JPS6284016A - Hair tonic - Google Patents

Abstract

PURPOSE:To provide a hair tonic having synergistic effect and containing 4- estren-3-one-17beta-carboxylic acid and its alkyl ester and a dermatic peripheral vasodilator. CONSTITUTION:A safe hair tonic free from side effect can be produced by using 0.0001-2wt%, preferably 0.0001-0.2wt% 4-estren-3-one-17beta-carboxylic acid and 0.0001-5wt%, preferably 0.01-3.0wt% dermatic peripheral vasodilator (e.g. carpronium chloride, minoxidil, spironolactone, vitamin B6 hydrochloride, etc.). It can be used in the form of liquid, emulsion, ointment, etc. EFFECT:A synergistic hair tonic effect can be achieved by the effective interaction between the above active component and the dermatic peripheral vasodilator effective to dilate the peripheral vessel of scalp and promote the blood flow.

Description

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

[Conventional technology 1 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. In other words, testosterone produced in 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 Problem E] 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. As a result of intensive research in search of a substance that has both the effect of inhibiting the binding of
It has been found that the above object can be achieved by blending one or more of -carboxylic acids and alkyl esters thereof (Japanese Patent Application Laid-open No. 6O-81122). This time, as a result of further research, we found that 4-estrene-3-one-17
It has been discovered that by combining one or more β-carboxylic acids and their alkyl esters with one or more skin peripheral vasodilators, the effects are synergistically increased, and the present invention has been completed. It's arrived.

That is, the present invention provides 4-estren-3-one-17β
- It is a hair nourishing product characterized by containing one or more types of carboxylic acids and alkyl esters thereof, and one or more types of skin peripheral vasodilators.

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

The blending amount of 4-estren-3-one-17β-carboxylic acid and its alkyl ester is 0 in the hair nourishing material of the present invention.
．． 0001 to 2% by weight is preferred. Particularly preferably,
It 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. In addition, the higher the amount, the greater the hair growth effect, but considering the occurrence of unexpected side effects when used in large amounts, 2% by weight
The following are preferred.

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 the amount 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-estren-3-one-17β-carboxylic acid and its alkyl ester and a skin peripheral vasodilator, the hair nourishment according to the present invention contains additives commonly used in hair cultivation, such as hinokitiol and hexachloro. Fen,
Antibacterial agents such as phenol, benzalkonium chloride, cetylviridinium chloride, undecylenic acid, trichlorocarbanilide and bithionol, cooling agents such as menthol, agents such as salicylic acid, zinc and its derivatives, lactic acid and its alkyl esters, olive oil , squalane, liquid paraffin, isopropyl myristate, higher fatty acids, higher alcohols and other oils, other surfactants, fragrances, antioxidants, ultraviolet absorbers, pigments, ethanol, water, humectants, thickeners, etc. It can be blended as appropriate within a range that does not impair the effects of.

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-estren-3-one-17
β-carboxylic acid and its alkyl ester and a skin peripheral vasodilator that dilates the peripheral blood vessels of the scalp and promotes an increase in blood flow act effectively to exert a synergistic hair growth 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.

51. 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 hair was collected, collected for one week, and 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. The value was expressed as the number of hairs pulled per session 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 10 or more: g-), and it could be said that there was a slight effect.

-: 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 (blank below) (Manufacturing method) 4-estren-3-one-17β in 95% ethanol
- adding carboxylic acid methyl ester, benzyl nicotinate, and hydrogenated castor oil E O (40 mol) adduct;
The mixture was stirred and dissolved, and then ion-exchanged water was added and mixed to obtain a transparent liquid hair nourishment of Example 1. Example 2, comparative example 1
Also, 9 fathoms were carried out in the same manner as in Example 1.

(Left below) All the results mentioned above are based on 4-estrene-3-one-1
The hair nourishment according to the present invention containing 7β-carboxylic acid and its alkyl ester and a skin peripheral vasodilator is the same as the conventionally known 4
-Estren-3-one-17β-carboxylic acid and its alkyl ester are synergistically superior in its hair nourishing effect.

Example 3 (Phase A) 4-estren-3-one-17β-carboxylic acid ethyl ester 2.0 Oriental japonica extract 3.0 Polyoxyethylene (60 moAJ) hydrogenated castor oil 2.0 Glycerin 7.0 Dipropylene glycol 8.41.3-Butylene glycol 5.0 Polyethylene glycol 15
00 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 a 0/W emulsion type hair nourishing composition.

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-estren-3-one-17β-carboxylic acid propyl ester 0.14-estren-3-one-17β-carboxylic acid pentyl ester 0.1 Cephalanthine 5.0 Fluidity 2,
In 5.0 Cetostearyl 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 55.04-estren-3-one-17β-carboxylic acid hebutyl ester 0.0001D
L-α-tocopherol nicotinic acid ester 0.01 EO (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-estren-3-one-17β-carboxylic acid hebutyl 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 agent.

Example 6 4-estren-3-one-17β-carboxylic acid methyl ester 0.2 g 1 ginger tincture 0.0001 g
, liquid paraffin 5.0 g 1 cetostearyl alcohol 5.5 g, vaseline s, sg < glyceryl monostearate 3.0 g, EO (20 mol) -2-octyldodecyl ether 3.0 g, propyl paraben 0.28
1 and 0.1 g of fragrance were dissolved and mixed by heating. to this,
Glycerin 7, og.

Dipropylene glycol 20. A hot melted mixture of Og, 5.0 g of polyethylene glycol 4000, 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 has an excellent hair nourishing effect, is locally effective, has no systemic side effects, and has little skin irritation, and is a highly safe hair nourishing agent. be.

Claims (1)

[Claims] 1. A hair nourishment containing one or more 4-estren-3-one-17β-carboxylic acid and its alkyl ester, and one or more skin peripheral vasodilators.