JPH09157172A - Skin external agent and treating agent for eczema - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject external agent capable of improving rough skin attributable to atopic dermatitis, sensitive skin and skin xerosis and useful as a treating agent for eczema such as atopic dermatitis by compounding a specific compound in combination with a betaine. SOLUTION: This agent is composed of (A) one or more kinds of compounds selected from dipotassium glycyrrhizinate, glycyrrhizic acid and stearyl glycyrrhizinate and (B) a betaine (e.g. trimethyl glycine) as active components. Further, e.g. 0.1-2wt.% component A and 1-5wt.% component B are preferably compounded in the preparation. Regarding dosage, it is preferable that the agent is applied 1-5 times a day and a single coating dose is 0.25-15mg of the component A and 2.5-50mg of the component B.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin and an eczema drug, and is particularly useful for preventing and improving rough skin associated with atopic dermatitis, sensitive skin and dry skin disease.

[0002]

2. Description of the Related Art With the westernization of eating habits, changes in living environment, aging and increasing stress, various skin diseases, especially atopic dermatitis, sensitive skin, and dryness The number of people with dermatosis is increasing. For these diseases, symptomatic treatment is mainly performed, and treatment with steroids and non-steroids for pharmaceuticals is mainly used for quasi-drugs and cosmetics, such as glycerin, urea, collagen and sodium hyaluronate. Care is carried out with a formulation containing a moisturizer.

However, these treatments and cares have not been able to improve the rough skin associated with atopic dermatitis, sensitive skin and dry skin disease. That is, although inflammatory symptoms can be suppressed by administration of steroids or non-steroids,
It has been reported that it is difficult to improve the condition of rough skin, and conversely causes side effects such as redness and a feeling of tightness. In addition, quasi-drugs mainly containing moisturizers, etc. are effective to some extent for rough skin caused by lack of sebum and water in cosmetics, but against rough skin where a large amount of sebum is observed and desquamation is observed. Had little effect, and had the problem that it could not be expected to be effective enough to improve a wide range of types of rough skin.

The present invention has been made in view of the above circumstances, and has an effect of improving and preventing not only rough skin but also rough skin associated with skin diseases such as atopic dermatitis, sensitive skin and dry dermatosis. It is an object of the present invention to provide an external preparation for skin and an eczema drug used for prevention or treatment of eczema such as atopic dermatitis.

[0005]

Means for Solving the Problems and Modes for Carrying Out the Invention As a result of intensive studies to achieve the above-mentioned object, the present inventors have found that dipotassium glycyrrhizinate, glycyrrhetinic acid, and stearyl glycyrrhetinate are used alone or in combination. By using in combination with betaines, as seen in the results of Examples and Comparative Examples described later, dipotassium glycyrrhizinate, anti-inflammatory action of glycyrrhetinic acid and stearyl glycyrrhetinate and / or antiallergic action and the moisturizing action of betaine are synergistic. And atopic dermatitis, a wide range of rough skin including rough skin associated with sensitive skin and dry dermatosis, etc., and an excellent preventive and ameliorating effect on skin eczema, and thus the present invention is formed. It came to.

Accordingly, the present invention provides (1) a skin external preparation characterized by containing one or more compounds selected from dipotassium glycyrrhizinate, glycyrrhetinic acid and stearyl glycyrrhetinate, and betaines, and
(2) To provide an eczema drug containing, as an active ingredient, one or more compounds selected from dipotassium glycyrrhizinate, glycyrrhetinic acid and stearyl glycyrrhetinate, and betaines.

The present invention is described in more detail below. In the external preparation for skin of the present invention, the compounding amount of one or more compounds selected from dipotassium glycyrrhizinate, glycyrrhetinic acid and stearyl glycyrrhetinate is 0. 05-3% by weight, preferably 0.1-2% by weight
It is. If the amount is less than 0.05% by weight, the effect is not exhibited, and if the amount exceeds 3% by weight, it is meaningless in terms of effectiveness and may cause inconvenience such as deterioration of usability of the preparation.

On the other hand, the betaines used in the present invention are N-trialkyl substituted amino acids, such as trimethylglycine, γ-butyrobetaine, β-alanine betaine, betaine glutamate, phenylalanine betaine, alanine betaine, valine betaine and lysine. Betaine, ornithine betaine, taurobetaine, tomarin,
Examples include trigonein, carnitine, atrinin, homoserine betaine, antopreurin, stachydrin and the like. Of these, trimethylglycine is particularly preferable. These betaines can be used alone or in combination of two or more, and the total amount of the betaines is 0.5 to 10% by weight, preferably 1 to 5% by weight in the total composition. When the amount is less than 0.5% by weight, the effect is not exhibited, and when the amount is more than 10% by weight, the stickiness of the preparation may be a problem.

As described above, the eczema drug of the present invention contains, as active ingredients, one or more compounds of dipotassium glycyrrhizinate, glycyrrhetinic acid and stearyl glycyrrhetinate, and betaines. , Which is appropriately selected according to the symptoms, etc., but is usually administered by applying it to the affected area about 1 to 5 times a day, and the dose (application amount) per dose is dipotassium glycyrrhizinate, glycyrrhetinic acid, or stearyl glycyrrhetinate. 0.25
˜15 mg, betaines can be 2.5 to 50 mg.

The external preparation for skin or eczema of the present invention contains, in addition to the above-mentioned essential components, an oily component, a water-soluble component, a preservative, a pH adjusting agent, a thickener, which are usually used for external preparations for skin or eczema. Antioxidants, surfactants, coloring agents, flavoring agents and the like can be added as required. As the oil component, for example, liquid paraffin, petrolatum, squalane, microcrystalline wax, almond oil, olive oil, hydrogenated oil,
Jojoba oil, coconut oil, castor oil, palm oil, beeswax, lanolin, lauryl alcohol, cetanol, stearyl alcohol, oleyl alcohol, octyldodecanol, behenyl alcohol, lauric acid, myristic acid,
Palmitic acid, stearic acid, isostearic acid, oleic acid, isopropyl myristate, myristyl myristate, isopropyl palmitate, isopropyl adipate, etc. can be added. As the water-soluble component, for example,
Glycerin, propylene glycol, sorbitol, polyethylene glycol, 1,3-butylene glycol,
Ethanol, isopropanol, etc. can be added. Examples of the preservative include parabens, benzoic acids, benzalkonium chloride, benzethonium chloride, cetylpyridinium chloride, alkyltrimethylammonium chloride, alkyldiaminoethylglycine hydrochloride, chlorhexidine hydrochloride, chlorobutanol, salicylic acids, domifen bromide, and sorbin. An acid, phenoxyethanol or the like can be added. Examples of pH adjusters include citric acid, tartaric acid,
Acids such as lactic acid and alkalis such as sodium hydroxide, potassium hydroxide and triethanolamine can be added. Examples of the thickener include sodium carboxymethyl cellulose, sodium alginate, carboxy vinyl polymer, methyl cellulose, hydroxyethyl cellulose,
Hydroxypropyl cellulose, polyvinyl alcohol and the like can be added. Tocopherol as an antioxidant,
Erythorbic acid, propyl gallate, BHT, BHA,
NDGA etc. can be mixed. As the surfactant, fatty acid glycerin ester, sorbitan fatty acid ester, sucrose fatty acid ester, polyglycerin fatty acid ester, polyhydric alcohol fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene alkyl allyl ether, polyoxyethylene fatty acid ester, poly Oxyethylene sorbitan ester, polyoxyethylene glycerin fatty acid ester, polyoxyethylene hydrogenated castor oil and the like can be blended.

The external preparation for skin or the eczema preparation of the present invention may have any dosage form, and examples thereof include lotions, emulsions, creams, gels, ointments, packs, aerosols and body shampoos. However, the dosage form is not limited to the above.

[0012]

EXAMPLES The present invention will be described below in detail with reference to examples and comparative examples, but the present invention is not limited to the following examples.

[Examples 1 to 3 and Comparative Examples 1 to 4] With respect to the formulations shown in Table 1, the oil phase portion of A heated to 70 ° C. was added to the water phase portion of B similarly heated to 70 ° C. and emulsified. Then, a cream was prepared and the following tests were conducted.

[0014]

[Table 1]

<Rough skin improvement test associated with atopic dermatitis, sensitive skin and dry skin disease> Hartley guinea pig 1
A group of 0 animals is soaked in an acetone / ether mixture (1: 1) on the back of a shaved guinea pig for 10 minutes to create a rough skin model associated with atopic dermatitis, sensitive skin and dry skin disease. The invention product and the comparative product were continuously applied twice a day for 3 days (application amount: 5 μl in an area of 1 × 1 cm), and then the recovery state of rough skin at the application site was judged according to the criteria of Table 2. The judgment results are shown in Table 3.

[0016]

[Table 2]

[0017]

[Table 3]

From these results, by combining betaine with one or more compounds selected from dipotassium glycyrrhizinate, glycyrrhetinic acid and stearyl glycyrrhetinate, atopic dermatitis, sensitive skin and rough skin associated with dry dermatosis can be obtained. Was confirmed to be improved.

[Example 4] Lotion agent Dipotassium glycyrrhizinate 0.1% by weight Allantoin 0.1 Trimethylglycine 3.0 Glycerin 3.0 Hydroxypropyl methylcellulose 0.1 Phenoxyethanol 0.3 Purified water Total residual amount 100.0 % % Dissolve each component in purified water to prepare a lotion. The product of the present invention is used as a daily care agent for patients with atopic dermatitis.

[Example 5] Gel agent Dipotassium glycyrrhizinate 0.2% by weight Water-soluble placenta extract 0.1 Trimethylglycine 5.0 1,3-butylene glycol 3.0 Carboxyvinyl polymer 0.6 Phenoxyethanol 0.3 Ethanol 5.0 Sodium hydroxide 0.1 Purified water Residual total 100.0% by weight Each component is dissolved in purified water and neutralized with an aqueous sodium hydroxide solution to prepare a transparent gel agent. The product of the present invention is used as a sensitive skin care agent.

Example 6 Emulsion Oil phase Stearyl glycyrrhetinate 0.3% by weight Cetanol 5.0 Squalane 2.0 Soybean lecithin 1.0 POE (20) cetyl ether 3.5 Glycerin monostearate 1.5 l- Menthol 1.0 Aqueous phase Betaine (trimethylglycine) 5.0 Glycerin 5.0 Dibucaine hydrochloride 0.5 Sodium carboxymethylcellulose 0.2 Purified water Residual total 100.0% by weight Heated to 70 ° C. and dissolved oil phase An emulsion is prepared by adding to an aqueous phase heated to 70 ° C. and emulsifying with an emulsifying machine. The product of the present invention is used for the treatment and care of dry skin disease.

[0022]

INDUSTRIAL APPLICABILITY According to the present invention, by combining betaine with one or more compounds selected from dipotassium glycyrrhizinate, glycyrrhetinic acid and stearyl glycyrrhetinate, atopic dermatitis, sensitive skin and dryness can be obtained. It can improve rough skin associated with dermatosis and is effective as an eczema drug for atopic dermatitis.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁶ Identification code Internal reference number FI Technical display part A61K 9/06 A61K 9/06 G 31/205 31/205

Claims (2)

[Claims] 1. An external preparation for skin, comprising one or more compounds selected from dipotassium glycyrrhizinate, glycyrrhetinic acid and stearyl glycyrrhetinate, and betaines. 2. An eczema drug containing, as an active ingredient, one or more compounds selected from dipotassium glycyrrhizinate, glycyrrhetinic acid and stearyl glycyrrhetinate, and betaines.