Composition

Abstract

To suppress crystal deposition in a composition comprising niacinamide and tranexamic acid.SOLUTION: There is provided a composition which comprises the following components (A) to (C): (A) 1 to 10 mass% of niacinamide, (B) 1 to 7 mass% of tranexamic acid, (C) a mucopolysaccharide and (D) an amphiphilic polymer.SELECTED DRAWING: None

Description

[Technical Field]

[0001] This invention relates to a composition. [Background technology]

[0002] Maintaining healthy and beautiful skin is a matter of great concern for many people. Skin can develop various problems such as roughness, wrinkles, sagging, and hyperpigmentation due to various factors including UV radiation, dryness, aging, and stress. To comprehensively improve these skin concerns, it is believed that applying multiple ingredients with different effects to the skin is effective.

[0003] For example, niacinamide, a type of vitamin, has skin-related effects such as wrinkle reduction, improved skin barrier function, whitening, and improved skin texture (see, for example, Non-Patent Document 1). Tranexamic acid has anti-inflammatory properties and is used as an active ingredient in pharmaceuticals, and is also known to inhibit melanin production (see, for example, Patent Document 1). Compositions containing these two components, which have different effects, are expected to provide multifaceted effects on multiple skin concerns.

[0004] On the other hand, compositions containing niacinamide or tranexamic acid alone are known to precipitate crystals over time. Regarding tranexamic acid, it is known that a topical skin preparation containing 0.1 to 5% by mass of tranexamic acid, 0.01 to 5% by mass of a long-chain acyl sulfonate type anionic surfactant, and a higher alcohol, with the pH adjusted to 3 to 6, prevents the precipitation of tranexamic acid crystals (see, for example, Patent Document 2). [Prior art documents] [Patent Documents]

[0005] [Patent Document 1] Japanese Patent Publication No. 2008-100933 [Patent Document 2] Japanese Patent Publication No. 2011-084551 [Non-patent literature]

[0006] [Non-Patent Document 1] Cosmeceuticals and Cosmetic practice Chap.10.2014 page 103-112 [Overview of the project] [Problems that the invention aims to solve]

[0007] Conventionally, compositions containing high concentrations of niacinamide or tranexamic acid have suffered from significant crystal precipitation, and when the composition adheres to the dispensing nozzle or lid of a container during use, crystals precipitate, posing a problem. However, no studies have been conducted to date on suppressing crystal precipitation in compositions containing both niacinamide and tranexamic acid. The present invention aims to solve the problem of finding that crystal precipitation in compositions containing niacinamide and tranexamic acid is more severe than in compositions where each component was present alone. [Means for solving the problem]

[0008] To solve this problem, the inventors conducted diligent research and found that including mucopolysaccharides and amphiphilic polymers in a formulation containing niacinamide and tranexamic acid has an effect of suppressing crystal precipitation.

[0009] In other words, the present invention comprises the following components (A) to (D); (A) Niacinamide 1-10% by mass (B) Tranexamic acid 1-7% by mass (C) Mucopolysaccharide (D) Amphiphilic polymers This relates to a composition containing [the specified substance]. [Effects of the Invention]

[0010] The present invention makes it possible to provide a composition that suppresses crystallization in a composition containing niacinamide and tranexamic acid, a crystallization inhibitor, and a cosmetic or external preparation for skin. MODE FOR CARRYING OUT THE INVENTION

[0011] Hereinafter, the present invention will be described in detail. In the present specification, the symbol "~" shall mean a range including the numerical values before and after the symbol.

[0012] Component (A): Niacinamide Component (A) niacinamide in the present invention is an amide of nicotinic acid (vitamin B3 / niacin). Niacinamide is a water-soluble vitamin, which is a known substance that is one of the B vitamins, and can be extracted from natural products (such as rice bran) or synthesized by a known method. Specifically, those listed in the 15th revised Japanese Pharmacopoeia 2008 can be used.

[0013] The content of component (A) in the present invention is 1 to 10% by mass (hereinafter simply abbreviated as "%"). In a composition containing 1 to 10% of component (A) niacinamide and 1 to 7% of component (B) tranexamic acid, it is more difficult to suppress crystal precipitation than in a composition containing component (A) niacinamide and component (B) tranexamic acid each alone. In the present invention, the content of component (A) is not particularly limited as long as it is 1 to 10%, but from the viewpoint of the crystal precipitation suppression effect, it is preferably 3 to 8%, and more preferably 4 to 7%.

[0014] Component (B): Tranexamic acid Tranexamic acid as component (B) used in the present invention is a type of amino acid represented by trans-4-(aminomethyl)cyclohexane-1-carboxylic acid. Tranexamic acid is sometimes used for its whitening effect and anti-inflammatory effect on the skin, and is also sometimes used as a hemostatic agent.

[0015] The content of component (B) in the present invention is 1 to 7%. In a composition containing 1 to 10% of component (A) niacinamide and 1 to 7% of component (B) tranexamic acid, it is more difficult to suppress crystal precipitation than in a composition containing component (A) niacinamide and component (B) tranexamic acid individually. In the present invention, the content of component (B) is not particularly limited as long as it is between 1 and 7%, but from the viewpoint of suppressing crystal precipitation, it is preferably 1.3 to 6%, and more preferably 1.5 to 5%.

[0016] Ingredients (C): Mucopolysaccharide The mucopolysaccharide (C) used in the present invention is a general term for polysaccharides containing amino sugars and is not particularly limited, but a typical example is glycosaminoglucan. Glycosaminoglucan is composed of repeating disaccharides, one of which is composed of either D-glucosamine or D-galactosamine. Examples of glycosaminoglucans include hyaluronic acid, chondroitin sulfate, chondroitin, ketaran sulfate, heparin, heparin sulfate, and dermatan sulfate. The mucopolysaccharide of the present invention may have a carboxyl group structure in addition to a sulfate ester. Furthermore, the mucopolysaccharide of the present invention can be used without particular limitation as long as it is commonly used in the fields of pharmaceuticals, quasi-drugs, cosmetics, or food and beverages, and may be used alone or in any combination of two or more types.

[0017] The method and origin of obtaining the mucopolysaccharide of the present invention are not particularly limited, but for example, it can be obtained in a state containing a large amount of protein by alkaline treatment, enzymatic treatment, etc. of bones, cartilage, skin, scales, etc. (hereinafter referred to as mucopolysaccharide-containing tissues) of fish such as sharks and salmon, other aquatic animals such as whales and sea cucumbers, and land animals such as cattle, pigs, chickens, and horses. Alternatively, the proteins may be removed from the mucopolysaccharide containing proteins, etc., and a treatment such as ultrafiltration may be performed to obtain high-purity mucopolysaccharide. Mucopolysaccharides can also be obtained by synthesis, semi-synthesis, fermentation, etc.

[0018] The decomposition products of the present invention are mucopolysaccharides with reduced molecular weight. Examples of decomposition methods include decomposition by heating, chemical hydrolysis with acids or bases, and hydrolysis with various enzymes.

[0019] The derivatives of the present invention are obtained by introducing various substituents to mucopolysaccharides, but those obtained by introducing substituents to at least one carboxyl group or hydroxyl group of the mucopolysaccharide, or by forming a salt, are preferred. Examples include esters of mucopolysaccharides to which acetyl groups or benzyl groups have been introduced as substituents, and those that have been crosslinked by introducing formyl groups.

[0020] The salts of the present invention include alkali metal salts such as sodium and potassium, alkaline earth metal salts such as magnesium and calcium, ammonium salts, alkanolamine salts such as monoethanolamine, and mixtures thereof. Preferably, they are alkali metal salts such as sodium salts.

[0021] The hyaluronic acid of the present invention is a high-molecular-weight polysaccharide formed by the alternating linkage of the 3rd position of β-DN-acetylglucosamine and the 4th position of β-D-glucuronic acid. The method of production and origin of hyaluronic acid are not particularly limited, but it can be obtained, for example, by extraction from animal tissue such as chicken combs or by microbial fermentation.

[0022] The weight-average molecular weight of the hyaluronic acid in the present invention is not particularly limited, and may be obtained by decomposing hyaluronic acid to reduce its molecular weight, but is preferably 5,000 to 300,000, and particularly preferably 50,000 to 110,000. The weight-average molecular weight of the hyaluronic acid used in the present invention can also be determined by using hyaluronic acid with a known weight-average molecular weight as a standard, subjecting the sample and the standard to high-performance liquid chromatography, obtaining a standard curve from the weight-average molecular weight and retention time of the standard, and determining the weight-average molecular weight corresponding to the retention time of the sample solution. The weight-average molecular weight of the standard product can be calculated by measuring the intrinsic viscosity according to the 13th edition of the Japanese Pharmacopoeia: General Test Methods, Section 36, Viscosity Measurement Method, and using the formula by Laurent et al. (Biochim. Biophys. Acta, 42, 476 (1960)). There are no particular restrictions on the hyaluronic acid used in the present invention, and it can be appropriately selected depending on the purpose. Examples include hyaluronic acid FCH-201S (weight-average molecular weight 1.8 million to 2.2 million), FCH-121S (weight-average molecular weight 1 million to 1.4 million), FCH-SU-S (weight-average molecular weight 50,000 to 110,000) (manufactured by Food Chemifah Co., Ltd.), and BIO-SODIUM HYALURONATE (manufactured by BIOLAND).

[0023] The hyaluronic acid derivatives of the present invention are obtained by introducing substituents to at least one carboxyl group or hydroxyl group of hyaluronic acid or by forming a salt thereof. Preferred substituents are esters such as acetyl groups and benzyl groups, or groups capable of crosslinking, such as formyl groups. Examples include substances in which one or more carboxyl groups in hyaluronic acid are esterified (e.g., benzyl esterified hyaluronic acid (trade name Hyaff®, Fidia Advanced Biopolymers)), substances in which hyaluronic acid is crosslinked with formaldehyde and further polymerized (e.g., trade name Synvisc®, Biomatrix)), and acetylated hyaluronic acid in which one or more hydroxyl groups in hyaluronic acid are acetylated. Among these, acetylated hyaluronic acid is particularly preferred.

[0024] The sodium chondroitin sulfate of the present invention is the sodium salt of a sugar chain in which sulfuric acid is bonded to a repeating disaccharide of β-DN-acetylgalactosamine and β-D-glucuronic acid. Examples of commercially available products include sodium chondroitin sulfate (manufactured by Maruha Nichiro Corporation).

[0025] In the present invention, it is preferable that component (C) is one or more selected from the group consisting of hyaluronic acid, its salts, and hyaluronic acid derivatives.

[0026] In the present invention, the content of component (C) is not particularly limited, but from the viewpoint of suppressing crystal precipitation, it is preferably 0.000001 to 0.1%, and more preferably 0.00001 to 0.01%.

[0027] In the present invention, although the product can be obtained by appropriately including components (A) to (D), specifying the mass ratio of the components is preferable because it provides a superior crystal precipitation suppression effect. Such mass ratios are not particularly limited, and the mass ratio (A) / (C) of component (A) and component (C) is preferably 10 or more, more preferably 300 or more, and even more preferably 3500 or more. Furthermore, it is preferably 5,000,000 or less, more preferably 1,000,000 or less, even more preferably 100,000 or less, and particularly preferably 45,000 or less.

[0028] In the present invention, although the product can be obtained by appropriately including components (A) to (D), specifying the mass ratio of the components is preferable because it provides a superior effect in suppressing crystal precipitation. Such mass ratios are not particularly limited, and the lower limit of the mass ratio (B) / (C) of component (B) and component (C) is preferably 10 or more, more preferably 50 or more, even more preferably 150 or more, and particularly preferably 1000 or more. The upper limit is preferably 2,000,000 or less, more preferably 1,000,000 or less, even more preferably 250,000 or less, and particularly preferably 2,000 or less.

[0029] In the present invention, although the product can be obtained by appropriately including components (A) to (D), specifying the mass ratio of the components is preferable because it provides a superior effect in suppressing crystal precipitation. Such mass ratios are not particularly limited, and the lower limit of the mass ratio of the total amount of components (A) and (B) to the content of component (C) [(A)+(B)] / (C) is preferably 20 or more, more preferably 100 or more, even more preferably 500 or more, and particularly preferably 5000 or more. The upper limit is preferably 17,000,000 or less, more preferably 10,000,000 or less, even more preferably 1,400,000 or less, particularly preferably 120,000 or less, and most preferably 60,000 or less.

[0030] Ingredient (D): Amphiphilic polymer The amphiphilic polymer (D) used in the present invention is a polymer having hydrophobic and hydrophilic groups. It is preferable that it has affinity for both aqueous and oily media, and in the present invention, a water-soluble or water-dispersible amphiphilic polymer is more preferable. Component (D) is not particularly limited as long as it is used in various formulations such as cosmetics, quasi-drugs, pharmaceuticals, and other topical skin preparations, and may be a synthetic product or extracted or derived from a natural product, and the hydrophobic and hydrophilic groups may be distributed randomly, in blocks, or in grafts. Component (D) may be ionic or nonionic, but anionic or nonionic is preferred considering application to the skin. Examples of the hydrophobic group include cyclic, linear, or branched hydrocarbon groups having about 4 to 30 carbon atoms, cholesteryl groups or cholesterol-derived groups, polyorganosiloxane groups, etc., and may be substituted with fluorine or contain heteroatoms such as oxygen, nitrogen, or sulfur.

[0031] In the present invention, component (D) includes, for example, hydrophobic group-modified acrylic acid derivatives (including alkali-soluble (or swellable) emulsions), hydrophobically modified polyether urethanes, hydrophobically modified hydroxyethyl cellulose, polyoxyalkylene alkyl ethers, homopolymers of 2-methacryloyloxyethyl phosphorylcholine, copolymers of 2-methacryloyloxyethyl phosphorylcholine and hydrophobic monomers, etc. One or more of these can be selected and used.

[0032] As the hydrophobic group-modified acrylic acid derivative, specifically, a linear or branched alkyl group having 4 to 30 carbon atoms is preferable. Commercially available products include, for example, "PEMULEN TR-1" (manufactured by NOVEON), which is an acrylic acid / alkyl acrylate (C10-30) copolymer, "Aculyn 22" (manufactured by ROHM), which is an (alkyl acrylate / steareth-20 methacrylate) copolymer, and as (acrylates / beheneth-25 methacrylate) copolymers, Novethix L-10 (manufactured by Lubrizol Advanced Materials), ACULYN 28 (manufactured by Dow Chemical Group), and the like can be mentioned.

[0033] As the hydrophobically modified polyether urethane, the following general formula (1): R 1 ─(O─R 2 ) k ─OCONH─R 3 ─NHCOO─[ (R 4 ─O) n ─(R 5 ─O) m ─CONH─R 3 ─NHCOO] h ─(R 2 ─O) k ─R 1 (1) (In the above formula (1), R 1 represents a hydrogen group or a hydrocarbon group, and R 2 ~R 5R represents hydrocarbon groups that may be identical or different from each other, where h is a number greater than or equal to 1, and k, n, and m are independently numbers in the range of 0 to 1000, but cannot be 0 at the same time. 2 , R 4 and R 5 The number of carbon atoms is 2 to 4, R 3 The number of carbon atoms is 1 to 30, R 1 The group is preferably a hydrogen group or a hydrocarbon group having 1 to 40 carbon atoms. k is preferably 0 to 100, more preferably 0 to 30. n and m are preferably 0 to 700, more preferably 10 to 500. Examples of copolymers represented by ( ) include:

[0034] Examples of commercially available products include "Adekanol GT-700" (manufactured by ADEKA Corporation), which is a PEG-240 / decyltetradeceth-20 / hexamethylene diisocyanate copolymer; "EXPERT GEL EG 412" (manufactured by POLYMEREXPERT Corporation), which is a (PPG-12 / methylenediphenyl diisocyanate) copolymer; "POLYOL PREPOLYMER-15" (manufactured by Beltech Pharmaceutical Co., Ltd.), which is a (PEG-8 / methylenediphenyl diisocyanate) copolymer; and "EXPERT GEL EG230" (manufactured by POLYMEREXPERT Corporation), which is a bismethoxyPEG-13 (PEG-502 / PPG-57 / methylenediphenyl diisocyanate) copolymer.

[0035] The homopolymer of 2-methacryloyloxyethyl phosphorylcholine (sometimes referred to as MPC), and the copolymer of MPC and a hydrophobic monomer, are represented by the following general formula (2). [ka]

[0036] For MPC homopolymers, a weight-average molecular weight of 5000 or more is preferred, and more preferably 10000 or more, from the viewpoint of suppressing crystal precipitation. For copolymers of MPC and hydrophobic monomers, the type of hydrophobic monomer is not particularly limited, but styrene, acrylic acid esters, and methacrylic acid esters are preferred. The weight-average molecular weight of the copolymer with hydrophobic monomer is also preferably 5000 or more, and more preferably 10000 or more. Furthermore, the molar ratio of MPC to hydrophobic monomer is preferably in the range of 50:50 to 97:3.

[0037] The weight-average molecular weight of the MPC homopolymer and the copolymer of MPC and hydrophobic monomer was measured by dissolving 5 mg of each polymer in a methanol / chloroform mixture (mass ratio: 80 / 20) to prepare a sample solution, and then measuring it by gel permeation chromatography under the following analytical conditions. Column: PLgel-mixed-C Standard substance: polyethylene glycol Detector: Differential refractometer RI-8020 (manufactured by Tosoh Corporation) Method for calculating weight-average molecular weight: Molecular weight calculation program (GPC program for SC-8020) Flow rate: 1 mL per minute Injection volume: 100μL Column oven: Maintains a constant temperature of around 40°C.

[0038] Component (D) is not particularly limited, but to give specific examples, as a homopolymer of MPC, for example, LIPIDURE-HM, LIPIDURE-HM-500, LIPIDURE-HM-600 (all manufactured by NOF Corporation), which contain polyacrylate phosphorylcholine glycol (polymethacryloyloxyethyl phosphorylcholine); LIPIDURE-PMB, LIPIDURE B (all manufactured by NOF Corporation), which contain polyquaternium-51 as a copolymer of MPC and butyl methacrylate; LIPIDURE A (manufactured by NOF Corporation), which contains polyquaternium-65 as a copolymer of MPC, butyl methacrylate and sodium methacrylate; LIPIDURE NA, LIPIDURE-NR (both manufactured by NOF Corporation), which contain polyquaternium-61 as a copolymer of MPC and stearyl methacrylate; and LIPIDURE, which contains polyquaternium-64. Examples of commercially available products include C (manufactured by NOF Corporation), and one or more types selected from these can be used.

[0039] Component (D) is not particularly limited, but from the viewpoint of suppressing crystal precipitation, it is preferably one or more selected from the group consisting of acrylic acid / alkyl acrylate (C10-30) copolymer, 2-methacryloyloxyethyl phosphorylcholine homopolymer, and copolymer of 2-methacryloyloxyethyl phosphorylcholine and a hydrophobic monomer, and more preferably one or more selected from the group consisting of acrylic acid / alkyl acrylate (C10-30) copolymer and polyacrylate phosphorylcholine glycol.

[0040] The content of component (D) used in the present invention is not particularly limited, but from the viewpoint of suppressing crystal precipitation, it is preferably 0.00005 to 0.5%, and more preferably 0.0005 to 0.05%.

[0041] In the present invention, although the product can be obtained by appropriately including components (A) to (D), specifying the mass ratio of components is preferable because it provides a superior crystal precipitation suppression effect. Such mass ratios are not particularly limited, and the lower limit of the mass ratio (A) / (D) of components (A) and (D) is preferably 5 or more, more preferably 10 or more, and even more preferably 40 or more. The upper limit is preferably 200,000 or less, more preferably 20,000 or less, even more preferably 10,000 or less, and particularly preferably 1,000 or less.

[0042] In the present invention, although the product can be obtained by appropriately including components (A) to (D), specifying the mass ratio of the components is preferable because it provides a superior crystal precipitation suppression effect. Such mass ratios are not particularly limited, and the lower limit of the mass ratio (B) / (D) of component (B) and component (D) is preferably 2 or more, more preferably 5 or more, and even more preferably 10 or more. The upper limit is preferably 100,000 or less, more preferably 10,000 or less, even more preferably 5,000 or less, and particularly preferably 1,000 or less.

[0043] In the present invention, although the product can be obtained by appropriately including components (A) to (D), specifying the mass ratio of the components is preferable because it provides a superior effect in suppressing crystal precipitation. Such mass ratios are not particularly limited, and the lower limit of the mass ratio of the total amount of components (A) and (B) to the content of component (D) [(A)+(B)] / (D) is preferably 4 or more, more preferably 10 or more, even more preferably 20 or more, and preferably 100 or more. The upper limit is preferably 340,000 or less, more preferably 200,000 or less, even more preferably 100,000 or less, particularly preferably 50,000 or less, and most preferably 20,000 or less.

[0044] The present invention may further contain component (E) phosphate. The salt is not particularly limited, including organic salts and inorganic salts, but from the viewpoint of adjusting the pH of the composition and providing a buffering effect, an inorganic salt is preferred, and a sodium salt is particularly preferred. By including phosphate in the present composition, it is expected that it will be stably present in compositions containing both components (A) and (B). In the present invention, component (E) phosphate may be used by combining one or more types, for example, monosodium hydrogen phosphate, disodium hydrogen phosphate, potassium dihydrogen phosphate, etc. are preferably used. Among these, one or more selected from the group consisting of monosodium hydrogen phosphate and disodium hydrogen phosphate are preferred, and it is more preferable to include monosodium hydrogen phosphate and disodium hydrogen phosphate.

[0045] The content of component (E) in the present invention is not particularly limited, but it is preferably 0.01% or more, more preferably 0.05% or more, and even more preferably 0.1% or more in the composition. Furthermore, it is preferably 1% or less, more preferably 0.5% or less, and even more preferably 0.3% or less. Within this range, it is more preferable because it provides superior crystal precipitation suppression.

[0046] The present invention may further contain component (F) sugar alcohol. In the present invention, the addition of sugar alcohol is more preferable because it provides a superior effect in suppressing crystal precipitation. In the present invention, the sugar alcohol is not particularly limited, and any of them can be used. For example, erythritol, sorbitol, mannitol, maltitol, xylitol, galactitol, arabitol, trehalose, pentaerythritol, etc., can be used in combination of one or more of these. Among these, one or more selected from the group consisting of erythritol, sorbitol, mannitol, and maltitol are preferred, one or more selected from the group consisting of erythritol, sorbitol, and maltitol are more preferred, and one or more selected from the group consisting of erythritol and sorbitol are even more preferred.

[0047] In the present invention, the content of component (F) is not particularly limited, but it is preferably 0.1% or more, more preferably 0.2% or more, and even more preferably 0.3% or more in the composition. Furthermore, it is preferably 5% or less, more preferably 3% or less, and even more preferably 2% or less. Within this range, it is more preferable because it provides superior crystal precipitation suppression.

[0048] Furthermore, the composition containing components (A) to (F) of the present invention may, if necessary, contain components commonly used in various formulations such as cosmetics, quasi-drugs, and pharmaceuticals for topical use on the skin, to the extent that the effects of this technology are not impaired. Examples of such components include water, oils, surfactants, metal soaps, gelling agents, powders, alcohols, water-soluble polymers, film-forming agents, resins, UV protection agents, inclusion compounds, antibacterial agents, fragrances, deodorants, pH adjusters, cooling agents, animal and microbial extracts, plant extracts, blood circulation promoters, astringents, anti-seborrheic agents, whitening agents, anti-inflammatory agents, free radical scavengers, cell activators, moisturizers, chelating agents, keratolytic agents, enzymes, hormones, vitamins, and the like. One or more of these may be appropriately selected and used.

[0049] The present invention is not particularly limited as long as it can contain water and is used in various formulations such as cosmetics, quasi-drugs, pharmaceuticals, and other topical skin preparations. The water may be purified water, hot spring water, deep sea water, or steam-distilled water from plants, and one or more of these may be appropriately selected and used as needed. The water content is not particularly limited, but is preferably 10-97%, and more preferably 20-95%.

[0050] The composition containing components (A) to (F) of the present invention can be obtained by known manufacturing methods. The manufacturing method is not particularly limited, but for example, it can be obtained by dissolving components (A), (B), and (E) in water, and then adding and mixing components (C), (D), and (F).

[0051] The composition of the present invention is not particularly limited, but is preferably a cosmetic or a topical skin preparation. Specifically, as a cosmetic or topical skin preparation, it may take any of the following forms: basic cosmetics such as lotions, creams, toners, serums, packs, all-in-one gels, sunscreens, and cleansers; makeup cosmetics such as makeup bases, BB creams, foundations, blushes, and lipsticks; hair cosmetics such as hair tonics, hair tonics, shampoos, and conditioners; dispersions, ointments, liquids, aerosols, patches, poultices, and liniments. It is preferably a cosmetic or topical skin preparation used on the skin, with the expectation of whitening effects, emollient effects, etc.

[0052] The composition containing components (A) to (F) of the present invention is not particularly limited, but is preferably a crystal precipitation inhibitor. As a crystal precipitation inhibitor, it can be used in cosmetics, quasi-drugs, pharmaceuticals and other topical skin preparations, oral preparations, injectable preparations, etc., and is particularly preferred for use in cosmetics and topical skin preparations applied to the skin. [Examples]

[0053] The present invention will be described in further detail below with reference to examples, but the present invention is not limited thereto.

[0054] Examples 1-16 and Comparative Examples 1-6: Lotions Lotions were prepared according to the formulations shown in Tables 1-3 below. The crystal precipitation inhibition effect was evaluated for each sample (Examples 1-16, Comparative Examples 1-6) using the evaluation method described below. The results are also shown in Tables 2 and 3.

[0055] (Evaluation criteria) I. Effect of suppressing crystal precipitation

[0056] <Evaluation Method> To evaluate the crystal precipitation suppression effect, 3g of each sample (Examples 1-16, Comparative Examples 1-6, and Reference Examples 1-16) was applied to a 3cm diameter dish (material: polystyrene, manufactured by Corning), and after air-drying at room temperature for 3 days, the height of the precipitated crystals in each sample (Examples 1-16, Comparative Examples 1-6, and Reference Examples 1-16) was measured. The improvement rate of Example X or Comparative Example X was calculated using the following formula (3), and the evaluation was made according to the following criteria.

[0057] Improvement rate (%) in Example X or Comparative Example X = 100 × [(Height of precipitated crystals in Reference Example X) - (Height of precipitated crystals in Example X or Comparative Example X)] / (Height of precipitated crystals in Reference Example X) ... (3) Here, X represents the number of the example, comparative example, or reference example. <Judgment criteria> (Judgment): (Evaluation) ◎: Improvement rate of 45% or more ○: Improvement rate of 30% or more but less than 45% △: Improvement rate of 15% or more but less than 30% ×: Improvement rate less than 15%

[0058] [Table 1] [Table 2] *1:Bio-Sodium Hyaluronate 1% Solution (N Type) (manufactured by BIOLAND) *2: TORNARE (manufactured by Hayashibara Co., Ltd.) *3: Lipidure-HM-600 (manufactured by NOF Corporation) *4: PEMULEN TR-1 (manufactured by Lubrizol) [Table 3]

[0059] (Manufacturing method) A: Ingredients 1-12 were uniformly dissolved and mixed at 60°C, and then cooled to room temperature to obtain a lotion.

[0060] As is clear from the results in Tables 2 and 3, the lotions of Examples 1 to 16 were excellent in all aspects of inhibiting crystal precipitation. On the other hand, Comparative Example 1, which did not contain component (C), sometimes did not exhibit excellent crystal precipitation inhibiting effects. Comparative Example 2, which did not contain component (C) or component (D), sometimes did not exhibit excellent crystal precipitation inhibiting effects. Comparative Example 3, which did not contain component (C), sometimes did not exhibit excellent crystal precipitation inhibiting effects. Comparative Example 4, which did not contain component (D), sometimes did not exhibit excellent crystal precipitation inhibiting effects. Comparative Example 5, which did not contain component (C) or component (D), sometimes did not exhibit excellent crystal precipitation inhibiting effects. Comparative Example 6, which did not contain component (D), sometimes did not exhibit excellent crystal precipitation inhibiting effects.

[0061] Example 17: Oil-in-water emulsion (Ingredients) (%) 1,1,3-Butylene glycol 12.0 2. Tranexamic acid 4.0 3. Purified water remaining amount 4. Niacinamide 6.0 5. Polyethylene glycol monostearate (40 E.O.) 0.5 6. Sorbitan sesquioleate 0.1 7. Hydrogenated lecithin 0.1 8. Cholesteryl hydroxystearate (Note 1) 3.0 9. Vaseline 2.0 10. α-olefin oligomer 5.0 11. Shea butter 2.0 12. Dimethylpolysiloxane (10CS) 1.0 13. Ceramide 3 0.1 14. Astaxanthin 0.1 15. Tocopherol 0.01 16. Cetostearyl alcohol 2.0 17. Behenyl alcohol 1.0 18. Methyl parahydroxybenzoate 0.1 19. Acrylic acid / alkyl methacrylate copolymer (Note 2) 0.1 20. Xanthan gum 0.1 21. Sodium hydroxide 0.03 22.Fragrance 0.2 23. Sodium hyaluronate 0.0005 24. Polymethachloroyloxyethyl phosphorylcholine solution 0.0025 Note 1) Saracos HS (manufactured by Nisshin Oillio Co., Ltd.) Note 2) CARCOPOAL ULTREZ21 (manufactured by LUBRIZOL)

[0062] (Manufacturing method) A: Dissolve and mix components 1-4 uniformly at 70°C. B: Dissolve and mix components 5-17 uniformly at 80°C. Add B to C:A and emulsify at 70°C. After adding components 18-24 to D:C and mixing, the mixture was cooled to 40°C to obtain an oil-in-water emulsion.

[0063] The oil-in-water emulsion of Example 17 exhibited excellent crystal precipitation suppression effects.

[0064] Example 18: Oil-in-water emulsion beauty serum (Ingredients) (%) 1,1,3-Butylene glycol 5.0 2. Tranexamic acid 5.0 3. Tripropylene glycol 3.0 4. Purified water remaining amount 5. Niacinamide 1.0 6. Polyoxyethylene sorbitan monooleate (20 E.O.) 0.1 7. Polyethylene glycol monostearate (55 E.O.) 0.25 8. Macadamia nut oil fatty acid phytosteryl (Note 3) 2.0 9. Light liquid isoparaffin (Note 4) 3.0 10. Dimethylpolysiloxane (6CS) 3.0 11. Cholesterol 0.1 12. Tocopherol 0.01 13. Cetostearyl alcohol 0.5 14. Methyl parahydroxybenzoate 0.1 15. Carbomer (Note 5) 0.15 16. (Sodium Acrylate / Sodium Acryloyldimethyl Taurate) Copolymer (Note 6) 0.1 17. Sodium hydroxide 0.05 18. Ethanol 5.0 19. Collagen 0.1 20. Elastin 0.1 21. Hyaluronic acid 0.1 22.Fragrance 0.05 23. Sodium hyaluronate 0.0001 24. Polymethachloroyloxyethyl phosphorylcholine solution 0.0005 Note 3) PLANDOOL-MAS (manufactured by Nippon Seika Co., Ltd.) Note 4) Chloratum LES (manufactured by Croda) Note 5) CARCOPOAL 980 (manufactured by LUBRIZOL) Note 6) SIMULGEL EG (manufactured by SEPIC)

[0065] (Manufacturing method) A: Dissolve and mix components 1-5 uniformly at 70°C. B: Dissolve and mix components 6-12 uniformly at 80°C. Add B to C:A and emulsify at 70°C. After adding ingredients 13-24 to D:C and mixing, the mixture was cooled to 40°C to obtain an oil-in-water emulsion beauty serum.

[0066] The oil-in-water emulsion serum of Example 18 exhibited excellent crystal precipitation suppression effects.

[0067] Example 19: Liquid hair serum (Ingredients) (%) 1. Oleic acid 0.15 2. Ethyl oleate 0.2 3. Tocopherol acetate 0.02 4. Menthol 0.5 5. Methyl parahydroxybenzoate 0.1 6. Vinyl acetate / vinylpyrrolidone copolymer (Note 7) 0.1 7.Fragrance 0.2 8. Polyoxyethylene (20 mol) hydrogenated castor oil 0.3 9. Ethanol 50.0 10. Alkyl-modified carboxyvinyl polymer 0.1 11. Carboxyvinyl polymer 0.1 12,2-amino-2-methylpropanol 0.05 13. Niacinamide 4.0 14. Tranexamic acid 4.0 15. Purified water remaining amount 16. Sodium hyaluronate 0.0005 17. Polymethachloroyloxyethyl phosphorylcholine solution 0.0025 (Note 7) Acorn KS (manufactured by Osaka Organic Chemical Industry Co., Ltd.)

[0068] (Manufacturing method) A: Mix ingredients 1-9 together. B: Mix ingredients 10-17. A was added to CB and mixed to obtain a liquid hair serum.

[0069] The liquid hair serum obtained in Example 19 exhibited excellent crystal precipitation inhibition effects.

[0070] Example 20: Sheet-type cosmetic pack (Ingredients) (%) 1. Isostearic acid 0.05 2. Polyoxyethylene (60 mol) hydrogenated castor oil 0.3 3. 2-Ethylhexyl Methoxycinnamate 0.05 4. Glycerin 3.0 5.1,3-Butylene glycol 5.0 6. Ethanol 8.0 7. Sodium citrate 0.02 8. Citric acid 0.05 9. Dipotassium glycyrrhizinate 0.1 10. Phenoxyethanol 0.05 11. Niacinamide 4.0 12. Tranexamic acid 2.0 13. 40% aqueous solution of pentasodium diethylenetriaminepentaacetate 0.15 14. Purified water remaining amount 15. Sodium hyaluronate 0.01 16. Polymethachloroyloxyethyl phosphorylcholine solution 0.05

[0071] (Manufacturing method) A: Mix and dissolve ingredients 1-6. Mix and dissolve ingredients B:7-16. Add C:A to B and mix. D:C was impregnated into a nonwoven fabric to obtain a sheet-like cosmetic pack.

[0072] The sheet-type cosmetic pack of Example 20 exhibited excellent crystal precipitation suppression effects.

[0073] Example 21: Ointment (Ingredients) (%) 1. Triethanolamine 2.0 2. Glycerin 8.0 3. Purified water remaining amount 4. Niacinamide 3.0 5. Tranexamic acid 4.0 6. Sodium hyaluronate 0.003 7. Polyquaternium-64 0.004 8. Cetanol 4.0 9. Vaseline 30.0 10. Tocopherol 0.01 11. Stearic acid 18.0 12. Sorbitan sesquioleate 1.5

[0074] (Manufacturing method) A. Dissolve components (8) to (12) uniformly at 75°C. B. Dissolve components (1) to (7) uniformly at 75°C. B was gradually added to CA, emulsified at 75°C, and cooled to room temperature to obtain an ointment.

[0075] The ointment of Example 21 showed excellent crystal precipitation inhibition effects.

[0076] Example 22: Foundation (Ingredients) (%) 1. PEG-9 Polydimethylsiloxyethyl Dimethicone 1.2 2. Lauryl PEG-9 Polydimethylsiloxyethyl Dimethicone 0.5 3. Isododecane 25.0 4. (PEG-15 / Lauryl Dimethicone) Crosspolymer 0.1 5. Isotridecyl isononanoate 6.0 6. Trifluoroalkyldimethylsiloxysilicate 2.0 7. Dimelpolysiloxane (kinematic viscosity at 25°C: 20 CS) 0.5 8. Ethylhexyl Methoxycinnamate 5.0 9. Dextrin palmitate 0.1 10. Triethoxycaprylylsilane 3% treated titanium dioxide (Average particle size 30nm) 6.0 11. Titanium dioxide treated with 3% isopropyl titanium triisostearate. (Average particle size 250nm) 7.0 12. Disodium Stearoyl Glutamate 2% Red Iron Ore 0.6 13. Dimethylpolysiloxane 2% treated yellow iron oxide 1.2 14. 2% dextrin palmitate treated black iron oxide 0.4 15. Distearyldimonium hectorite 1.0 16. Stearalkonium hectorite 1.0 17. Silica (spherical, non-porous, average particle size 10 μm) 0.5 18. Purified water remaining amount 19. PEG-240 / Decyltetradeceth-20 Hexamethylene diisocyanate copolymer 0.05 20. Ethanol 8.0 21.1,3-Butylene glycol 0.1 22. Sodium monohydrogen phosphate 0.01 23. Sodium dihydrogen phosphate 0.01 24. Sorbitol 0.2 25. Maltitol 0.4 26. Sodium Chloride 0.3 27. Niacinamide 2.0 28. Tranexamic acid 6.0 29. Sodium hyaluronate 0.05 30. Tremella fuciformis polysaccharide 3.0

[0077] (Manufacturing method) A. Mix ingredients (1) to (9) uniformly at 80°C. Add ingredients (10) to (17) to BA and mix uniformly at room temperature. C. Mix components (18) to (30) uniformly at 60°C. Gradually add C to DB and emulsify at room temperature. The ED was filled into a dispenser container to obtain the foundation.

[0078] The foundation in Example 22 exhibited excellent crystal precipitation suppression effects.

[0079] Example 23: Sunscreen (water-in-oil emulsion) (Ingredients) (%) 1. Stearic acid / aluminum hydroxide treated titanium dioxide microparticles 5.0 2. Hydrogen dimethicone treated zinc oxide microparticles 15.0 3. Polyhydroxystearic acid 2.0 4. Isononyl isononanoate 10.0 5. Isopropyl palmitate 8.0 6. PEG-30 Dipolyhydroxystearate 1.0 7. PEG-9 Dimethicone 2.0 8. Cyclopentasiloxane 10.0 9. Purified water remaining amount 10. Niacinamide 4.5 11. Tranexamic acid 3.0 12.1,3-Butylene glycol 3.0 13. Glycerin 4.0 14. Sodium hyaluronate 0.01 15. Polymethachloroyloxyethyl phosphorylcholine solution 0.05

[0080] (Manufacturing method) A: Mix components (1) to (4) and disperse them in a roll mill at 25°C. B: Mix components (5) to (8), add A, and mix and disperse at 25°C. C: Components (9) to (15) were uniformly mixed and added to B, and emulsified at 25°C to obtain a sunscreen (water-in-oil emulsion).

[0081] The sunscreen (water-in-oil emulsion) of Example 23 exhibited excellent crystal precipitation suppression effects. [Industrial applicability]

[0082] This invention can be applied to cosmetics, quasi-drugs, topical skin preparations, and the like.

Claims

1. The following components (A) to (F): (A) Niacinamide 1-10% by mass (B) Tranexamic acid 1-7% by mass (C) Mucopolysaccharide (D) Amphiphilic polymers (E) Phosphate (F) Sugar alcohol It contains, The total amount of components (A) and (B) relative to component (C) is [(A) + (B)] / (C), and the mass ratio of these components is between 160 and 10,000,000. The total mass ratio of components (A) and (B) to component (D) [(A) + (B)] / (D) is between 4 and 110. Component (D) amphiphilic polymer is one or more selected from the group consisting of polymethacroyloxyethyl phosphorylcholine solution, polyquaternium-51, polyquaternium-61, polyquaternium-64, polyquaternium-65, (acrylic acid / alkyl acrylate (C10-30)) copolymer, (alkyl acrylate / steareth-20 methacrylate) copolymer, (acrylates / beheneth-25 methacrylate) copolymer, and PEG-240 / decyltetradeceth-20 / hexamethylene diisocyanate copolymer, (PPG-12 / methylenediphenyl diisocyanate) copolymer, (PEG-8 / methylenediphenyl diisocyanate) copolymer, and bismethoxyPEG-13 (PEG-502 / PPG-57 / methylenediphenyl diisocyanate) copolymer. A composition in which component (E) phosphate is one or more selected from the group consisting of monosodium hydrogen phosphate, dihydrogen dihydrogen phosphate, and potassium dihydrogen phosphate.

2. The composition according to claim 1, wherein the component (C) is one or more selected from the group consisting of hyaluronic acid, its salts, benzyl esterified hyaluronic acid, and acetylated hyaluronic acid.

3. The composition according to claim 1 or 2, wherein the composition is a crystal precipitation inhibitor.

4. The composition according to any one of claims 1 to 3, wherein the composition is a cosmetic or a topical skin preparation.

5. A method for inhibiting crystal precipitation, characterized by blending a composition containing components (A) niacinamide and (B) tranexamic acid with (C) mucopolysaccharide, (D) amphiphilic polymer, (E) phosphate, and (F) sugar alcohol, wherein component (D) amphiphilic polymer is polymethacycloyloxyethyl phosphorylcholine solution, polyquaternium-51, polyquaternium-61, polyquaternium-64, polyquaternium-65, (acrylic acid / alkyl acrylate (C10-30)) copolymer, (alkyl acrylate / methacrylic acid A method for suppressing crystal precipitation, comprising one or more selected from the group consisting of (Steareth-20 acid copolymer), (Acrylates / Beheneth-25 methacrylate) copolymer, and PEG-240 / Decyltetradeceth-20 / Hexamethylene diisocyanate copolymer, (PPG-12 / Methylenediphenyl diisocyanate) copolymer, (PEG-8 / Methylenediphenyl diisocyanate) copolymer, and bismethoxyPEG-13 (PEG-502 / PPG-57 / Methylenediphenyl diisocyanate) copolymer.

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