JPH0920624A - Hair restorer - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a hair growing agent having a higher hair growing efficacy than that of the conventionally known hair growing agent by blending the extracted material of a specific crude drug with Minoxidil showing a hair growing efficacy albeit insufficient. SOLUTION: This hair growing agent is obtained by using Minoxidil together with the extracted material of Magnolia officinalis (also, M. obovata and M. var. biloba). It is preferable that the blending amount of Minoxidil is 0.1-2wt.% and that of the extracted essence of the Magnolia officinalis is 0.01-5wt.%. Minoxidil is a compound having a chemical name of 6-(1-piperidinyl)-2, 4- pyrimidinediamine-3-oxide and its medically acceptable salts. The extracted material of the Magnolia officinalis is obtained by cutting the bark of the Magnolia officinalis to a suitable size, preferably drying, crushing, then immersing the crushed bark into a water soluble solvent at a room temperature or under heating, sufficiently extracting and then filtering insoluble materials off. To use this hair growing agent for treatment or prevention of male-type dspilations, it is used as a usual preparation for external use such as a lotion and a tonic preparation.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a hair-growing agent containing a combination of minoxidil and an extract of Koboku.

[0002]

2. Description of the Related Art Heretofore, various techniques have been proposed and actually used for hair-growth agents used for promoting or maintaining the growth of human hair. However, none of them are satisfactory in both efficacy and safety, such as insufficient hair-growth action and skin irritation in terms of safety. An anti-androgen agent is a typical drug that has been developed for the purpose of using male pattern hair removal. However, many anti-androgen agents have a steroid skeleton, have other hormonal actions, and develop systemic side effects, and thus are generally problematic in terms of safety. In addition, it has a peripheral vasodilatory effect and has been used for the treatment of hypertension, minoxidil (Mino).
It was discovered that hirsutism was seen as a side effect of xidil), and it was proposed to use it as an external preparation for topical administration (US Pat. Nos. 4,139,619 and 4,5).
96, 812). However, for minoxidil, the hair-growing effect is still insufficient with an external preparation. Further, with respect to the other hair-growing agents, none of them has problems such as insufficient hair-growing effect, skin irritation and side effects.

[0003]

SUMMARY OF THE INVENTION An object of the present invention is to provide a hair restorer which satisfies both efficacy and safety.

[0004]

Means for Solving the Problems The inventors of the present invention have conducted extensive studies in view of the above-mentioned reasons, and as a result, it has been found that when minoxidil and the extract of Koboku are simultaneously blended, the respective hair-growth effects are synergistically enhanced. Found and completed the present invention.
That is, the present invention is a composition containing minoxidil and an extract of Aspergillus flavus.

Minoxidil is a compound whose chemical name is 6- (1-piperidinyl) -2,4-pyrimidinediamine-3-oxide or a pharmaceutically acceptable salt thereof. In addition, as a general rule, the magnolia family Magnolia obovata Thun
In many cases, the bark of b. b) is shown, but in the present invention, in addition to this, a carahou (M. officinalis) which is a plant belonging to the same family
Rehd. et Wils) or Yahazuhonoki (M. officinalis var. bilo).
ba Rehd. Bark of et Wils) can also be used.

[0006] Koboku is a crude drug used as an internal medicine in Kampo preparations mainly for the purpose of digesting stomach and antitussive and expectorant. Further, "12th Revised Japanese Pharmacopoeia Manual (Hirokawa Shoten)" describes nematicidal action, central depressant action, calcium influx inhibitory action, anti-gastric ulcer action, antibacterial action and the like of Koboku extract. However, it has not been known so far that the Koboku extract has a hair-growing effect.

[0007] The red bark used in the present invention is usually obtained by cutting the bark into an appropriate size and drying the bark, and the extract is obtained by the following method.

After the koboku is preferably dried and crushed,
Immerse in a water-soluble solvent at room temperature or under heating. After being sufficiently extracted, the insoluble matter is filtered to obtain an extract. If necessary, the extraction solvent can be distilled off and the residue can be used. Here, the water-soluble solvent includes alcohols such as methanol, ethanol, and isopropanol, ketones such as acetone, purified water, and a mixed solution of alcohol and purified water. Among these, alcohols or a mixed solution of alcohols and purified water is most preferable. The amount of the extraction solvent is preferably 2 to 5 times the dry weight of Koboku.

In the present invention, the amount of minoxidil compounded is preferably 0.1 to 2% by weight, more preferably 0.5 to 1% by weight, based on the whole preparation. Further, the amount of the extract of Komokubu extract is such that the amount of the extract obtained by distilling off the solvent of the extract is preferably 0.01 to 5% by weight, more preferably 0.1 to 1% by weight of the whole preparation. .

In order to use the hair restorer of the present invention for the treatment or prevention of male pattern hair loss, it is used as a usual external preparation such as lotion, tonic, cream, ointment and aerosol. These external preparations can be manufactured according to a conventional method using a commonly used base.

Depending on the purpose of use, these external preparations include vasodilators (carpronium chloride, benzyl nicotinate, cembly extract, ginseng extract, vitamin E acetate, capsicum tincture, etc.), adrenal cortex hormones (hydrocortisone acetate, propionate butyrate). Hydrocortisone, etc., anti-androgen agents (cyproterone acetate, finasteride, oxendron, spironolactone, etc.), antihistamines (diphenhydramine hydrochloride, isotipendyl hydrochloride, etc.), anti-inflammatory agents (glycyrrhetinic acid, guaiazulene, etc.), keratolytic agents (urea, salicylic acid, etc.) ), Bactericides (chlorhexidine gluconate, isopropylmethylphenol, quaternary ammonium salts, hinokitiol, piroctone olamine, etc.), moisturizers (hyaluro Sodium acid, glycerin,
Chondroitin sulfate, Cordyceps sinensis extract, saffron extract, etc.), oil (isopropyl myristate, lecithin,
Squalane, etc., surfactants (polyoxyethylene sorbitan fatty acid ester, sorbitan fatty acid ester,
Polyoxyethylene fatty acid ester, glycerin fatty acid ester, propylene glycol fatty acid ester, etc.), crude drug extract (Pleurotus cornucopia extract, yew extract, guarana extract etc.), polyhydric alcohol (propylene glycol, glycerin, macrogol etc.), anti An oxidizing agent (dibutylhydroxytoluene, isopropyl gallate, etc.), a sequestering agent (ethylenediaminetetraacetate or its salt, etc.), a cooling agent (menthol, camphor, etc.), a coloring agent, a fragrance, etc. are added unless the effects of the present invention are impaired. can do.

To use the hair-growth agent of the present invention for the treatment or prevention of male pattern baldness, it is usually applied to the scalp once or several times a day as an external preparation, and then applied in an appropriate amount.

[0013]

As is apparent from the test examples described below, the present invention makes it possible to provide a hair-growth agent having an excellent hair-growth effect.

[0014]

EXAMPLES The present invention will be described in more detail with reference to Examples and Comparative Examples.

Example 1 65 parts by weight of ethanol, 5 parts by weight of propylene glycol, 0.5 parts by weight of minoxidil, 70% ethanol extract of red syrup (70 parts by weight of bark of crushed honoki)
5% by weight of ethanol was added, the mixture was extracted at room temperature for 1 week, and then filtered through filter paper to obtain a filtrate. Hereinafter, Example 2,
The same in 3 and the test example. ) 5 parts by weight and 24.5 parts by weight of purified water were added and dissolved by stirring to prepare a lotion type hair restorer.

Example 2 To 47.7 parts by weight of purified water was added carboxyvinyl polymer 0.
4 parts by weight were dispersed with stirring. 40 parts by weight of ethanol, 1 part by weight of propylene glycol, 5 parts by weight of glycerin, 0.5 part by weight of minoxidil, 5 parts by weight of 70% ethanol extract of Koboku, and 0.4 parts by weight of diisopropanolamine were dissolved with stirring. The liquid was added and mixed with stirring to prepare a gel type hair restorer.

Example 3 Polyoxyethylene (20) sorbitan monostearate 5 parts by weight, sorbitan monostearate 3 parts by weight, cetanol 2 parts by weight, stearyl alcohol 2 parts by weight, liquid paraffin 10 parts by weight, vitamin E acetate 0. Two
Part by weight was mixed and dissolved while heating. Separately, 1 part by weight of minoxidil, 3 parts by weight of 70% ethanol extract of red syrup, 0.5 part by weight of pantotenyl ethyl ether, 0.1 part by weight of methyl paraoxybenzoate, 10 parts by weight of propylene glycol, 63.2 parts by weight of purified water. While heating the parts, a solution dissolved by stirring was added, and the mixture was stirred and cooled to room temperature to prepare a cream type hair restorer.

Example 4 0.5 part by weight of minoxidil and an absolute ethanol extract of red knotweed (3 parts by weight of absolute ethanol was added to 1 part by weight of crushed pine tree bark, extracted at room temperature for 1 week, and then filtered through a filter paper. The obtained filtrate. The same applies to Examples 5 and 6 below.) 8 parts by weight, hinokitiol 0.1 part by weight,
Assembly extract 0.1 part by weight, carrot extract 0.1 part by weight, glycyrrhetinic acid 0.2 part by weight, vitamin E acetate 0.02 part by weight, placenta extract 0.1 part by weight, L-menthol 0.2 part by weight, 1,3-butanediol 5 parts by weight, polyoxyethylene (60) hydrogenated castor oil 0.4 parts by weight, octyldodecyl myristate 1 part by weight, glyceryl monoisostearate 1 part by weight, ethanol 65 parts by weight and purified water 18 0.28 parts by weight was dissolved by stirring to prepare a lotion type hair restorer.

Example 5 0.5 part by weight of minoxidil, 5 parts by weight of an absolute ethanol extract of red knot, 5 parts by weight of propylene glycol, 5 parts by weight of polyoxyethylene (20) monooleate, 50 parts by weight of ethanol, 30.5 parts of purified water. Part by weight was dissolved by stirring. This liquid was put in an aerosol can and pressurized with 4 parts by weight of liquefied petroleum gas to prepare an aerosol type hair restorer.

Example 6 To 48.7 parts by weight of purified water was added carboxyvinyl polymer 0.
4 parts by weight were dispersed with stirring. To this, a solution prepared by stirring and dissolving 40 parts by weight of ethanol, 5 parts by weight of propylene glycol, 0.5 part by weight of minoxidil, 5 parts by weight of Mokko's absolute ethanol extract, and 0.4 parts by weight of diisopropanolamine was added and stirred. The mixture was mixed to prepare a gel type hair restorer.

Example 7 Minoxidil 0.5 part by weight and Konoboku's isopropanol extract (5 parts by weight of isopropanol was added to 1 part by weight of crushed pine tree bark, and the mixture was extracted at room temperature for 1 week.
It is the filtrate obtained by filtering with filter paper. The same applies to Example 8 below. 4 parts by weight, 1,3-butanediol 2 parts by weight, propylene glycol 4 parts by weight, polyoxyethylene (20) polyoxypropylene (6) decyltetradecyl ether 3 parts by weight, ethanol 55 parts by weight, purified water 31. A lotion type hair restorer was prepared by dissolving 5 parts by weight with stirring.

Example 8 0.5 part by weight of minoxidil, 5 parts by weight of an isopropanol extract of red knot, pantotenyl ethyl ether.
5 parts by weight, ethinyl estradiol 0.0008 parts by weight, glycyrrhetinic acid 0.2 parts by weight, vitamin E acetate 0.02 parts by weight, capsicum tincture 0.5 parts by weight,
1 part by weight of glyceryl monoisostearate, 5 parts by weight of propylene glycol, 1.5 parts by weight of polyoxyethylene (20) sorbitan monooleate, 70 parts by weight of ethanol, 15.792 parts by weight of purified water are dissolved by stirring to obtain a lotion type. A hair restorer was prepared.

Samples having the formulations of Examples 9 to 13 and Comparative Examples 1 to 3 shown in Table 1 were prepared in the same manner as in Example 1.

[0024]

[Table 1]

Test Example [Hair Growth Effect Test] Hair growth effect tests were carried out for Examples 9 to 13 and Control Examples 1 to 3. The test animals consisted of 10 C3H mice (male, 7 weeks old) as one group, and the animals in each group were hair-removed with a hair clipper in the area of 2 cm × 3 cm on the back of each group and used for the test.

For each sample, a different group of test animals was assigned, and the hair-removing part of the sample was 0.2 m once a day.
1 was applied. The hair color of the test animal is black, and the skin color of the hair removing part is gray.Since the color tone changes from gray to black with the growth of the hair, the degree of blackness of the hair color is And evaluated for hair growth. That is, a spectrocolorimeter (high-speed spectrophotometer CMS-1200, manufactured by Murakami Color Research Laboratory Co., Ltd.) was used, and the L ^* value a ^* of the test part immediately after hair removal based on the L ^* a ^* b ^* color system ^. The value b ^* value and ΔL ^* , Δa ^* , and Δb ^* of the test portion after 7 days and 15 days after the sample application were calculated,
The color difference ΔE ^* ab was obtained from the following formula, and the blackness of the hair color was shown by the average value of the 1 group.

[0027]

## EQU1 ## ΔE ^* ab = {(ΔL ^* ) ² + (Δa ^* ) ² + (Δ
b ^* ) ² } ^{1/2 In} addition, the degree of hair growth in the test area 7 days and 15 days after application of the sample was visually evaluated in the following 6 grades. Table 2 shows the above results.

* Judgment criteria in macroscopic evaluation 0: Hair growth is not recognized at all 1: Hair growth is present 2: Hair bristles are growing 3: Hair bristles grow about 50% of normal 4: Hair bristles About 75% of normal growth 5: About 100% of normal bristles grow

[0029]

[Table 2]

Claims (3)

[Claims] 1. A hair restorer containing an extract of minoxidil and pearl syrup. 2. The content of minoxidil is 0.1 to 2% by weight.
And the amount of the extract of Koboku is 0.01 to 5
2. The hair restorer according to claim 1, which is present in a percentage by weight. 3. The hair restorer according to claim 1, which is an external preparation.