JPS6284012A - Hair tonic - Google Patents

Abstract

PURPOSE:A hair tonic containing a 4-androstene-3-one-17beta-carboxylic acid alkyl ester and a telangiectatic agent for the skin, having synergistic effects. CONSTITUTION:A safe hair tonic containing 0.0001-2wt%, preferably 0.0001-0.2wt% 4-androstene-3-one-17beta-carboxylic acid alkyl ester and 0.0001-5wt%, especially preferably 0.01-3wt% telangiectatic agent for the skin (e.g., carpronium chloride, minoxidil, spironolactone, vitamin B6 hydrochloride, etc.,), a substance to increase hair nourishing effect synergistically, free from side effects. Solution, milky lotion, ointment for the exodermis, etc., may be applied as the form.

Description

[Detailed description of the invention] C industrial application field] The present invention relates to a hair nourishing agent having excellent hair nourishing effects.

[Prior Art] Physiological symptoms such as male-pattern baldness and seborrhea are said to be due to increased stimulation of male hormones due to excessive accumulation of male hormones. The main body of this male hormone activity is 5α-dihydrotestosterone (hereinafter referred to as 5α-DHT), which is produced by reducing testosterone (male hormone) in these target organs by an enzyme called testosterone-5α-reductase (hereinafter referred to as reductase). ) is becoming well known. That is, testosterone produced in the adrenal glands and the adrenal glands travels through the bloodstream to the sebaceous glands, where it is converted into 5α-DHT, a more powerful male hormone, by reductase in the sebaceous gland cells. This 5α-
DHT binds to intracellular receptors and acts on the nucleus to promote the proliferation of sebaceous gland cells, while DHT itself exits the sebaceous gland cells and enters the bloodstream, acting on the hair matrix cells and stimulating the growth of the hair matrix in the hair bulb. It is said to suppress cell division, inhibit hair growth, and promote hair pulling and hair loss.

[Problems to be Solved by the Invention] Therefore, symptoms such as male pattern baldness and hair loss can be reduced or prevented by inhibiting the activity of reductase and the binding of 5α-DHT to receptor proteins. Based on this viewpoint, substances such as chlormadinone acetate, oleic acid, and linoleic acid have been discovered so far. However, even though these substances have a high inhibition rate of reductase activity, they have undesirable side effects, and their inhibition rate of binding between 5α-DHT and receptor protein is very low, so they are inferior to the actual hair growth effect. There was a drawback.

[Means for Solving the Problems] In view of the above circumstances, the present inventors have developed a method that does not have undesirable side effects such as hormonal effects, is safe, inhibits reductase activity, and inhibits 5α-DHT and receptor protein. 4-Androsten-3-one-1
It has been found that the above object can be achieved by blending one or more types of 7β-carboxylic acid alkyl esters (Japanese Patent Application Laid-Open No. 184114/1983). This time, as a result of further research, we found that 4-androsten-3-one-17
The present inventors have discovered that by combining one or more β-carboxylic acid alkyl esters with one or more skin peripheral vasodilators, the effects can be synergistically increased, leading to the completion of the present invention. .

That is, the present invention provides 4-androsten-3-one-1
This hair nourishing material contains one or more 7β-carboxylic acid alkyl esters and one or more skin peripheral vasodilators.

Hereinafter, the configuration of the present invention will be explained in detail.

The blending amount of 4-androsten-3-one-17β-carboxylic acid alkyl ester is 0.00 in the hair nourishing material of the present invention.
01-2% by weight is preferred. Particularly preferably 0.000
It is 1 to 0.2% by weight. If the amount is less than 0.0001% by weight, the hair nourishing effect may not be exhibited. Further, the higher the amount, the greater the hair-nourishing effect, but considering the occurrence of unexpected side effects when used in large amounts, the amount is preferably 2% by weight or less.

In the present invention, the skin peripheral vasodilators, which are substances that synergistically increase the hair-nurturing effect, include carpronium chloride, minoxidil, spironolactone, vitamin B6 hydrochloride, cephalanthine (Tamasa Kidzurafji extract), D-camphor, DL-camphor, DL-α-tocopherol, iodized garlic extract, DL-α-tocopherol lyric acid ester, Jasmine japonica extract, inositol hexanicotinic acid ester, vitamin E1 dextran sodium sulfate, nicotinic acid, DL-α-tocopherol nicotinic acid ester, nicotine Butoxyethyl acid, γ-oryzanol, benzyl nicotinate, methyl nicotinate, vanillyl nonanoate, DL-α-tocopherol succinate,
These include DL-α-tocopherol acetate, capsicum tincture, cantharis tincture, and ginger tincture, as well as cephalanthine (Tamasakidzurafuji extract), DL-α-
Tocopherol, iodized garlic extract, Jasmine japonica extract, DL-α-tocopherol nicotinic acid ester, benzyl nicotinate, nonanoic acid vanillylamide, DL acetate
-α-tocopherol, capsicum tincture, cantharis tincture, ginger tincture, etc. are preferred.

The compounding amount of the skin peripheral vasodilator is 0.0001 to 5% by weight.
is preferable, particularly preferably 0.01 to 3.0% by weight
It is. If it is less than 0.0001% by weight, the hair nourishing effect may not be exhibited, and even if it exceeds 5% by weight, no further hair nourishing effect may be expected.

The hair nourishing material according to the present invention includes the above-mentioned 4-androstene-3.
In addition to -one-17β-carboxylic acid alkyl ester and skin peripheral vasodilator, additives commonly used in hair growth materials,
For example, antibacterial agents such as hinokitiol, hexachlorophene, phenol, benzalkonium chloride, cetylpyridinium chloride, undecylenic acid, trichlorocarbanilide and bithionol, cooling agents such as menthol, salicylic acid, zinc and its derivatives, lactic acid and its alkyl esters. Drugs such as olive oil, squalane,
Oils such as liquid paraffin, isopropyl myristate, higher fatty acids, higher alcohols, other surfactants, fragrances, antioxidants, ultraviolet absorbers, pigments, ethanol, water, humectants, thickeners, etc. are effective in the present invention. It can be blended as appropriate within a range that does not impair the properties.

The hair growth material of the present invention may be in any form as long as it can be applied to the outer skin, such as liquid, emulsion, or ointment.

The hair nourishing material according to the present invention is 4-androsten-3-one-
The 17β-carboxylic acid alkyl ester and the skin peripheral vasodilator, which dilates the peripheral blood vessels of the scalp and promotes an increase in blood flow, act effectively to exert a synergistic hair-nourishing effect.

[Example] Next, the present invention will be explained in detail with reference to Examples. The present invention is not limited thereby. The blending amount is in weight%.

The test method will be explained in Examples below.

■Hair Shyness 1 Judgment was made based on the change in the number of strands removed during hair washing before and after using the main sample. There were 10 subjects in each of the seven groups of Examples 1 to 6 and Comparative Example 1. The measurement period is 4 months, and the first two
The first month was the period when no sample was applied, and the second half of the second month was the period when the sample was applied. During this period, the hair was washed every two days and the pulled hair was collected, and the number of hairs for one week was counted. To display the number of hairs pulled out for each period, data on the number of hairs pulled out 8 times in 2 months without sample application and data on the number of hairs pulled out 8 times in 2 months with hair tonic applied are summarized for each period, and the average is calculated. Value ±
The number of hairs pulled per session was expressed in the form of α. The unit is a book. The effectiveness was determined based on the difference between the average values for each period as shown below.

++: The number of hair-pulled trees decreased by 70 or more, and a remarkable effect was observed.

+: The number of hairs pulled was reduced by 40 or more, indicating a considerable effect.

±: The number of hairs pulled was reduced by 10 or more, indicating that it was somewhat effective.

-: The reduction in the number of hairs pulled is less than 10, and it cannot be said that there is an effect.

Example 1.2, Comparative Example 1 (Production method) 4-androsten-3-one-1 in 95% ethanol
7β-carboxylic acid methyl ester, benzyl nicotinate, and hydrogenated castor oil E○ (40 mol) adduct were added, stirred and dissolved, and then ion-exchanged water was added and mixed to produce the transparent liquid hair growth of Example 1. I got the material. Example 2 and Comparative Example 1 were also obtained in the same manner as Example 1.

All of the above results show that the hair nourishing agent of the present invention containing 4-androsten-3-one-17β-carboxylic acid alkyl ester and a skin peripheral vasodilator is different from the conventionally known 4-androsten-3-one-17β- This shows that the hair nourishing effect is synergistically superior to hair nourishing products containing carboxylic acid alkyl esters.

Example 3 (Phase A) 4-androsten-3-one-17β-carboxylic acid ethyl ester 2.0 Oriental japonica extract 3.0 Polyoxyethylene (60 mol) Hydrogenated castor oil 2,0 Glycerin
7.0 Dipropylene glycol 8.4 1.3-Butylene gelicol 5.0 Polyethylene glycol 1500
5.0 (Phase B) Cetyl isooctanate 10.0 Squalane 5.0 Vaseline
2.0 Propylparaben
2.0 (C phase) Carboxyvinyl polymer 1% aqueous solution 30.0 Sodium hexametaphosphate 0.03 Ion exchange water 8.95 (D phase) Ion exchange water 4.5 (E phase) Caustic potash 0.12 Ion exchange water 5.0 (Manufacturing method) Phase A and phase B are respectively heated and dissolved at 60°C, mixed and treated with a homomixer to form a gel. Phase D is gradually added to this and dispersed using a homomixer.

Next, the dissolved phase C was added thereto, and finally the dissolved phase E was added and emulsified with a homomixer to obtain an O/W emulsion type hair nourishment.

When this hair nourishing agent was subjected to a practical use test in the same manner as in Example 1.2, it was confirmed that its hair nourishing effect was excellent.

Example 4 (Phase A) 4-androsten-3-one-17β-carboxylic acid propyl ester 0.14-androsten-3-one-17β-carboxylic acid pentyl ester 0.1 Cephalanthine 5.0 Liquid paraffin 5. 0 Cetostear alcohol 5.1 Glyceryl monostearate
3.0 EO (20 mol) -2-octyldodecyl ether 3.0 Propylparaben 0.3 Fragrance
0.1 (Phase B) Glycerin 8.0 Dipropylene glycol 20.0 Polyethylene glycol 4000 5.0 Sodium hexametaphosphate 0.005 Ion exchange water
45.295 (Manufacturing method) Phase A and phase B were respectively heated and dissolved, mixed, and emulsified with a homomixer to obtain an ointment-like hair nourishing agent.

When this hair nourishing agent was subjected to a practical use test in the same manner as in Example 3, it was confirmed that its hair nourishing effect was excellent.

Example 5 Ethanol 55.0 4-androsten-3-one-17β-carboxylic acid hebutyl ester 0.000
1DL-α-tocopherol nicotinic acid ester 0.0IEO (
8 mol) Oleyl alcohol ether 2.0 Hinokitiol 0.05 Fragrance
0.1 dye
0.0899 ion exchange water
42.75 (Production method) Add EO (8 mol) oleyl alcohol ether, 4-androsten-3-one-17β-carboxylic acid hebutyl ester, DL-α-tocopherol nicotinic acid ester, and hinokitiol to ethanol; After adding and dissolving perfume and dye, ion-exchanged water was added to solubilize to obtain a hair nourishing agent.

Example 6 4-androsten-3-one-17β-carboxylic acid methyl ester 0.2 g, ginger tincture 0.000
1g1 liquid paraffin 5.0g, cetostearyl alcohol 5.5g, Vaseline S, 5g, glyceryl monostearate 3.0g, EO (20 mol)-2-octyldodecyl ether 3.0g, propylparaben 0.2g
, and 0.1 g of fragrance were dissolved and mixed by heating. to this,
Glycerin 7.0g, dipropylene glycol 20.0
g, 5.0 g polyethylene glycol 4000,
A hot melt mixture of 0.005 g of sodium hexametaphosphate and 45.4949 g of ion-exchanged water was added and emulsified in a homomixer to obtain a cream-like hair nourishing agent. The obtained hair nourishing agent showed an excellent hair nourishing effect.

[Effects of the Invention] The hair nourishing agent of the present invention is a highly safe hair nourishing agent that has an excellent hair nourishing effect, is locally effective, has no systemic effects, and is less irritating to the skin. It is.

Claims (1)

[Claims] A hair nourishment containing one or more 4-androsten-3-one-17β-carboxylic acid alkyl esters and one or more skin peripheral vasodilators.