JPH0232006A - External preparation for skin - Google Patents

Abstract

PURPOSE:To obtain an external preparation for skin capable of preventing and improving skin disorder and physiological aging by blending an external preparation for skin with N-(2hydroxyethyl)nicotinic acid amide nitrate ester or a salt thereof as an active ingredient. CONSTITUTION:An external preparation for skin such as toilet lotion, milky lotion, cream, foundation or dispersion is blended with usually 0.00001-10wt.%, preferably 0.0001-5wt.%, especially 0.01-1wt.% based on total amounts of external preparation for skin of N-(2-hydroxyethyl)nicotinic acid amide nitrate ester (nicorandil) shown by the formula or a salt thereof well-known as a remedy for angina pectoris as an active ingredient to give an external preparation for skin capable of effectively preventing and improving skin disorder such as heat after sunburn, razor rash or chapped skin and physiological aging of skin.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Application Field] The present invention relates to an external skin preparation, particularly to an external skin preparation that prevents and improves skin disorders and physiological aging of the skin.

[Conventional Techniques 14] [Problems to be Solved by the Invention] However, conventional skin preparations do not prevent sunburn from causing hot flashes, razor burn, rough skin, etc. and physiological aging of the skin. The improvement effect is insufficient, and although there is a long-awaited topical skin preparation with excellent these effects, no sufficient product has been provided yet.

The present invention was made in view of the problems of the prior art, and its purpose is to provide an external preparation for skin that can effectively prevent skin disorders and physiological aging. be.

In order to achieve the above object, the present inventors have conducted intensive research to obtain raw materials that have a particularly soothing effect on the skin. The present invention has been achieved by focusing on nicorandil and its salts as substances that have the effect of preventing and improving physiological aging.

[Means for Solving the Problem of Protecting the Country] That is, the claimed invention is an external skin preparation characterized by containing nicorandil or its salts.

The present invention will be explained in detail below.

Nicorandil in the present invention was invented and developed in Japan (
Hiroyuki Nagano et al. 2 Proceedings of the 98th meeting of the Pharmaceutical Society of Japan, 232.1
978) It is a drug for treating angina pectoris. Although it has a coronary vasodilator effect and an inhibitory effect on coronary artery curvature, it has little effect on cardiac hemodynamics and cardiac function, making it an effective drug for the treatment of various types of angina (Japanese Patent Publication No. 17463/1989, Showa 5
3-9323). Many reports have been made regarding its pharmacological effects on the circulatory system, but there have been reports of mild changes in the central nervous system and renal function when administered in doses 100 times or more of the clinical dose in other areas. is being done.

However, its application to the field of external skin preparations was completely unknown.

In the present invention, the amount of nicorandil or its salts added to the skin external preparation is usually 0.0000 in the total amount of the skin external preparation.
1-10 (wt%), preferably Shikuha 0.0o01-5 (
(% by weight), more preferably from 0.01 to 1 (% by weight). If it is less than 0.00001%, the effect of the present invention cannot be sufficiently obtained, and if it is more than 10%, it is disadvantageous in terms of formulation. Various ingredients commonly used in external skin preparations within a range that does not impair the effects of the present invention, namely aqueous ingredients, powder ingredients, oils, surfactants, humectants,
Thickeners, preservatives, antioxidants, fragrances, pigments, etc. can be added.

Moreover, the dosage form of the skin external preparation of the present invention is arbitrary, and can be, for example, a solubilized system such as a lotion, an emulsified system such as a milky lotion or a cream, or a dosage form such as a foundation or a dispersion.

[Example 1 Next, the present invention will be explained in more detail with reference to Examples.

Note that the present invention is not limited to this.

The effects of applying the external skin preparation of the present invention using Ni-S'nicorandil to the skin were evaluated in terms of improvement rates for skin hot flashes, rough skin, and razor bumps by carrying out a practical test using the method described below.

Sunburn was conducted on 2 subjects each who suffered from symptoms of hot flashes or rough skin after sunburn, and a lotion with the composition shown in Table 1 was applied to the face. was determined.

In addition, the lotions shown in Table 1 were applied to 20 male test subjects who shaved their beards immediately after shaving, and the effects on shaving were evaluated.

The determination results are shown in Table 2.

The criteria for each evaluation were as follows.

Improving effect on hot flashes or rough skin after sun exposure: Significantly effective: Symptoms disappeared Effective: Symptoms weakened Slightly effective: Symptoms slightly weakened Ineffective: No change observed in symptoms Significant improvement effect: Effective after the razor sharpness disappears: Effective after the razor sharpness disappears: Slightly effective after the razor sharpness has improved significantly: Razor sharpness has slightly improved Ineffective: No change is observed in the razor sharpness Judgment 0: Subject notices The percentage of subjects showing excellent, effective, and somewhat effective (effectiveness rate) is 80% or more O: The percentage of subjects showing excellent, effective, and somewhat effective (effectiveness rate) is 50 to 80% ×: The percentage of subjects showing excellent, effective, and somewhat effective The ratio showing effectiveness (effectiveness rate) is 50% or less Example 1-2 Table 2 (Amounts are weight %) (Hereinafter in the margin) (Hereinafter in the margin) The following Table 2 shows the H constant results.

Table 2 As is clear from Table 2, nicorandil is 0.0
At a concentration of 1 to 0.0001%, tanning showed an excellent improvement effect on hot flashes, rough skin, and razor burn after tanning.

Other examples are shown below, but as a result of the same actual test, it was found that sun tanning had an excellent improvement effect on later hot flashes, rough skin, and razor burn.

In addition, the blending amount is shown in weight%.

Example 3 Lotion (1) Nicorandil 0.0001 (2
) Glycerin 4.0 (3) 1.3-
Butylene glycol 4.0(4) Ethanol
7.0 (5) Polyoxyethylene (20
Mol) Oleyl Alcohol 0.5 (6) Methylparaben 0.05 (7) Citric #0.01 (8) Sodium Citrate 0.1 (9) Fragrance
0.01 (10) Purified water
The remaining manufacturing method is as follows.

First, glycerin, 1,3-butylene glycol, citric acid, and sodium citrate are dissolved in purified water.

Separately, nicorandil, polyoxyethylene (20 mol), oleyl alcohol, methyl paraben, and fragrance were dissolved in ethanol, added to the purified aqueous solution, dissolved, and filtered to obtain a lotion.

Example 4 Pack (1) Nicorandil o, oos (2
) Polyvinyl alcohol 15.0 (3) Polyethylene glycol 3.0 (4) Propylene glycol 7.0 (5) Ethanol
10.0(6) Methylparaben
0.05 (7) Fragrance 0.
05(8) Purified water The remaining manufacturing method is as follows.

First, polyethylene glycol, propylene glycol, and methylparaben are added to purified water and dissolved with stirring.

Next, polyvinyl alcohol was added and stirred with heating, and ethanol and nicorandil in which the fragrance had been dissolved were added and dissolved with stirring to obtain a bag.

Example 5 Solid white powder (1) Talc 85.4 (2)
Stearic acid 1.5 (3) Lanolin 5.0 (4) Squalane
5.0 (5) Sorbitan sesquioleate 2.0 (6) Triethanolamine 1.0 (7) Nicorandil 0.05 (8) Pigment
Appropriate amount (9) Fragrance
The appropriate amount manufacturing method is as follows.

First, talc and pigment are thoroughly mixed in a kneader (powder part).

Then, add triethanolamine to 50% equivalent amount of purified water and keep it at 70℃ (water phase). Mix other ingredients except fragrance and dissolve by heating (oil phase).
.

The oil phase is added to the water phase and uniformly emulsified using a homomixer, and this is added to the powder portion and kneaded using a kneader.The water is then evaporated and the mixture is processed using a pulverizer.

Stir this well in a colander and spray the fragrance evenly.
A solid white powder was obtained by compression molding.

[Effects of the Invention] Since the present invention is configured as described above, it produces the effects described below.

According to the claimed invention, since nicorandil or its salts are blended into the skin external preparation, skin disorders and physiological aging of the skin can be effectively prevented and improved.

Patent applicant: Shiseido Co., Ltd.

Claims (1)

[Claims] N-(2-hydroxyethyl)nicotinamide nitrate (generic name: nicorandil) represented by the following structural formula ▲ Numerical formula, chemical formula, table, etc. ▼ or its salts as an active ingredient External skin preparation.