add A and emulsify to obtain a water-in-oil type cream sunscreen cosmetic. Got it.

[0086] The sunscreen cosmetic of Example 8 (water-in-oil cream type) had a yellowing inhibition effect of A, and was excellent in inhibiting the yellowing of tranexamic acid, non-reducing sugar, and sugar alcohol.

[0087] Example 9 [Ointment] (Component) (%) 1. Triethanolamine 2.0 2. Glycerin 5.0 3. Purified water remaining amount 4. Nicotinamide 6.0 5. Tranexamic acid 5.0 6. Trehalose 5.0 7. Sorbitol 3.0 8. Stearic acid 18.0 9. Cetanol 4.0 10. dl-α-tocopherol acetate 0.2 11. Methyl parahydroxybenzoate 0.1

[0088] (Manufacturing method) A. Dissolve ingredients (1) to (7) uniformly and keep at 75°C. B. Heat and mix ingredients (8) to (11) and maintain at 75°C. B was gradually added to CA to obtain an ointment.

[0089] The ointment of Example 9 had a yellowing inhibitory effect of C, and was excellent in inhibiting the yellowing of tranexamic acid, non-reducing sugars, and sugar alcohols. [Industrial Applicability]

[0090] The method for inhibiting yellowing of the present invention can be applied to foods, beverages, and compositions, and cosmetics or topical skin preparations are useful for exerting effects on the skin, such as preventing aging, and preventing and improving spots and wrinkles.

Claims

1. The following components (A) to (D): (A) Tranexamic acid (B) Non-reducing sugar (C) Sugar alcohol (D) Organic acid, its salt, or its derivative A cosmetic or topical skin preparation comprising the compound.

2. The cosmetic or topical skin preparation according to claim 1 , wherein the component (D) is nicotinamide.

3. 3. The cosmetic or topical skin preparation according to claim 1, wherein the component (B) is trehalose.

4. 3. The cosmetic or topical skin preparation according to claim 1, wherein the component (C) is sorbitol.

5. The cosmetic or topical skin preparation according to claim 1 or 2, further comprising a component (E) a sorbitan surfactant.

6. The following components (A) to (C) each containing an organic acid, a salt thereof, or a derivative thereof as an active ingredient: (A) Tranexamic acid (B) Non-reducing sugar (C) Sugar alcohol An agent for inhibiting yellowing of a composition containing the compound.

7. The following components (A) to (C) are used, which include an organic acid, a salt thereof, or a derivative thereof; (A) Tranexamic acid (B) Non-reducing sugar (C) Sugar alcohol A method for inhibiting yellowing of a composition comprising:

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