JPH10218737A - Hair grower - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a hair grower having an efficient hair growing effect with a low content of minoxidil. SOLUTION: This hair grower contains 0.1 to 2wt.% of minoxidil and at least one kind of crude drug extract selected from the following: (1) Lithospermum officinale L., (2) Angelica tuhou Radix, (3) Ephedra sinica Stapf, (4) Zingiber officinale Roscoe, (5) Rehmannia glutinosa Libos., (6) Zanthoxylum piperitum, (7) Scutellaria baicalensis Georgi, (8) Ginkgo biloba L., (9) Sophora japonica L. (100 Tyhae pollen.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a hair restorer containing minoxidil.

[0002]

2. Description of the Related Art Minoxidil has a chemical name of 6- (1-piperidinyl) -2,4-pyrimidinediamine-3-oxide, and its application as a hair restorer is described in U.S. Pat. No. 4,139,619. A hair restorer containing minoxidil is used worldwide and is used for treating alopecia.

[0003] Conventionally, various techniques for promoting percutaneous absorption of minoxidil have been proposed for the purpose of increasing the hair growth effect when minoxidil is used as an external preparation.

[0004]

DISCLOSURE OF THE INVENTION The present inventors have found that when minoxidil is administered as an external preparation, the percutaneously absorbed minoxidil is absorbed and diffused into the body without staying in the affected area, and therefore, a hair growth effect is exhibited. Was found to be inefficient.

[0005] Therefore, it has been considered that if minoxidil is percutaneously absorbed and stays in the skin at the applied portion, a sufficient hair-growth effect can be obtained even with a small amount of minoxidil.

[0006] It is an object of the present invention to provide a hair-growth agent which can efficiently exhibit a hair-growth effect with a small amount of minoxidil.

Conventionally, attempts have been made to promote the percutaneous absorption of minoxidil, but since hair growth agents generally aim at promoting blood circulation in the scalp, there is no idea that the absorbed drug will remain in the dermis. That was not possible.

[0008]

Means for Solving the Problems As a result of intensive studies, the present inventors have found that a hair restorer containing minoxidil and an extract of a certain crude drug allows minoxidil to efficiently stay in the scalp and has a low concentration of minoxidil. It has been found that a sufficient hair growth effect is exhibited. In addition, the inventor has further found that when a certain kind of polar solvent is further blended, the effect of minoxidil on the skin is further improved, thereby completing the present invention.

That is, the present invention relates to 0.1% to 2% by weight of minoxidil and purple root (silicon), lonely (dokatsu), mahuang (maoh), ginger (shokyo), ground yellow (jiou) and sansho (sansho). It is a hair restorer containing at least one extract of a crude drug selected from the group consisting of, pentagon, ginkgo, Ginkgo biloba, and kaohou.

[0010]

BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, the amount of minoxidil is 0.1 to 2% by weight of the whole preparation. If the amount of minoxidil is less than 0.1% by weight, the hair growth effect is not sufficient, and if the concentration is higher than 2% by weight, a sufficient hair growth effect can be expected without using the present invention.

The crude drug extract used in the present invention is an extract of a crude drug having an effect of retaining minoxidil in the dermis or a dried product thereof. Preferred crude drugs include purple root (silcon), indigenousness (dokatsu), mahuang (ephedra), ginger (shokyo), ground yellow (jiou), sansho (sansho),
Ogun, ginkgo (Ginkgo), Sophora (Kaika), kabuki (Gourd) and the like can be mentioned, and these crude drugs can be used in organic solvents (eg, ethanol) and water-containing organic solvents (eg, 30 to 7).
A crude drug extract can be obtained by an ordinary method such as extraction with 0 vol% ethanol or water (dry weight of crude drug: solvent weight = 1: 2 to 5). As the extract used in the present invention, a crude extract may be used as it is, or a dry extract may be used.

In the present invention, the blending amount of the crude drug extract is 0.1 to 50% by weight, preferably 1 to 50% by weight, based on the total amount of the preparation in terms of the crude drug. If the amount is less than 0.1% by weight, the effect of staying on the skin is not sufficient, and if the amount exceeds 50% by weight, the formulation design becomes difficult.

In the present invention, the composition has a melting point of 37.
C. or lower, preferably 25 C. or lower, and an ester compound having a total carbon number of 10 to 40, preferably 12 to 34,
It is preferable to add at least one polar solvent composed of a monohydric alcohol having 8 to 24 carbon atoms, preferably 12 to 20 carbon atoms, or a dihydric alcohol having 3 to 8 carbon atoms, because the permeation of minoxidil through the skin is improved. As the polar solvent, an ester compound or a monohydric alcohol is particularly preferred.

As the ester compound satisfying the condition as a polar solvent, an ester of a monovalent or divalent carboxylic acid having 6 to 18 carbon atoms and a monovalent to trivalent alcohol having 3 to 20 carbon atoms is preferable. 1 that satisfies the conditions as a solvent
As the monovalent alcohol, those having a branched chain are particularly preferable.

Among the polar solvents, particularly preferred ester compounds include glycerin monoisostearate, propylene glycol monoisostearate, isopropyl myristate, octidodecyl myristate, isopropyl palmitate, diisopropyl adipate and the like. Particularly preferred monohydric alcohols are 2-hexyl-1-decanol, isooctadecanol and cis-9-octadecene-.
1-ol and the like can be mentioned. Further, preferred dihydric alcohols include propylene glycol,
Examples thereof include 1,3-butylene glycol and dipropylene glycol.

When the polar solvent is blended in the present invention, the blending amount is 0.1 to 30% by weight, preferably 0.5 to 30% by weight of the whole preparation.
-20% by weight. If the amount is less than 0.1% by weight, the effect of staying on the skin is not sufficiently improved, and if the amount is more than 30% by weight, the balance with other ingredients is poor, and the formulation design becomes difficult.

The external preparation for skin of the present invention can be produced in a usual form, for example, a lotion, an emulsion, a suspension, a tonic, a cream, an ointment, an aerosol or the like according to a conventional method.

Further, antihistamines such as diphenhydramine hydrochloride and isopendyl hydrochloride, anti-inflammatory agents such as glycyrrhetinic acid and guaiazulene, keratolytic agents such as urea and salicylic acid, chlorhexidine gluconate, isopropylmethylphenol, quaternary ammonium salts, hinokitiol, pyro Bactericides such as cuton olamine, sodium hyaluronate, glycerin, chondroitin sulfate, 1,3
Moisturizers such as butylene glycol and dipropylene glycol, and fauna and flora such as yew, buttonpig, licorice, hypericum perforatum, fushi, loquat, valerium, comfrey, ashitaba, saffron, sanshin, rosemary, sage, mockup, seimokko, hop, placenta Extracts, vitamins such as retinol acetate, pyridoxine hydrochloride, ascorbic acid, thiamine nitrate, cyanocobalamin, biotin, and tocopherol acetate, oils such as squalane, liquid paraffin, lecithin, surfactants such as polyoxyethylene hydrogenated castor oil, menthol, Essential oil components such as camphor, antioxidants such as dibutylhydroxytoluene and isopropyl gallate, sequestering agents such as ethylenediaminetetraacetate or its salts, dyes and fragrances The components to be blended in agent can be added in amounts not detrimental to the effect of the composition of the present invention.

The hair restorer of the present invention is used by applying an appropriate amount to the scalp once or several times a day.

[0020]

Industrial Applicability According to the present invention, it has become possible to provide an effective hair restorer.

[0021]

The present invention will be described in detail below with reference to examples and test examples.

Example 1 10 parts by weight of propylene glycol, 1 part by weight of minoxidil, and a 70% ethanol extract of makoto (20 parts by weight of ethanol, 5 parts by weight of 70% ethanol were added to 1 part by weight of malt, and extracted at room temperature for one week) Thereafter, 20 parts by weight of a filtrate (filtrate obtained by filtration through filter paper) was added, and the total amount was adjusted to 100 ml with purified water, followed by stirring and dissolving to obtain a lotion type hair restorer. The minoxidil used was labeled with ¹⁴ C.

Examples 2 to 11 Hair growth agents were prepared in the same manner as in Example 1 except that the makoto in Example 1 was changed to the following crude drugs. The extract was prepared in the same manner as in the crude drug extraction method in Example 1.

Example 2: Shikon, Example 3: Independence, Example 4: Mao, Example 5: Ginger, Example 6: Ground yellow, Example 7: Sansho, Example 8: Ogon, Example 9: Ginkgo , Example 10: Sophora, Example 11: Kaoh Comparative Example 1 A lotion was prepared in the same manner as in Example 1, except that the crude drug of Example 1 was omitted.

Examples Examples 12 to 30 were prepared in accordance with the formulations shown in Tables 1 to 3 by a conventional method.
Also, the liquid preparations of Comparative Examples 2 and 3 were produced.

[0026]

[Table 1]

[0027]

[Table 2]

[0028]

[Table 3]

Test Example 1 Minoxidil blood concentration Wistar rats (7 weeks old) Male abdomen was dehaired, fixed in a dorsal position under ether anesthesia, and abdominal fixed area (2 × 4c)
m ² ) was applied with 40 μl of the hair restorer shown in Examples 1 to 30 and Comparative Examples 1 to 3, and 1 hour later, blood 2 was injected from the thoracic vein.
00 μl was collected and the blood concentration of minoxidil was measured.
Minoxidil concentration in blood was measured with a liquid scintillation counter. The results are shown in Table 4.

[0030]

[Table 4]

The blood concentration one hour after the application was significantly reduced when the crude drug was added, as compared with the hair restorer not added. Therefore, it was clarified that the absorption of minoxidil into the whole body can be suppressed by blending a crude drug having a local retention effect.

Test Example 2 Intradermal concentration of minoxidil Hair-growth agents (Examples 1 to 3) were prepared in a fixed area (2 cm ² ) by removing hair from the abdomen of male Wistar rats (7 weeks old).
0, Comparative Examples 1 to 3) 10 μl was applied. After a certain time (1, 24 h), the rats were sacrificed by cervical dislocation, and ethanol was poured into the application parts to wash the application parts. After washing, the ethanol was removed, the abdominal skin was excised, and a transparent adhesive tape was strongly adhered to the entire surface, wrapped in a food protection wrap, and immersed in a 60 ° C. warm bath for 60 seconds. After leaving to cool, the transparent adhesive tape was peeled off to remove the epidermal layer from the skin, and the weight of the specimen was measured. The amount of minoxidil in the skin was measured with a liquid scintillation counter, and the amount of minoxidil retained per gram of skin was determined. Table 5 shows the results.

[0033]

[Table 5]

The incorporation of a crude drug having a local retention effect significantly increased the intradermal concentration both 1 hour and 24 hours after application.

Test Example 3 Hair Restoration Effect The hair restorer of Example 1 (not ¹⁴ C-labeled) was applied to all the scalp once a day after bathing in 6 subjects (30s to 40s) with male pattern baldness. As a result of confirming the hair growth effect after 3 months, 5 out of 6 subjects showed good hair growth and one was unchanged.

 ────────────────────────────────────────────────── ─── Continuing on the front page (72) Inventor Susumu Morioka 3- 24-1, Takada, Toshima-ku, Tokyo Taisho Pharmaceutical Co., Ltd. (72) Inventor Shigeo Tanaka 3- 24-1, Takada, Toshima-ku, Tokyo Taisho Pharmaceutical Co., Ltd.

Claims (4)

[Claims] (1) 0.1 to 2% by weight of minoxidil and
A hair restorer comprising at least one of the following crude drug extracts: (1) Shikon, (2) Dokatsu, (3) Ephedra, (4) Ginger, (5) Giochi, (6) Sansho, (7) Giant gourd, (8) Ginkgo, (9) Kaika, (10) Kaohou 2. The hair restorer according to claim 1, further comprising a polar solvent. 3. A polar solvent having a melting point of 37 ° C. or less and an ester compound having a total of 10 to 40 carbon atoms, a monohydric alcohol having a total of 8 to 24 carbon atoms or a dihydric alcohol having a total of 3 to 8 carbon atoms. The hair restorer according to claim 2, which is one or more kinds selected from alcohols. 4. The polar solvent is propylene glycol, 1,3
-Butylene glycol, dipropylene glycol, glycerin monoisostearate, propylene glycol monoisostearate, isopropyl myristate, octidodecyl myristate, isopropyl palmitate, diisopropyl adipate, 2-hexyl-1-decanol, isooctadecanol , Cis-
The hair restorer according to any one of claims 1 to 5, which is at least one member selected from the group consisting of 9-octadecene-1-ol.