JPS6284015A - Hair tonic - Google Patents

Abstract

PURPOSE:A hair tonic having synergistic effects, containing a 4- androsten-3,17-one-17beta-ethoxy derivative and a telangiectatic agent. CONSTITUTION:A hair tonic containing 0.0001-2wt%, especially preferably 0.0001-0.2wt% compound [e.g., 17beta-(2-hydroxyethoxy)-4-androsten-3-one, etc.,] shown by the formula [R is -CH2OH, -CH2OCOX (X is 1-5C alkyl or phenyl), -CH2Y (Y is F, Cl, Br or I), -CH2CN, etc.,) and 0.0001-5wt%, especially preferably 0.01-3.0% telangiectatic agent for the skin (e.g., carpronium chloride, minoxidil, vitamin B6 hydrochloride, etc.,). Solution, milky lotion, ointment, etc., may be used as the form. EFFECT:The compound shown by the formula and the telangiectatic agent for the skin for dilating peripheral blood vessels of the scalp and for promoting increase in the amount of blood steam act effectively and have synergistic effects.

Description

[Detailed description of the invention] [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 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, enters the bloodstream, enters the hair matrix cells, and is absorbed into the hair matrix at the hair bulb. It is said to suppress cell division, inhibit hair growth, and promote hair pulling and hair loss.

[Problem to be solved by the invention 1 Therefore, symptoms such as male pattern baldness and hair loss can be reduced or prevented by inhibiting reductase activity and the binding of 5α-DHT to receptor protein. 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 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 7β-ethoxy derivatives (Japanese Patent Application Laid-open No. 6O-81121). This time, as a result of further research, we found that by combining one or more 4-androsten-3-one-17β-ethoxy derivatives with one or more skin peripheral vasodilators, the effect can be enhanced. The present invention was completed based on the discovery that this effect increases synergistically.

That is, the present invention is characterized by containing one or more 4-androsten-3-one-17β-ethoxy derivatives represented by the following general formula and one or more skin peripheral vasodilators. It is a hair nourishing material.

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

4-androsten-3-one-1 used in the present invention
7β-ethoxy derivatives are represented by the following general formula, and the chemical names are 17β-(2-hydroxyethoxy)-4-androsten-3-one, 17β-(2-
hydroxyethoxy)-4-androsten-3-one acetate, 17β-(2-hydroxyethoxy)-
4-androsten-3-one butyrate, 17β-
(2-hydroxyethoxy)-4-androstene-3
-one p-toluenesulfonate, 17β-(2-
Hydroxyethoxy)-4-androsten-3-one Methanesulfonate, 17β-(2-chloroethoxy)-4-androsten-3-one, 17β-(2-
iodoethoxy)-4-androsten-3-one, 1
7β-carboxymethoxy-4-androstene-3-
17β-carboxymethoxy-4-androsten-3-one methyl ester, 17β-(2-cyanoethoxy)-4-androsten-3-one, 17β-
(2-piperidinoethoxy)-4-androstene-3
-one, 17β-[2-((tetrahydrobilane-2-
yl)oxy)ethoxy]-4-androstene-3-
On, etc.

The amount of the 4-androsten-3-one-17β-ethoxy derivative in the hair nourishing material of the present invention is preferably 0.0001 to 2% by weight. Particularly preferably 0.0001 to 0.2
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, 7-oryzanol, benzyl nicotinate, methyl nicotinate, panillylamide nonanoate, DL-α-tocopherol succinate,
ft-acid DL-α-tocopherol, capsicum tincture,
Cantharis tincture, ginger tincture, etc., cephalanthine (Tamasakidzurafuji extract), DL-α
-Tocopherol, iodized garlic extract, Jasmine japonica extract, DL-α-tocopherol nicotinic acid ester,
Benzyl nicotinate, vanillyl nonanoate, acetic acid D
L-α-tocopherol, capsicum tincture, cantharis tincture, ginger tincture and the like are preferred.

The compounding amount of the skin peripheral vasodilator is 0.0001 to 5% by weight.
is preferred, particularly preferably 0.01 to 3.0% by weight. If it is less than 0.0001% by weight, it may not be able to exhibit a curing effect, and even if it exceeds 5% by weight, it may not be possible to expect any further hair-nourishing effect.

The hair nourishment according to the present invention includes the above-mentioned 4-androstene-3.
In addition to -one-17β-ethoxy derivatives and skin peripheral vasodilators, additives commonly used in hair care products, such as hinokitiol, hexachlorophene, phenol, benzalkonium chloride, cetylpyridinium chloride, undecylenic acid, and trichlorocarbanilide. and antibacterial agents such as bithionol, coolants such as menthol, drugs such as salicylic acid, zinc and its derivatives, lactic acid and its alkyl esters, oils such as olive oil, squalane, liquid paraffin, isopropyl myristate, higher fatty acids, higher alcohols, etc. Surfactants, fragrances, antioxidants, ultraviolet absorbers, pigments, ethanol, water, humectants, thickeners, and the like can be appropriately blended within the range that does not impair the effects of the present invention.

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

The hair nourishing agent according to the present invention is 4-androsten-3-one-
The 17β-ethoxy derivative 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.

-'l-' Judgment was made based on the change in the number of hair removed during hair washing before and after using the 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.

(Left below) Example 1.2, Comparative Example 1 (Production method) 17β-(2-hydroxyethoxy)-4-androsten-3-one, benzyl nicotinate and hydrogenated castor oil EO (40%) in 95% ethanol. The mole) adduct was added, stirred and dissolved, and then ion-exchanged water was added and mixed to obtain a transparent liquid hair nourishment of Example 1. Example 2 and Comparative Example 1 were also obtained in the same manner as Example 1.

(Results) All of the above results show that the hair nourishing material of the present invention containing 17β-(2-hydroxyethoxy)-4-androsten-3-one and a skin peripheral vasodilator is different from the conventionally known 17β-
(2-hydroxyethoxy)-4-androstene-3
This shows that the hair nourishing effect is synergistically superior to that of the hair nourishing material containing -ON.

Example 3 (Phase A) 17β-(2-Hydroxyethoxy)-4-androsten-3-one Methanesulfonate 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 150
0 5.0 (B phase) 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 nourishing material.

When this hair nourishing material 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) 17β-(2-chloroethoxy)-4-androsten-3-one 0.117β-(2-bromoethoxy)-4-androsten-3-one
0.1 Cephalanthine 5.0
Liquid paraffin 5.0 Cetostearyl alcohol 5.1 Glyceryl monostearate 3.0 EO (20 mol)-2-octyl dodecyl ether 3.0 Propyl paraben 0.3 Fragrance
0.1 (Phase B) Glycerin 8.0 Dipropylene glycol 20.0 Polyethylene glycol 4000 5.0 Sodium hexametaphosphate o, oos 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 55.017β
-Carbomethoxy-4-androsten-3-one methyl ester 0.0001DL-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) Ethanol, EO (8 mon) oleyl alcohol ether, 17β-carbomethoxy-4-androstene-3
-one methyl ester, DL-α-tocopherol nicotinic acid ester, and hinokitiol were added, perfume and dyed pattern were added and dissolved, and then ion-exchanged water was added to solubilize to obtain a hair nourishing agent.

Example 6 17β-(2-piperidinoethoxy)-4-androsten-3-one 0.2 g, ginger tincture 0.00
01 g 1 Liquid paraffin 5.0 g, cetostearyl alcohol 5.5 g, petrolatum 5.5 g, glyceryl monostearate 3.0 g, EO (20 mol)-2-octyl dodecyl ether 3.0 g, propylparaben 0
．． 2g and 0.1g of fragrance are heated and dissolved and mixed. To this, 7.0 g of glycerin, 2 g of dipropylene glycol
0. Og, 5.0g polyethylene glycol 400
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 nourishment of the present invention has an excellent hair nourishing effect, is locally effective, has no systemic side effects, and has little skin irritation. It is hair material.

Claims (1)

[Claims] The following general formula ▲ Numerical formulas, chemical formulas, tables, etc. are included ▼ [In the formula, R is -CH_2OH, -CH_2OCOX (However, X represents an alkyl group having 1 to 5 carbon atoms or a phenyl group.)
, -CH_2Y (however, Y represents F, Cl, Br, I), -CH_2CN, -COOX (however, X is the same as above), -CH_2OSO_2C_6H_4CH_3, -C
H_2OSO_2CH_3, ▲There are mathematical formulas, chemical formulas, tables, etc.▼, ▲Mathematical formulas, chemical formulas,
There are tables etc. Represents ▼. 1. A hair tonic comprising one or more 4-androsten-3-one-17β-ethoxy derivatives represented by the following formula and one or more skin peripheral vasodilators.