JPH10265343A - Long-acting hair restorer - Google Patents

Abstract

(57) [Summary] [Problem] To provide a sufficient hair-growth effect in an external preparation containing minoxidil by retaining the absorbed minoxidil in the dermis and increasing the concentration of minoxidil around the hair bulb as a hair growth point. Provide a hair restorer obtainable. SOLUTION: Minoxidil and dipropylene glycol are blended, and when diluted 20 times with purified water, the pH is 4
Long-acting hair restorer, characterized in that it is from 9 to 9.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a hair restorer containing minoxidil as an active ingredient.

[0002]

BACKGROUND OF THE INVENTION 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.

[0003] Conventionally, a minoxidil-containing hair restorer has to be applied several times a day, so that it is complicated, so that the application may be forgotten and a sufficient hair restorer effect may not be obtained.

[0004]

DISCLOSURE OF THE INVENTION The present inventors have studied to improve the hair-growth effect of minoxidil. The improvement of the hair-growth effect of minoxidil is not only enhanced by percutaneous absorption but also by absorption. It has been found that it is necessary that the minoxidil obtained stays in the dermis.

It is an object of the present invention to provide an external preparation containing minoxidil in which the absorbed minoxidil is retained in the dermis and the concentration of minoxidil around the hair bulb, which is the growth point of the hair, is increased for a long time. An object of the present invention is to provide a hair restorer capable of obtaining a sufficient hair restore effect by single administration.

[0006]

The present inventors have found that, as a result of research, when dipropylene glycol is added to a hair restorer containing minoxidil as an active ingredient and the pH is adjusted to a range of 4 to 9, minoxidil is converted into dermis. The present invention was found to be a long-lasting hair growth agent that is maintained for a long time in the inside, and completed the present invention.

[0007] That is, the present invention is a long-lasting hair restorer comprising minoxidil and dipropylene glycol and having a pH of 4 to 9.

[0008]

BEST MODE FOR CARRYING OUT THE INVENTION The present invention can be applied to 0.1 to 10% by weight of a preparation, which is a general amount of minoxidil.

In the present invention, the compounding amount of dipropylene glycol is preferably 5 to 40% by weight. If the amount is less than 5% by weight, the effect of retaining minoxidil in the dermis is not sufficient, and if it is more than 40% by weight, the feeling of use in the preparation becomes poor.

Furthermore, in the present invention, the preparation is purified with purified water for 20 minutes.
The pH of the double dilution is preferably from 4 to 9, and more preferably from 5 to 8. If the pH of the preparation is out of this range, the retention effect of minoxidil in the dermis decreases, and skin irritation occurs.

The hair restorer of the present invention can shorten the time to reach the maximum intradermal concentration (Tmax) when 1,3-butylene glycol or propylene glycol is added to the preparation. Further, at least one polar solvent selected from 2-hexyl-1-decanol, isooctadecanol, glycerin dicaprate, glycerin dicaprylate, glycerin monoisostearate, and propylene glycol monoisostearate in the preparation Can extend the residence time of minoxidil in the skin. That is, the amount of application, the number of applications, and the like can be controlled by combining these compounding agents.

In the present invention, when 1,3-butylene glycol or propylene glycol is blended, the amount is preferably 0.1 to 10 parts by weight, more preferably 0.1 to 10 parts by weight, per 1 part by weight of dipropylene glycol. ~ 5
Parts by weight. If the amount is less than 0.1 part by weight, the effect of accelerating Tmax is hardly exhibited, and if the amount exceeds 10 parts by weight, the effect of retaining minoxidil in the dermis is weakened. Further, at least one polar solvent selected from 2-hexyl-1-decanol, isooctadecanol, glycerin dicaprate, glycerin dicaprylate, glycerin monoisostearate, and propylene glycol monoisostearate in the preparation Is preferably 0.005 to 5 parts by weight, more preferably 0.01 to 2 parts by weight, based on 1 part by weight of dipropylene glycol. 0.005
If the amount is less than parts by weight, the effect of extending the residence time of minoxidil cannot be expected, and if it is added in an amount of 5 parts by weight or more, the maximum intradermal concentration becomes low, and the hair growth effect is weakened.

In the present invention, excipients, vasodilators (carpronium chloride, benzyl nicotinate, assembly extract, panax ginseng extract,
Vitamin E acetate, pepper tincture, etc.), antihistamines (diphenhydramine hydrochloride, isotipendyl hydrochloride, etc.), anti-inflammatory agents (glycyrrhetinic acid, guaiazulene, etc.), keratolytic agents (urea, salicylic acid, etc.), fungicides (chlorhexidine gluconate, isopropylmethylphenol) , Quaternary ammonium salts, hinokitiol, pyrocton olamine, etc.), moisturizers (sodium hyaluronate, chondroitin sulfate, etc.), various animals and plants (yew, buttonpi, licorice, hypericum, batsushi,
Extracts of loquat, pearl mugwort, comfrey, ashitaba, saffron, sanshishi, rosemary, sage, mock, mushroom, potato, hop, placenta, etc., vitamins (retinol acetate, pyridoxine hydrochloride, ascorbic acid, thiamine nitrate, cyanocobalamin, biotin, etc.) ), Water, lower alcohols (methanol, ethanol,
Denatured ethanol, isopropyl alcohol, etc.), antioxidants (dibutylhydroxytoluene, sodium pyrosulfite, tocopherol, sodium edetate, ascorbic acid, isopropyl gallate, etc.), dissolution aids (diisopropyl adipate, isopropyl myristate, polyethylene glycol, etc.) Medium-chain fatty acid triglycerides, fatty acid esters, various vegetable oils, various animal oils, polyhydric alcohol fatty acid esters, alkyl glyceryl ethers, hydrocarbons, lactic acid, sodium hydroxide, etc.), metabolic activators (panthenol, etc.), surfactants ( Sorbitan fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, propylene glycol fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene Nsorubitto fatty acid ester,
Polyoxyethylene glycerin fatty acid ester, polyethylene glycol fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene alkyl phenyl ether, polyoxyethylene hydrogenated castor oil,
Polyoxyethylene castor oil, polyoxyethylene beeswax derivative, polyoxyethylene lanolin derivative, polyoxyethylene alkylamide, polyoxyethylene alkylamine, lecithin derivative, polymer emulsifier, etc.),
Emulsion stabilizers (higher alcohols, etc.), gelling agents (water-soluble polymers, etc.), adhesives, fragrances, fresheners (menthol,
Commonly used components such as peppermint oil and camphor) and dyes can be blended within a range that does not impair the effects of the present invention.

When water or a lower alcohol is mixed with the above-mentioned hair restorer, water is preferably 0.5 to 30% by weight, and ethyl alcohol or isopropyl alcohol is preferably mixed as a lower alcohol at 50 to 90% by weight. .

The hair restorer of the present invention can be used in external preparations such as creams, ointments, aerosols, lotions and tonics.

[0016] The long-acting hair restorer of the present invention comprises one to several days.
It is used by transdermally administering an appropriate amount.

[0017]

Industrial Applicability According to the present invention, it has become possible to provide a long-lasting hair restorer for retaining minoxidil in the dermis.

[0018]

The present invention will be described more specifically with reference to the following examples and test examples.

Example According to the formulation shown in Table 1, minoxidil and dipropylene glycol were mixed with other components, the total amount was made up to 100 ml with absolute ethanol and purified water, and the mixture was stirred and dissolved to prepare a lotion type external preparation for medicine. did.

[0020]

[Table 1]

Test Example 1 Minoxidil blood concentration and dermal content Male Wistar rats (7 weeks old) were dehaired and fixed in a dorsal position under ether anesthesia, and a fixed area of the abdomen (2 × 4
cm), 40 μl of each of the lotions shown in Table 1 were applied. Blood was collected from the thoracic vein every predetermined time (1, 2, 4, 6, 8, 12, 24 hours), and the concentration of minoxidil in the blood was measured with a liquid scintillation counter.
Table 2 shows changes in blood concentration. Furthermore, in order to measure the minoxidil content in the dermis, the rat was decapitated and sacrificed, the surface of the lotion application area was washed with ethanol, the skin was excised, and a clear adhesive tape was applied strongly to the entire epidermis,
This was wrapped in a food protection wrap and immersed in a 60 ° C. warm bath for 60 seconds. After cooling to stand, the tape was peeled off to remove the remaining drug and the epidermal layer from the skin, and the weight of the remaining dermis and the amount of minoxidil in the dermis were measured to determine the amount of minoxidil per 1 g of dermis. Table 3 shows changes in the dermal concentration.

[0022]

[Table 2]

[0023]

[Table 3]

As is clear from the results shown in Tables 2 and 3, the lotion preparations of the present invention suppressed the diffusion of minoxidil in blood and increased the dermal content for a long time as compared with the comparative examples. Effect was observed.

Test Example 2 Hair growth test A group of 10 C3H mice (male, 7 weeks old) was used as a group, and a 2 × 3 cm area on the back of each animal in each group was shaved with a clipper and subjected to a test. A separate group of animals was assigned to each of the formulations in Table 1 and its hair removed once daily.
Each 0.2 ml was applied.

The hair of the animal used in the test was black and the skin color of the depilated portion was brown, and the color tone changed from gray to black with the growth of the hair. 0: No hair growth is observed by the naked eye, 1: Hair is growing, 2: Hard hairs are fully grown, 3: Hard hairs grow about 50% of normal, 4: Hard hairs Were grown in about 70% of normal and 5: Hard hair was grown in almost 100% of normal. The results are shown in Table 4.

[0027]

[Table 4]

As is clear from Table 4, it was confirmed that all of the preparations of the present invention exhibited a higher degree of hair growth than the comparative examples.

 ──────────────────────────────────────────────────続 き Continued on the front page (72) Inventor Shigeo Tanaka 3-24-1, Takada, Toshima-ku, Tokyo Inside Taisho Yaku Co., Ltd.

Claims (8)

[Claims] Claims: 1. Minoxidil and dipropylene glycol are blended, and the formulation is diluted 20 times with purified water.
H is 4 to 9, and a long-acting hair restorer. 2. The compounding amount of minoxidil is 0.1% of the whole preparation.
The long-acting hair restorer according to claim 1, wherein the amount is 1 to 10% by weight. 3. The long-acting hair restorer according to claim 1, wherein the amount of dipropylene glycol is 5 to 40% by weight of the preparation. 4. At least one polar solvent selected from the group consisting of 2-hexyl-1-decanol, isooctadecanol, glycerin dicaprate, glycerin dicaprylate, glycerin monoisostearate, and propylene glycol monoisostearate. The long-acting hair restorer according to any one of claims 1 to 3, further comprising: 5. The long-acting hair restorer according to claim 4, wherein the amount of the polar solvent is 0.005 to 5 parts by weight per 1 part by weight of dipropylene glycol. 6. The hair restorer according to claim 1, further comprising at least one polyhydric alcohol selected from 1,3-butylene glycol and propylene glycol. 7. The long-acting hair restorer according to claim 6, wherein the amount of at least one polyhydric alcohol selected from 1,3-butylene glycol and propylene glycol is 0.1 to 10% by weight of the preparation. . 8. The compounding amount of at least one polyhydric alcohol selected from 1,3-butylene glycol and propylene glycol with respect to 1 part by weight of dipropylene glycol is 0.1 to 10 parts by weight. 3. A long-acting hair restorer according to item 1.