JP3162962B2 - Hair restoration - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a hair restorer containing an eugenol glycoside, and more particularly to a hair restorer having the ability to inhibit the activity of 5α-reductase by eugenol released by scalp resident bacteria. The present invention relates to a hair restorer having an excellent hair loss preventing effect and an anti-dandruff effect.

[0002]

2. Description of the Related Art There has been known a hair restorer containing a scalp blood circulation promoting substance such as pepper tincture, pepper extract, Korean ginseng extract, nicotinic acid and methyl nicotinate. However, a substance that is effective enough to exhibit effects such as hair growth, hair loss prevention, and dandruff has not yet been developed. In recent years, the involvement of hormones in hair growth has been suggested. In other words, in the hair follicle including the hair matrix, the male hormone (testosterone) is 5α-
The reductase (delta ^4-3-keto steroid 5α- oxidoreductase), is activated to active androgen (dihydrotestosterone), further binds to the receptor, is incorporated into the nucleus, to transmit information at the DNA level.
The transmitted information controls the synthesis of enzymes involved in keratin synthesis, suppresses keratin synthesis in hair, reduces hair growth, and ultimately promotes hair loss. Therefore,
In the development of hair restorer, attention has been paid to studies on inhibitors of the activity of 5α-reductase, which is an androgen-activating enzyme in the scalp and scalp.

[0003]

Eugenol is an example of a 5α-reductase activity inhibitor that is effective when incorporated into a hair restorer (JP-A-63-284125). However, it has been suggested that eugenol has a peculiar aroma component, is low in stability, is insoluble in aqueous systems, and may have sensitizing properties in terms of safety.
Therefore, an object of the present invention is to provide a hair restoration which is easy to produce, has low skin irritation, and is excellent in hair growth, hair loss prevention and dandruff prevention effects.

[0004]

Means for Solving the Problems The present inventors have conducted studies to maintain the inhibition of eugenol 5α-reductase activity and to solve the above-mentioned problems. The inventors have found that the object can be achieved, and have completed the present invention. The eugenol glycoside in the present invention, glucose, galactose, carboxymethyl <br/> loin, compounds Ma Ruto scan and the eugenol is O- glucoside bond.

The present inventors have already found that fragrance glycosides such as eugenol glycosides are appropriately decomposed into eugenol and the like and sugar moieties by resident bacteria and scalp bacteria.
JP-A-7-179328 for sustained release fragrance composition for human body
The present inventors have found that eugenol glycosides in particular exhibit a sustained-release hair growth effect and exhibit excellent properties as a hair growth agent.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION The eugenol glycoside used in the present invention can be easily synthesized by a known method. For example, U.S. S. P. An eugenol glycoside as a mixture of an α-form and a β-form can be obtained according to the method for synthesizing arbutin described in No. 3201385. Also, Flavo
ur and Fragrance Journal
(Vol 4, 163-167, 1989), a β-form alone can be synthesized according to the method of synthesizing glucovanillin. Among these eugenol glycosides, a glucose glycoside is preferable from the degree of manifestation of the effect,
Specifically, it is eugenyl α-D-glucoside and / or eugenyl β-D-glucoside. In this case, β-
The isomer is preferable, but there is no particular problem in the effect even if the α-isomer is contained.

[0007] The amount of the eugenol glycoside in the present invention is 0.1 to 0.1% of the total weight of the hair restorer composition of the present invention.
To 10.0% by weight (hereinafter abbreviated as wt%), more preferably 0.1 to 8.0% by weight. If the compounding amount is less than 0.1 wt%, the effect intended by the present invention may not be sufficient, while if it exceeds 10.0 wt%, improvement of the effect corresponding to the increase may not be expected in many cases.

[0008] The hair restorer of the present invention can be produced according to a conventional method, for example, by blending it into a dosage form directly applied to the scalp, such as hair tonic, hair lotion, and hair armose.

[0009] The hair restorer of the present invention includes a pigment, a fragrance, a bactericide, a preservative, a keratolytic agent, an antiandrogen, a hair restorer,
Antioxidants and the like can be appropriately compounded within a range that achieves the object of the present invention.

[0010]

The present invention will be described below in detail based on examples and comparative examples.

The test methods for promoting the hair growth of C3H mice, the test methods for promoting the growth of human scalp hair, and the practical test methods described in the Examples are shown below.

(1) Test Method for Promoting Hair Growth of C3H Mice C3H mice (8 weeks old, male, average weight 35 g) cut back skin (2 cm × 4 cm) with an electric clipper and a shaver, and from the next day, Examples and Comparative Examples Each sample was applied to the skin of the test portion twice a day in the morning and evening at a rate of 0.2 ml per animal for two weeks. A group of 10 animals was used for one sample. On the 14th day from the start of application, the skin of the test portion of each sample was photographed with a video camera, and the areas of the shaved portion and the hair growth portion were measured with an image analyzer. The determination of the hair growth effect was performed by comparing the hair growth rate (%) shown below with the control group. Hair growth rate (%) = (Area of hair growth part / Area of shaved part) × 1
00

(2) Test method of human scalp hair growth promoting effect Test hair of 10 test subjects with male pattern baldness was placed at 5 cm above the ears of the heads at two places on the left and right at a circular shape having a diameter of 1 cm. Approximately 3 ml of each sample of Example and Comparative Example was applied to the left side of the test site twice daily in the morning and evening, and compared with the untreated right side. The effect was determined on the 28th day after the start of the test.
Twenty hairs at each of the left and right test sites were shaved, and the degree of hair growth promotion was evaluated by the value obtained by the following equation. Degree of hair growth promotion = (B) / (A) (A): Average value of length of 20 right hairs (untreated) hairs (B): Left hair (samples of Examples and Comparative Examples applied) 2
Average length of 0 lines

(3) Practical test method The effect of applying to the heads of 20 test subjects who are male pattern alopecia twice daily in the morning and evening for 6 consecutive months was evaluated. The test results show that for each item of hair growth effect, hair loss prevention effect, and dandruff prevention effect, “hair has become bristle or hair has increased,” “hair loss has decreased,” and “hair loss has decreased. And the number of respondents.

Examples 1 to 9 and Comparative Examples 1 to 9 (oily hair tonics) In the following raw material composition, various hair growth promoting substances were blended as shown in Table 1 to prepare respective hair tonics. The above-described tests were performed.

[0016]

[0017] (2) regulating production method (B) in component, nicotinate, methyl nicotinate,
In the component (A), pepper tincture and eugenol glycoside are dissolved in the component (C ), and then the components (A) and (C ) are mixed, dispersed by stirring, and then filled in a container. When used, the contents are shaken and dispersed uniformly. As the eugenol glycoside, a mixture of an α-form and a β-form (3: 7) or a β-form was used.

(3) Characteristics Table 1 shows the results of various tests conducted on each oily hair art tonic. As shown in Table 1, Examples 1 to 5 of the present invention
The hair growth agent of No. 9 has a higher hair growth promoting effect as compared with the comparative example,
It showed the effects of preventing hair loss and dandruff. In addition, when the human patch test was performed in advance by 10 persons for each sample, the samples of Comparative Examples 2 to 5 showed mild skin irritation to 2 to 3 persons. Did not do.

[0019]

[Table 1]

[0020]

INDUSTRIAL APPLICABILITY As described above, the present invention is excellent in effects such as hair growth, hair loss prevention and dandruff, and has the ability to inhibit 5α-reductase activity by eugenol released by scalp resident bacteria. Obviously, it provides a less-prone hair restorer. That is, the present invention is, eugenol glucose, galactose, xylose, by a glycoside circle <br/> toe scan, reduces the specific odoriferous enhance security against material stability and human skin, Improved solubility in aqueous systems. In addition, eugenol glycosides were appropriately decomposed into eugenol and a sugar moiety by scalp resident bacteria, and inhibited the process in which the male hormone was activated into the active male hormone (dihydrotestosterone).
It is presumed that the ability to inhibit 5α-reductase activity suppresses the production of the active androgen (dihydrotestosterone) in hair papilla cells, further normalizes the scalp metabolic function, and enhances the antidandruff effect.

──────────────────────────────────────────────────続 き Continued on front page (58) Field surveyed (Int.Cl. ⁷ , DB name) A61K ⁷ /06-7/155

Claims (1)

(57) [Claims] 1. Eugenyl glucoside, eugenyl gala
Cutoside, eugenyl xyloside and eugenyl malt
A hair restorer comprising an eugenol glycoside selected from the group consisting of SIDs.