JP2021161111A - Composition - Google Patents

Abstract

[Problem] To suppress crystal precipitation in a composition containing niacinamide and tranexamic acid [Solution] A composition containing the following components (A) to (C): (A) 1 to 10% by mass of niacinamide, (B) 1 to 7% by mass of tranexamic acid, (C) mucopolysaccharide, and (D) amphiphilic polymer. [Selected Figure] None

Description

The present invention relates to compositions.

Maintaining healthy and beautiful skin is a matter of great concern to many. The skin causes various problems such as rough skin, wrinkles, sagging, and pigmentation due to various factors such as ultraviolet rays, dryness, aging, and stress. In order to improve these skin problems from various aspects, it is considered effective to act on the skin with a plurality of components having different actions.

For example, niacinamide is a kind of vitamin, but has effects on the skin such as wrinkle improving effect, skin barrier ability improving, whitening effect, and skin texture improving effect (see, for example, Non-Patent Document 1). .. Since tranexamic acid has an anti-inflammatory effect, it is known to be used as an active ingredient of a pharmaceutical product and to have an effect of suppressing melanin production (see, for example, Patent Document 1). A composition containing these two components having different actions is expected to bring about a multifaceted effect on a plurality of skin problems.

On the other hand, it is known that crystals of a composition containing niacinamide or tranexamic acid alone are precipitated with time. Regarding tranexamic acid, it contains 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, and the pH is adjusted to 3 to 6. It is known that the external preparation for the skin prevents the precipitation of crystals of tranexamic acid (see, for example, Patent Document 2).

Japanese Unexamined Patent Publication No. 2008-100933 Japanese Unexamined Patent Publication No. 2011-084551

Cosmeceuticals and Cosmetic practice Chap.10.2014 page 103-112

Conventionally, a composition containing a high concentration of niacinamide or tranexamic acid causes remarkable crystal precipitation, and when the composition is used, if the composition adheres to the discharge portion or lid portion of the container, the crystal precipitates. Had. However, the suppression of crystal precipitation of the composition containing the two components of niacinamide and tranexamic acid has not been studied so far. In the present invention, it has been found that in the composition containing niacinamide and tranexamic acid, the degree of crystal precipitation is worse than that in which each one occurs, and it is an object of the present invention to solve this.

As a result of diligent studies to solve this problem, the present inventors have found that the niacinamide and tranexamic acid-containing preparations contain a mucopolysaccharide and an amphoteric polymer to have an effect of suppressing crystal precipitation. rice field.

That is, the present invention describes the following components (A) to (D);
(A) Niacinamide 1-10% by mass
(B) Tranexamic acid 1-7% by mass
It relates to a composition containing (C) mucopolysaccharide (D) amphipathic polymer.

INDUSTRIAL APPLICABILITY According to the present invention, in a composition containing niacinamide and tranexamic acid, a composition that suppresses crystallization, a crystallization inhibitor, and a cosmetic or an external preparation for skin can be provided.

Hereinafter, the present invention will be described in detail. In addition, in this specification, "~" means the range including the numerical values before and after it.

Component (A): Niacinamide The 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 belonging to the B vitamin group, and can be extracted from a natural product (rice bran, etc.) or synthesized by a known method. Specifically, those listed in the 15th revised Japanese Pharmacopoeia 2008 can be used.

The content of the component (A) in the present invention is 1 to 10% by mass (hereinafter, simply abbreviated as "%"). In a composition in which the content of the component (A) niacinamide is 1 to 10% and the content of the component (B) tranexamic acid is 1 to 7%, the component (A) niacinamide and the component (B) tranexamic acid are contained respectively. It is more difficult to suppress crystal precipitation than the composition contained alone. In the present invention, the content of the component (A) is not particularly limited as long as it is 1 to 10%, but is preferably 3 to 8% and 4 to 7% from the viewpoint of the effect of suppressing crystal precipitation. Is more preferable.

Component (B): Tranexamic acid Tranexamic acid of the component (B) used in the present invention is a kind of amino acid represented by trans-4- (aminomethyl) cyclohexane-1-carboxylic acid. Tranexamic acid may be used as a whitening effect or anti-inflammatory effect on the skin, and may also be used as a hemostatic agent.

The content of the component (B) in the present invention is 1 to 7%. In a composition in which the content of the component (A) niacinamide is 1 to 10% and the content of the component (B) tranexamic acid is 1 to 7%, the component (A) niacinamide and the component (B) tranexamic acid are contained respectively. It is more difficult to suppress crystal precipitation than the composition contained alone. In the present invention, the content of the component (B) is not particularly limited as long as it is 1 to 7%, but is preferably 1.3 to 6%, preferably 1.5 to 5 from the viewpoint of the effect of suppressing crystal precipitation. More preferably.

Component (C): Mucopolysaccharide The mucopolysaccharide of the component (C) used in the present invention is a general term for polysaccharides containing amino sugars, and is not particularly limited, but is typically glycosamino. Glucan can be mentioned. Glycosaminoglucans are repeatedly composed of disaccharides, one of which is composed of either D-glucosamine or D-galactosamine. Examples of glycosaminoglucan include hyaluronic acid, chondroitin sulfate, chondroitin, ketalan sulfate, heparin, heparin sulfate, dermatan sulfate and the like. The mucopolysaccharide of the present invention may have a carbosyl group structure in addition to the sulfate ester. Further, the mucopolysaccharide of the present invention can be used without particular limitation as long as it is usually used in the fields of pharmaceuticals, quasi-drugs, cosmetics or foods and drinks, and it may be used alone or as a single type. Two or more types may be used in any combination.

The method and origin of the mucopolysaccharide of the present invention are not particularly limited, but for example, fish such as sharks and salmon, other aquatic animals such as whales and sea cucumbers, and land animals such as cows, pigs, chickens and horses. It can be obtained in a state containing a large amount of protein or the like by subjecting bone, cartilage, skin, scales and the like (hereinafter referred to as mucopolysaccharide-containing tissue) to alkali treatment, enzyme treatment and the like. Further, the protein or the like may be removed from the mucopolysaccharide containing the protein or the like, and treatment such as ultrafiltration may be performed in order to obtain a high-purity mucopolysaccharide. Mucopolysaccharide can also be obtained by synthesis, semi-synthesis, fermentation or the like.

The decomposition product of the present invention is a low-molecular-weight mucopolysaccharide, and examples of the decomposition method include decomposition by heating, chemical hydrolysis by acid or base, and hydrolysis by various enzymes. can.

The derivative of the present invention is a mucopolysaccharide in which various substituents are introduced, and a mucopolysaccharide in which a substituent is introduced into at least one or more carboxy group or a hydroxy group, or a salt is formed. preferable. For example, an ester of a mucopolysaccharide having an acetyl group or a benzyl group introduced as a substituent, or a cross-linked product having a formyl group introduced therein can be mentioned.

The salt of the present invention includes alkali metal salts such as sodium and potassium, alkaline earth metal salts such as magnesium and calcium, alkanolamine salts such as ammonium salt and monoethanolamine, and may be a mixture thereof. .. An alkali metal salt such as a sodium salt is preferable.

The hyaluronic acid of the present invention is a high molecular weight polysaccharide formed by alternately binding the 3-position of β-DN-acetylglucosamine and the 4-position of β-D-glucuronic acid. The production method and origin of hyaluronic acid are not particularly limited, but can be obtained by, for example, extraction from animal tissues such as combs or microbial fermentation methods.

The weight average molecular weight of the hyaluronic acid of the present invention is not particularly limited, and hyaluronic acid may be decomposed to reduce the molecular weight, but 5,000 to 300,000 is preferable, and 50,000 to 110,000 is particularly preferable. The weight average molecular weight of the hyaluronic acid used in the present invention is determined by using hyaluronic acid having a known weight average molecular weight as a standard product, subjecting the sample and the standard product to high performance liquid chromatography, and based on the weight average molecular weight and retention time of the standard product. It is also possible to obtain a standard curve and obtain a weight average molecular weight corresponding to the retention time of the sample solution. For the weight average molecular weight of the standard product, the ultimate viscosity was measured according to the 13th revised Japanese Pharmacopoeia: General Test Method, Paragraph 36 Viscosity Measurement Method, and the formula of Laurent et al. It can be calculated according to 1960). The hyaluronic acid of the present invention is not particularly limited and may be appropriately selected depending on the intended purpose. For example, hyaluronic acid FCH-201S (weight average molecular weight 1.8 million to 2.2 million), Examples thereof include 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 Chemifa), and BIO-SODIUM HYALULONATE (manufactured by BIOLAND).

The hyaluronic acid derivative of the present invention is obtained by introducing a substituent into at least one or more carboxy group or hydroxy group of hyaluronic acid or forming a salt. As the substituent, an ester such as an acetyl group or a benzyl group, or a group capable of forming a crosslink, for example, a formyl group or the like is preferable. For example, a substance in which one or more carboxyl groups in hyaluronic acid are esterified (for example, benzyl esterified hyaluronic acid (trade name Hyaff®, Fidia Advanced Biopolymers)), hyaluronic acid is crosslinked with formaldehyde, and further. Examples thereof include polymerized substances (for example, trade name Synvisc (registered trademark), Biomatrix), and acetylated hyaluronic acid in which one or more hydroxy groups in hyaluronic acid are acetylated. Of these, acetylated hyaluronic acid is particularly preferable.

The sodium chondroitin sulfate of the present invention is a sodium salt obtained by binding sulfuric acid to a sugar chain in which the disaccharides of β-DN-acetylgalactosamine and β-D-glucuronic acid are repeated. Examples of commercially available products include sodium chondroitin sulfate (manufactured by Maruha Nichiro Co., Ltd.).

In the present invention, the component (C) is preferably one or more selected from the group consisting of hyaluronic acid, a salt thereof, and a hyaluronic acid derivative.

In the present invention, the content of the component (C) is not particularly limited, but is preferably 0.000001 to 0.1%, preferably 0.00001 to 0.01%, from the viewpoint of the effect of suppressing crystal precipitation. Is more preferable.

In the present invention, although it can be obtained by appropriately containing the above components (A) to (D), it is preferable because the effect of suppressing crystal precipitation is more excellent by specifying the mass ratio of the components (A) to (D). Such a mass ratio is not particularly limited, and the content mass ratio (A) / (C) of the component (A) and the component (C) is preferably 10 or more, more preferably 300 or more, still more preferably 3500 or more. Further, 5,000,000 or less is preferable, 1,000,000 or less is more preferable, 100,000 or less is even more preferable, and 45,000 or less is particularly preferable.

In the present invention, although it can be obtained by appropriately containing the above components (A) to (D), it is preferable because the effect of suppressing crystal precipitation is more excellent by specifying the mass ratio of the components (A) to (D). Such a mass ratio is not particularly limited, and the lower limit of the content mass ratio (B) / (C) of the component (B) and the component (C) is preferably 10 or more, more preferably 50 or more, and 150 or more. More preferably, 1000 or more is particularly preferable. The upper limit is preferably 20000 or less, more preferably 1000000 or less, even more preferably 250,000 or less, and particularly preferably 2000 or less.

In the present invention, although it can be obtained by appropriately containing the above components (A) to (D), it is preferable because the effect of suppressing crystal precipitation is more excellent by specifying the mass ratio of the components (A) to (D). Such a mass ratio is not particularly limited, and the lower limit of the content mass ratio [(A) + (B)] / (C) between the total amount of the components (A) and (B) and the component (C) is 20. The above is preferable, 100 or more is more preferable, 500 or more is further preferable, and 5000 or more is particularly preferable. The upper limit is preferably 17,000,000 or less, more preferably 10000000 or less, even more preferably 14000000 or less, particularly preferably 120,000 or less, and most preferably 60,000 or less.

Component (D): Amphiphilic polymer The component (D) amphipathic polymer used in the present invention is a polymer having a hydrophobic group and a hydrophilic group. It is preferable that it has an affinity for both an aqueous medium and an oil-based medium, and in the present invention, a water-soluble or water-dispersible amphipathic polymer is more preferably mentioned. The component (D) is not particularly limited as long as it is used in various preparations such as cosmetics, quasi-drugs, and external skin preparations such as pharmaceuticals, and even if it is a synthetic product, it can be derived from a natural product. It may be an extracted and derived product, and the hydrophobic group and the hydrophilic group may be randomly distributed, or may be distributed in a block shape or a graft shape. The component (D) may be ionic or nonionic, but is preferably anionic or nonionic in consideration of application to the skin. Examples of the hydrophobic group include a cyclic, linear or branched hydrocarbon group having about 4 to 30 carbon atoms, a cholesteryl group or a cholesterol-derived group, a polyorganosiloxane group and the like. It may be substituted with fluorine or may contain heteroatoms such as oxygen, nitrogen or sulfur.

In the present invention, the component (D) is, for example, a hydrophobic group-modified acrylic acid derivative (including an alkali-soluble (or swellable) emulsion), a hydrophobically modified polyether urethane, a hydrophobically modified hydroxyethyl cellulose, a polyoxyalkylene alkyl ether, and the like. Examples thereof include a homopolymer of 2-methacryloyloxyethyl phosphorylcholine, a copolymer of 2-methacryloyloxyethyl phosphorylcholine and a hydrophobic monomer, and one or more of these can be selected and used.

As the hydrophobic group-modified acrylic acid derivative, specifically, a linear or branched alkyl group having 4 to 30 carbon atoms is preferable, and as a commercially available product, for example, acrylic acid / alkyl acrylate (C10-). 30) Copolymer "PEMULEN TR-1" (manufactured by NOVEON), (alkyl acrylate / steareth methacrylate-20) copolymer "Accurin 22" (manufactured by ROHM), (Acrylate / Behenes methacrylate-25) Examples of the copolymer include Novellix L-10 (manufactured by Lubrizol Advanced Materials) and ACULYN 28 (manufactured by Dow Chemical Group).

The hydrophobically modified polyether urethane has 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, R ^{2 to} R ⁵ represent hydrocarbon groups that may be the same or different from each other, h is a number of 1 or more, and k. And n and m are numbers in the range 0 to 1000 independently, but do not become 0 at the same time. R ² , R ⁴ and R ⁵ have 2 to 4 carbon atoms, and R ³ has 1 to 30 carbon atoms. R ¹ 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, and n and m are preferably 0 to 700 and 10 ~ 500 is more preferred).

Examples of commercially available products include "ADEKANOLT GT-700" (manufactured by ADEKA Corporation), which is a PEG-240 / decyltetradeceth-20 / hexamethylene diisocyanate copolymer. (PPG-12 / methylene diphenyl diisocyanate) copolymer "EXPERT GEL EG 412" (manufactured by POLYMEREXPERT Co., Ltd.), (PEG-8 / methylene diphenyl diisocyanate) copolymer "POLYOL PREPOLYMER-15" (Manufactured by Co., Ltd.), “EXPERT GEL EG230” (manufactured by POLYMEREXPERT Co., Ltd.), which is a bismethoxyPEG-13 (PEG-502 / PPG-57 / methylene diphenyl diisocyanate) copolymer.

The homopolymer of 2-methacryloyloxyethyl phosphorylcholine (sometimes referred to as MPC) and 2-methacryloyloxyethyl phosphorylcholine constituting the copolymer of MPC and the hydrophobic monomer are represented by the following general formula (2).

The homopolymer of MPC preferably has a weight average molecular weight of 5,000 or more, and more preferably 10,000 or more, from the viewpoint of the effect of suppressing crystal precipitation. The type of the hydrophobic monomer is not particularly limited as the copolymer of the MPC and the hydrophobic monomer, but it is preferably styrene, acrylic acid ester, or methacrylic acid ester. The weight average molecular weight of the copolymer with the hydrophobic monomer is also preferably 5000 or more, and more preferably 10000 or more. The composition molar ratio of MPC to the hydrophobic monomer is preferably in the range of 50:50 to 97: 3.

The weight average molecular weight of the homopolymer of MPC and the copolymer of MPC and the hydrophobic monomer was obtained by dissolving 5 mg of each obtained polymer in a mixed solution of methanol / chloroform (mass ratio: 80/20) to prepare a sample solution. It is measured 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)
Calculation method of weight average molecular weight: Molecular weight calculation program (GPC program for SC-8020)
Flow rate: 1 mL per minute
Injection volume: 100 μL
Column oven: Constant temperature around 40 ° C

The component (D) is not particularly limited, but to be specifically exemplified, LIPIDURE-HM and LIPIDURE-, which contain, for example, phosphorylcholine glycol polyacrylate (polymethacryloyloxyethyl phosphorylcholine) as a homopolymer of MPC. HM-500, LIPIDURE-HM-600 (above, manufactured by NOF CORPORATION), LIPIDURE-PMB, LIPIDURE B (above, manufactured by NOF Corporation) containing polyquaternium-51 as a copolymer of MPC and butyl methacrylate. ), MPC, LIPIDURE A (manufactured by NOF CORPORATION) containing polyquaternium-65 as a polymer with MPC, butyl methacrylate and sodium methacrylate, and polyquaternium-61 as a polymer with MPC and stearyl methacrylate. Commercial products such as LIPIDURE NA, LIPIDURE-NR (above, manufactured by NOF Corporation), and polymer-64 containing LIPIDURE C (manufactured by NOF Corporation), which are contained, can be mentioned, and one or two kinds selected from these can be mentioned. The above can be used.

The component (D) is not particularly limited, but from the viewpoint of the effect of suppressing crystal precipitation, an acrylic acid / alkyl acrylate (C10-30) copolymer, a homopolymer of 2-methacryloyloxyethyl phosphorylcholine, and 2-methacryloyloxyethylphosphorylcholine. It is preferably one or more selected from the group consisting of a copolymer of and a hydrophobic monomer, and preferably selected from the group consisting of an acrylic acid / alkyl acrylate (C10-30) copolymer and phosphorylcholine glycol polyacrylate. More preferably, it is one kind or two or more kinds.

The content of the component (D) used in the present invention is not particularly limited, but is preferably 0.00005 to 0.5%, preferably 0.0005 to 0.05%, from the viewpoint of the effect of suppressing crystal precipitation. More preferred.

In the present invention, although it can be obtained by appropriately containing the above components (A) to (D), it is preferable because the effect of suppressing crystal precipitation is more excellent by specifying the mass ratio of the components (A) to (D). Such a mass ratio is not particularly limited, and the lower limit of the content mass ratio (A) / (D) of the component (A) and the component (D) is preferably 5 or more, more preferably 10 or more, and 40 or more. More preferred. 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.

In the present invention, although it can be obtained by appropriately containing the above components (A) to (D), it is preferable because the effect of suppressing crystal precipitation is more excellent by specifying the mass ratio of the components (A) to (D). Such a mass ratio is not particularly limited, and the lower limit of the content mass ratio (B) / (D) of the component (B) and the component (D) is preferably 2 or more, more preferably 5 or more, and 10 or more. More preferred. 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.

In the present invention, although it can be obtained by appropriately containing the above components (A) to (D), it is preferable because the effect of suppressing crystal precipitation is more excellent by specifying the mass ratio of the components (A) to (D). Such a mass ratio is not particularly limited, and the lower limit of the content mass ratio [(A) + (B)] / (D) between the total amount of the components (A) and (B) and the component (D) is 4. The above is preferable, 10 or more is more preferable, 20 or more is even more preferable, and 100 or more is preferable. The upper limit is preferably 340000 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.

The present invention can further contain the component (E) phosphate. The salt is not particularly limited, such as an organic salt or an inorganic salt, but is preferably an inorganic salt, and a sodium salt is particularly preferable, from the viewpoint of adjusting the pH of the composition and exerting an effect as a buffer. By containing the phosphate in the composition of the present application, it is expected that it will be stably present in the composition containing both the components (A) and (B). The component (E) phosphate in the present invention may be used alone or in combination of two or more, and for example, sodium monohydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate and the like are preferably used. Among these, one or more selected from the group consisting of sodium monohydrogen phosphate and sodium dihydrogen phosphate is preferable, and sodium monohydrogen phosphate and sodium dihydrogen phosphate are more preferable. ..

The content of the component (E) in the present invention is not particularly limited, but is preferably 0.01% or more, more preferably 0.05% or more, and even more preferably 0.1% or more in the composition. Further, 1% or less is preferable, 0.5% or less is more preferable, and 0.3% or less is even more preferable. This range is more preferable because it is more excellent in the effect of suppressing crystal precipitation.

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

In the present invention, the content of the component (F) is not particularly limited, but is preferably 0.1% or more, more preferably 0.2% or more, and even more preferably 0.3% or more in the composition. Further, 5% or less is preferable, 3% or less is more preferable, and 2% or less is even more preferable. This range is more preferable because it is more excellent in the effect of suppressing crystal precipitation.

In addition, the composition containing the components (A) to (F) of the present invention is usually applied to the skin of cosmetics, quasi-drugs, pharmaceuticals, etc., as long as it does not impair the effects of the present technology. Ingredients used in various formulations such as agents can be added. Examples of the components include water, oil agents, surfactants, metal chelate, gelling agents, powders, alcohols, water-soluble polymers, film-forming agents, resins, ultraviolet protective agents, inclusion compounds, antibacterial agents, and fragrances. , Deodorant, pH adjuster, refreshing agent, animal / microorganism-derived extract, plant extract, blood circulation promoter, astringent, anti-seborrheic agent, whitening agent, anti-inflammatory agent, active oxygen scavenger, cell activator , Moisturizers, chelating agents, keratolytic agents, enzymes, hormones, vitamins and the like. From these, one kind or two or more kinds can be appropriately selected and used.

The present invention is not particularly limited as long as it can contain water and is used in various preparations such as cosmetics, quasi-drugs, and external skin preparations such as pharmaceuticals. The water may be purified water, hot spring water, deep water, steam distilled water of a plant, or the like, and one or more of them can be appropriately selected and used as needed. The water content is not particularly limited, but is preferably 10 to 97%, more preferably 20 to 95%.

The composition containing the components (A) to (F) of the present invention can be obtained by a known production method. The production method is not particularly limited, but for example, the component (A), the component (B), and the component (E) are dissolved in water, and the component (C), the component (D), and the component (F) are added and mixed. Can be obtained.

The composition of the present invention is not particularly limited, but is preferably a cosmetic or an external preparation for skin. Specifically, as cosmetics and skin external preparations, for example, basic cosmetics such as milky lotion, cream, lotion, beauty essence, pack, all-in-one gel, sunscreen, cleaning agent, makeup base, BB cream, foundation, cheek red , Makeup cosmetics such as lipstick, hair nourishing agents, hair tonics, shampoos, hair cosmetics such as rinses, dispersions, ointments, liquids, aerosols, patches, poultices, liniments, etc. May be good. It is preferably a cosmetic or external skin preparation used on the skin, which is expected to have a whitening effect, an emollient effect, and the like.

The composition containing the components (A) to (F) of the present invention is not particularly limited, but is preferably a crystal precipitation inhibitor. As the crystal precipitation inhibitor, it can also be used for cosmetics; quasi-drugs, external skin preparations for pharmaceuticals, etc .; oral preparations, injections, etc., and in particular, cosmetics and skin, which are applied to the skin. It is suitable to be used as an external preparation.

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

Examples 1 to 16 and Comparative Examples 1 to 6: Toners Toners having the formulations shown in Tables 1 to 3 below were prepared. In each sample (Examples 1 to 16 and Comparative Examples 1 to 6), the crystal precipitation suppressing effect was evaluated by the following evaluation method. The results are also shown in Tables 2 and 3.

(Evaluation item)
stomach. Crystal precipitation suppressing effect

<Evaluation method>
Regarding the evaluation of the crystal precipitation suppressing effect, 3 g of each sample (Examples 1 to 16, Comparative Examples 1 to 6, Reference Examples 1 to 16) was applied to a dish (material: polystyrene, manufactured by Corning Co., Ltd.) having a diameter of 3 cm, and at room temperature. The height of the precipitated crystals in each sample (Examples 1 to 16, Comparative Examples 1 to 6, and Reference Examples 1 to 16) after being air-dried for 3 days was measured, and the following formula (3) was used to measure Example X. Alternatively, the improvement rate of Comparative Example X was calculated, and the determination was made according to the following criteria.

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)] / (Reference Height of precipitated crystal in Example X) ... (3)
Here, X represents a number of an example, a comparative example, or a reference example.
<Criteria>
(Judgment): (Evaluation)
◎: Improvement rate is 45% or more ○: Improvement rate is 30% or more and less than 45% △: Improvement rate is 15% or more and less than 30% ×: Improvement rate is less than 15%

※１：Ｂｉｏ−Ｓｏｄｉｕｍ Ｈｙａｌｕｒｏｎａｔｅ １％ Ｓｏｌｕｔｉｏｎ（Ｎ Ｔｙｐｅ）（ＢＩＯＬＡＮＤ社製）
※２：ＴＯＲＮＡＲＥ（林原社製）
※３：Ｌｉｐｉｄｕｒｅ−ＨＭ−６００（日油社製）
※４：ＰＥＭＵＬＥＮ ＴＲ−１（Ｌｕｂｒｉｚｏｌ社製）

* 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)

(Production method)
A: Ingredients 1 to 12 were uniformly dissolved and mixed at 60 ° C. and cooled to room temperature to obtain a lotion.

As is clear from the results in Tables 2 and 3, the lotions of Examples 1 to 16 were excellent in all of the crystal precipitation suppressing effects. On the other hand, Comparative Example 1 containing no component (C) may not have an excellent effect of suppressing crystal precipitation. Comparative Example 2 containing no component (C) or component (D) may not have an excellent effect of suppressing crystal precipitation. Comparative Example 3 which does not contain the component (C) may not be excellent in the crystal precipitation suppressing effect. Comparative Example 4 containing no component (D) may not have an excellent effect of suppressing crystal precipitation. Comparative Example 5 containing no component (C) or component (D) may not have an excellent effect of suppressing crystal precipitation. Comparative Example 6 containing no component (D) may not have an excellent effect of suppressing crystal precipitation.

Example 17: Oil-in-water emulsified emulsion (ingredient) (%)
1.1,3-butylene glycol 12.0
2. Tranexamic acid 4.0
3. 3. Remaining amount of purified water 4. Niacinamide 6.0
5. Polyethylene glycol monostearate (40EO) 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. Setostearyl alcohol 2.0
17. Behenyl alcohol 1.0
18. Methyl paraoxybenzoate 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. Polymethacloyloxyethyl phosphorylcholine solution 0.0025
Note 1) Sarakos HS (manufactured by Nisshin Oillio)
Note 2) CARCOPOAL ULTREZ21 (manufactured by LUBRIZOL)

(Production method)
A: Ingredients 1 to 4 are uniformly dissolved and mixed at 70 ° C.
B: Ingredients 5 to 17 are uniformly dissolved and mixed at 80 ° C.
C: B is added to A and emulsified at 70 ° C.
After adding and mixing components 18 to 24 to D: C, the mixture was cooled to 40 ° C. to obtain an oil-in-water emulsified emulsion.

The oil-in-water emulsified emulsion of Example 17 was excellent in the effect of suppressing crystal precipitation.

Example 18: Oil-in-water emulsified beauty essence (ingredient) (%)
1.1,3-butylene glycol 5.0
2. Tranexamic acid 5.0
3. 3. Tripropylene glycol 3.0
4. Remaining amount of purified water 5. Niacinamide 1.0
6. Polyoxyethylene sorbitan monooleate (20EO) 0.1
7. Polyethylene Glycol Monostearate (55EO) 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. Setostearyl alcohol 0.5
14. Methyl paraoxybenzoate 0.1
15. Carbomer (Note 5) 0.15
16. (Na acrylate / Na acryloyl dimethyl taurine) 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. Polymethacloyloxyethyl phosphorylcholine solution 0.0005

Note 3) PLANDOOL-MAS (manufactured by Nippon Fine Chemical Co., Ltd.)
Note 4) Chloratum LES (manufactured by Croda)
Note 5) CARCOPOAL 980 (manufactured by LUBRIZOL)
Note 6) SIMULGEL EG (manufactured by SEPIC)

(Production method)
A: Ingredients 1 to 5 are uniformly dissolved and mixed at 70 ° C.
B: Ingredients 6 to 12 are uniformly dissolved and mixed at 80 ° C.
C: B is added to A and emulsified at 70 ° C.
After adding and mixing components 13 to 24 to D: C, the mixture was cooled to 40 ° C. to obtain an oil-in-water emulsified beauty essence.

The oil-in-water emulsified beauty essence of Example 18 was excellent in the effect of suppressing crystal precipitation.

Example 19: Beauty essence for liquid hair (ingredient) (%)
1. 1. Oleic acid 0.15
2. Ethyl oleate 0.2
3. 3. Tocopherol acetate 0.02
4. Menthol 0.5
5. Methyl paraoxybenzoate 0.1
6. Vinyl acetate / vinylpyrrolidone copolymer (Note 7) 0.1
7. Fragrance 0.2
8. Polyoxyethylene (20 mol) hardened 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. Remaining amount of purified water 16. Sodium hyaluronate 0.0005
17. Polymethacloyloxyethyl phosphorylcholine solution 0.0025
(Note 7) Acorn KS (manufactured by Osaka Organic Chemical Industry Co., Ltd.)

(Production method)
A: Ingredients 1 to 9 are mixed.
B: Ingredients 10 to 17 are mixed.
C. A was added to B and mixed to obtain a liquid hair essence.

The liquid hair essence obtained in Example 19 was excellent in the effect of suppressing crystal precipitation.

Example 20: Sheet pack cosmetics (ingredients) (%)
1. 1. Isostearic acid 0.05
2. Polyoxyethylene (60 mol) hardened castor oil 0.3
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. Diethylenetriamine pentaacetic acid pentasodium 40% aqueous solution 0.15
14. Remaining amount of purified water 15. Sodium hyaluronate 0.01
16. Polymethacloyloxyethyl phosphorylcholine solution 0.05

(Production method)
A: 1 to 6 are mixed and dissolved.
B: 7 to 16 are mixed and dissolved.
C: Add A to B and mix.
D: C was impregnated into the non-woven fabric to obtain a sheet-shaped pack cosmetic.

The sheet-shaped pack cosmetic of Example 20 was excellent in the effect of suppressing crystal precipitation.

Example 21: Ointment (ingredient) (%)
1. 1. Triethanolamine 2.0
2. Glycerin 8.0
3. 3. Remaining amount of purified water 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. Sorbitane sesquioleate 1.5

(Production method)
A. Ingredients (8) to (12) are uniformly dissolved at 75 ° C.
B. Ingredients (1) to (7) are uniformly dissolved at 75 ° C.
C. B was gradually added to A, emulsified at 75 ° C., and cooled to room temperature to obtain an ointment.

The ointment of Example 21 was excellent in the effect of suppressing crystal precipitation.

Example 22: Foundation (ingredient) (%)
1. 1. PEG-9 Polydimethylsiloxyethyl Dimethicone 1.2
2. Lauryl PEG-9 Polydimethylsiloxyethyl Dimethicone 0.5
3. 3. Isododecane 25.0
4. (PEG-15 / Lauryl Dimethicone) Cross Polymer 0.1
5. Isotridecyl isononanoate 6.0
6. Trifluoroalkyldimethylsiloxysilicic acid 2.0
7. Dimelpolysiloxane (25 ° C kinematic viscosity 20CS) 0.5
8. Ethylhexyl methoxycinnamate 5.0
9. Dextrin palmitate 0.1
10. Triethoxycaprylylsilane 3% treated titanium oxide
(Average particle size 30 nm) 6.0
11. Isopropyl Titanium Triisostearate 3% Treated Titanium Oxide
(Average particle size 250 nm) 7.0
12. Stearoyl Glutamic Acid 2Na 2% Bengala 0.6
13. Dimethylpolysiloxane 2% treated yellow iron oxide 1.2
14. Dextrin palmitate 2% treated black iron oxide 0.4
15. Distearyl Dimonium Hectorite 1.0
16. Stairalconium Hectorite 1.0
17. Silica (spherical non-porous, average particle size 10 μm) 0.5
18. Remaining amount of purified water 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. Na chloride 0.3
27. Niacinamide 2.0
28. Tranexamic acid 6.0
29. Sodium hyaluronate 0.05
30. White fungus polysaccharide 3.0

(Production method)
A. Ingredients (1) to (9) are uniformly mixed at 80 ° C.
B. Ingredients (10) to (17) are added to A and mixed uniformly at room temperature.
C. Ingredients (18) to (30) are uniformly mixed at 60 ° C.
D. Gradually add C to B and emulsify at room temperature.
E. D was filled in a dispenser container to obtain a foundation.

The foundation of Example 22 was excellent in the effect of suppressing crystal precipitation.

Example 23: Sunscreen (water-in-oil emulsification)
(Ingredient) (%)
1. 1. Stearic acid / AL hydroxide treated fine particles Titanium oxide 5.0
2. Hydrogen Dimethicone Treated Fine Particle Zinc Oxide 15.0
3. 3. Polyhydroxystearic acid 2.0
4. Isononyl isononanoate 10.0
5. Isopropyl palmitate 8.0
6. Dipolyhydroxystearate PEG-30 1.0
7. PEG-9 Dimethicone 2.0
8. Cyclopentasiloxane 10.0
9. Remaining amount of purified water 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. Polymethacloyloxyethyl phosphorylcholine solution 0.05

(Production method)
A: Ingredients (1) to (4) are mixed and dispersed in a roll mill at 25 ° C.
B: Ingredients (5) to (8) are mixed, A is added, and the mixture is mixed and dispersed at 25 ° C.
C: Ingredients (9) to (15) were uniformly mixed, added to B, and emulsified at 25 ° C. to obtain a sunscreen (water-in-oil emulsification).

The sunscreen agent (water-in-oil emulsification) of Example 23 was excellent in the effect of suppressing crystal precipitation.

The present invention can be applied to cosmetics, quasi-drugs, external skin preparations, and the like.

Claims (9)

The following components (A) to (D);
(A) Niacinamide 1-10% by mass
(B) Tranexamic acid 1-7% by mass
A composition containing (C) mucopolysaccharide (D) amphipathic polymer. The composition according to claim 1, wherein the component (C) is one or more selected from the group consisting of hyaluronic acid, a salt thereof, and a hyaluronic acid derivative. The group in which the component (D) is composed of an acrylic acid / alkyl acrylate (C10-30) copolymer, a homopolymer of 2-methacryloyloxyethyl phosphorylcholine, and a copolymer of 2-methacryloyloxyethyl phosphorylcholine and a hydrophobic monomer. The composition according to claim 1 or 2, which is one or more selected from. Any one of claims 1 to 3, wherein the content mass ratio [(A) + (B)] / (C) of the total amount of the components (A) and (B) to the component (C) is 20 to 17000000. The composition according to the section. Any one of claims 1 to 4, wherein the content mass ratio [(A) + (B)] / (D) of the total amount of the components (A) and (B) to the component (D) is 4 to 340000. The composition according to the section. The composition according to any one of claims 1 to 5, further comprising the component (E) phosphate. The composition according to any one of claims 1 to 6, further comprising the component (F) sugar alcohol. The composition according to any one of claims 1 to 7, wherein the composition is a crystal precipitation inhibitor. The composition according to any one of claims 1 to 8, wherein the composition is a cosmetic or an external preparation for skin.