JPS6064910A - Hair tonic - Google Patents

Abstract

PURPOSE:To provide an excellent hair tonic containing oxendolone in combination with a dermatic peripheral vasodilating agent, having synergistically increased hair tonic effect, and free from undesirable side effects such as hormone- like actions. CONSTITUTION:The objective hair tonic contains (A) oxendolone (16beta-ethyl-17beta- hydroxy-4-estren-3-one) and (B) one or more dermatic peripheral vasodilating agent such as carpronium chloride, vitamin E nicotinate, benzyl nicotinate, vitamine B6 hydrochloride, etc. The amounts of the components A and B are 0.001- 2wt% and 0.1-2wt%, respectively. The component A is free from the above side effects, has high safety and both effects to inhibit the reductase activity and to inhibit the bonding of 5alpha-dihydrotestosterone and a receptor protein, and exhibits excellent hair tonic effect, and the activity of the component can be synergistically improved by the combined use of the component B.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention eliminates unfavorable side effects such as hormonal effects.
``Hair nourishing with outstanding and excellent hair nourishing effects.

Physiological symptoms such as male-pattern baldness and seborrhea (well, it is said that male + 1 is caused by excessive accumulation of male hormones, and increased hormonal stimulation, but recently, male hormones in organs such as hair roots and sebaceous glands) The main body of activity is testosterone crab testosterone-5α in these target organs.
It has become well known that 5α-dihydrotestosterone (hereinafter abbreviated as 5α-DHT) is produced by an enzyme called -reductase (hereinafter abbreviated as reductase). In other words, testosterone (a male hormone) produced by Sumimaru and the adrenal glands travels through the bloodstream to the sebaceous glands, where it is converted into the more powerful male hormone 5α-1) I-IT by reductase in the sebaceous gland cells. converted. This 5α-D I-IT binds to intracellular receptors and acts on the nucleus to promote the proliferation of sebaceous gland cells, while it also exits the sebaceous gland cells, enters the bloodstream, and acts on hair matrix cells. It is said to suppress the division of hair matrix cells in the hair bulb and hinder hair growth.

Therefore, it is thought that symptoms such as male pattern baldness and hair loss can be reduced or prevented by inhibiting reductase activity and the binding of 5α-1)HT to receptor proteins. Based on this viewpoint, several substances have been discovered so far. However, these substances have a high inhibition rate of reductase activity and may have undesirable side effects even if they are 0, and their inhibition rate of the binding between 5α-D HT and receptor protein is very low, so they have virtually no effect on hair growth. It had the disadvantage of being less effective.

In view of the above circumstances, the present inventors have developed a substance that is safe, does not have undesirable side effects such as hormonal effects, and has both the effects of inhibiting reductase activity and inhibiting the binding of 5a-DIIT to receptor protein. As a result of intensive research in order to obtain a hair nourishing agent with excellent hair nourishing effects, it was discovered that the above objective could be achieved by incorporating oxendron, and as a result of further research, autocendron was found. The present inventors have discovered that the effects can be synergistically increased by blending the skin peripheral vasodilators with one or more skin peripheral vasodilators, and have completed the present invention.

That is, the present invention relates to oxendrone and skin powder.

+f'J This is a hair tonic characterized by a combination of one or more vasodilators.

The configuration of the present invention will be explained in detail below.

Oxendrone used in the present invention has a chemical name of 16β.
- Ejiru 17β-Hydroxitoestren-3-one It is a white to pale yellowish white powder and is odorless.

The blending amount of oxendron is 0.00 in the hair nourishing material of the present invention.
It is about 1 to 2% by weight. The larger the amount, the greater the hair-nourishing effect, but considering the occurrence of unexpected side effects when used in large amounts, it is preferably less than 0.2% by weight.

In the present invention, the skin peripheral vasodilator which is a substance that additively increases the hair-nurturing effect includes carpronium chloride, vitamin E6 nitinate, benzyl nicodinate, and vitamin 13e hydrochloride. The blending amount is 0.1 to 2% by weight in the hair nourishing material of the present invention.

In addition to the above-mentioned oxendrone and skin peripheral vasodilator, the hair nourishment according to the present invention contains additives used in hair cultivation, such as hinokitiol, bactericidal agents such as kadio/surfactants, and cooling agents such as menthol. , Oliveura, Sufwara/, oil such as higher alcohol, glycerin, l, 3
- Moisturizing agents such as butylene gellicol, maletitol, and PCA-sodium, herbal medicines such as glycyrrhizia, amino acids and amino sugars, other surfactants, fragrances, antioxidants, certain external radiation absorbers, pigments, ethanol, water, etc. They can be blended within a range that does not impair the effects of the present invention.

Furthermore, the hair nourishment according to the present invention can be implemented in various types such as lotion, milky lotion, and cream.

Next, a comparative example will be given regarding the effect of inhibiting reductase activity and the effect of inhibiting the binding between the receptor protein and 5α-D II T of oxendrone used in the present invention.

and explain.

Reductase activity inhibition effect Takayasu's method (Western Japan Dermatological Association Journal, 43.1215-
1217.1981), the sebaceous glands on the back of hamsters were used to determine if destosterone was 5α-DIIT.
The amount of f element was measured. The sample used for the experiment at 0 degrees is IO
and IO molar concentration. The inhibition rate was calculated from the obtained data using the following formula. The results are shown in Table 1.

Inhibition rate (%) = (C-t/C) Dermato
The binding between the receptor protein and 5α-D 11 T was determined based on the method (Res. 1, Res., 204.50-51.1979). The sample concentration used in the experiment was lO molar concentration. The inhibition rate was calculated from the obtained data using the following formula. The results are shown in Table 2.

Inhibition rate (%) = (C-t/C) -IT As is clear from Tables 1 and 2, Oxendronha,
Conventionally known 4-androsten-3-one-17β-
Although the inhibitory effect on reductase activity is comparable to that of carbo/acid, the inhibitory effect on the binding between the receptor protein and 5α-D II T is greater, and it can be said that this substance achieves the object of the present invention.

The hair care product of the present invention has the effect of oxendrone having the above-mentioned effects and a skin peripheral vasodilator that expands peripheral blood vessels in the scalp and promotes an increase in blood flow, resulting in complementary hair growth. It is considered to be effective.

Next, the present invention will be explained in more 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 growth effect measurement method Judgment was made based on the change in the number of strands removed during hair washing before and after using the hair growth product. There were 10 subjects in each of the 914 groups of Examples 1 to 3 and Comparative Example 1. The measurement period was 4 months, with the first 2 months being a period in which no hair tonic was applied, and the latter 2 months being a period in which hair tonic was applied.

During this period, hair was washed every two days, and hair was collected once a week and the number of hairs was counted. The number of hairs pulled out for each period is displayed by summarizing the data of the number of hairs pulled out for 8 times in total, including the 2 months without hair care product application, R18 hair loss data, and the 2 months of R18 hair growth treatment application, for each period, The number of hairs pulled per session was expressed as the average value + 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 more than 70, indicating a significant effect.

The number of plucked trees decreased by more than 40, indicating a significant effect.

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

The reduction in the number of hairs pulled was less than 10, so it cannot be said to be effective.

Examples 1 to 3, Comparative Example 1 (Production method) Oxendrone or 4-antr in 95% ethanol
! Stan-3-ono-17β-carvone Wi, lh-based barbuOium, and hardened Himashiura E0 40 mol [Add the adduct, stir and dissolve, then add 1 mol of ion-exchanged water.
The mixture was then added and mixed to obtain a transparent liquid hair nourishing agent.

(Results) All of the above results indicate that the hair nourishing material of the present invention containing oxendrone was compared to the conventionally known 4-androsten-3-one-
This shows that the hair-nourishing effect is superior to that of hair-nourishing materials containing 17β-carboxylic acid.

Example 4 Polyoxyethylene (8) added to 55.0 g of hair nourishing ethanol
Oleyl alcohol ether 2.0g, oxendrone 0.05g, vitamin E nicotinic acid ester 0.5g,
Add 0.05g of hinokitiol and add fragrance and dye to it! ['u (Add 4 quarts of ion-exchanged water after dissolving
1.95 g was added and solubilized to obtain a hair nourishing material.

When the hair nourishing material was tested in the same way as in Example 1, it was confirmed that the hair nourishing effect was excellent.

Example 5 Oxendrone 0.5g 1 polyoxyethylene (60 (
) Heat and dissolve 2.0 g of hydrogenated castor oil, 10.0 g of glycerin, 5.0 g of dipropylene glycol jo, Og, and 1,3-butylene glycol, and 5.0 g of polyethylene glycol 1500 at 60°C (A Department)
. Sejiruin Octanoate IO, Ogs Squalane 5
．． 0g, Vaseline 2.0g1 Benzyl Nicotinate 0.
Lg and 2.0 g of propylparaben are dissolved by heating at 60°C (Part B). Carboxyvinyl polymer 1% aqueous solution 30.0 & and sodium hexametaphosphate 0.03g
is dissolved in 8.25 g of ion-exchanged water (0 parts). Part A and Part B are mixed at 60°C and treated with a homomixer to form a gel. ``5.0 g of ion-exchanged water was gradually added to this and dispersed with a homomixer. Next, 0 part was added to this, and finally an aqueous solution of 0.12 g of caustic potash dissolved in 5.0 g of ion-exchanged water was added and emulsified with a homomixer to obtain an O/W emulsion type rose hair preparation.

Example 6 Liquid paraffin 5.0H, cetostearyl alcohol 5
．． 5g, Vaseline 5.5Hs Glyceryl monostearate 3.0gs Polyoxyethylene (20 liters) 2-octyl dodecyl ether 3.0g, Vitamin E acetate 0.05g 5 Propylparaben 0.3g and fragrance 0.05g dissolved by heating, Mix. Oxent 1 for this
Non 0.5g1 Vitamin IIG sulfate 0.5 Toglycerin 7.0g1 Dipropylene glycol 20.0g15
．． 0 g of polyethylene glycol 4000, 0.005 g of sodium hexametaphosphate and 44.5 g of ion exchange water
95 g of the heated and dissolved mixture was added and emulsified using a homomixer to obtain a cream-dependent hair material.

Patent Applicant Shiseido Co., Ltd. Amendment May 1980 r ``Special I1'r Director General Kazuo Wakasugi 1 Indication of Case 1982 Patent Application No. 173395 2 Title of Invention Hair Tonic 3 Amendment Relation to the patent applicant's case 1 of the amendment order 5. Subject of the amendment a Contents of the amendment First, we corrected "Kobon" to "eJ power accumulation".

(2) In the specification, page 3, line 6, 1--by the left to mix" has been amended to read "by the rise to mix."

ν (3) In the bottom line of page 4 of the specification, "Herbal medicines such as glycyrrhizin," is amended to read "Anti-inflammatory agents such as glycyrrhizin, Herbal medicines such as licorice, purple root, and Oriental japonica, J.0 (4) In the specification No. In the first line of page 5, after "sugars", insert "Puke" and "drugs such as ethinyl estradiol, vintai≠n, and bantotenyl ethyl ether" to make the correction.

(The following is a margin) (5) "10 and 10 molar concentration" in the fifth line from the bottom of page 5 of the specification, [o-' and 10-5 molar concentration] as "1o-' molar concentration", right Change "10" in the column to "1o"
- 'Molar concentration' and corrected.

(7) Correct the "lO molar concentration" in the sixth line from the bottom of page 6 of the specification to "10-6 molar degree."

(8) In the second line from the bottom of page 8 of the specification, insert the sign “+10:J” and write “+10 bales of hair removed”.
・” and corrected it.

(9) In the (Results) table on page 10 of the detailed statement, insert "10+" into the blank space in the 5th line of the "Judgment" column and make the correction.

(10) Clear all t) In the table on page ■, 4.6, u, 13, 16, ], '1 in the "Judgment" column
Insert "1000" into the blank space in the first line to correct the correction.

Claims (1)

[Claims] A hair nourishing agent characterized by co-producing otocendron and one or more skin peripheral vasodilators.