Composition

Abstract

To provide a technology that enables suppression of viscosity decrease over time in a composition containing an acrylic copolymer.SOLUTION: A composition contains (A) diisopropylamine dichloroacetate and (B) a thickener, wherein the component (B) contains an acrylic copolymer.SELECTED DRAWING: None

Description

[Technical Field]

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

[0002] Patent Document 1 (JP 2023-108014 A) describes a technique for adjusting the viscosity of a composition containing a water-soluble polymer. The document describes a method for suppressing a decrease in viscosity of an ophthalmic composition containing a water-soluble polymer compound, polyoxyethylene polyoxypropylene glycol, and a specific fat-soluble component, an ophthalmic composition, a container filled with the ophthalmic composition, and an enclosure for packaging the container, by using one of the following means: injecting an inert gas into the enclosure, including an oxygen absorber, or including a container or an enclosure with oxygen absorption capacity, and incorporating a specific component (claim 5). Examples of highly water-soluble polymer compounds include cellulose-based polymer compounds such as hydroxypropylmethylcellulose, methylcellulose, and hydroxyethylcellulose; polyvinyl-based polymer compounds such as polyvinylpyrrolidone and polyvinyl alcohol; hyaluronic acid and its salts; and carboxyvinyl polymers (paragraph 0010).

[0003] On the other hand, Patent Document 2 (JP 2012-211130 A) describes a pharmaceutical or cosmetic composition containing tranexamic acid and diisopropylamine dichloroacetate (DADA) (Claim 1), and describes, as Formulation Example 2, an emulsion containing specific amounts of specific ingredients including DADA, carboxyvinyl polymer, and xanthan gum (Paragraph 0026). [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Japanese Patent Publication No. 2023-108014 [Patent Document 2] Japanese Patent Application Laid-Open No. 2012-211130 Summary of the Invention [Problem to be solved by the invention]

[0005] The present inventors have newly discovered that compositions containing acrylic copolymers are prone to a decrease in viscosity during storage.

[0006] The present invention provides a technique for suppressing a decrease in viscosity over time of a composition containing an acrylic copolymer. [Means for solving the problem]

[0007] The aspects of the present invention are as follows. [1] (A) diisopropylamine dichloroacetate, (B) a thickener; A composition comprising: The composition, wherein the component (B) comprises an acrylic copolymer. [2] The composition according to [1], wherein the acrylic copolymer comprises at least one selected from the group consisting of (acrylates / C10-30 alkyl acrylate) crosspolymer and (sodium acrylate / sodium acryloyldimethyltaurate) copolymer. [3] The composition according to [1] or [2], wherein the mass ratio of the content of the component (A) to the content of the acrylic copolymer in the composition ((A) / acrylic copolymer) is 0.1 or more. [4] The composition according to any one of [1] to [3], wherein the content of the acrylic copolymer in the composition is 0.01% by mass or more and 1% by mass or less with respect to the total amount of the composition. [5] The composition according to any one of [1] to [4], further comprising at least one selected from the group consisting of component (C): tranexamic acid and salts thereof. [6] The composition according to [5], wherein the mass ratio ((C) / (A)) of the content of the component (C) to the content of the component (A) in the composition is 0.1 or more and 20 or less. [7] The viscosity of the composition measured using a Brookfield viscometer at 25°C for 60 seconds is 1.0 mPa·s or more and 1.0×10 5 The composition according to any one of [1] to [6], wherein the viscosity is 0.05 mPa·s or less. [8] An agent for suppressing viscosity reduction in a composition containing a thickener, Contains diisopropylamine dichloroacetate as the active ingredient. A viscosity reduction inhibitor, wherein the thickener comprises an acrylic copolymer. [Effects of the Invention]

[0008] According to the present invention, it is possible to suppress the viscosity decrease over time of a composition containing an acrylic copolymer. DETAILED DESCRIPTION OF THE INVENTION

[0009] Hereinafter, an embodiment of the present invention will be described. In this embodiment, the composition may contain each component either alone or in combination of two or more. In this specification, the symbol "to" indicating a numerical range means "greater than or equal to" or "less than or equal to," and both of the numerical values ​​at both ends are included.

[0010] (composition) In this embodiment, the composition comprises the following components (A) and (B): (A) Diisopropylamine dichloroacetate (DADA) (B) Thickener The component (B) contains an acrylic copolymer.

[0011] The composition of this embodiment contains a combination of components (A) and (B), which effectively prevents viscosity loss over time and also prevents viscosity loss during storage at high temperatures, such as around 50°C.

[0012] Here, when the decrease in viscosity of the composition over time is suppressed, the viscosity of the composition after storage may be similar to the viscosity before storage, or may be higher than the viscosity before storage. The viscosity after storage measured at 25°C is, for example, 0.9 times or more, preferably 0.92 times or more, and more preferably 0.95 times or more of the viscosity before storage, thereby making it possible to further suppress a decrease in viscosity over time. Furthermore, the viscosity after storage measured at 25° C. is, for example, 1.2 times or less, and preferably 1.1 times or less, the viscosity before storage. This makes it possible to more stably suppress fluctuations in viscosity due to storage. The storage conditions can be, for example, 50°C for 2 weeks.

[0013] The composition is preferably an aqueous gel having no fluidity, but it is also preferable that the composition has fluidity, and more preferably is a liquid composition. The viscosity of the composition measured at 25°C for 60 seconds using a Brookfield viscometer is preferably 1.0 mPa·s or more, and more preferably 5.0×10 2 mPa·s or more, more preferably 1.0×10 3 This allows for a formulation that is easy to apply with minimal dripping. 4 It may be mPa·s or more. The viscosity of the composition is preferably 1.0×10 5 mPa·s or less, and more preferably 8.0×10 4 mPa·s or less, more preferably 5.0×10 4 This allows for preparations with properties that can be applied to various containers. 3 It may be less than mPa·s.

[0014] After storage at 50°C for 2 weeks, the viscosity of the composition measured at 25°C for 60 seconds using a Brookfield viscometer is preferably 1.0 mPa·s or more, more preferably 5.0×10 2 mPa·s or more, more preferably 1.0×10 3This allows for the production of a formulation that does not change significantly from the initial sensation upon use. The viscosity of the composition is preferably 1.0×10 5 mPa·s or less, and more preferably 9.0×10 4 mPa·s or less, more preferably 8.0×10 4 This allows for the production of a formulation that does not change significantly from the initial feeling when used.

[0015] Specifically, the viscosity of the composition is measured using a Brookfield viscometer (e.g., TVB-25L, manufactured by Toki Sangyo Co., Ltd.) at 25°C for a measurement time of 60 seconds. The rotor, rotation speed, and measurement range are selected, for example, depending on the properties of the agent, and more specifically, can be selected so that the lower measurement limit of the agent is not less than 10% of the upper measurement limit specified in the instruction manual for the measuring device.

[0016] The composition is applied, for example, to the skin. The composition may also be applied to the skin as an impregnation solution impregnated into a substrate such as a sheet mask, wipe, or cosmetic cotton pad.

[0017] The composition is preferably a cosmetic such as a skin cosmetic; or an external preparation such as a skin topical preparation, and may be a quasi-drug (such as a medicated cosmetic) or a pharmaceutical, and is preferably a cosmetic, a skin topical preparation or a quasi-drug (such as a medicated cosmetic), and more preferably a cosmetic or a quasi-drug (such as a medicated cosmetic). Furthermore, the cosmetic is made of, for example, the composition of this embodiment, which allows the cosmetic to have excellent storage stability. Next, the components contained in the composition will be described.

[0018] (Component (A)) Component (A) is DADA. Component (A) is a known substance and is listed, for example, in the Japanese Pharmacopoeia Non-Drug Standards 2002. Component (A) can be produced by a known method, or a commercially available product can be used.

[0019] The content of component (A) in the composition is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, more preferably 0.1% by mass or more, and even more preferably 0.15% by mass or more, based on the total mass of the composition. This makes it possible to more stably suppress the decrease in viscosity of the composition over time. It also makes it easier to use the composition in various applications such as cosmetics, topical skin preparations, and quasi-drugs. The content of component (A) in the composition is preferably 1.25% by mass or less, more preferably 1% by mass or less, and even more preferably 0.75% by mass or less, based on the total mass of the composition, which makes it possible to more stably suppress a decrease in viscosity of the composition over time.

[0020] (Component (B)) Component (B) is a thickener and contains an acrylic copolymer. Component (B) is preferably a water-soluble polymer, which can improve the viscosity of a water-based composition.

[0021] (acrylic copolymer) Specifically, the acrylic copolymer is a copolymer containing at least one monomer selected from the group consisting of (meth)acrylic acid and (meth)acrylic acid derivatives as a constituent monomer unit, where the (meth)acrylic acid is at least one of acrylic acid and methacrylic acid.

[0022] Among the constituent monomer units of the acrylic copolymer, (meth)acrylic acid derivatives include, for example, (meth)acrylic acid salts such as sodium (meth)acrylate and ammonium (meth)acrylate dimethyltaurate; alkyl (meth)acrylate; and (meth)acrylamide.

[0023] The acrylic copolymer may be, for example, at least one selected from the group consisting of anionic polymers and nonionic polymers. In addition, the acrylic copolymer is preferably a water-soluble polymer, which can further improve the stability of the composition containing water as a base.

[0024] Specific examples of acrylic copolymers include nonionic polymers such as (acrylates / C10-30 alkyl acrylate) crosspolymer, (PEG-240 / decyltetradeceth-20 / HDI) copolymer, and alkyl acrylate copolymer emulsion; and At least one selected from the group consisting of anionic polymers such as (sodium acrylate / sodium acryloyldimethyltaurate) copolymer, (dimethylacrylamide / sodium acryloyldimethyltaurate) crosspolymer, and sodium acrylate-sodium acryloyldimethyltaurate copolymer may be used.

[0025] As the acrylic copolymer, for example, a commercially available product can be used. Commercially available examples of acrylic copolymers include acrylates / C10-30 alkyl acrylate crosspolymers such as Carbopol ETD2020 (manufactured by Lubrizol Advanced Materials Inc.); and sodium acrylate / sodium acryloyldimethyltaurate copolymers such as SIMULGEL EG and SIMULGEL EG QD (both manufactured by SEPPIC).

[0026] The acrylic copolymer preferably contains at least one selected from the group consisting of (acrylates / C10-30 alkyl acrylate) crosspolymer and (sodium acrylate / sodium acryloyldimethyltaurate) copolymer, which allows for the stable blending of a wider variety of ingredients by utilizing the emulsifying power of these ingredients.

[0027] The content of the acrylic copolymer in the composition is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, and even more preferably 0.1% by mass or more, based on the total mass of the composition, thereby enabling a preparation with the desired viscosity to be obtained. The content of the acrylic copolymer in the composition is preferably 1.5% by mass or less, more preferably 1% by mass or less, and even more preferably 0.8% by mass or less, based on the total mass of the composition, thereby providing a smooth formulation with little resistance during application.

[0028] Component (B) may further contain a thickener other than the acrylic copolymer. Specific examples of such a thickener include one or more selected from the group consisting of polysaccharides such as xanthan gum, hydroxyethyl cellulose, carboxymethyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl methyl cellulose stearoxy ether, soluble starch, starch derivatives, alginic acid, locust bean gum, gellan gum, tamarind gum, guar gum, quince seed, carrageenan, hyaluronic acid, dextran, dextran sulfate, and chondroitin sulfate; polyphosphoric acid; highly polymerized polyethylene glycol (e.g., number-average molecular weight of 20,000 or more); vinyl polymers such as polyvinyl alcohol, polyvinylpyrrolidone, polyacrylic acid, and polystyrene sulfonic acid; and salts thereof.

[0029] The total content of component (B) in the composition is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, and even more preferably 0.1% by mass or more, based on the total mass of the composition, thereby enabling a preparation with the desired texture to be obtained. The total content of component (B) in the composition is preferably 3% by mass or less, more preferably 2% by mass or less, and even more preferably 1% by mass or less, based on the total mass of the composition, thereby providing a preparation that causes less resistance and discomfort when applied.

[0030] The mass ratio of the content of component (A) to the content of the acrylic copolymer in the composition ((A) / acrylic copolymer) is preferably 0.1 or more, more preferably 0.2 or more, and even more preferably 0.3 or more, thereby efficiently suppressing the decrease in viscosity of the formulation over time. On the other hand, from the viewpoint of controlling the texture of the preparation, the mass ratio ((A) / acrylic copolymer) is, for example, not more than 8, preferably not more than 3, and more preferably not more than 1.5. This makes it possible to increase the viscosity of the preparation immediately after preparation.

[0031] The composition may contain ingredients other than those mentioned above.

[0032] (water) The composition specifically comprises water. Specific examples of water include those used in various preparations such as cosmetics, quasi-drugs, and pharmaceuticals. More specifically, at least one type selected from the group consisting of purified water, hot spring water, deep sea water, and steam-distilled water from plants can be used.

[0033] The content of water in the composition can be, for example, the remainder after excluding components other than water in the composition. The water content in the composition is, for example, 50% by mass or more, preferably 60% by mass or more, more preferably 70% by mass or more, even more preferably 80% by mass or more, and even more preferably 90% by mass or more, based on the total composition, and specifically less than 100% by mass, preferably 99.8% by mass or less.

[0034] (Component (C)) Component (C) is at least one selected from the group consisting of tranexamic acid and its salts. By further including component (C) in the composition, the effect of inhibiting the viscosity decrease over time of the composition can be more stably obtained. It is also possible to impart additional effects to the composition, such as anti-inflammatory effects and melanin production inhibitory effects. Component (C) is a known compound such as tranexamic acid, etc. Component (C) can be produced by a known method, or a commercially available product can be used.

[0035] The content of component (C) in the composition is preferably 0.1% by mass or more, more preferably 0.5% by mass or more, and even more preferably 0.8% by mass or more, based on the total mass of the composition, which makes it possible to more stably suppress the decrease in viscosity of the composition over time and also to obtain the desired efficacy (e.g., anti-inflammatory effect, melanin production inhibitory effect). The content of component (C) in the composition is preferably 10% by mass or less, more preferably 5% by mass or less, even more preferably 3% by mass or less, still more preferably 2.5% by mass or less, and even more preferably 2% by mass or less, based on the total mass of the composition, thereby preventing a decrease in solubility in the composition.

[0036] The mass ratio ((C) / (A)) of the content of component (C) to the content of component (A) in the composition is preferably 0.1 or more, more preferably 0.5 or more, and even more preferably 1 or more. This makes it possible to efficiently obtain the effect of suppressing the viscosity decrease of the composition over time. Furthermore, the mass ratio ((C) / (A)) is preferably 20 or less, more preferably 10 or less, even more preferably 5 or less, even more preferably 4 or less, and even more preferably 3 or less. This can reduce deterioration in formulation stability other than viscosity reduction, such as crystal precipitation.

[0037] (pH adjuster) The composition may further contain a pH adjuster, such as one or more selected from the group consisting of inorganic acids such as phosphoric acid and salts thereof (e.g., sodium dihydrogen phosphate, potassium dihydrogen phosphate), organic acids such as citric acid and salts thereof (e.g., trisodium citrate), acidic amino acids (e.g., glutamic acid, aspartic acid), basic amino acids (e.g., arginine, lysine, histidine, tryptophan), neutral amino acids (e.g., glycine), and hydroxides such as sodium hydroxide and potassium hydroxide. The amount of the pH adjuster may be, for example, about 0.01 to 10% by mass, about 0.02 to 5% by mass, or about 0.05 to 1% by mass relative to the entire composition.

[0038] The pH of the composition is preferably 4 or higher, more preferably 4.5 or higher, more preferably 5 or higher, and even more preferably 5.25 or higher, which allows, for example, the thickening effect of the thickener to be efficiently maintained. The pH of the composition is preferably 9 or less, more preferably 7 or less, more preferably less than 7, and even more preferably 6.75 or less. This makes it possible to efficiently maintain the thickening effect of the thickener, for example.

[0039] (Other ingredients) In this embodiment, the composition may contain one or more components other than the above-mentioned components, for example, oily components such as fats and oils (vegetable oils, etc.), waxes, hydrocarbon oils (isohexadecane, etc.), ester oils, higher alcohols, higher fatty acids, and silicone oils; ultraviolet absorbers; ultraviolet scattering agents; moisturizers; surfactants; skin protectants; plant extracts; preservatives; sequestering agents; antioxidants; pearlizing agents; colorants; cooling agents; and fragrances.

[0040] Specific examples of the humectant include polyhydric alcohols other than component (B), such as 1,3-butylene glycol, glycerin, methyl gluceth-10, and hydrogenated starch hydrolysates. The humectant is preferably a polyhydric alcohol having a molecular weight of 2,000 or less, more preferably a polyhydric alcohol having a molecular weight of 1,000 or less, more preferably a polyhydric alcohol having a molecular weight of 500 or less, and even more preferably a polyhydric alcohol having a molecular weight of 200 or less. The content of the humectant in the composition can be, for example, 0.1 to 20% by mass of the total composition. Specific examples of surfactants include one or more selected from the group consisting of nonionic surfactants, anionic surfactants, cationic surfactants, and amphoteric surfactants. Examples of nonionic surfactants include polyoxyethylene sorbitan fatty acid esters such as polysorbate-80, and polyoxyethylene hydrogenated castor oils such as PEG-60 hydrogenated castor oil. The content of the nonionic surfactant in the composition can be, for example, 0.01 to 5% by mass of the total composition. A specific example of a skin protective agent is trehalose. The content of the skin protective agent in the composition can be, for example, 0.01 to 1% by mass based on the total mass of the composition. A specific example of the preservative is phenoxyethanol. The content of the preservative in the composition can be, for example, 0.01 to 1% by mass based on the total mass of the composition.

[0041] In this embodiment, the composition can be obtained, for example, by a production method including a step of mixing components (A) and (B) and, if necessary, other ingredients. The other ingredients can be selected depending on, for example, the dosage form of the composition and the desired performance. When the composition is an external preparation, it can be prepared according to the usual method described in, for example, the 18th edition of the Japanese Pharmacopoeia.

[0042] (Viscosity reduction inhibitor, viscosity reduction inhibitor) In this embodiment, the viscosity change inhibitor is an inhibitor of viscosity decrease in a composition containing an acrylic copolymer as a thickener, i.e., component (B), and contains DADA, i.e., component (A), as an active ingredient. Additionally, a method for inhibiting viscosity loss involves adding DADA, component (A), to a composition containing an acrylic copolymer as a thickener, component (B). As described above, by blending component (A) into a composition containing an acrylic copolymer, it is possible to effectively suppress a decrease in viscosity of the composition over time.

[0043] Although the embodiments of the present invention have been described above, these are merely examples of the present invention, and various other configurations can also be adopted. [Example]

[0044] The present embodiment will be specifically described below with reference to examples, but the present embodiment is not limited to these examples.

[0045] (Examples 1 to 5, Comparative Examples 1 to 5) In this example, compositions were prepared and evaluated.

[0046] (Method of preparing the composition) The components shown in Table 1 were mixed and dissolved at room temperature (25°C) to obtain compositions of each example.

[0047] (viscosity) The composition obtained in each example was placed in a 50 g glass bottle and stored at 50°C for 2 weeks ("2w" in Table 1). The viscosity on the day of preparation and after storage was measured using the following method. The pH of each example composition on the day of preparation and after storage was within the range of 5 to 7. Apparatus: B-type viscometer (Toki Sangyo Co., Ltd., TVB-25L) Measurement temperature: 25℃ Measurement time: 60 seconds Conditions: The lower measurement limit must be set to the following value so that it does not fall below 10% of the upper measurement limit (page 111) stated in the instruction manual for the above device (TKV-M0184B: August 2011). Rotor: No. 4 (Comparative Examples 1 to 4), No. 3 (Comparative Example 5, Examples 1 to 4), or No. 2 (Example 5) Rotation speed: 12 rpm (Comparative Examples 1 to 5, Examples 1 to 4) or 30 rpm (Example 5) Measurement range: 1 (Comparative Examples 1 to 5, Examples 1, 2, and 5), 2.5 (Example 3), or 5 (Example 4)

[0048] (evaluation) Based on the viscosity before and after the above-mentioned storage, the product was judged according to the following criteria, with the following A and B being considered acceptable. The evaluation results are also shown in Table 1. A: When the viscosity on the day of preparation is taken as 1.0, the relative viscosity after storage (2w) is greater than 0.95 and less than 3. B: The relative viscosity is greater than 0.90 and not greater than 0.95. C: The relative viscosity is 0.90 or less.

[0049] [Table 1]

[0050] As can be seen from Table 1, in each Example, the decrease in viscosity due to storage was successfully suppressed compared to each Comparative Example.

Claims

1. (A) diisopropylamine dichloroacetate; (B) a thickener; A composition comprising: The composition, wherein the component (B) comprises an acrylic copolymer.

2. The composition according to claim 1, wherein the acrylic copolymer comprises at least one selected from the group consisting of an acrylates / C10-30 alkyl acrylate crosspolymer and a sodium acrylate / sodium acryloyldimethyltaurate copolymer.

3. 3. The composition according to claim 1, wherein the mass ratio of the content of the component (A) to the content of the acrylic copolymer in the composition ((A) / acrylic copolymer) is 0.1 or more.

4. The composition according to claim 1 or 2, wherein the content of the acrylic copolymer in the composition is 0.01% by mass or more and 1% by mass or less with respect to the total mass of the composition.

5. 3. The composition according to claim 1, further comprising at least one component selected from the group consisting of component (C): tranexamic acid and salts thereof.

6. 6. The composition according to claim 5, wherein the mass ratio ((C) / (A)) of the content of the component (C) to the content of the component (A) in the composition is 0.1 or more and 20 or less.

7. The viscosity of the composition measured at 25°C for 60 seconds using a Brookfield viscometer is 1.0 mPa s or more and 1.0 x 10 5 The composition according to claim 1 or 2, having a viscosity of 0.05 mPa·s or less.

8. An agent for inhibiting viscosity reduction in a composition containing a thickener, comprising: Contains diisopropylamine dichloroacetate as the active ingredient. A viscosity reduction inhibitor, wherein the thickener comprises an acrylic copolymer.

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