JPH0610127B2 - Hair nourishment - Google Patents

Description

TECHNICAL FIELD The present invention relates to a hair nourishing agent which does not have undesirable side effects of female hormones and adrenocortical hormones and has an excellent hair nourishing effect.

[Prior art]

There have been many studies on hair loss, elucidation of baldness and treatment methods, but as of now, the cause of baldness is (1)
Abnormalities due to excessive accumulation of male hormones, (2) abnormalities caused by impaired blood circulation and lack of nutrient supply to hair roots, (3) genetic theory, etc. are said to be based on various countermeasures It has been beaten up, but not enough has been obtained yet.

The hair nourishing agents proposed so far include, for example, vitamins such as vitamin E, amino acids such as serine and methionine, vasodilators such as acetylcholine derivatives, anti-inflammatory agents such as purple root extract, and cepharanthin. Although a skin function enhancer such as, a melanin synthesis catalyst such as copper pantothenate, and a keratolytic agent such as salicylic acid are mixed, hair growth is promoted to some extent, but almost no hair growth effect is observed.

〔Purpose〕

An object of the present invention is to provide a hair nourishing agent which has a high hair nourishing effect and does not have undesirable side effects of female hormones and corticosteroids.

〔Constitution〕

The present inventor is able to produce a hair nourishing agent that does not have an undesired hormonal action and also has an energy producing effect of an odd fatty acid by converting a substance having a female hormone adrenocortical hormone action into an ester with an odd fatty acid. Therefore, various compounds were investigated. As a result, in particular, it was found that an ester with a female hormone or a corticosteroid has an excellent hair-growth effect, and the present invention has been completed.

The present invention is a hair nourishing agent containing an ester of a substance having a female hormone action or a corticosteroid action and an odd fatty acid as an active ingredient.

Hereinafter, the hair nourishing agent of the present invention will be described in detail. Examples of preferred esters used as the hair nourishing active ingredient in the present invention are as follows.

(1) Estrone fatty acid ester represented by the following general formula [I] (2) Elastodiol fatty acid ester represented by the following general formula [II] (3) Benzoic acid elastradiol fatty acid ester represented by the following general formula [I] (4) Estriol fatty acid ester represented by the following general formula [IV] (5) Ethinyl esteradiol fatty acid ester represented by the following general formula [V] (6) Diethylstilbestrol fatty acid ester represented by the following general formula [VI] (7) Hexestrol fatty acid ester represented by the following general formula [VII] (8) Pregnanediol fatty acid ester represented by the following general formula [VIII] (9) Ethisterone fatty acid ester represented by the following general formula [IX] (10) Norethindrone fatty acid ester represented by the following general formula [X] (11) Dimethylsterone fatty acid ester represented by the following general formula [XI] (12) Allylestrenol fatty acid ester represented by the following general formula [XII] (13) Cortisone fatty acid ester represented by the following general formula [XIII] (14) Cortisone acetate fatty acid ester represented by the following general formula [XIV] (15) Hydrocortisone fatty acid ester represented by the following general formula [XV] (16) Prednisone fatty acid ester represented by the following general formula [XVI] (17) Prenizolone fatty acid ester represented by the following general formula [XVII] (18) Methylprednisolone fatty acid ester represented by the following general formula [XVIII] (19) Desamethasone fatty acid ester represented by the following general formula [XIX] (20) Betamethasone fatty acid ester represented by the following general formula [XX] (21) Paramesazone fatty acid ester represented by the following general formula [XX] (22) Fluocinolone acetonide fatty acid ester represented by the following general formula [XXII] Alopecia can occur for a variety of causes, but in each case, the result is that the hair cannot undergo a normal hair cycle,
The state of telogen is reached. In order to improve the hair loss state and promote hair growth, it is necessary to bring the hair follicles in the resting phase into the normal growing phase (Anagen). The present invention has been completed as a result of research on the conversion of resting hair into anagen hair, and is based on the discovery that fatty acids having an odd carbon chain length and derivatives thereof have excellent hair-growth effects. . It is thought that the reason why the odd-chain-length fatty acids and their derivatives have an excellent improving effect is that, firstly, because they are lipophilic, they are easily secreted from the sebaceous glands and easily dissolve in the cortex that coexists with the hair follicles and penetrate into the hair roots. Secondly, it ’s easy
Since it is not decomposed and metabolized via phosphofructokinase, it is not directly affected by hormones, that is, it is advantageous for alopecia caused by the action of hormones. Thirdly, it has an extremely excellent energy production effect. Is.

The fatty acid used in the hair nourishing agent of the present invention may be saturated fatty acid or unsaturated fatty acid as long as it has an odd number of carbon atoms constituting the carbon chain. The unsaturated fatty acid may contain a plurality of double bonds. In addition, even with lower fatty acids such as propionic acid (carbon chain length 3) and valeric acid (carbon chain length 5), pentadecanoic acid (carbon chain length 15)
And higher fatty acids such as heptadecanoic acid (carbon chain length 17).

The compounding amount of the ester used as a medicinal component of the hair nourishing agent in the present invention is about 0.001 to 2% by weight in the hair nourishing agent. The greater the amount of this compound, the greater the hair-growth effect, but considering the occurrence of unexpected side effects when used in too large an amount, 0.01-
About 0.5% by weight is preferable.

[Effect]

The hair nourishing agent of the present invention is composed of the above-mentioned ester component, has an excellent hair nourishing effect, does not show an undesired hormonal action like female hormones and adrenocortical hormones, and is remarkably improved as compared with conventional hormonal agents. is there.

In the hair nourishing agent according to the present invention, in addition to the ester component, additives usually used in hair nourishing agents, for example, bactericides such as hinokitiol and cationic surfactants, refreshing agents such as menthol, olive oil, squalane, higher alcohols, etc. Oil, other surfactants, fragrances, antioxidants, ultraviolet absorbers, dyes, ethanol, water and the like can be added.

Next, the reductase (testosterone-5α-reductase) activity inhibitory effect of the esters used in the present invention and the binding inhibitory effect between the receptor protein and 5α-DHT (5α-dihydrotestosterone) will be described with reference to comparative examples.

〔Example〕

 Next, the present invention will be described in more detail with reference to examples.

Example 1 [Effect of reductase activity inhibition] Takayasu et al.'S method (West Japan Dermatological Association, 43, 1215-1217,
1981), using the sebum line on the back of the hamster,
The amount of testosterone converted to 5α-DHT was measured. The sample concentration used in the experiment is 0.005% by weight. The inhibition rate was calculated from the obtained data using the following formula. The results are shown in Table-1.

Inhibition rate (%) = (ct−c) × 100 c: Production amount of control 5α-DHT t: Production amount of 5α-DHT when a sample was added [Binding of receptor protein and 5α-DHT Inhibitory Effect] The method of Takayasu et al. (Arch. Deraato
l. Ras. , 264, 50-51, 1979), and the amount of binding between the receptor protein and 5α-DHT was measured. The sample concentration used in the experiment is 0.005% by weight. The inhibition rate was calculated from the obtained data using the following formula. The results are shown in Table-1.

Inhibition rate (%) = (ct−c) × 100 c: binding amount of control receptor protein to 5α-DHT t: binding amount of receptor protein to 5α-DHT when sample was added [ Hair growth test (promoting days)] New Zealand White male rabbit 6 weighing about 2.5 kg
A group of 8 to 8 birds was depilated on the back and only those in the resting period were used for the experiment. 0.2 ml each of the test sample (concentration: 0.3% by weight) was applied to the back of the hair, which was in the quiescent period, after removing hair, 2 times a week.
It was applied once, for 30 to 60 days, and the number of days required for converting resting hair to growing hair was examined. The results are shown in Table-1. In Table 1, "promotion days" indicates how many days the conversion from resting hair to anagen hair was promoted as compared with the case of applying ethanol containing no test substance.

Example 2 A hair nourishing agent having the component composition shown in Table 2 was prepared, the hair nourishing effect was measured, and the result is shown in Table 2.

[Method of measuring hair-growth effect]

It was judged by the change in the number of hair loss when washing hair before and after using the hair nourishing agent. There were 10 test subjects in each experiment. Measurement time is 4
The first 2 months is the period for applying the hair nourishment,
During this period, the hair was washed every 2 days, and the extracted hair was collected once a week, and the number thereof was counted. The number of hairs removed during each period is summarized as follows: Data for the number of hair removals for a total of 8 times for 2 months without application of the hair nourishment and data for 8 months for a total of 8 months for the application of the hair nourishment. The average number ± α was shown as the number of plucked hairs. The unit is the number. The judgment of the effect was displayed as follows from the difference of the average value of each period.

Remarkable effect: The number of plucked hairs decreased by 70 or more, showing a remarkable effect.

Effective ... The number of plucked hairs decreased by 40 or more, showing a considerable effect.

Slightly effective ... The number of plucked hairs decreased by 10 or more, and it was said that there was some effect.

Ineffective ... The number of plucked hairs is reduced by less than 10, and it cannot be said to be effective.

In Table 1, the experiment No. 1-3, and experiment N
o. 6 (Comparative Example) shows the results for the special hair nourishing agent,
Experiment No. No. 4 is hair tonic and hair nourishing agent, experiment No. No. 5 is hair liquid and hair nourishing agent, and experiment No. 7 is shampoo and hair nourishing agent, experiment No. No. 8 is a rinse and hair nourishing agent, and Experiment No. 9 shows the results for the hair cream and hair nourishing agent.

Claims (3)

[Claims] 1. A hair nourishing agent comprising an ester of a substance having a female hormone action or a corticosteroid action and an odd fatty acid as an active ingredient. 2. A substance having a female hormone action is estrone, estradiol, estradiol benzoate,
The hair nourishing agent according to claim 1, which is at least one selected from estriol, ethinyl estradiol, diethylstilbestrol, hexestrol, pregnanediol, etisterone, norethindrone, dimethisterone and allylestrenol. 3. A substance having a corticosteroid effect, which is at least one selected from cortisone, cortisone acetate, hydrocortisone, prednisone, prednisolone, methylprednisolone, dexamethasone, betamethasone, paramethasone and fluocinolone acetonide. The hair nourishing agent according to claim 1.