JP3723728B2 - Skin topical solution - Google Patents

Description

評価項目毎の平均評価点を以下に示す。
【００２１】

【００２２】
上記の平均評価点より、実施例２は市販品２剤と比較して、べたつき感が少ないことがわかった。また、液ダレの評価結果は乳剤である市販品Ｂが最も高かったものの、全体的な使いやすさでは液剤である実施例２が最も優れていた。以上のことから、本発明の液剤は、べたつき感の少ない、塗布時の液ダレを少なくした使いやすい皮膚外用液剤であるといえる。
【００２３】
【効果】
以上の結果より明らかなように、本発明の外用液剤は、優れた皮膚水分保持機能を有し、かつ塗布時の液だれが少なく、べたつき感の小さい使いやすい乾燥性皮膚疾患治療剤である。[0001]
BACKGROUND OF THE INVENTION
TECHNICAL FIELD The present invention relates to an external skin preparation having an excellent feeling of use having both a keratin moisture retention function and an antipruritic action.
[0002]
[Prior art]
Dry skin disease is one of the diseases that has been increasing in recent years, such as senile xeroderma associated with aging and atopic dermatitis. This disease is caused by a decrease in skin function due to aging and other causes, and a decrease in sebum secretion and skin blood flow. Dry skin causes severe itching due to slight irritation or changes in the temperature of the outside world, so that the affected area is unwittingly scratched, inflammation occurs in the scratched portion, and skin symptoms are further worsened. In addition, severe itching causes insomnia and irritability and suffers from mental anxiety. From these facts, it is necessary for treatment of dry skin diseases to enhance the water retention ability of dry skin and to suppress itching.
[0003]
Therefore, an external skin preparation containing a large amount of alcohol containing urea, which enhances the water retention function of the keratin, an antihistamine having an antipruritic action, and a local anesthetic is known (Japanese Patent Laid-Open No. 3-291221). Similarly, a skin disease treatment emulsion containing urea, diphenhydramine and lidocaine and reducing the amount of alcohol to form an emulsion is known (Japanese Patent Laid-Open No. 7-291856).
[0004]
[Problems to be solved by the invention]
Since the liquid preparation described in JP-A-3-291221 contains a large amount of lower alcohol, the skin irritation to the scratched part was large. In addition, since it is a non-viscous solution, it spilled until the solution in the palm of the hand was applied to the affected area, and it was not an easy-to-use preparation. Japanese Patent Laid-Open No. 7-291856 reduced the content of lower alcohol to reduce skin irritation and increased the transdermal absorption of diphenhydramine and lidocaine. In order to disperse the drug uniformly, an emulsion was added, and a thickener was added for the purpose of preventing dripping and stabilizing the emulsification. However, emulsions to which thickeners have been added are not suitable for coating over a wide range because of the large stickiness during coating. Accordingly, there has been a demand for a liquid agent that has low skin irritation, prevents liquid dripping at the time of application, and has an excellent usability.
[0005]
[Means for Solving the Problems]
Under such circumstances, the present inventors have made extensive studies on a liquid agent that has a feeling of use, for example, a good touch, a low stickiness, and prevents dripping during application. As a result, (1) urea, 8- 23% by weight, (2) diphenhydramine or a salt thereof, 0.3 to 4% by weight, (3) lidocaine, 0.5 to 5% by weight, (4) lower alcohol, 20 to 32% by weight, (5) humectant , 0.1 to 20% by weight, (6) thickener, 0.1 to 2% by weight, (7) water, the remaining liquid agent has a small skin irritation, good usability, and dripping during application As a result, the present invention was completed.
[0006]
The present invention is described in detail below.
The liquid medicine of the present invention contains urea. Urea is used as a medicinal component for dry skin diseases because it has a keratin moisture retention effect, and a sufficient therapeutic effect can be obtained by blending 8 to 23% by weight, preferably 10 to 20% by weight. .
[0007]
The solution of the present invention contains diphenhydramine or a pharmacologically acceptable salt thereof such as hydrochloride or tannate thereof. The blending amount is 0.3 to 4% by weight, preferably 0.5 to 2% by weight. Moreover, this invention liquid mix | blends a lidocaine. The blending amount is 0.5 to 5% by weight, preferably 1 to 3% by weight.
[0008]
Examples of the lower alcohol used in the present invention include ethanol and / or isopropanol, and the blending amount is 20 to 32% by weight, preferably 25 to 30% by weight. If it is the compounding quantity of this range, it will become a liquid agent which has a suitable usability | use_condition.
[0009]
The humectant is not particularly limited as long as it is conventionally used. For example, polyhydric alcohols such as glycerin, propylene glycol, 1,3-butylene glycol, polyethylene glycol 200, polyethylene glycol 300, and polyethylene glycol 400, Examples thereof include lactic acid and sodium lactate, and these can be used alone or in combination. The blending amount varies slightly depending on the type of humectant, but is 0.1 to 20% by weight, preferably 5 to 20% by weight.
[0010]
Examples of the thickener used in the present invention include water-soluble polymer substances such as polyvinyl pyrrolidone or cellulose derivatives such as hydroxypropylcellulose and hydroxypropylmethylcellulose. Preferred is a cellulose derivative such as hydroxypropylmethylcellulose. Most preferred is hydroxypropylmethylcellulose. A compounding quantity is 0.1 to 2 weight%, Preferably it is 0.2 to 1 weight%.
[0011]
In addition to the above-mentioned components, the external preparation for skin of the present invention contains other medicinal components, for example, camphor, salicylic acid, glycyrrhetinic acid, dipotassium glycyrrhizinate and other anti-inflammatory agents, menthol, mint oil and other refreshing agents, It can contain vitamins such as tocopherol and antipruritic agents such as crotamiton. Moreover, sodium hydroxide, triethanolamine, hydrochloric acid, lactic acid, etc. as pH adjusters; methyl paraoxybenzoate, propyl paraoxybenzoate, etc. as preservatives; eucalyptus oil, etc. as perfumes; polyoxyethylene as surfactants Hardened castor oil, sorbitan sesquioleate, and the like; lactic acid, hydrochloric acid, and the like can be appropriately blended as a solubilizing agent.
[0012]
The preferred composition of the external preparation for skin of the present invention is: (1) urea, 10 to 20% by weight, (2) diphenhydramine or a salt thereof, 0.5 to 2% by weight, (3) lidocaine, 1 to 3% by weight, 4) ethanol and / or isopropanol 25-30% by weight, (5) humectant, 5-20% by weight, (6) thickener, 0.2-1% by weight, (7) water, balance.
[0013]
The solution of the present invention thus prepared is filled into a suitable container to obtain a product, which is applied by appropriately applying to the affected part. The external preparation for skin of the present invention can be produced by a generally known method.
(1) Dissolve the thickener in water.
(2) Dissolve lidocaine, diphenhydramine or a salt thereof, urea, humectant, etc. in lower alcohol and water.
The liquid agent of the present invention can be produced by adding (2) to (3) and (1) and stirring.
The shape of the external preparation for skin of the present invention produced as described above is pH 5.0 to 6.0 and is transparent.
[0014]
【Example】
Hereinafter, the present invention will be described with reference to examples, but the present invention is not limited thereto.
[0015]
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
The remainder of the water The above components were dissolved to obtain a transparent solution having a pH of 5.5.
[0016]
Example 2
Urea 10.0 (wt%)
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
Remaining water The above components were dissolved to obtain a transparent solution having a pH of 5.7.
[0017]
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 balance The above components were dissolved to obtain a transparent solution having a pH of 5.8.
[0018]
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
The remainder of the water The above components were dissolved to obtain a transparent solution having a pH of 5.5.
[0019]
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
Remaining water The above components were dissolved to obtain a transparent solution having a pH of 5.7.
[0020]
[Test Example 1]
For the purpose of evaluating the feeling of use of the external preparation of the present invention, the stickiness of the commercial product A (solution) and the commercial product B (emulsion) which are Example 2 and urea-containing preparations, the difficulty of dripping, and the overall Ease of use was compared and examined using a questionnaire of 11 people, 6 men and 5 women, using the following evaluation axes.

The average evaluation score for each evaluation item is shown below.
[0021]

[0022]
From the above average evaluation points, it was found that Example 2 had less stickiness compared to two commercially available products. In addition, the evaluation result of the liquid sag was highest in the commercial product B as an emulsion, but in terms of overall ease of use, Example 2 as a liquid agent was the most excellent. 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 with little stickiness and reduced liquid dripping at the time of application.
[0023]
【effect】
As is clear from the above results, the external preparation of the present invention is an easy-to-use dry skin disease treatment agent that has an excellent skin moisture retention function, little dripping at the time of application, and little stickiness.

Claims (1)

(1) Urea, 8-23% by weight
(2) Diphenhydramine or a salt thereof, 0.3 to 4% by weight
(3) Lidocaine, 0.5-5% by weight
(4) Lower alcohol, 20 to 32% by weight
(5) Moisturizer, 0.1 to 20% by weight
(6) Hydroxypropyl methylcellulose , 0.1 to 2% by weight
(7) A liquid preparation for external use consisting of water and the remainder.