JPH0232007A - Hair tonic - Google Patents

Abstract

PURPOSE:To obtain a hair tonic showing more excellent preventing effects on hair removal and tonic effects on hair than existing same kinds of cosmetics by blending a hair tonic with N-(2hydroxyethyl)nicotinic acid amide nitrate ester or a salt thereof as an active ingredient. CONSTITUTION:A hair tonic is blended with 0.001-10wt.%, preferably 0.01-5wt.%, N-(2-hydroxyethyl)nicotinic acid amide nitrate ester (general name: nicorandil) or a salt thereof well-known as a remedy for angina pectoris as an active ingredient. When the blend is used for ordinary people, 0.0001-20mg, preferably 0.001-2mg of the active ingredient is percutaneously applied (directly applied to the skin or scattered) once or 2-4 times dividedly to give a hair tonic having specific preventing effects on hair removal and tonic effects on hair.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to a novel hair nourishing agent containing nicorandil as an active ingredient.

[Prior Art] Conventionally, the causes of baldness and hair loss include activation of male hormones in various chambers such as hair roots and sebaceous glands, decreased blood flow to hair follicles, excessive secretion of sebum, production of peroxide, and bacteria. Scalp abnormalities due to breeding, genetic factors, neurosis due to stress, etc.
It is thought to be secondary to disease and aging.

For this reason, conventional hair growth agents generally contain compounds that have the effect of eliminating or alleviating the above-mentioned causes.

On the other hand, nicorandil has a coronary vasodilatory effect and an inhibitory effect on coronary artery constriction, and is an effective drug for treating various types of angina pectoris with little effect on cardiovascular dynamics and cardiac function. issue.

JP-A No. 53-9323).

[Protecting the country that the invention seeks to solve 1 Despite the above-mentioned attempts, the mechanism of hair loss and hair growth is extremely complex, and it is difficult to simply inhibit the activation of male hormones or to inhibit the growth of hair follicles. Simply increasing blood flow cannot sufficiently prevent baldness and hair loss.

In view of the above circumstances, the present inventors have conducted intensive research to obtain a substance that has an effective preventive effect against hair loss, and as a result,
We have discovered a novel fact that nicorandil has a hair-nourishing effect, and have completed the present invention based on this knowledge.

[Means and effects for solving the problems] That is, the gist of the present invention is a hair nourishing agent containing nicorandil as an active ingredient. The present invention will be explained in more detail below.

Nicorandil in the present invention was invented and developed in Japan (
Hiroyuki Nagano Haka1 98th Abstracts of the Pharmaceutical Society of Japan, 232.1
978) It is a drug for treating angina pectoris. Many reports have been made regarding its pharmacological effects on the circulatory system, but it has been reported that administration of doses 100 times or more of the clinical dose showed mild changes in the central nervous system and renal function. Of course, it is not known that it has a hair-nourishing effect, although it has only been reported.

As used herein, "hair nourishing effect" or "hair nourishing effect" means prevention of hair loss, promotion of caterpillars and hair growth, and hair growth.

The hair growth agent of the present invention is used in the form of a mixture containing pharmaceutically acceptable additives and other drugs in addition to nicorandil.

Examples of the additives include hinokitiol, hexachlorophene, phenol, benzalkonium chloride,
Antibacterial agents such as cetylpyridinium chloride, undecylenic acid, trichlorocarbanilide and bithionol, derivatives such as glycyrrhizinic acid and its ammonium salts, anti-inflammatory or cooling agents such as allantoin and menthol, salicylic acid, zinc and its compounds, lactic acid and its alkyl Drugs such as esters, animal and vegetable oils such as olive oil, macadamia nut oil, and squalane, hydrocarbon oils such as liquid paraffin, ester oils such as isopropyl myristate, cetyl isooctanoate, and 2-ethylhexyl palmitate, and beeswax. Waxes such as, higher fatty acids, oils such as higher alcohols, water, derivatives such as lactic acid and its ethyl ester, polyhydric alcohols such as polyethylene glycol, glycerin, sorbitol, lower alcohols such as ethanol, mucopolysaccharides, pyrrolidone carboxylic acid Moisturizing agents such as salt, surfactants, fragrances, antioxidants, ultraviolet absorbers,
Examples include pigments, and these may be used alone or in combination of two or more.

The dosage form of the hair tonic of the present invention may be any form as long as it can be used externally, such as liquid preparations for external use such as lotions, liniments, milky lotions, semi-solid preparations for external use such as creams, ointments, pasta, jelly, sprays, etc. can be mentioned.

The hair tonic of the present invention contains 0 nicorandil as an active ingredient.
．． 001-10% by weight, preferably 0.01-5% by weight
Contains within the range of .

The hair growth agent of the present invention is administered by transdermal administration, in which it is directly applied or sprayed onto the skin. Furthermore, the dosage of the hair tonic of the present invention cannot be clearly defined as it varies depending on age, individual differences, medical conditions, etc.; however, in general, when targeting humans, the transdermal dosage of nicorandil is based on body weight I kg and 0.0001-20 mg per day preferably o,ooi-2
mg, and this amount can be administered once every 10 times or divided into 2 to 4 times.

EXAMPLES Below, the formulation method of the hair growth agent and the hair growth effect according to the present invention will be specifically explained with reference to Examples. Note that the present invention is not limited to this.

1 Kogo-yo- A lotion having the following composition was prepared.

(Weight%) 95% ethanol 80.0 nicorandil 0.1 hinokitiol
0.01 Ethylene oxide adduct of hydrogenated castor oil 0.5 (40 mol) Purified water 19.0 Fragrance and pigment Appropriate amount of nicorandil, hinokitiol, ethylene oxide (40 mol) adduct of hydrogenated castor oil, fragrance and pigment in 95% ethanol. Then, purified water was added to obtain a transparent liquid lotion.

1"]"u [1 animal In order to investigate the hair-growth effect of the hair-growth agent of the present invention, a tricogram test and a trial of terminal hair conversion rate were conducted. In both trials, 20 male subjects were divided into two groups of 10 subjects each, and two different test solutions were given to the subjects in each group for comparison.

Two types of test solutions are shown in Table 1.

0 kg of hair roots were removed per subject and examined immediately after and before placement. The results are shown in Table 2.

applied to the scalp of a person.

(1) Trichogram Observe the removed hair roots before and after using both test solutions above under a microscope, calculate the number of telogen hair roots from the morphology of the hair roots, and calculate the difference between the two test solutions by increasing or decreasing the ratio. We compared the hair growth effects of A telogen hair root is a hair root that has stopped growing. People who complain of hair loss have more telogen hair roots than normal people, so the hair-nourishing effect was evaluated based on the decrease in telogen hair roots. Each trial! ! ! The solution was continued to be applied to the scalp for 3 months, and (2) Hair conversion rate test was applied to the down hair area of each of the 40 subjects with androgenetic alopecia.
The conversion rate of downy hair to fluff was compared before and after application of each of the above test solutions. Fluff refers to hair other than downy hair, that is, long hair of 14 mm or more, and the conversion from downy hair to downy hair means a hair-nourishing effect. Immediately after application of each test solution and immediately after completion of the 4-month application, close-up photographs of the above-mentioned down hair region of the head were taken to measure the conversion rate. The conversion rate to fluff is expressed as a percentage of the average of the three locations. The results are shown in Table 3.

The average value of conversion rate was calculated. The results of the hair regeneration surface chain after 28 days are shown in Table 4 as a percentage.

(3) Measurement of hair growth effect (method using mice) Male C3H
Using mice (50 days old), Ogawa et al.'s method (M, 5e
Edited by iji et al., Norm-al and Abn
normal Epide-rmal Differ
The experiment was conducted in accordance with the publication published by the University of Tokyo Press. The backs of the mice were shaved into a large piece of about 2 x 4 cm, and the sample was applied once a day from the next day. Changes in the area ratio of the area where hair regeneration had started were determined and the speed of hair regeneration was compared. Nicorandil was dissolved in 90% ethanol.

90% ethanol was used as a control in the test. Each group 1
Using 0 mice each, it was found that nicorandil exhibits an excellent hair growth effect, as is clear from the results above average.

Examples of the ponds are shown below, and as a result of similar practical tests, all of them showed excellent effects on hair loss prevention and hair growth.

Moreover, the present invention is not limited to this.

SJJL-21 Hair Tonic (% by weight) Nicorandil 0.1 Lauryl dimethylamine oxide 0.5 Sodium lauryl sulfate Propylene glycol Sodium hyaluronate Fragrance 75% Ethanol Hair Tonic Nicorandyl Polyoxyethylene (8 mol) Oleyl Alcohol Ether 1.3-Butylene Glycol Fragrance 60% Ethanol Uragengo-Kouichi Shampoo Nicorandyl Cocoyl Methyl Taurine Sodium Lauryl Dimethyl Amino Acetate Betaine Lauric Acid Jetanolamide Ethylene Glycol Fatty Acid Ester 0 .05 5.0 0.01 Proper amount remaining (li amount%) 0.01 0.05 0.05 Proper amount remaining (weight%) 0.05 1.0 8.0 4.0 1.5 Propylene glycol edetic acid 2 Sodium Flavor Purified Water 1 已发IL-5, Rinse Nicorandyl Skearyl Trimethyl Ammonium Chloride Cetyl Alcohol Silicone Oil Polyoxyethylene (10 mol) Oleyl Alcohol Ether Glycerin Purified Water Preservative Ultraviolet Absorber 2.0 0.1 Appropriate amount remaining (weight) %) 0.001 2.0 2.0 3.0 1.0 5.0 84.0 Appropriate amount Appropriate amount (hereinafter referred to as the margin) [Effects of the invention] Since the present invention has been configured as described above, the following will be explained below. It produces the effects described.

According to the claimed invention, since nicorandil is blended into the hair growth agent, the hair growth prevention effect and hair growth effect are significantly greater than that of conventional cosmetics of the same type.

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 Hair nourishing agent.