JP2001163777A - Skin lotion - Google Patents

Abstract

PROBLEM TO BE SOLVED: To prepare a skin lotion causing only a little skin irritation, preventing liquid drops in its application and excellent in sense of use. SOLUTION: This skin lotion consists of (1) 8-23 wt.% of urea, (2) 0.3-4 wt.% of diphenhydramine or its salt, (3) 0.5-5 wt.% of lidocaine, (4) 20-32 wt.% of a lower alcohol, (5) 0.1-20 wt.% of a humectant, (6) 0.1-2 wt.% of a thickener and (7) the remainder of water, and is useful as a therapeutic agent for dry skin diseases.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a solution for external use on the skin which has a keratin water retention function and an antipruritic effect and has an excellent feeling upon use.

[0002]

2. Description of the Related Art Dry skin diseases are one of the diseases which have been increasing in recent years, such as senile xeroderma associated with aging and atopic dermatitis. The disease is caused by decreased skin function due to aging and other causes, resulting in decreased sebum secretion and cutaneous blood flow. Dry skin is severely itchy due to slight irritation or a change in the temperature of the outside world, so that the affected area is unconsciously scraped, inflammation occurs at the scratched part, and the skin condition is further worsened. In addition, severe itching causes insomnia and irritation, and suffers from mental anxiety. From these facts, it is therapeutically necessary for dry skin diseases to increase the water retention ability of dry skin and to suppress itching.

[0003] Therefore, there is known a skin external preparation containing a large amount of alcohol containing urea which enhances the water retention function of the stratum corneum, an antihistamine having an antipruritic effect, and a local anesthetic (JP-A-3-291221). Similarly, there is known a skin disease treatment emulsion containing urea, diphenhydramine and lidocaine, and reducing the amount of alcohol to prepare an emulsion (Japanese Patent Application Laid-Open No. 7-291856).

[0004]

Problems to be Solved by the Invention
The liquid preparation described in Japanese Patent Publication No. 1 contains a large amount of lower alcohol, so that skin irritation to the scratched portion was large. In addition, since the liquid preparation had no viscosity, the liquid preparation taken on the palm spilled before being applied to the affected area, and it could not be said that the preparation was easy to use. JP-A-7-291856 has reduced the content of lower alcohol to reduce skin irritation and increased the percutaneous absorption of diphenhydramine and lidocaine. An emulsion was prepared to uniformly disperse the drug, and a thickener was added for the purpose of preventing dripping and stabilizing the emulsion. However, an emulsion containing a thickener has a large stickiness at the time of application, and is not suitable for application over a wide range. Therefore, there has been a demand for a liquid preparation which has a small skin irritation, prevents liquid dripping at the time of application, and has an excellent feeling upon use.

[0005]

Under these circumstances, the inventors of the present invention have intensively studied a liquid agent which has a feeling of use, for example, a good touch, a low stickiness, and which prevents liquid dripping at the time of application. As a result, urea, 8 to 23% by weight, diphenhydramine or a salt thereof, 0.3 to 4% by weight, lidocaine, 0.5 to 5% by weight, lower alcohol, 20 to 3
2% by weight, humectant, 0.1-20% by weight, thickener,
It has been found that a liquid preparation comprising 0.1 to 2% by weight, water and the balance is a transparent liquid preparation for external use with minimal skin irritation, good usability, and little dripping when applied. Reached.

Hereinafter, the present invention will be described in detail. The solution of the present invention contains urea. Since urea has a keratin water retention effect, it is used as a medicinal ingredient for dry skin diseases, and a sufficient therapeutic effect can be obtained by adding 8 to 23% by weight, preferably 10 to 20% by weight. .

[0007] The liquid preparation of the present invention contains diphenhydramine or a pharmaceutically acceptable salt thereof such as a hydrochloride or a tannate thereof. The compounding amount is 0.3 to 4% by weight, preferably 0.5 to 2% by weight. Further, the liquid preparation of the present invention contains lidocaine. The compounding amount is 0.5 to 5% by weight,
Preferably, it is 1 to 3% by weight.

The lower alcohol used in the present invention includes ethanol and / or isopropanol, and the compounding amount is 20 to 32% by weight, preferably 25 to 30% by weight.
% By weight. When the amount is within this range, the liquid preparation has an appropriate feeling of use.

The humectant is not particularly limited as long as it is conventionally known. Examples thereof include glycerin, propylene glycol, 1,3-butylene glycol, polyethylene glycol 200 and polyethylene glycol 30.
0, polyhydric alcohols such as polyethylene glycol 400, lactic acid, sodium lactate, etc., and one or more of these can be blended. The compounding amount is slightly different depending on the kind of the humectant, but is 0.1 to 20% by weight, preferably 5 to 20% by weight.

Examples of the thickener used in the present invention include water-soluble polymer substances such as polyvinylpyrrolidone and cellulose derivatives such as hydroxypropylcellulose and hydroxypropylmethylcellulose. Preferably, it is a cellulose derivative such as hydroxypropylmethylcellulose. Most preferably, it is hydroxypropyl methylcellulose. The compounding amount is 0.1 to 2% by weight,
Preferably it is 0.2 to 1% by weight.

The external preparation for skin of the present invention may contain, if necessary, other medicinal ingredients in addition to the above-mentioned components, such as anti-inflammatory agents such as camphor, salicylic acid, glycyrrhetinic acid and dipotassium glycyrrhizinate, and cooling agents such as menthol and peppermint oil. Agents, vitamins such as tocopherol acetate, and antipruritic agents such as crotamiton. Also, as a pH adjuster, sodium hydroxide, triethanolamine, hydrochloric acid, lactic acid, etc .; as a preservative, methyl paraoxybenzoate, propyl paraoxybenzoate, etc .; as a fragrance, eucalyptus oil, etc .; Hardened castor oil, sorbitan sesquioleate, and the like; lactic acid, hydrochloric acid, and the like can be appropriately added as a solubilizing agent.

A preferred composition of the external preparation for skin of the present invention is:
Urea, 10 to 20% by weight, diphenhydramine or a salt thereof, 0.5 to 2% by weight, lidocaine, 1 to 3% by weight, ethanol and / or isopropanol 25 to 3
0% by weight, humectant, 5-20% by weight, thickener, 0.1%
2 to 1% by weight, water and the balance.

The liquid preparation of the present invention thus prepared is
The product is filled into a suitable container to form a product, and is applied by appropriately applying to the affected part. The solution for external use on the skin of the present invention can be produced by a generally known method. For example, a thickener is dissolved in water. Dissolve lidocaine, diphenhydramine or its salt, urea, humectant, etc. in lower alcohol and water. , And the mixture is stirred, whereby the liquid preparation of the present invention can be produced. The external preparation for skin of the present invention produced as described above is transparent at pH 5.0 to 6.0.

[0014]

EXAMPLES The present invention will be described below with reference to Examples.
The present invention is not limited to these.

Example 1 Urea 10.0 (wt%) Diphenhydramine hydrochloride 1.0 Lidocaine 2.0 Tocopherol acetate 0.3 Ethanol 20.0 Polyethylene glycol 400 10.0 Sodium lactate 5.0 Hydroxypropyl methylcellulose 0.25 Lactic acid 1.5 Polyoxyethylene hydrogenated castor oil 60 3.0 Methyl paraoxybenzoate 0.05 Propyl paraoxybenzoate 0.025 Water Remainder The above components were dissolved to obtain a transparent liquid of pH 5.5.

Example 2 Urea 10.0 (% by weight) Diphenhydramine hydrochloride 1.0 Lidocaine 2.0 Tocopherol acetate 0.3 Ethanol 26.8 Polyethylene glycol 400 10.0 Sodium lactate 5.0 Hydroxypropyl methylcellulose 0.25 Lactic acid 1.6 Polyoxyethylene hydrogenated castor oil 60 3.0 Methyl paraoxybenzoate 0.05 Propyl paraoxybenzoate 0.025 Water Remainder The above components were dissolved to obtain a transparent solution having a pH of 5.7.

Example 3 Urea 10.0 (wt%) Diphenhydramine hydrochloride 1.0 Lidocaine 2.0 Tocopherol acetate 0.3 Ethanol 32.0 Polyethylene glycol 400 10.0 Sodium lactate 5.0 Hydroxypropyl methylcellulose 0.25 Lactic acid 1.5 Polyoxyethylene hydrogenated castor oil 60 3.0 Methyl paraoxybenzoate 0.05 Propyl paraoxybenzoate 0.025 Water Remainder The above components were dissolved to obtain a transparent liquid having a pH of 5.8.

Example 4 Urea 10.0 (wt%) Diphenhydramine hydrochloride 1.0 Lidocaine 2.0 Tocopherol acetate 0.3 Ethanol 26.9 Glycerin 10.0 Sodium lactate 5.0 Hydroxypropyl methylcellulose 0.25 Lactic acid 1. 5 Polyoxyethylene hydrogenated castor oil 60 3.0 Methyl paraoxybenzoate 0.05 Propyl paraoxybenzoate 0.025 Water Remainder The above components were dissolved to obtain a transparent liquid of pH 5.5.

Example 5 Urea 10.0 (wt%) Diphenhydramine hydrochloride 1.0 Lidocaine 2.0 Tocopherol acetate 0.3 Isopropanol 25.0 Polyethylene glycol 400 10.0 Sodium lactate 5.0 Hydroxypropyl methylcellulose 0.25 Lactic acid 1.5 Polyoxyethylene hydrogenated castor oil 60 3.0 Methyl paraoxybenzoate 0.05 Propyl paraoxybenzoate 0.025 Water Remainder The above components were dissolved to obtain a transparent solution having a pH of 5.7.

[0020]

Test Example 1 In order to evaluate the feeling of use of the liquid preparation for external use of the present invention, Example 2 and the urea-containing preparations, commercially available product A (solution) and commercially available product B (emulsion), had a sticky feeling and a dripping effect. The stiffness and overall ease of use were compared and examined using questionnaires of a total of 11 men, 6 men and 5 women, using the following evaluation axes.

Evaluation Items Example 2 Commercial Product A (Liquid) Commercial Product B (Emulsion) Stickiness 3.3 2.8 3.0 Liquid Sag 3.5 2.4 4.0 Overall Ease of Use 4. 0 3.0 3.6

From the above average evaluation points, it was found that Example 2 had less stickiness than the two commercial products.
In addition, the evaluation result of liquid dripping was the highest for the commercial product B as an emulsion, but Example 2 which was a liquid agent was the most excellent in overall ease of use. From the above, it can be said that the liquid preparation of the present invention is an easy-to-use liquid preparation for external use on the skin with less stickiness and less dripping during application.

[0023]

[Effects] As is clear from the above results, the external preparation of the present invention has an excellent skin moisture retention function, has little dripping when applied, and has an easy-to-use agent for treating dry skin diseases with a small sticky feeling. It is.

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Claims (1)

[Claims] 1. Urea, 8 to 23% by weight diphenhydramine or a salt thereof, 0.3 to 4% by weight lidocaine, 0.5 to 5% by weight lower alcohol, 20 to 32% by weight humectant, 0.1 to 20% by weight % Thickener, 0.1-2% by weight water, balance