JPH10218736A - Hair grower - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a hair grower which manifests an excellent hair growing acting with a low concentration of minoxidil by blending two specific substances. SOLUTION: This hair grower contains 0.1 to 2wt.% of minoxidil as well as a local retention agent and a polar solvent. A preferable local retention agent includes epinephrine, ephedrine, tetrahydrozoline, naphazoline, etc., and the salts thereof. Its amount of blending is preferably 0.0001 to 5wt.%. A preferable polar solvent includes propylene glycol,1,3-butylene glycol, dipropylene glycol, glycerol monoisostearate, etc., and is blended in an amount of 0.5 to 20wt.%. This hair grower manifests a sufficient effect even with a low concentration of minoxidil as its is retained in the scalp.

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]

As a result of various studies, the present inventors have found that a hair restorer containing minoxidil, a local retention agent and a polar solvent has a low concentration of minoxidil because minoxidil is retained in the scalp. The present inventors have found that a sufficient hair growth effect is exhibited, and completed the present invention.

That is, the present invention is a hair restorer comprising 0.1 to 2% by weight of minoxidil, a local retention agent and a polar solvent.

[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.

In the present invention, the local retention agent is a drug having an effect of retaining minoxidil in the dermis, which is an action site, that is, a drug having an effect of delaying blood flow in the dermis. Examples include ephedrine, tetrahydrozoline, naphazoline, phenylephrine, methylephedrine and the like, and salts thereof can also be used. Especially tetrahydrozoline,
It is preferable to use naphazoline, phenylephrine or salts thereof since the skin retention effect and the hair growth effect are good. Here, the salts are not particularly limited as long as they can be blended with the external preparation for skin, but preferred examples include salts with hydrochloric acid, sulfuric acid, nitric acid and the like.

The amount of the local retention agent is 0.1% of the whole preparation.
0001-5% by weight, preferably 0.001-1% by weight
It is.

[0013] If the amount is less than 0.0001% by weight, the effect of the drug on the skin is not sufficient, and if the amount exceeds 5% by weight, it becomes difficult to design the formulation due to the balance with other components. .

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,
At least one kind of polar solvent comprising 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, is required. This is because the absence of a polar solvent reduces the permeation of minoxidil through the skin. As the polar solvent, an ester compound or 1
Valent alcohols are 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.

The compounding amount of the polar solvent in the present invention is 0.1 to 30% by weight, preferably 0.5 to 20% by weight of the whole preparation. If it is less than 0.1% by weight, the effect of staying on the skin is not sufficient, and if it exceeds 30% by weight, the balance with other components 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, emulsion, suspension, tonic, cream, ointment, aerosol or the like according to a conventional method.

As long as the effects of the present invention are not impaired, 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,
Fungicides such as quaternary ammonium salts, hinokitiol, and pyroctone olamine; moisturizing agents such as sodium hyaluronate, glycerin, and chondroitin sulfate; yew, buttonpi, licorice, hypericum, bonito, loquat, valerium, comfrey, ashitaba, saffron , Sansin, rosemary, sage, mock, mock, hop,
Plant and plant extracts such as placenta, vitamins such as retinol acetate, pyridoxine hydrochloride, ascorbic acid, thiamine nitrate, cyanocobalamin, biotin, tocopherol acetate, oils such as squalane, liquid paraffin, lecithin, and interfaces such as polyoxyethylene hydrogenated castor oil Activator, menthol, essential oil components such as camphor, dibutylhydroxytoluene, antioxidants such as isopropyl gallate, sequestering agents such as ethylenediaminetetraacetate or a salt thereof, pigments, fragrances and the like within a range that does not impair the effects of the present invention. Can be blended.

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

[0021]

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

[0022]

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

Examples The hair restorers of the examples shown in Tables 1 to 3 were prepared by a conventional method. The minoxidil used was labeled with ¹⁴ C.

[0024]

[Table 1]

[0025]

[Table 2]

[0026]

[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)
To m ² ), 40 μl of the hair restorer of Example and Comparative Example was applied, and 1 hour later, 200 μl of blood was collected from the thoracic vein.
Minoxidil concentration in blood was measured with a liquid scintillation counter. The results are shown in Table 4.

[0028]

[Table 4]

As is clear from the table, it was revealed that the present invention can suppress the absorption of minoxidil into the whole body.

Test Example 2 Intradermal concentration of minoxidil Hair from the abdomen of male Wistar rats (7 weeks old) was removed, and hair growth agents 1 of Examples and Comparative Examples were placed in a fixed area (2 cm ² ).
0 μl was applied. After a certain period of time (1, 24 h), the rats were killed by cervical dislocation, and the drug-applied area was washed with ethanol. Thereafter, the ethanol was removed, the abdominal skin was removed, and a transparent adhesive tape was strongly adhered to the entire surface, wrapped with 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.
Minoxidil in the skin was measured by a liquid scintillation counter, and the result was determined as the amount of minoxidil retained per gram of skin. Table 5 shows the results.

[0031]

[Table 5]

As is clear from the table, it was found that minoxidil stayed in the skin for a long time according to the present invention.

Test Example 3 The hair tonic of the patient to an embodiment of the six hair growth effect male pattern baldness (30-40 years of age) 16 (not ¹⁴ C label goods) was applied to the treatment to all scalp. After three months, all six patients had good hair growth.

 ────────────────────────────────────────────────── ─── 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 (7)

[Claims] 1. A hair restorer comprising 0.1 to 2% by weight of minoxidil, a local retention agent and a polar solvent. 2. The content of the local retention agent is 0.0001 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, wherein the polar solvent is 0.5 to 20% by weight. 4. The hair restorer according to claim 1, wherein the local retention agent is at least one of epinephrine, ephedrine, tetrahydrozoline, naphazoline, phenylephrine, methylephedrine and salts thereof. 5. The hair restorer according to claim 1, wherein the local retention agent is at least one of tetrahydrozoline, naphazoline, phenylephrine and salts thereof. 6. A polar solvent having a melting point of 37 ° C. or lower 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 any one of claims 1 to 5, which is one or more kinds selected from alcohols. 7. 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.