JPS6284013A - Hair tonic - Google Patents

Abstract

PURPOSE:A hair tonic containing 4-estren-3-one-17beta-ethoxy derivative and a telangiectatic agent for the skin, having synergistic effects. CONSTITUTION:A hair tonic containing 0.0001-2wt%, especially preferably 0.0001-0.2wt% compound [e.g., 17beta-(2-hydroxyethoxy)-4-estren-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 0.01-3.0wt% 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 amount of blood stream act effectively and have synergistic effects.

Description

[Detailed description of the invention] [Industrial application field] TECHNICAL FIELD The present invention relates to hair nourishing plants that have 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 cilia 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 and enters the bloodstream, acting on hair matrix cells and stimulating 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-DI-(T and As a result of intensive research in search of a substance that has both the effect of inhibiting the binding with receptor proteins, and in order to obtain a hair nourishing agent with excellent hair nourishing effects by blending this substance, 4-nystrene-3-one-
It has been discovered that the above object can be achieved by blending one or more 17β-ethoxy derivatives (
JP-A-6O-54310). As a result of further research, we have found that by combining one or more 4-nystren-3-one-17β-ethoxy derivatives with one or more skin peripheral vasodilators, the effects are synergistic. The present inventors have discovered that the present invention can increase the number of particles.

That is, the present invention is a hair nourishment characterized by containing one or more derivatives of the following general formula and one or more skin peripheral vasodilators.

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

4-nystren-3-one-17β used in the present invention
The -ethoxy derivative is represented by the general formula below, and its chemical name is 17β-(2-
hydroxyethoxy)-4-nystren-3-one, ]
7β-(2-hydroxyethoxy)-4-nystrene-
3-one acetate, 17β-(2-hydroxyethoxy)-4-nystren-3-one butyrate, 17
β-(2-hydroxyethoxy)-4-nystrene-3
-one p-toluenesulfonate, 17β-(2-
hydroxyethoxy)-4-nystrene-3-one methanesulfonate, 17β-(2-chloroethoxy)
-4-Nistrene-3-one, 17β-(2-iodoethoxy)-4-Nistrene-3-one, 17β-carboxymethoxy-4-Nistrene-3-one, 17β-carboxymethoxy-4-Nistrene-3-one 17β-[2-((tetrahydrobilane- 2-yl)oxy)ethoxyco4
-Nistrene-3-one, etc.

The amount of the 4-nystren-3-one-17β-ethoxy derivative in the hair nourishing material of the present invention is preferably 0.0001 to 2% by weight. Particularly preferred is 0.0001 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, tuoryzanol, benzyl nicotinate, methyl nicotinate, panillylamide 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 preferred, particularly preferably 0.01 to 3.0% by weight. 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.

In addition to the above-mentioned 4-nystren-3-one-17β-ethoxy derivative and skin peripheral vasodilator, the hair care material of the present invention contains additives commonly used in hair care materials, such as hinokitiol, hexachlorophene, and phenol. , benzalkonium chloride, cetylpyridinium chloride, antibacterial agents such as undecylenic acid, trichlorocarbanilide and bitionol, cooling agents such as menthol, salicylic acid,
Zinc and its derivatives, drugs such as lactic acid and its alkyl esters, olive oil, squalane, liquid paraffin,
Isopropyl myristate, higher fatty acids, oils such as higher alcohols, other surfactants, fragrances, antioxidants,
Ultraviolet absorbers, pigments, ethanol, water, humectants, thickeners, and the like can be appropriately added within the range that does not impair the effects of the present invention.

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-nystrene-3-one-17
The β-ethoxy derivative and the skin peripheral vasodilator, which dilates the peripheral blood vessels of the scalp and promotes an increase in blood flow, work 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.

1' Judgment was made based on the change in the number of strands 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 hairs pulled was reduced by 70 or more, indicating a significant effect.

+: 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 two-haired trees was less than 10, so it cannot be said that it is effective.

(Left below) Example 1.2, Comparative Example 1 (Production method) 17β-(2-hydroxyethoxy)-4-nystren-3-one, benzyl nicotinate and hydrogenated castor oil EO (40 mol) in 95% ethanol. ) addition of adducts;
The mixture was stirred and dissolved, and then ion-exchanged water was added and mixed to obtain the transparent liquid hair nourishing material of Example 1. Example 2, comparative example 1
was also obtained in the same manner as in Example 1.

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

Example 3 (Phase A) 17β-(2-Hydroxyethoxy)-4-nystren-3-one Methanesulfonate 2.0 Jasperia japonica extract 3.0 Polyoxyethylene (60 mol) Hydrogenated castor oil 2.0 Glycerin 7.0 Dipropylene glycol 8.4 1.3-Butylene glycol 5.0 Polyethylene glycol 1500 5.0.

(Phase B) Cetyl isooctanate 10.0 Squalane 5.0 Vaseline
2゜0 Propyl paraben 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 dissolved by heating 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 to this, and finally the dissolved phase E was added and emulsified with a homomixer to obtain an O/W emulsion type hair nourishing agent.

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) 17β-(2-chloroethoxy)-4-nystrene-3
-one 0.117β-(2-bromoethoxy)-4-nystren-2-one
0.1 Cephalanthine
5.0 Liquid paraffin 5.
0 Cetostearyl alcohol 5.1 Glyceryl monostearate 3゜OEO (20
mole)-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 (Production method) Phase A and phase B were respectively heated and dissolved and mixed, and emulsified with a homomixer to obtain an ointment-like hair nourishing material.

When this hair nourishing material 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-nystren-3-one methyl ester 0.0001DL-α-tocopherol nicotinic acid ester 0.01EO(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, 17β-carbomethoxy-4-nystren-3-one-methyl ester, DL-α-tocopherol nicotinic acid ester, and hinokitiol to ethanol, and add fragrance to this. After adding and dissolving the dye, ion-exchanged water was added to solubilize to obtain a hair nourishing material.

Example 6 17β-(2-piperidinoethoxy)-4-nystren-3-one 0.2g1 ginger tincture 0.0001
g, 5.0 g of liquid paraffin, 5.581 g of cetostearyl alcohol, 5.5 g of vaseline, 3.0 g of glyceryl monostearate, 3.0 g of EO (20 mol)-2-octyl dodecyl ether, 1 propylparaben 0.
2g and 0.1g of fragrance are heated and dissolved and mixed. To this, 7.0 g of glycerin, 20 g of dipropylene glycol
．． Og, 5.0g 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 follicle. The obtained hair nourishing material showed an excellent hair nourishing effect.

[Effects of the Invention] The hair nourishing material of the present invention has an excellent hair nourishing effect, is locally effective, has no systemic side effects, has little skin irritation, and is highly safe. It is a 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 ▼. ] A hair tonic characterized by containing one or more 4-estren-3-one-17β-ethoxy derivatives represented by the following and one or more skin peripheral vasotonic agents.