External composition

Abstract

To provide an external composition superior in stability of ectoine.SOLUTION: An external composition containing ectoine and at least one selected from the group consisting of a heparin analogue, glycyrrhizic acid and / or a salt thereof, ascorbyl glucoside, and allantoin.SELECTED DRAWING: None

Description

[Technical Field]

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

[0002] Ectoine is a cyclic amino acid found in abundance in alkaliphilic bacteria that live in salt lakes in Egypt. Ectoine has the ability to retain moisture by forming hydration nuclei and protects cells from dryness, ultraviolet rays, air pollutants, temperature, and chemicals (Non-Patent Document 1). It is said to have moisturizing and improve skin barrier function, and is used as a moisturizer in topical preparations such as cosmetics and quasi-drugs.

[0003] Preparations containing ectoine are being developed, and Patent Document 1 describes skin care creams, sunscreen lotions, hair styling gels, etc. that contain ectoine. However, there have been no reports on the stability of ectoine in preparations, nor have there been any reports on the effect of blending it with other ingredients on the stability of ectoine. [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Special Publication 2003-528122 [Non-patent literature]

[0005] [Non-Patent Document 1] Clinics in Dermatology (2008) 26, 326-333 Summary of the Invention [Problem to be solved by the invention]

[0006] The object of the present invention is to provide a composition for external use that contains ectoine with excellent stability. [Means for solving the problem]

[0007] As a result of extensive research to solve the above problems, the inventors have found that the stability of ectoine in a topical composition can be improved by combining ectoine with one selected from heparinoids, glycyrrhizinic acid and / or its salts, and ascorbic acid glucoside.

[0008] That is, the present invention provides: (1) A composition for external use, characterized by containing (a) 1 w / w% or more of ectoine, and (b) at least one selected from the group consisting of heparinoids, glycyrrhizinic acid and / or salts thereof, ascorbic acid glucoside, and allantoin; (2) The composition for external use according to (1), wherein (b) the heparinoid is 0.01 to 10 parts by mass per part by mass of (a) ectoine. (3) The composition for external use according to (1) or (2), wherein (b) glycyrrhizinic acid and / or a salt thereof is 0.01 to 10 parts by mass per part by mass of (a) ectoine. (4) The composition for external use according to any one of (1) to (3), wherein (b) ascorbic acid glucoside is 0.1 to 10 parts by mass per part by mass of (a) ectoine. (5) (b) The composition for external use according to any one of (1) to (4), wherein the glycyrrhizinic acid and / or a salt thereof is dipotassium glycyrrhizinate; (6) The composition for external use according to any one of (1) to (5), wherein (b) allantoin is 0.1 to 10 parts by mass per 1 part by mass of (a) ectoine. (7) A method of (a) stabilizing ectoine by adding (b) at least one selected from the group consisting of heparinoids, glycyrrhizinic acid and / or salts thereof, ascorbic acid glucoside, and allantoin to a topical composition; is. [Effects of the Invention]

[0009] According to the present invention, it is possible to provide a composition for external use containing ectoine with excellent stability. DETAILED DESCRIPTION OF THE INVENTION

[0010] The components used in the topical composition of the present invention may be of the same quality as those used in ordinary pharmaceuticals, quasi-drugs, or cosmetics.

[0011] The ectoine of the present invention is a zwitterionic compound having a carboxy group (-COOH) and an amino group (-NH2), and is also a type of cyclic amino acid. The content of the ectoine of the present invention in the topical composition of the present invention is usually 1 w / w% or more, preferably 1 to 10 w / w%, more preferably 1 to 5 w / w%, and even more preferably 1 to 2 w / w%.

[0012] The heparinoid of the present invention is a type of polysaccharide called mucopolysaccharide, which has moisturizing, blood circulation promoting and anti-inflammatory effects, and is used in external preparations. The content of the heparinoid of the present invention is not particularly limited, but is preferably 0.01 to 5 w / w %, more preferably 0.1 to 0.5 w / w %, in the external use composition of the present invention. From the viewpoint of the stability of ectoine, the amount of the heparinoid is preferably 0.01 to 10 parts by mass, more preferably 0.01 to 1, per part by mass of ectoine.

[0013] Examples of glycyrrhizinic acid and / or salts thereof in the present invention include glycyrrhizinic acid, dipotassium glycyrrhizinate, trisodium glycyrrhizinate, and monoammonium glycyrrhizinate, and preferably glycyrrhizinic acid and dipotassium glycyrrhizinate, and more preferably dipotassium glycyrrhizinate. The content of glycyrrhizinic acid and / or a salt thereof of the present invention is not particularly limited, but is preferably 0.01 to 2 w / w %, more preferably 0.05 to 1 w / w %, in the topical composition of the present invention. From the viewpoint of stability of ectoine, the amount of glycyrrhizin and / or a salt thereof is preferably 0.01 to 10 parts by mass, more preferably 0.01 to 1, per part by mass of ectoine.

[0014] The content of ascorbic acid glucoside of the present invention is not particularly limited, but is preferably 0.1 to 10 w / w%, more preferably 0.1 to 5 w / w%, and even more preferably 1 to 3 w / w% in the topical composition of the present invention. From the viewpoint of stability of ectoine, the amount of ascorbic acid glucoside is preferably 0.1 to 10 parts by mass, more preferably 0.1 to 5 parts by mass, per part by mass of ectoine.

[0015] The content of allantoin in the present invention is not particularly limited, but is preferably 0.1 to 10 w / w %, more preferably 1 to 5 w / w %, in the topical composition of the present invention. From the viewpoint of stability of ectoine, the amount of allantoin is preferably 0.1 to 10 parts by mass, more preferably 0.1 to 1, per part by mass of ectoine.

[0016] In addition to the above-mentioned components, the topical composition of the present invention may contain various components used in ordinary cosmetics, quasi-drugs, pharmaceuticals, etc., as appropriate, provided that the effects of the present invention are not impaired. For example, pH adjusters (potassium hydroxide, sodium hydroxide, citric acid, sodium citrate, etc.), fragrances, refreshing agents (menthol, peppermint oil, camphor, etc.), anti-inflammatory agents (salicylic acid, glycyrrhetinic acid, allantoin, indomethacin, felbinac, diclofenac sodium, loxoprofen sodium, etc.), disinfectants (chlorhexidine gluconate, isopropylmethylphenol, etc.), preservatives (parabens (methylparaben, butylparaben, propylparaben, etc.), benzoic acid or its salts, etc.), etc. , moisturizers (hyaluronic acid or its salts, chondroitin sulfate, amino acids (L-serine, L-proline, L-hydroxyproline, glycine, etc.), lipidure, sorbitol, maltitol, etc.), thickeners (polyvinylpyrrolidone, sodium alginate, ethyl cellulose, hydroxypropyl methylcellulose, sodium carboxymethylcellulose, xanthan gum, carrageenan, etc.), extracts of various animals and plants (coprinus chinensis, Phellodendron bark, seaweed, moutan pi, licorice, rosemary, sage, etc.), vitamins (retinol palmitate, ascorbic acid, thiamine nitrate, cyanocobalamin, biotin, riboflavin, etc.), antioxidants (dibutylhydroxytoluene, tocopherol, sodium edetate, ascorbic acid, isopropyl gallate, etc.), solubilizers (various vegetable oils, various animal oils, alkyl glyceryl ethers, hydrocarbons, etc.), oily gelling agents (inulin stearate, dextrin palmitate, etc.), metabolic activators, adhesives, antihistamines (chlorpheniramine maleate, etc.), local anesthetics Examples of suitable anti-inflammatory agents include steroids (procaine, tetracaine, bupipacaine, mepipacaine, chloroprocaine, proparacaine, meprylcaine or salts thereof, orthocaine, oxethazaine, oxypolyethylenediamine, scopolia extract, percaminpase, tesitdecin, etc.), skin protectants (collodion, castor oil, etc.), blood circulation promoting ingredients (γ-oryzanol, nonylic acid vanillylamide, nicotinic acid benzyl ester, capsaicin, chili pepper extract, etc.), and mucopolysaccharides (glucosamine, hyaluronic acid, etc.). These ingredients may be used alone or in combination of two or more. The amounts of these ingredients added are not particularly limited and can be determined appropriately taking into consideration the feel when used, etc. When a pharmacological ingredient is contained, the content may be appropriately determined depending on the type of pharmacological ingredient used, the expected effect, etc. As described above, allantoin and retinol palmitate are listed as optional additional components of the topical composition of the present invention, but are not limited to these additional components and may be formulated together with ectoin.

[0017] The form of the topical composition of the present invention is not particularly limited as long as it is a dosage form that can be applied to the skin. Specific dosage forms include lotions, creams, emulsions, gels, packs, etc. The topical composition of the present invention may be a W / O or O / W emulsion formulation.

[0018] The topical composition of the present invention can be used for applications such as cosmetics, quasi-drugs, and pharmaceuticals. The topical composition of the present invention can be produced by a conventional method depending on the dosage form. For example, in the case of a lotion, it can be produced by mixing and homogenizing the respective components.

[0019] The present invention will be described in detail below with reference to examples and comparative examples, but the present invention is not limited to the following examples. In the examples and comparative examples, all numerical values mean mass %.

[0020] (Method for preparing a topical composition) According to the formulations shown in Tables 1 and 2 below, the components were uniformly mixed with purified water to obtain compositions of the examples and comparative examples.

[0021] (Evaluation of Ectoine Stability) Each topical composition from the Examples and Comparative Examples was filled into a 50 mL glass screw tube and stored at 65°C for two weeks. After storage, each liquid formulation was thoroughly mixed before testing. Immediately after preparation and after storage, each liquid formulation was diluted to an appropriate concentration with ultrapure water and tested by liquid chromatography. The residual rate of ectoine and / or the ratio relative to the comparative example was calculated using the following formulas 1 and 2. The results are shown in Tables 1 and 2.

[0022] <Expression 1> Residual rate (%) = Quantitative value after storage / Quantitative value immediately after preparation × 100 <Expression 2> Ratio to Comparative Example (%) = Residual rate of Example / Residual rate of Comparative Example × 100

[0023] [Table 1]

[0024] [Table 2]

[0025] As is clear from the results in Table 1, when ectoine was used alone (Comparative Examples 1 and 2), a decrease in the quantitative value of ectoine was observed after storage, but when a heparin-like substance, dipotassium glycyrrhizinate, ascorbic acid glucoside, or allantoin was added, stability was improved (Examples 1 to 8).

[0026] (Prescription example) Below, examples of formulations for external use compositions according to the present invention are shown in Tables 2 to 6. All units are w / w%. Table 2 shows the formula for lotion, Table 3 shows the formula for oil-in-water emulsion, Table 4 shows the formula for water-in-oil emulsion, Table 5 shows the formula for sun care, and Table 6 shows the formula for gel.

[0027] [Table 2]

[0028] [Table 3]

[0029] [Table 4]

[0030] [Table 5]

[0031] [Table 6] [Industrial Applicability]

[0032] According to the present invention, it is possible to provide a composition for external use containing ectoine with excellent stability.

Claims

1. A topical composition characterized by containing (a) 1 wt% or more of ectoine, and (b) at least one member selected from the group consisting of heparinoids, glycyrrhizinic acid and / or its salts, ascorbic acid glucoside, and allantoin.

2. 2. The topical composition according to claim 1, wherein (b) the heparinoid is present in an amount of 0.01 to 10 parts by mass per part by mass of (a) ectoine.

3. 2. The topical composition according to claim 1, wherein (b) glycyrrhizinic acid and / or a salt thereof is contained in an amount of 0.01 to 10 parts by mass per part by mass of (a) ectoine.

4. 2. The composition for external use according to claim 1, wherein (b) ascorbic acid glucoside is present in an amount of 0.1 to 10 parts by mass per part by mass of (a) ectoine.

5. 4. The topical composition according to claim 1, wherein (b) glycyrrhizinic acid and / or its salt is dipotassium glycyrrhizinate.

6. The topical composition according to claim 1, wherein (b) allantoin is present in an amount of 0.1 to 10 parts by mass per part by mass of (a) ectoin.

7. A method for stabilizing (a) ectoine by adding (b) at least one selected from the group consisting of heparinoids, glycyrrhizinic acid and / or its salts, ascorbic acid glucoside, and allantoin to an external composition.

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