Aqueous composition

A water-based composition combining niacinamide, tranexamic acid, water-soluble polysaccharides, and hydrophobic polyether urethane addresses aggregate issues, ensuring stability and smooth application in cosmetic and skin care products.

JP2025013701APending Publication Date: 2025-01-24KOSE CORPORATION
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Patent Information

Application Number
JP2024198639
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2020-03-31
Filing Date
2024-11-13
Publication Date
2025-01-24

AI Technical Summary

Technical Problem

Existing technologies fail to address the issue of aggregate formation when combining niacinamide and tranexamic acid with water-soluble polysaccharides, leading to crystallinity issues in cosmetic and skin care compositions.

Method used

A water-based composition incorporating niacinamide, tranexamic acid or their derivatives, water-soluble polysaccharides, and hydrophobic polyether urethane is used to suppress aggregate formation, with specific ratios and methods to ensure stability.

Benefits of technology

The composition effectively prevents aggregate formation, providing a smooth and non-sticky application experience while maintaining the efficacy of the active ingredients.

✦ Generated by Eureka AI based on patent content.

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Abstract

To provide a composition with a high aggregation-inhibitory effect.SOLUTION: Provided is an aqueous composition containing (A) one or more active ingredients selected from niacinamide (a1) and tranexamic acid (a2) or derivatives thereof, (B) one or more water-soluble polysaccharides selected from cellulose-based water-soluble polysaccharides and alginic acid or salts thereof, and (C) a hydrophobically modified polyetherurethane in an amount of 0.5 mass% or less. In the aqueous composition, the content of an oil solution is 3 mass% or less.SELECTED DRAWING: None
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Description

[Technical field]

[0001] The present invention relates to an aqueous composition. [Background technology]

[0002] The skin develops wrinkles, sagging, pigmentation such as age spots and freckles, etc. due to internal factors such as aging and stress, and external factors such as ultraviolet rays and dry air. In particular, morphological changes such as wrinkles and sagging, and visual changes such as pigmentation, greatly affect the impression of the skin's appearance, so many people wish to improve them, and various products are available. Many active ingredients have been proposed to prevent and improve these wrinkles, sagging, and pigmentation. Among them, niacinamide, an active ingredient for wrinkles and sagging, is known to be highly safe and to have an anti-aging effect on the skin. In addition, the use of tranexamic acid has been proposed as a whitening agent that improves or inhibits pigmentation.

[0003] However, niacinamide and tranexamic acid have very high crystallinity, and when incorporated into preparations or compositions such as cosmetics and topical skin preparations, crystal precipitation becomes a problem. In response to this, a technique has been disclosed for suppressing the crystal precipitation of niacinamide by blending one or more water-soluble polysaccharides selected from the group consisting of Tremella fuciformis polysaccharide, sodium chondroitin sulfate, and proteoglycan, a polyhydric alcohol, and a lower monohydric alcohol (see, for example, Patent Document 1). Also, a technique has been disclosed in which the crystal precipitation of tranexamic acid is suppressed by blending two or more water-soluble polymers selected from carboxyvinyl polymer, xanthan gum, and alginate (see, for example, Patent Document 2). [Prior art documents] [Patent documents]

[0004] [Patent Document 1] JP 2019-131547 A [Patent Document 2] JP 2018-177763 A Summary of the Invention [Problem to be solved by the invention]

[0005] However, the technology of Patent Document 1 makes no mention of the occurrence of aggregates due to the combination of niacinamide and a water-soluble polysaccharide. Furthermore, the technology of Patent Document 2 also makes no mention of the occurrence of aggregates due to the combination of tranexamic acid and a water-soluble polysaccharide. As mentioned above, no consideration was given to the occurrence of aggregates or the increase in aggregates over time due to the combination of niacinamide and / or tranexamic acid with a water-soluble polysaccharide.

[0006] Therefore, the present invention aims to provide an aqueous composition containing one or more active ingredients selected from niacinamide and tranexamic acid or its derivatives, and a water-soluble polysaccharide, in which aggregation caused by niacinamide and / or tranexamic acid and the water-soluble polysaccharide is alleviated by using a hydrophobic polyether urethane together, thereby providing a composition having an excellent aggregation inhibitory effect. [Means for solving the problem]

[0007] In view of the above circumstances, the present inventors conducted intensive research and discovered that the above problems could be solved by an aqueous composition using one or more active ingredients selected from niacinamide and tranexamic acid or its derivatives, a water-soluble polysaccharide, and a hydrophobic polyether urethane, thereby completing the present invention.

[0008] That is, the present invention provides an aqueous composition characterized by containing the following components (A) to (C) in order to inhibit the generation of aggregates and the increase of aggregates over time caused by combining one or more active ingredients selected from niacinamide and tranexamic acid or a derivative thereof with a water-soluble polysaccharide: [1] The following components: (A) to (C); (A) (a1) niacinamide and (a2) one or more active ingredients selected from tranexamic acid or its derivatives (B) Water-soluble polysaccharide (C) Hydrophobically modified polyether urethane It is an aqueous composition comprising: [2] The aqueous composition according to [1], wherein the content of the component (A) in the aqueous composition is 1 to 10% by mass. [3] The aqueous composition according to [1] or [2], wherein the component (B) is one or more water-soluble polysaccharides selected from the group consisting of water-soluble cellulose polysaccharides and alginic acid or a salt thereof. [4] The aqueous composition according to any one of [1] to [3], wherein the component (A) is a combination of two kinds of compounds, that is, (a1) niacinamide and (a2) tranexamic acid or a derivative thereof. [5] The aqueous composition according to any one of [1] to [4], wherein the content mass ratio of the components (A) to (C), [(A)+(B)] / (C), is greater than 1 and is 110 or less. [6]

[0023] A skin external preparation or cosmetic comprising the aqueous composition according to any one of [1] to [5]. [7] The present invention relates to an aggregation inhibitor comprising the aqueous composition according to any one of [1] to [5]. [8] This is a method for suppressing the generation of aggregates in a mixture of the component (A) and the component (B) by using the component (C). Effect of the Invention

[0009] The aqueous composition of the present invention can suppress the generation of aggregates of an active ingredient selected from niacinamide and tranexamic acid or its derivatives and a water-soluble polysaccharide. Furthermore, the aqueous composition of the present invention is excellent in smoothness and non-stickiness when applied, and can provide a good feeling when used. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0010] Hereinafter, the embodiments of the present invention will be described. Note that the present invention is not limited to only the following embodiments. In this specification, "X to Y" indicating a range includes X and Y and means "X or more and Y or less." Furthermore, unless otherwise specified, the operation and measurement of physical properties are performed under the conditions of room temperature (25°C) / relative humidity 40%RH.

[0011] (Component (A): (a1) niacinamide and (a2) one or more active ingredients selected from tranexamic acid or its derivatives)

[0012] The component (a1) niacinamide used in the present invention is an amide compound of nicotinic acid (vitamin B3 / niacin). Niacinamide is a water-soluble vitamin and a known substance that is one of the vitamin B group, and can be extracted from natural products (such as rice bran) or synthesized by known methods. Specifically, those listed in the 17th revised Japanese Pharmacopoeia can be used.

[0013] The component (a2) tranexamic acid used in the present invention is a type of amino acid represented by trans-4-(aminomethyl)cyclohexane-1-carboxylic acid, and is known as a component having a whitening effect and an anti-inflammatory effect on the skin as described above, and is also used as a hemostatic agent. In the present invention, a derivative of tranexamic acid can be used in place of or together with tranexamic acid. Derivatives of tranexamic acid include dimers of tranexamic acid (e.g., trans-4-(trans-aminomethylcyclohexanecarbonyl)aminomethylcyclohexanecarboxylic acid hydrochloride), esters of tranexamic acid and hydroquinone (e.g., trans-4-aminomethylcyclohexanecarboxylic acid 4'-hydroxyphenyl ester), esters of tranexamic acid and gentisic acid (e.g., 2-(trans-4-aminomethylcyclohexanecarbonyloxy)-5-hydroxybenzoic acid and its salts), amides of tranexamic acid (e.g., trans-4-aminomethylcyclohexanecarboxylic acid methylamide and its salts, trans-4-(P-methoxybenzoyl)aminomethylcyclohexanecarboxylic acid and its salts, trans-4-guanidinoaminomethylcyclohexanecarboxylic acid and its salts), and alkyl esters of tranexamic acid and its salts. Specifically, tranexamic acid lauryl ester, tranexamic acid myristyl ester, tranexamic acid cetyl ester, tranexamic acid stearyl ester, etc. may be mentioned. The derivative may also be in the form of a salt, and the types include mineral acid salts such as hydrochloride, phosphate, sulfate, bromate, nitrate, etc.; organic acid salts such as oxalate, lactate, citrate, etc.; carbonate, etc. In the present invention, tranexamic acid is preferred as a whitening agent that improves or inhibits pigmentation. One or more of these may be used.

[0014] The content of component (A) in the present invention is not particularly limited, but from the viewpoint of the action of the active ingredient and non-stickiness, etc., it is preferably 1% by mass (hereinafter, simply "% by mass" will be abbreviated to "%") or more in the aqueous composition, more preferably 2% or more, and even more preferably 5% or more. Also, from the viewpoint of the feeling of use such as stickiness upon application, the content of component (A) is preferably 10% or less, more preferably 8% or less, and even more preferably 7% or less.

[0015] In the present invention, one or more of (a1) niacinamide and (a2) tranexamic acid or its derivatives can be selected, but it is more preferable to use two of them in combination from the viewpoint of excellent action as an active ingredient. When two kinds of components (a1) and (a2) are used in combination, there is a preferred range for each content. In the present invention, the content of component (a1) niacinamide in the aqueous composition is preferably 1% or more, more preferably 2% or more, and even more preferably 3% or more. Also, it is preferably less than 10%, more preferably 7% or less, and even more preferably 5% or less from the viewpoint of usability such as non-stickiness. Also, the content of component (a2) tranexamic acid in the aqueous composition is preferably 1% or more, more preferably 1.5% or more, and even more preferably 2% or more. Also, it is preferably less than 10%, more preferably 4% or less, and even more preferably 3% or less from the viewpoint of usability such as non-stickiness.

[0016] (Component (B): water-soluble polysaccharide) The water-soluble polysaccharide is not particularly limited as long as it is one that is normally used in cosmetics, quasi-drugs, medicines, etc., but is preferably a polysaccharide that forms an elastic gel by swelling with water. For example, agar, carrageenan, pectin, gellan gum, locust bean gum, tamarind gum, xanthan gum, cellulose, methylcellulose, ethylcellulose, carboxymethylcellulose, sodium carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hyaluronic acid, alginic acid, etc., and salts thereof can be exemplified. These water-soluble polysaccharides can be used alone or in appropriate combination of two or more kinds. In the present invention, the use of polysaccharides derived from plants such as pectin, locust bean gum, tamarind gum, cellulose, polysaccharides derived from seaweed such as agar, carrageenan, alginic acid, or synthetic polysaccharides as water-soluble polysaccharides may be more effective in suppressing aggregation than the use of polysaccharides derived from microorganisms such as gellan gum and xanthan gum. In particular, among water-soluble polysaccharides, mucopolysaccharides such as hyaluronic acid and chondroitin sulfate, thickening polysaccharides derived from microorganisms such as gellan gum and xanthan gum, and polysaccharides containing two glucose and one glucuronic acid in the structural unit such as gellan gum and xanthan gum are less likely to produce aggregates in combination with component (A), and therefore may be less likely to suppress aggregation. In the present invention, mucopolysaccharides refer to linear polysaccharides having a repeating structure of disaccharide units of uronic acid and amino sugar.

[0017] In the present invention, from the viewpoint of usability such as smoothness and non-stickiness upon application, component (B) is preferably a cellulose-based water-soluble polysaccharide such as methylcellulose, ethylcellulose, carboxymethylcellulose, sodium carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, etc., and alginic acid or a salt thereof, of which carboxymethylcellulose, sodium carboxymethylcellulose, hydroxypropylmethylcellulose, and hydroxyethylcellulose are more preferred, and carboxymethylcellulose, sodium carboxymethylcellulose, and hydroxypropylmethylcellulose are even more preferred.

[0018] As the water-soluble cellulose polysaccharide, for example, CMC Daicel (manufactured by Daicel Chemical Industries Co., Ltd.), Metolose 90SH-15000 (manufactured by Shin-Etsu Chemical Co., Ltd.) and the like are commercially available. As the alginic acid or a salt thereof, for example, Snow Algin M (manufactured by Fuji Chemical Industry Co., Ltd.) and the like are commercially available.

[0019] The content of component (B) used in the present invention is preferably 0.1% or more in the aqueous composition, more preferably 0.2% or more, and even more preferably 0.25% or more, from the viewpoint of usability such as smoothness when applied. Also, from the viewpoint of usability such as non-stickiness, it is preferably 1% or less, more preferably 0.7% or less, and even more preferably 0.5% or less.

[0020] (Component (C): Hydrophobically modified polyether urethane) Hydrophobically modified polyether urethane is an amphiphilic copolymer with a hydrophilic backbone and hydrophobic ends, and is an associative thickener that exhibits a thickening effect when the hydrophobic parts of the copolymer associate with each other in an aqueous medium. Component (a) is represented by the following general formula (1). R 1 ─{(O─R 2 ) k ─OCONH─R 3 [─NHCOO─(R 4 ─O) n ─R 5 ]h} m (1)

[0021] In the above formula (1), R 1 , R 2 and R 4 R represents a hydrocarbon group which may be the same or different; 3 represents a hydrocarbon group which may have a urethane bond, R 5 represents a linear, branched or secondary hydrocarbon group, m is a number of 2 or more, h is a number of 1 or more, and k and n are independently numbers in the range of 0 to 1000. 1 , R 2 and R 4 The carbon number of R is 2 to 4. 3 The carbon number of R is 1 to 30. 5 The number of carbon atoms is preferably 8 to 36. Furthermore, m is preferably 2, h is preferably 1, and k is preferably 1 to 500, more preferably 100 to 300. Furthermore, n is preferably 1 to 200, more preferably 10 to 100.

[0022] The hydrophobically modified polyether urethane represented by the above general formula (1) is, for example, R 1 -[(OR 2 ) k -OH] m and one or more polyether polyols represented by R 3 -(NCO) h+1 and one or more polyisocyanates represented by the formula: 4 -O) n -R 5 The polyether monoalcohols can be obtained by reacting the polyether monoalcohols represented by the following formula (1):

[0023] In this case, R in general formula (1) 1 ~R 5 is the R used 1 -[(OR 2 ) k -OH] m , R 3 -(NCO) h+1 , HO-(R 4 -O) n-R 5 The charging ratio of the three is not particularly limited, but the ratio of hydroxyl groups derived from polyether polyol and polyether monoalcohol to isocyanate groups derived from polyisocyanate is preferably NCO / OH=0.8:1 to 1.4:1.

[0024] Among them, in the present invention, from the viewpoint of the effect of suppressing aggregation by components (A) and (B), those having a structure in which both ends of polyethylene glycol are modified with decyltetradecyl alcohol and having an average weight molecular weight of about 50,000 (GPC method) are preferred. Examples of commercially available products of such hydrophobically modified polyether urethane include "ADEKA NOL GT-700" (manufactured by ADEKA Corporation), which is a PEG-240 / decyltetradeceth-20 / hexamethylene diisocyanate copolymer.

[0025] The content of component (C) used in the present invention is preferably 0.1% or more in the aqueous composition, from the viewpoint of ensuring the aggregation-inhibiting effect while maintaining a smooth texture when applied, more preferably 0.2% or more, and even more preferably 0.5% or more. Also, from the viewpoint of excellent usability such as smoothness when applied and non-stickiness, and excellent aggregation-inhibiting effect, the content of component (C) is preferably 2% or less, more preferably 1.5% or less, and even more preferably 1% or more.

[0026] The content mass ratio of components (A) to (C) [(A)+(B)] / (C) is not particularly limited, but is preferably more than 1, 3 or more, more preferably 5 or more, and even more preferably 10 or more, and from the viewpoint of the aggregation suppression effect, etc., is particularly preferably 12 or more, 15 or more. Moreover, the content mass ratio [(A)+(B)] / (C) is preferably 110 or less, more preferably 80 or less, even more preferably 50 or less, and especially preferably 35 or less, 24 or less, in order to favorably exhibit non-stickiness and smoothness during application while ensuring the aggregation suppression effect.

[0027] The viscosity of the aqueous composition of the present invention at 25°C is not particularly limited, but from the viewpoints of smoothness when applied, aggregation suppression effect, etc., it is preferably 50 mPa·s or more, and more preferably 100 mPa·s or more. Furthermore, from the viewpoints of usability such as smoothness when applied and non-stickiness, and aggregation suppression effect, it is preferably 20,000 mPa·s or less, more preferably 10,000 mPa·s or less, and even more preferably 5,000 mPa·s or less. Here, the viscosity in the present invention means a value obtained by reading the measured value when a rotor is rotated at a speed of 60 revolutions per minute for 1 minute using a single cylinder rotational viscometer (manufactured by Shibaura Systems Co., Ltd.) after leaving the composition in a thermostatic chamber at 25°C for 24 hours, and multiplying the measured value by the respective multipliers.

[0028] In addition to the above components, the aqueous composition of the present invention may contain optional components contained in ordinary cosmetics and the like, so long as they do not impair the effects of the present invention, namely, water, oils, powders, water-soluble polymers other than component (B), film-forming agents, surfactants, lower alcohols, polyhydric alcohols, oil-soluble gelling agents, organically modified clay minerals, resins, colorants, UV absorbers, preservatives, antibacterial agents, fragrances, antioxidants, pH adjusters, chelating agents, vitamins, amino acids, cosmetic ingredients, etc. In the aqueous composition of the present invention, the aggregation-inhibiting effect is more suitably exhibited, so that the proportion of aqueous components in the composition is preferably 90% or more.

[0029] Here, the aqueous component may be any component soluble in water, and examples thereof include glycols such as propylene glycol, 1,3-butylene glycol, dipropylene glycol, and polyethylene glycol, glycerols such as glycerin, diglycerin, and polyglycerin, sugar alcohols such as sorbitol, maltitol, and glucose, lower alcohols such as ethanol, and moisturizing components such as polyoxyalkylene glycerin ether, polyoxyalkylene diglycerin ether, and polyoxyalkylene alkyl glucoside. The water is not particularly limited as long as it is generally used in cosmetics and the like, and examples thereof include purified water, hot spring water, ion-exchanged water, deep sea water, tap water, and steam-distilled water from plants, and one or more types may be appropriately selected and used as necessary.

[0030] The oil agent is not particularly limited as long as it is one generally used in cosmetics, etc., and examples thereof include higher alcohols, hydrocarbon oils, ester oils, waxes, silicone oils, etc. In the present invention, the content of the oil agent in the present invention is not particularly limited, but is preferably 3% or less in the aqueous component, and more preferably 1% or less. Within this range, an aqueous composition excellent in smoothness and non-stickiness when applied can be obtained.

[0031] The aqueous composition of the first embodiment of the present invention may be used as a cosmetic or topical skin preparation in its final form as is, or the aqueous composition may be mixed with other ingredients to produce a cosmetic or topical skin preparation. That is, the second embodiment is a cosmetic or topical skin preparation that contains the aqueous composition of the first embodiment. The cosmetic or topical skin preparation of the second embodiment is likely to exhibit the effects of the aqueous composition, such as smoothness and non-stickiness upon application, and aggregation suppression effect.

[0032] The formulation of the cosmetic or topical skin preparation containing the aqueous composition of the present invention is not particularly limited, but may be aqueous, solubilized, oil-in-water, water-in-oil-in-water, multi-layered, etc., with aqueous, solubilized, and oil-in-water being preferred.

[0033] The cosmetic or topical skin preparation containing the aqueous composition of the present invention may be in various forms such as liquid, gel, cream, mousse, etc., and among these, a liquid form is preferable in terms of obtaining the effects of the present invention. Here, liquid means a state having fluidity at 25° C. Specifically, the viscosity measured at 25° C. using a Brookfield rotational viscometer is 20,000 mPa s or less, preferably 10,000 mPa s or less, more preferably 5,000 mPa s or less.

[0034] The aqueous composition of the present invention can be used as a cosmetic product. For example, it is suitable as a skin lotion, milky lotion, cream, beauty essence, massage cosmetic product, pack cosmetic product, hand cream, body lotion, body cream, makeup cosmetic product, makeup base cosmetic product, eye cream, sunscreen, hair cream, hair wax, etc., and is preferably used as a skin care cosmetic product in terms of being able to realize the effect. Methods of use include a method of using it on hands, fingers, or cotton, a method of using it by impregnating nonwoven fabric, etc., a method of using it by directly spraying, etc.

[0035] The aqueous composition of the present invention can also be used as a skin external preparation. For example, it can be used as a liquid preparation, a gel preparation, a cream, an ointment, a liniment, a lotion, a cataplasm, a plaster, a spray, an aerosol, etc. The method of use can be the same as that of the above-mentioned cosmetic preparation.

[0036] The method for producing the aqueous composition of the present invention is not particularly limited, and the composition is prepared by a conventional method. For example, the aqueous composition can be produced by dissolving or dispersing the above-mentioned components (A) to (C) and, if necessary, the above-mentioned optional components in water to form an aqueous composition or an oil-in-water emulsion, for example, by using a homomixer or a high-pressure emulsifier.

[0037] The present invention can also be configured as a method for suppressing the formation of aggregates in a mixture of components (A) and (B) by using component (C). Here, in the method of the present invention, any of the following procedures can be used: mixing components (A) to (C) in a coexisting state, adding component (C) to a mixture of components (A) and (B), adding a mixture of components (A) and (B) to component (C), mixing component (C) with one of components (A) and (B), and then adding the remaining one of components (A) and (B). In the present invention, in order to suppress the generation of aggregates, it is preferable to use the procedure of adding component (C) to a mixture of components (A) and (B), adding a mixture of components (A) and (B) to component (C), or mixing components (C) and (B), and then adding component (A). Specifically, the method of the present invention may be carried out by uniformly dissolving and mixing all of component (B), all of component (C), and all or a part of the optional components at 70 to 80°C, cooling to 30 to 40°C to prepare a first mixture, and separately, uniformly dissolving and mixing only all of component (A), or all of component (A) and the remainder of the optional components, at room temperature (25°C) to prepare a second mixture, and then adding the first mixture to the second mixture at room temperature (25°C) and mixing. EXAMPLES

[0038] The effects of the present invention will be described using the following examples and comparative examples. However, the technical scope of the present invention is not limited to the following examples. Furthermore, unless otherwise specified, each operation is performed at room temperature (25°C). Examples 1 to 19 and Comparative Examples 1 to 5: Aqueous Compositions (Cosmetic Serums) The aqueous compositions shown in Tables 1 to 3 were prepared and evaluated for smoothness when applied, non-stickiness, and aggregation suppression effect by the following methods. The results are also shown in Tables 1 to 3.

[0039] [Table 1]

[0040] [Table 2]

[0041] [Table 3] (Note 1) ADEKA NOL GT-700 (ADEKA Corporation) (Note 2) CMC Daicel 1170 (manufactured by Daicel Chemical Industries, Ltd.) (Note 3) Metrose 90SH-15000 (manufactured by Shin-Etsu Chemical Co., Ltd.) (Note 4) Snow Argin M (manufactured by Fuji Chemical Industry Co., Ltd.)

[0042] (Manufacturing method) A. Components (3) to (7) and a portion of (8) are homogeneously dissolved and mixed at 70°C, and then cooled to 40°C. B. Dissolve and mix ingredients (1), (2), (8) to (11) uniformly at room temperature. A was added to CB and mixed to obtain an aqueous composition.

[0043] (Evaluation method 1) B: Smoothness when applied Regarding the smoothness when applied, a test was conducted by a panel of 20 cosmetic evaluation specialists, who applied 1.5g of each sample to the entire face, and each panelist rated the smoothness when blending the sample on a 5-point scale using the absolute evaluation below, and calculated the average score from the total scores of all panelists for each sample, and judged it according to the following 3-point judging criteria. If it is ○ or above, it is acceptable for practical use. Absolute evaluation criteria (Score):(Evaluation) 5: Very sensitive 4: Somewhat 3: Normal 2: I don't feel much 1: I don't feel it Three-level evaluation criteria (Judgment): (Average score) ◎: 4 points or more: Very good ○: 3 points or more but less than 4 points: Good △: Less than 3 points: Poor

[0044] (Evaluation method 2) B: Non-stickiness Regarding non-stickiness, a use test was conducted by a panel of 20 cosmetic evaluation specialists, who applied 1.5g of each sample to the entire face, and each panelist rated the stickiness immediately after applying it on a 5-point scale using the absolute evaluation below, and calculated the average score from the total scores of all panelists for each sample, and judged it according to the following 4-point judging criteria. If it is rated as ◯ or above, it is acceptable for practical use. Absolute evaluation criteria (Score):(Evaluation) 5: No sticky feeling 4: Not very sticky 3: Normal 2: Feels slightly sticky 1: Very sticky 4-level evaluation criteria (Judgment): (Average score) ◎: 4 points or more: Very good ○: 3 points or more but less than 4 points: Good △: 2 points or more and less than 3 points: slightly poor ×: Less than 2 points: Defective

[0045] (Evaluation method 3) C: Aggregation inhibition effect The aggregation-inhibiting effect was evaluated by placing each sample in a 40 mL transparent glass container, storing it in a thermostatic chamber at 50°C for two weeks, and then visually observing it and rating it into one of three categories according to the following evaluation criteria: ◯ or higher is acceptable for practical use. Three-level evaluation criteria (Judgment): (Evaluation) ◎: No aggregates observed ○: Aggregates are observed in some areas, or aggregates have not increased ×: Aggregates are observed throughout the sample, or the number of aggregates has increased.

[0046] As is clear from the results in Tables 1 to 3, the aqueous compositions of Examples 1 to 19 of the present invention were smoother when applied, less sticky, and had better aggregation inhibition effects than the aqueous compositions of Comparative Examples 1 to 5.

[0047] In contrast, no aggregates were observed in Comparative Examples 1 and 2, which did not contain component (A) or component (B). Moreover, in Comparative Examples 3 to 5, which did not contain component (C), aggregates of components (A) and (B) were observed, and furthermore, satisfactory lack of stickiness was not obtained.

[0048] Example 20: Lotion (Component) (mass%) (1) Niacinamide (ingredient (a1)) 4 (2) Tranexamic acid (ingredient (a2)) 3 (3) Sodium monohydrogen phosphate 0.02 (4) Sodium dihydrogen phosphate 0.02 (5) Sodium pyrosulfite 0.003 (6) Purified water 20 (7) Methyl parahydroxybenzoate 0.1 (8) Disodium edetate 0.05 (9)Fragrance 0.2 (10) Ethanol 10 (11) Phenoxyethanol 0.2 (12) Polyoxyethylene hydrogenated castor oil isostearate Note 5 0.1 (13) Polyoxyethylene polyoxypropylene decyl tetra Decyl ether Note 6 0.1 (14) 1,3-butylene glycol 10 (15) Glycerin 5 (16) Dipropylene glycol 5 (17) Diglycerin 0.5 (18) Remaining purified water (19)(PEG-240 / Decyltetradeceth-20 / HDI) Copolymer (Component (C)) Note 1 0.5 (20) Sodium carboxymethylcellulose (component (B)) Note 2 0.5 (Note 5) EMALEX RWIS-150 (manufactured by Nippon Emulsion Co., Ltd.) (Note 6) NILLOL PEN-4620 (manufactured by Nippon Surfactant Industries Co., Ltd.)

[0049] (Manufacturing method) A: Components (1) to (8) are dissolved and mixed uniformly at room temperature. B: Components (9) to (13) are dissolved and mixed uniformly at room temperature. C: Components (14) to (20) are homogeneously dissolved and mixed at 70°C. D: Add A to C which has been cooled to 40℃ and mix. E: A lotion was obtained by adding B to D and mixing. The lotion of Example 20 obtained as described above was excellent in all respects: smoothness upon application, non-stickiness, and aggregation-inhibiting effect. The mass ratio of the components (A) to (C), [(A)+(B)] / (C), was 15.

[0050] Example 21: Oil-in-water emulsion (Component) (mass%) (1) 1,3-butylene glycol 5 (2) Glycerin 5 (3) Remaining amount of purified water (4) Polyethylene glycol monostearate (40E.O.) 0.5 (5) Sorbitan sesquioleate 0.1 (6) Hydrogenated soybean phospholipid Note 7 0.2 (7) Cholesterol Note 8 0.1 (8) Caprylic / caprylic triglyceride 1 (9) α-Olefin Oligomer 1 (10) Phytosteryl Macadamiate Note 9 0.5 (11) Vaseline 0.5 (12) Dimethylpolysiloxane (10CS) 0.5 (13) Cetostearyl alcohol 1 (14) Behenyl alcohol 0.5 (15) Methyl parahydroxybenzoate 0.1 (16) Carboxyvinyl polymer 0.2 (17)(PEG-240 / Decyltetradeceth-20 / HDI) Copolymer (Component (C)) Note 1 0.2 (18) Hydroxypropyl methylcellulose (component (B)) Note 3 0.5 (19) (Sodium acrylate / sodium acryloyldimethyltaurate) Copolymer Note 10 0.5 (20) Sodium hydroxide 0.04 (21) Niacinamide (ingredient (a1)) 5 (22) Tranexamic acid (ingredient (a2)) 4 (23) Sodium monohydrogen phosphate 0.02 (24) Sodium dihydrogen phosphate 0.02 (25) Sodium pyrosulfite 0.003 (26) Purified water 10 (27) Ethanol 5 (28)Fragrance 0.1 (29) Phenoxyethanol 0.2 (Note 7) PRESOME CS2-101 (manufactured by Nippon Fine Chemicals) (Note 8) Kairei Marine Cholesterol (manufactured by Nippon Suisan Kaisha) (Note 9) PLANDOOL-MAS (manufactured by Nippon Fine Chemicals) (Note 10) SIMULGEL EG QD (SEPPIC)

[0051] (Manufacturing method) A: Components (1) to (3) are homogeneously dissolved and mixed at 75°C. B: Components (4) to (14) are uniformly dissolved and mixed at 75°C. C: Add B to A and emulsify at 70℃. D: Components (15) to (29) were added to E and mixed, then cooled to 40° C. to obtain an oil-in-water emulsion. The oil-in-water emulsion of Example 21 obtained as described above was excellent in all respects: smoothness upon application, non-stickiness, and aggregation-inhibiting effect. The mass ratio of the components (A) to (C), [(A)+(B)] / (C), was 47.5.

[0052] Example 22: Cosmetic serum (oil-in-water type) (Component) (%) (1) 1,3-butylene glycol 5 (2) Dipropylene glycol 5 (3) Remaining amount of purified water (4) Polyoxyethylene sorbitan monooleate (20E.O.) 0.1 (5) Polyethylene glycol monostearate (55E.O.) 0.25 (6) Hydrogen Lecithin Note 11 0.1 (7) Meadowfoam oil 1 (8) Liquid paraffin 2 (9) Cetostearyl alcohol 0.5 (10) Methyl parahydroxybenzoate 0.1 (11) (Acrylates / Alkyl acrylate (C10-30)) Crosspolymer Note 12 0.02 (12) (PEG-240 / Decyltetradeceth-20 / HDI) Copolymer (Component (C)) Note 1 0.5 (13) Sodium alginate (ingredient (B)) Note 4 0.5 (14) Sodium hydroxide 0.01 (15) Niacinamide (ingredient (a1)) 4 (16) Tranexamic acid (ingredient (a2)) 3 (17) Sodium monohydrogen phosphate 0.02 (18) Sodium dihydrogen phosphate 0.02 (19) Sodium pyrosulfite 0.003 (20) Purified water 10 (21) Ethanol 5 (22)Fragrance 0.1 (23) Phenoxyethanol 0.2 (Note 11) Resinol S-10 (manufactured by Nikko Chemicals) (Note 12) CARBOPOL 1382 (manufactured by LUBRIZOL ADVENCED MATERIALS)

[0053] (Manufacturing method) A: Components (1) to (3) are homogeneously dissolved and mixed at 75°C. B: Components (4) to (9) are uniformly dissolved and mixed at 75°C. C: Add B to A and emulsify at 70°C. D: Components (10) to (23) were added to and mixed with C, and then cooled to 40° C. to obtain an oil-in-water type cosmetic essence. The cosmetic essence (oil-in-water type) of Example 22 obtained as described above was excellent in all respects: smoothness upon application, non-stickiness, and aggregation-inhibiting effect. The mass ratio of the components (A) to (C), [(A)+(B)] / (C), was 15.

[0054] Example 23: Sunscreen (oil-in-water type) (Component) (%) (1) 1,3-butylene glycol 5 (2) Glycerin 5 (3) Remaining amount of purified water (4) Behentrimonium chloride 0.1 (5) Hydrogenated lecithin Note 11 0.5 (6) Cholesterol Note 8 0.6 (7) Phytosterol 0.1 (8) Dimethicone diethyl benzalmalonate 1.2 (9) 4-tert-Butyl-4´-methoxy-dibenzoylmethane 2 (10) 2-Ethylhexyl p-methoxycinnamate 7 (11) Diethylamino hydroxybenzoyl hexyl benzoate 2.5 (12) Hydrogenated castor oil (stearic acid) Note 14 1 (13) Propylene glycol dicaprylate 5 (14) Ethyl oleate 0.3 (15) (Acrylic acid / alkyl acrylate (C10-30)) Copolymer Note 13 0.4 (16)(PEG-240 / Decyltetradeceth-20 / HDI) Copolymer (Component (C)) Note 1 0.1 (17) Hydroxyethyl cellulose (component (B)) Note 15 0.5 (18) Xanthan gum 0.1 (19) Triethanolamine 0.4 (20) Niacinamide (ingredient (a1)) 5 (21) Tranexamic acid (ingredient (a2)) 4 (22) Sodium monohydrogen phosphate 0.02 (23) Sodium dihydrogen phosphate 0.02 (24) Sodium pyrosulfite 0.003 (25) Purified water 10 (26) Ethanol 5 (27) Zinc oxide 2 (28)Fragrance 0.1 (29) Phenoxyethanol 0.2 (Note 13) Pemulen TR-2 (manufactured by NOVEON) (Note 14) Castride MS (National Mimatsu) (Note 15) NATROSOL250 HHR (ASHLAND SPECIALTY INGREDIENTS)

[0055] (Manufacturing method) A: Components (1) to (3) are homogeneously dissolved and mixed at 75°C. B: Components (4) to (14) are uniformly dissolved and mixed at 75°C. C: Add B to A and emulsify at 70°C. D: Components (15) to (29) were added to and mixed with C, and then cooled to 40° C. to obtain a sunscreen (oil-in-water type). The sunscreen (oil-in-water type) of Example 23 obtained as described above was excellent in all respects: smoothness upon application, non-stickiness, and aggregation inhibitory effect. The mass ratio of the components (A) to (C), [(A)+(B)] / (C), was 95.

Claims

[Claim 1] The following components (A) to (C): (A) One or more active ingredients selected from (a1) niacinamide and (a2) tranexamic acid (or a derivative thereof). (B) Water-soluble polysaccharide (C) Hydrophobically modified polyether urethane 0.5% by mass or less An aqueous composition comprising: The component (B) is one or more water-soluble polysaccharides selected from the group consisting of cellulose-based water-soluble polysaccharides and alginic acid or a salt thereof, The content of the oil agent in the aqueous composition is 3% by mass or less in the aqueous composition. Aqueous composition.

Citation Information

Patent Citations

  • Pharmaceutical preparation containing tranexamic acids

    JP2018177763A

  • Aqueous composition

    JP2019131547A