JPS61171413A - Hair tonic - Google Patents

Abstract

PURPOSE:A hair tonic which has improved hair growth promoting effect, is observed to have improved effect on male type baldness patient, shows improved effect on prevention of dandruff and fallen hair, etc., has improved effect and high safety, blended with a 10 hydroxy-DELTA<2>-decenoic acid. CONSTITUTION:A hair tonic is blended with 10 hydroxy-DELTA<2>-decenoic acid shown by the formula or one or more of its salts such as Na, K, 1/2Ca, NH4, ethanolamine, basic amino acid such as alginine, etc. directly or after it is dissolved in an alcohol and blended. The hair cosmetic contains 0.1-5.0wt% compound shown by the formula, and shows more improved effect when it is blended with a peripheral vasodilator of the skin such as CAPRONIUM chloride, vitamin E acetate, vitamin E nicotinate, etc. Types such as lotion, milky lotion, cream, oil gel, spray, etc., may be possible as the hair tonic, it is applied properly to the scalp once - twice daily, and preferably light massage or patting with brush, etc., is carried out.

Description

DETAILED DESCRIPTION OF THE INVENTION OBJECT OF THE INVENTION The present invention aims to provide a highly safe hair nourishing group that has excellent hair nourishing and hair growth promoting effects.

``Conventional technology'' Traditionally, physiological symptoms such as androgenetic alopecia and seborrhea are
It is said that this is due to increased stimulation of androgen due to excessive accumulation of androgen, but recently it has been revealed that the main body of this androgen activity in organs such as hair roots and sebaceous glands is that testosterone is activated by testosterone-5α in these target organs.
- It has become well known that 5α-dihydrotestosterone (hereinafter abbreviated as 5α-DHT) is reduced by an enzyme named reductase (hereinafter abbreviated as reductase). That is, testosterone (male hormone) produced by lightning and the adrenal glands travels through the bloodstream to the sebaceous glands, where it is converted to 5α-DHTK, a more powerful male hormone, by reductase in the sebaceous gland cells. While this 5α-DHT binds to intracellular receptors and acts on the nucleus to promote the proliferation of sebaceous gland cells, it is not clear by what process it leaves the sebaceous gland cells and acts on hair matrix cells. However, 5α-DHT is said to suppress the division of hair matrix cells in the hair bulb and impede hair growth.

Therefore, it is thought that 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 the receptor tannogiri. Several substances have been discovered so far based on this viewpoint. However, these substances have a high inhibition rate of reductase activity (although they have disadvantages such as having undesirable side effects such as hormonal effects, and having a weak hair growth effect when actually applied to the scalp). In addition, skin peripheral vasodilators such as vitamin E nicotinate, which have been used since ancient times, have been insufficient in terms of hair growth effect.

As mentioned above, the products currently used as hair nourishing agents are:
As mentioned above, they have more or less drawbacks, and the development of new hair nourishing agents is desired.

[Problems to be Solved by the Invention] Therefore, the inventors of the present invention first observed the bald area of a male's bald head in detail using a Leitz MZ surface microscope (X25), and found that the area had a Rather than having no hair at all, it was observed that downy hair was sparsely occurring.

In other words, male pattern baldness is a result of long hair becoming thinner and shorter as it grows back through the hair cycle, becoming downy hair, and the function of the hair matrix cells and hair follicles at the root of the hair improves for some reason. This is thought to be due to this. Furthermore, the present inventors biopsied the skin of this patient with androgenetic alopecia and histologically observed it. Although no particular abnormality was observed in the epidermis or dermis, the hair roots atrophied and became rod-shaped. It was also discovered that the sebaceous glands were abnormally developed and enlarged. In other words, abnormal development of sebaceous glands, which is not seen in normal long hair, was observed. Furthermore, as a result of similar investigations and examinations of a large number of patients with androgenetic alopecia, it was found that the development of sebaceous glands in the scalp at the site of hair loss was more pronounced than in normal scalp, and the activities of sebaceous gland cells and hair matrix cells were contradictory. It turned out that the relationship was

In other words, by suppressing the abnormal development of sebaceous glands, it is possible to improve the seborrhea and bran condition of the scalp, and also to effectively prevent alopecia that is thought to be caused by these.

The present inventors extensively searched for substances that have such an effect through animal experiments using hamsters, and found that 10-hydroxy-Δ2-decenoic acid and its salts had the above-mentioned effect.Based on this knowledge, the present inventors developed the present invention. The invention was completed.

That is, the present invention provides a hair-nourishing effect characterized by incorporating one or more selected from 10-hydroxy-d-decenoic acid or its salt represented by the following formula (1) % formula % (1) , relates to a highly safe hair nourishing agent that has an excellent hair growth promoting effect.

"Structure of the Invention" The 10-hydroxy-Δ2-decenoic acid and its salts used in the present invention can be used as they are commercially available, or can be newly synthesized or extracted from natural products. It is possible.

As the above-mentioned salt of 10hydroxy-△2-decenoic acid,
The carboxylic acid part of decenoic acid is Na% and 1%Ca.

3AMgs NHa,) Reethanolamine, basic amino acids such as arginine, histidine, lysine, hydroxylysine, ornithine, etc., and oligos having these as residues must be substituted with peptide, etc.
A specific example is 10 human o xy-Δ2- f
ill Potassium salt [HOCH2<CH2)6-CH=
CHCOOK], 10-hydroxy-Δ2-decenoic acid arginine salt, and the like. Of course, these salts may be blended as they are, or may be added separately and reacted to form salts during the hair tonic manufacturing process. These substances are generally pale yellow to white crystalline powders that have no odor and are soluble in hair nourishment bases such as water, ethanol, and vegetable oil. Further, a hair tonic containing a skin peripheral vasodilator in addition to the above-mentioned 10-hydroxy-Δ2-decenoic acid and/or its salt has a more favorable effect. Examples of such skin peripheral vasodilators include capronium chloride, benzyl nicotinate, vitamin E acetate, vitamin E lyluate, vitamin E nicotinate, etc., and one or more of these may be used. Ru.

Next, the hair nourishing agent according to the present invention can be of various types such as lotion, milky lotion, cream, oil gel, water-soluble gel, spray, etc., and the present invention also provides a hair styling agent having a hair nourishing effect. It goes without saying that it is included in hair nourishing products. Also, the method of compounding is 10 hydroxy-
Δ2-decenoic acid and/or its salt can be blended into the hair nourishing agent as it is or by dissolving it in alcohol or the like in the same manner as conventional medicinal ingredients are blended. The blending amount is approximately 0.01 to 15.0% by weight, preferably 0.1 to 5.0% by weight.

As for how to use it, it is preferable to apply an appropriate amount of the hair nourishing agent to the scalp once or twice a day, and lightly pat it with a pine surge or brush.

In addition, the hair nourishment according to the present invention contains 10 hydroxy-Δ2
- In addition to decenoic acid and/or its salts, additives commonly used in hair nourishing agents, such as hinokitiol, cationic surfactants, disinfectants such as parabens, cooling agents such as t-menthol and chili pepper tincture, squalane, higher alcohols, etc. Oil, other surfactants, fragrances, antioxidants, sunscreen agents, pigments, ethanol, water, etc. can be added.

〔Example〕

Next, examples of the present invention will be shown.

Example 1 Hair nourishing agent (a) (lotion type) Weight % B Purified water
155.6 (Production method) The above formulation A was stirred and dissolved, and the above formulation B was added thereto and mixed to obtain a transparent liquid hair nourishing agent.

Example 2 Hair nourishing agent (b) (lotion type) weight% (Manufacturing method) A product was obtained in the same manner as in Example 1.

Example 3 Hair nourishing agent (emulsion type) Weight % (Production method) The above formulations A and B were heated to 80°C and mixed and stirred to uniformly dissolve them, and then both components were mixed and emulsified at the same temperature and stirred. A product was obtained by cooling to room temperature.

Example 4 Hair nourishing agent (cream type) Weight% C fragrance 0.2 (
Manufacturing method) The above formulation A is mixed and heated to 80°C.

To this is added Formulation B, which has been mixed and heated to 80° C. in the same manner, and homogeneously emulsified with a homomixer, and the above C is added and cooled to obtain a product.

"Effect of the invention" Next, 10 hydroxy-Δ2 used in the present invention
- Decenoic acid and its salts were subjected to a sebaceous gland hypertrophy inhibition test using Normstar auricular sebaceous glands, and the results are shown in Table 1. The greater the inhibition rate of sebaceous gland hypertrophy, the stronger the anti-androgen effect.

The test method is as follows.

Specimen> Using an equal volume mixture of propylene glycol and ethanol as the vehicle, α1% of each of 10-hydroxy-Δ2-decene and 10-hydroxy-Δ2-decenoic acid potassium salts was added.
A total of 7 samples were used, one containing α5%, 10 heavy vehicle solution and one using only vehicle as a blank.

Sebaceous gland hypertrophy inhibition test: 10-week-old female Syrian hamsters were divided into groups of 6, and after being divided into each sample group, the male hormone agent Testosterone Propionate T was applied to the 1st and 48th molars of the experimental tube. O'Ik (vr/v) liquid No. 7 rough in solution 1
- Injected subcutaneously in the back to enlarge the auricular sebaceous gland, and at the same time, each sample was applied to the auricle of the hamster once a day for 7 days from the first molar of the experimental tube.

On the 8th day of the disaster, the central part of the auricle of each group of animals was necropsied, and 5μ thick vertical sections were prepared using the standard tissue preparation method. Gland cross-sectional area was measured. The sebaceous gland hypertrophy inhibition rate was determined by the following formula.

Note that the sebaceous gland cross-sectional area of each group is the average value of 6 animals.

Sebaceous gland hypertrophy inhibition rate (chronic) = Table 1 Sample Sebaceous gland hypertrophy inhibition rate @) 10 hydroxy-Δ2-decenoic acid 0, 11 17 0, 51 34 1, O% 4610 hydroxy-Δ2-decenoic acid potassium 0 .1%
150.5chi 30
1,01 42 or more (,1
0-hydroxy-Δ2-decenoic acid and its salts have an inhibitory effect on the hamster auricular sebaceous gland hypertrophy induced by testosterone propionate, that is, an anti-androgen effect, and the effect is Concentration dependence was confirmed in the - range.

Next, 10 hydroxy-Δ2 used in the present invention
-Decenoic acid was tested for hair growth promoting effect using mice, and the results are shown in Table 2.

The test method is as follows.

Hair growth promotion effect test: Sample (1) 10hydroxy-Δ2-decenoic acid 0.1% C-/
V) 95% ethanol solution (product of the present invention) (B) 95% ethanol solution (blank) Test method> Experiment No. 18 was conducted using 10 8-week-old male 03H mice whose hair cycle is in the resting phase. Hair was removed from the back of the mouse to the tail, and two hairs were drawn on each side, centering around the spine.
A cm square part was prepared. Next, on the 6th day of the experiment, continue to apply α3d to each site once a day, and on the 14th day, collect hair from each site and measure its length.
The average value of the 10 hairs was taken as the length of the hair in that part of the animal. The values in the table are the average values of 10 animals.

Table-2 Specimen hair length) 0) Invention product Z4±0.5 (B) Blank 5.8±0.4 (A) - (B)
t6±026±0 promotion rate (%) = As described above, the product of the present invention promoted hair growth in approximately 28% arrogant mice compared to the blank, and a hair growth effect was observed. It was speculated that this was probably due to the cell activation effect in the hair root.

Next, a hair growth effect test was conducted on the hair growth group provided by the present invention, and the results are shown in Table 3.

″#1°″TffiO! D”r66・Rei hair growth effect test: 9 patients with seborrheic alopecia, 3 patients with pityriasis alopecia, 12 patients in total
The hair growth group of Example 1 was administered twice a day (1
2 times. 〇-Administration) Administered to the hair removal area of the scalp while performing a light massage.

The test was conducted for 6 months under the supervision of a doctor and
The following three items were evaluated based on the judgment of the doctor.

・Hair growth promotion effect 10: Increased growth of long hair 90: Increased downy hair ±: No change m: Hair loss area expanded ・Dandruff prevention effect +: Reduced dandruff m: No change・Hair removal prevention Effect +: Reduced hair removal m: No change Table 3 The numbers in the table are the number of cases; the upper row is for patients with seborrheic alopecia, and the lower row is for patients with alopecia pityriasis.

As described above, the hair growth group of the present invention has an excellent hair growth promoting effect, and a remarkable effect was observed in patients with androgenetic alopecia, particularly in patients with seborrheic alopecia. It also exhibited excellent effects in preventing dandruff and hair removal, and no undesirable side effects such as hormonal effects were observed. Taking all the above points into consideration, the hair growth group provided by the present invention is unprecedented, has an excellent hair growth effect, and is highly safe.

Claims (1)

[Claims] 1) The following formula (1) HOCH_2(CH_2)_6CH=CHCOOH(1
) 10hydroxy-Δ^2-decenoic acid or its salts, characterized in that it contains one or more selected from the following. 2) The hair nourishment according to claim 1), which contains 0.1 to 5.0% by weight of 10-hydroxy-Δ^2-decenoic acid and/or its salt. 3) Claim 1) or 2), wherein the hair nourishing agent contains a skin peripheral vasodilator such as capronium chloride, benzyl nicotinate, vitamin E acetate, vitamin E linoleate, vitamin E nicotinate, etc. Hair nourishment.