JP3314785B2 - Minoxidil-containing hair restorer - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a hair restorer whose hair growth effect is enhanced by using minoxidil in combination with a saffron extract or a sanshishi extract.

[0002]

2. Description of the Related Art Various hair restorers have been known.
These have disadvantages such as insufficient hair-growth effect and skin irritation.

[0003]

SUMMARY OF THE INVENTION An object of the present invention is to provide a hair restorer which has an excellent hair restorer effect and has no skin irritation.

[0004]

Means for Solving the Problems The present inventors have conducted intensive studies and as a result, when minoxidil is used in combination with a specific crude drug extract,
The present inventors have discovered that a synergistic effect of the hair restorer action of the crude drug extract and minoxidil is produced, and a hair restorer having excellent hair restorer effect and less skin irritation can be obtained. That is, the present invention is a hair restorer containing (a) minoxidil and (b) saffron extract or sanshishi extract as active ingredients.

The saffron extract can be obtained, for example, by extracting dried saffron stigma and the upper part of the style with ethyl alcohol or an aqueous solution of ethyl alcohol. The Sanshishi extract can be obtained by, for example, extracting a gardenia fruit with ethyl alcohol or an ethyl alcohol aqueous solution. The compounding amount of the saffron extract or the sanshishi extract is, for example, a tincture of a crude drug extracted with a 30% ethyl alcohol aqueous solution (refer to the one prescribed in the Japanese Pharmacopoeia, the 12th revision. The same applies hereinafter. Extracted with 5 g) is 0.5 to 20% by weight, preferably 1 to 10% by weight, based on the total amount of the preparation. The amount of minoxidil is 0.05 to 2.0% by weight, preferably 0.2 to 1.0% by weight, based on the total amount of the preparation.

In the hair restorer of the present invention, if necessary, anti-inflammatory agents (glycyrrhetinic acid, guaiazulene, etc.), peripheral vasodilators (tocopherol acetate, benzyl nicotinate, panax ginseng extract, assembly extract, capsicum extract, etc.) ), Corticosteroids (hydrocortisone acetate, betamethasone valerate, hydrocortisone butyrate propionate, etc.), antihistamines (diphenhydramine hydrochloride, isothibenzyl hydrochloride, etc.), local anesthetics (dibucaine hydrochloride, lidocaine hydrochloride, etc.), keratolytic agents (urea) , Salicylic acid, etc.), vitamin preparations (vitamin E acetate, retinol acetate, retinal, retinoic acid, etc.), estrogen (17β-estradiol, estrone, etc.), progesterone (progesterone, 17α-
Hydroxyprogesterone acetate, etc.), antiandrogens (cybroterone acetate, 4-androsten-3-one-17β-carboxylic acid, etc.),
Humectants (propylene glycol, glycerin, diglycerin, etc.), solvents (ethyl alcohol, isopropyl alcohol, 1,3-butanediol, purified water, etc.), preservatives (parabens, etc.), oils (liquid paraffin, cetyl alcohol, squalane) , Olive oil, etc.), disinfectants (sulfur, chlorhexidine gluconate, isopropylmethylphenol, quaternary ammonium salts, hinokitiol, etc.), surfactants (polyoxyethylene sorbitan fatty acid ester, polyoxyethylene fatty acid ester, glycerin mono fatty acid ester, Propylene glycol monofatty acid ester, polyoxyethylene hydrogenated castor oil derivative, etc.), gelling agent (methylcellulose, hydroxypropylcellulose, carboxyvinyl polymer, etc.), pH
Modifiers (such as diisopropanolamine), antioxidants (such as dibutylhydroxytoluene), cooling agents (such as 1-menthol and camphor), fragrances, sequestering agents, ultraviolet absorbers, dyes, and the like impair the effects of the present invention. It can be blended in a range that does not exist.

The hair restorer of the present invention can be prepared in the form of lotions, emulsions, creams, gels, aerosols and the like according to commonly used methods (for example, the method prescribed in the 12th revised Japanese Pharmacopoeia). The administration method and dosage of the hair restorer of the present invention are performed by applying an appropriate amount to the scalp once to several times a day.

[0008]

Industrial Applicability According to the present invention, it has become possible to provide a hair restorer which has an excellent hair restorer effect and has less skin irritation.

[0009]

The present invention will be described below in more detail with reference to examples and test examples. Example 1 65 parts by weight of ethyl alcohol, 5 parts by weight of propylene glycol, 0.5 part by weight of minoxidil, saffron extract [extracted with a 30% aqueous solution of ethyl alcohol, tincture of stigma and upper part of style of saffron (extraction of saffron) (Extracted with 5 g of solvent for 1 g of product). Hereinafter, the same applies to Examples 2 and 3 and Test Examples. ] 5
Parts by weight and 24.5 parts by weight of purified water were added and dissolved by stirring.
A lotion type hair restorer was prepared.

Example 2 45 parts by weight of ethyl alcohol, 5 parts by weight of saffron extract and 5 parts by weight of 1,3-butanediol were mixed and dissolved, and 0.7 part by weight of a carboxyvinyl polymer was dispersed therein. Minoxidil 0.5
Parts by weight and 43.1 parts by weight of purified water were added and dissolved. 0.7 parts by weight of diisopropanolamine was added to this solution, and the mixture was stirred and mixed to prepare a gel type hair restorer.

(Example 3) 5 parts by weight of glycerin monostearate, 2 parts by weight of isopropyl myristate, 5 parts by weight of liquid paraffin, 4 parts by weight of polyoxyethylene (20) sorbitan monostearate, propylene glycol monoisostearate 4 Parts by weight, 2 parts by weight of cetyl alcohol, 2 parts by weight of stearyl alcohol, 0.2 parts by weight of vitamin E acetate, 0.1 parts by weight of hinokitiol, 0.2 parts by weight of glycyrrhetinic acid and 5 parts by weight of saffron extract are stirred while heating. And dissolved. In advance, 1 part by weight of minoxidil, 7 parts by weight of propylene glycol, 0.1 part by weight of ethyl paraoxybenzoate and purified water
A solution obtained by stirring and dissolving 4 parts by weight of the solution was added to the solution, and mixed by stirring to prepare a cream type hair restorer.

Example 4 0.5 parts by weight of minoxidil
Saffron extract [The extract of saffron stigma and upper part of the style extracted with 30% ethyl alcohol aqueous solution (No. 1
2 Refers to those prescribed in the revised Japanese Pharmacopoeia. same as below. )
It is. Hereinafter, the same applies to the fifth embodiment. 5 parts by weight, β
0.0008 parts by weight of estradiol, 0.2 parts by weight of hinokitiol, 0.2 parts by weight of glycyrrhetinic acid, 0.1 parts by weight of vitamin E acetate, 55 parts of ethyl alcohol
Parts by weight, 5 parts by weight of polyethylene glycol 400, 5 parts by weight of glycerin monoisostearate and 0.3 part by weight of 1-menthol were dissolved by stirring. A solution obtained by previously stirring and dissolving 4 parts by weight of polyoxyethylene (20) polyoxypropylene (6) decyltetradecyl ether and 24.7 parts by weight of purified water is added to the above solution, and mixed by stirring to obtain a lotion-type hair growth. An agent was prepared.

(Example 5) Polyoxyethylene (20)
3 parts by weight of sorbitan monooleate, 5 parts by weight of propylene glycol, 15 parts by weight of ethyl alcohol, 0.5 parts by weight of minoxidil, 5 parts by weight of saffron extract and 67.5 parts by weight of purified water were mixed and dissolved by stirring. This was put in an aerosol can, and 4 parts by weight of liquefied petroleum gas was charged under pressure to prepare an aerosol-type hair restorer.

(Example 6) 70 parts by weight of ethyl alcohol, 5 parts by weight of propylene glycol, 0.5 part of minoxidil
Parts by weight, Sanshishi extract [Tined tincture of gardenia fruit extracted with a 30% aqueous solution of ethyl alcohol (extracted with 5 g of solvent for 1 g of gardenia extract). Hereinafter, the same applies to Examples 7 and 8 and Test Examples. ] 5
Parts by weight and 19.5 parts by weight of purified water are added and dissolved by stirring.
A lotion type hair restorer was prepared.

Example 7 45 parts by weight of ethyl alcohol, 1 part by weight of minoxidil, 0.5 part by weight of Sanshishi extract, 5 parts by weight of 1,3-butanediol, and 47.
1 part by weight was added and dissolved by stirring, and after dispersing 0.7 part by weight of a carboxyvinyl polymer, 0.7 part by weight of diisopropanolamine was added and stirred and mixed to prepare a gel type hair restorer. .

Example 8 5 parts by weight of glycerin monostearate, 2 parts by weight of sorbitan monostearate, 2 parts by weight of isopropyl myristate, 13 parts by weight of liquid paraffin, 4 parts by weight of polyoxyethylene (20) sorbitan monooleate Propylene glycol monoisostearate 4 parts by weight, cetyl alcohol 2 parts by weight, stearyl alcohol 2 parts by weight, vitamin E acetate 0.2 parts by weight, hinokitiol 0.1 parts by weight, glycyrrhetinic acid 0.2 parts by weight and Sanshishi extract 1 part by weight The mixture was stirred and dissolved while heating. A solution obtained by previously stirring and dissolving 1 part by weight of minoxidil, 7 parts by weight of propylene glycol, 0.2 parts by weight of ethyl paraoxybenzoate and 56.3 parts by weight of purified water was added to the above solution, and the mixture was stirred and mixed. A cream type hair restorer was prepared.

(Example 9) 0.5 parts by weight of minoxidil,
Sanshishi extract (1% by weight of gardenia fruit extract extracted with 30% ethyl alcohol aqueous solution. The same applies to Example 10 below), 0.0008 part by weight of β-estradiol, 0.2 part by weight of hinokitiol,
Glycyrrhetinic acid 0.2 parts by weight, vitamin E acetate 0.1 parts by weight, assembly extract 1 part by weight, cepharanthin 0.02 parts by weight, ethyl alcohol 70 parts by weight, polyethylene glycol 400 5 parts by weight, glycerin monoisostearate 1 part by weight And 0.3 part by weight of 1-menthol and 0.5 part by weight of a fragrance were dissolved by stirring. in advance,
4 parts by weight of polyoxyethylene (20) polyoxypropylene (6) decyltetradecyl ether, purified water 1
A solution obtained by stirring and dissolving 6.18 parts by weight was added to the solution, followed by stirring and mixing to prepare a lotion-type hair restorer.

Example 10 Polyoxyethylene (2
0) 3 parts by weight of sorbitan monooleate, 5 parts by weight of propylene glycol, 15 parts by weight of ethyl alcohol, 0.5 parts by weight of minoxidil, 1 part by weight of Sanshishi extract and 71.5 parts by weight of purified water were mixed and dissolved by stirring. This was put into an aerosol can, and 4 parts by weight of liquefied petroleum gas was charged under pressure to prepare an aerosol-type hair restorer.

(Test Example)

[Hair growth effect test]

(1) Preparation of Test Samples Samples 1 to 8 and Control Sample 1 were prepared according to the formulation shown in Table 1 in accordance with the preparation method of Example 1. In addition, the sixth embodiment
Samples 9 to 16 and Control Sample 2 were prepared according to the formulation shown in Table 2 according to the preparation method described in Table 1.

[0020]

[Table 1]

[0021]

[Table 2]

(2) Test Animals Ten C3H mice (male, 7 weeks old) were grouped into one group, and the animals of each group were subjected to hair removal using a clipper in the area of 2 cm × 3 cm on the back of the animals. . (3) Test Method Separate groups of test animals were allocated to each of Samples 1 to 16 and Control Samples 1 and 2, and 0.2 ml of the test animal was applied to the depilated portion once a day. The color of the hair of the test animal is black, and the color of the skin at the depilated part is gray, and the color tone changes from gray to black as the hair grows. And hair growth was evaluated.
That is, a spectral colorimeter (high-speed spectral colorimeter CMS-120)
Type 0, manufactured by Murakami Color Research Laboratory)

[0023]

[Outside 1] The color difference DE ^* ab value was determined from the formula, and the average value of a group of the values indicated the blackness of the hair color.

Further, the degree of hair growth of the test portion 10 days and 20 days after application of the sample was visually evaluated by the following six grades. Table 3 shows the results. Twenty days after the application of the sample, the hair of the test portion in a range of 2 cm × 2 cm was clipped with a clipper, and the weight was measured to determine the amount of hair growth by the sample.

[0025]

[2] Hair growth (mg) and color difference DE ^* obtained in the previous section
FIG. 1 shows the relationship of ab.

From this figure, it can be seen that the two are clearly proportional. * Judgment criteria in the visual evaluation 0: Hair growth is not recognized at all 1: Hair is growing 2: Hard hair is fully grown 3: Hard hair is growing about 50% of normal 4: Hard hair is normal 75% grow 5: Hard hair grows about 100% of normal.

[0027]

[Table 3]

[Brief description of the drawings]

FIG.

1 is a graph showing the relationship between the amount of hair growth and the color difference DE ^* ab.

────────────────────────────────────────────────── ─── Continued on the front page (51) Int.Cl. ⁷ Identification code FI A61P 17/14 A61P 17/14 (72) Inventor Takako Okajima 3-24-1, Takada, Toshima-ku, Tokyo Taisho Pharmaceutical Co., Ltd. 72) Inventor Masami Nemoto 3-24-1, Takada, Toshima-ku, Tokyo Taisho Pharmaceutical Co., Ltd. (56) References JP-A-58-88307 (JP, A) JP-A-2-48514 (JP, A) Kaihei 2-121911 (JP, A) (58) Fields investigated (Int. Cl. ⁷ , DB name) A61K 7/00 A61K 7/06 A61K 31/506 A61K 35/78 A61P 17/14

Claims (1)

(57) [Claims] 1. A hair restorer comprising (a) minoxidil and (b) saffron extract or sanshishi extract as active ingredients.