JP3113056B2 - 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 excellent in hair growth and hair growth, hair loss prevention, dandruff prevention and the like.

[0002]

2. Description of the Related Art Alopecia is thought to be caused by various factors intricately intertwined with each other, and at present, the mechanism of its occurrence has not yet been fully elucidated. Conventionally, hair restorations containing various agents have been used for prevention and treatment of hair loss, but no agent effective enough to suppress hair loss and promote hair growth and hair growth has yet been found.

[0003] Fuzi used as a raw material for the hair restorer of the present invention has been described in ancient times in China as a herbal sutra, and is known as an important crude drug widely used in various Chinese herbal prescriptions in Chinese herbal medicine, and it is known as Ranunculaceae. ) Of Aconitum species (Aconitum specie)
prepared from tuberous roots of s). Japanese Unexamined Patent Publication (Kokai) No. 3-271213 proposes a hair-growing / hair-restoring agent characterized by containing an extract of the root, stem or leaf of aconite, which is the base plant, but using an extract of aconite alone The hair growth and hair growth effects were insufficient.

[0004]

SUMMARY OF THE INVENTION In view of the above circumstances, the present inventors have conducted intensive studies and as a result, have found that at least one kind selected from the group of low-molecular-weight acidic mucopolysaccharides and salts thereof, and an extract of a sticky fish. By blending, safety is high,
The present invention has been found to show excellent effects on mouse hair growth promotion and human hair growth promotion, and also has a remarkable effect on dandruff prevention effect, thereby completing the present invention. That is, an object of the present invention is to provide a hair restorer having excellent effects such as hair growth, hair restoration, hair loss prevention, and dandruff prevention.

[0005]

SUMMARY OF THE INVENTION The present invention is a hair restoration comprising at least one selected from the group consisting of low-molecular-weight acidic mucopolysaccharides and salts thereof, and an extract of Fuzi.

As the acidic mucopolysaccharide used in the hair restorer of the present invention, hyaluronic acid, dermatan sulfate, chondroitin tetrasulfate, chondroitin hexasulfate, heparin, heparan sulfate and the like can be used, all of which are known substances. It is widely distributed in animals as a matrix component in cartilage, joints, eyeballs, skin and other connective tissues and bound to proteins.

The low molecular weight acidic mucopolysaccharide used in the present invention is obtained by further reducing the molecular weight of a natural product. The molecular weight of hyaluronic acid is 1,000 to less than 100,000, dermatan sulfate, chondroitin 4 Sulfuric acid and chondroitin 6-sulfuric acid preferably have a molecular weight of 1,000 to less than 10,000, and heparin and heparan sulfate have a molecular weight of 1,000 to less than 7,000.

The salts of the acidic mucopolysaccharide used in the present invention include alkali metal salts such as sodium and potassium salts of the mucopolysaccharide, alkaline earth metal salts such as magnesium salt and calcium salt, ammonium salts, and triethanol. Preferable are basic amino acid salts such as alkanolamine salts such as amine salts, lysine salts, arginine salts and histidine salts. These acidic mucopolysaccharides can also be used as free acids.

The acidic mucopolysaccharide and its salt used in the present invention can be obtained as follows. (1) Low molecular weight hyaluronic acid and its salts Commercially available hyaluronic acid 5 having an average molecular weight of 1,000,000
g was dispersed and dissolved in 100 ml of a 0.02 N aqueous hydrochloric acid solution, adjusted to pH 2-3, and heated to 65 ° C. in a warm bath with stirring. By changing the heating time from 10 minutes to 120 minutes, the average molecular weight becomes 1,000 to 10 minutes.
000 hyaluronic acid can be obtained. Next, after neutralizing with 0.1 N sodium hydroxide, the solution was cooled to room temperature, and the precipitate obtained by adding 3 volumes of ethanol was dried to obtain a powder of sodium hyaluronate of low molecular weight. Further, this low-molecular-weight sodium hyaluronate is treated with an acid to give free hyaluronic acid, and then treated with another basic substance to remove salts such as potassium salt, triethanol salt and L-arginine salt. Prepared.

(2) Low molecular weight chondroitin tetrasulfate and salts thereof 5 g of commercially available sodium chondroitin tetrasulfate having an average molecular weight of 30,000 is dissolved in 50 ml of water, and the resulting solution is applied to a resin column of Amberlite IR-120 (H type). The resulting effluent is heated to 75 ° C. in a warm bath with stirring.
By changing the heating time from 10 minutes to 120 minutes, chondroitin tetrasulfate having an average molecular weight of 1,000 to 10,000 can be obtained. Then
After neutralization with 0.1N sodium hydroxide, the solution was cooled to room temperature, and a precipitate obtained by adding 3 volumes of ethanol was centrifuged, washed with ethanol, dried and dried to obtain low-molecular-weight chondroitin tetrasulfate. A sodium salt powder was obtained.
Further, this low-molecular-weight sodium chondroitin tetrasulfate was treated with an acid to form a free acid, and then treated with another basic substance to prepare, for example, potassium salts, triethanol salts, L-arginine salts and the like.

Also, low-molecular-weight chondroitin-6-sulfate, low-molecular-weight dermatan sulfate, low-molecular-weight heparin, low-molecular-weight heparan-sulfate, etc. were prepared in the same manner as in the case of chondroitin-4 sulfate, or in their free form. In addition, the measuring method of the average molecular weight of the acidic mucopolysaccharide obtained by each processing time is as follows:
ogyi-Nelson) method.

On the other hand, the raw material crude drug used for the hair nourishes of the present invention is attached to Ranunculaceae.
Aconitum species of Aconitum species
Any material may be used as long as it is prepared from the tuberous root of s), and its source and place of production are not limited. In general, Aconitum plants contain highly toxic aconitine alkaloids and must be used with extreme caution when used. It is good to use what is done.

[0013] As a base plant of Fuzi, for example, Aconitum c.
armichaeli Debx), wild species (Aconitum kusnezoffii Rei) from various parts of China
chb. ), Such as Korean beetle (Acon)
itum triphyllum Nakai, Aconitum coreanum
Rap. ), Japanese Aconitum beetle (Aconitu)
m japonicum Thumb. ), Aconitum beetle (Aconitum chinense Pax)
t. ). In particular, Chinese beetle from Sichuan, China is preferable in terms of quality stability and supply with a certain cultivation method.

[0014] As the detoxification processing method, Patent Publication 3
No. 7-18498, tuber root is autoclaved at 100-130 ° C., pressure 1.0-1.5 kg /
The method of preparing by pressurization and heat treatment for 20 to 40 cm ² is a particularly preferable method because a simple, effective and safe crude drug can be stably produced. As an example prepared by this method, there is a trade name “processed bush powder” of a Japanese Pharmacopoeia exotic product. Also, mainly in China,
The washed roots are immersed in bitter solution for several days and dried. And then applying heat, pressure, etc., and drying. As an example of the preparation by this method, the one sold in the market in Sichuan, China as a sticky ball (referred to as a gun stick in Japan) is preferable because it is sufficiently detoxified with a certain quality.

The extract of the seaweed of the present invention, when the seaweed is extracted with a solvent, shifts from the seaweed to the solvent and refers to the component. This extract is used in a dry state after the solvent is removed. It can also be used after being dissolved in a solvent. In the latter case, the extraction solvent constitutes a part of the base in the hair restoration of the present invention.

Solvents include water, alcohols such as methanol, ethanol, butanol ethers such as diethyl ether, dioxane, ketones such as acetone aliphatic hydrocarbons such as pentane, hexane, cyclohexane, esters such as ethyl acetate Etc. can be used. When the extract is used as a dried product after removing the solvent, any of the above-mentioned solvents can be used alone or in combination. However, when the extract is used in a state of being dissolved in a solvent, it is preferable to use water, ethanol, or a mixture thereof, which has no harmful effect on the human body.

At the time of extraction, the azuki bean can be used as it is, or it can be crushed or pulverized to improve contact with a solvent. The ratio between the attachment and the solvent is not particularly limited, but from the viewpoint of extraction efficiency and convenience, the attachment 1
It is preferred to use 100 to 5000 ml of solvent per 00 g. The extraction temperature is conveniently in the range of room temperature to the boiling point of the solvent under normal pressure, and the extraction time varies depending on the extraction temperature, the presence or absence of stirring, and the like, but is preferably in the range of 30 minutes to 2 weeks.

The present inventor has conducted intensive studies on the above-mentioned constituents to be incorporated into the hair restorer. As a result, the hair restorer prepared by blending the extract of the Fusatsu of the present invention with a low-molecular-weight acidic mucopolysaccharide and salts thereof is: It has been found that the synergistic effect has an excellent hair-growth effect (mouse hair growth promoting effect, human hair growth promoting effect), hair-growing effect, hair loss prevention, dandruff prevention and the like.

The mixing ratio of the Fusuki extract of the present invention and the low-molecular-weight acidic mucopolysaccharide and salts thereof is appropriately selected according to the dosage form of the hair restorer, and is based on the total amount of the hair restorer. And the extract of Fuzi are 0.0001-20.
0 wt% (in terms of dry matter), low-molecular-weight acidic mucopolysaccharide and salts thereof may be 0.01 to 3.0 wt%, and if it is less than the lower limit of each compounding amount, the effect of the present invention is sufficient. On the other hand, even if it exceeds the upper limit, the improvement of the effect corresponding to the increase cannot be expected.

The hair restorer of the present invention can be made into a dosage form such as a hair tonic, a hair lotion, a hair cream, a shampoo, a rinse, a hair foam, a hair gel and the like according to a conventional method.

The hair nourishes of the present invention include pigments, fragrances, bactericides, preservatives, keratolytic agents, anti-inflammatory agents, antiandrogens,
Hair restorers, vitamins, antioxidants, cooling agents, other crude drug extracts, and the like can be appropriately compounded within a range that achieves the object of the present invention.

[0022]

The present invention will be described below in detail based on examples and comparative examples. The mouse hair growth promotion effect test method, the human hair growth promotion effect test method, and the practical test method described in the Examples are shown below.

(1) Mouse hair growth promoting effect test The hair at the center of the back of a C3H mouse (male, 7 weeks old) was shaved with a clipper and a shaver, etc., and the sample was placed on the shaved site once a day, per mouse. 0.2 ml was applied. A group of 10 animals was used for one sample. On the 15th day after the start of the experiment, a photograph of the back of the mouse was taken, the shaved area and the hair growth area were calculated, the hair growth rate (%) was determined, and the hair growth promoting effect was determined by the average value of 10 cases.

(2) Test Method for Promoting Human Hair Growth The hair of a subject, who is a male pattern baldness, at a position 5 cm above the ears of the heads of the 10 test subjects was formed into a circular shape having a diameter of 1 cm at two places on the left and right. About 3 ml of the sample of the example or the comparative example was applied to the shaved test site on the left side 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 on each of the left and right test sites were shaved, and the average value (B) of the lengths of the 20 hairs on the left side (to which the example or the comparative example was applied) was calculated as the length of the 20 right hairs (untreated). The value divided by the average value (A) of the height was obtained and evaluated. The judgment results were shown as the average of (B) / (A) of 10 test subjects.

(3) Practical Test Method The effect of applying the sample to the heads of 20 test subjects who are male pattern baldness patients twice daily in the morning and evening for 6 consecutive months was evaluated. The test results showed that for each item of hair growth effect, hair loss prevention effect, and dandruff prevention effect, "hair was bristle or hair was increased", "hair loss was reduced", and "hair loss was reduced" And the number of respondents.

Production Example 1 (Preparation of Bushi Extract) (1) A crushed dried tuber of Bushi (produced as Kawa Ozu or Hoshibushi) from Shikoku, China, is autoclaved at 100-130 ° C. The pressure is adjusted to ¹ to 1.5 kg / cm ² , and pressure and heat treatment are performed for 40 minutes. Attachment 1 processed
00g in 1500 ml of 70 v / v% ethanol (hereinafter, v / v% is abbreviated to%) at room temperature (20-25%).
C.) for 16 hours, and the supernatant was collected by filtration, concentrated at 45 ° C. under reduced pressure for 3 hours, and the solvent was distilled off to obtain 11.7 g of a brown extract.

(2) 100 g of Fuchu produced in Sichuan, China processed in the same manner as in Production Example 1 (1) was immersed in 1500 ml of 40% ethanol at room temperature (20 to 25 ° C.) for 16 hours.
The supernatant was collected by filtration, concentrated at 45 ° C. under reduced pressure for 4 hours, and the solvent was distilled off to obtain 13.4 g of a brown extract.

(3) 50 g of a gun stick (produced as a stick valve) from Sichuan Province, China, is immersed in 500 ml of 70% ethanol at room temperature (20 to 25 ° C.) for 16 hours, and the supernatant is filtered. The extract was concentrated at 45 ° C. under reduced pressure for 2 hours, and after evaporating the solvent, 5.3 g of a brown extract was obtained.

(4) Non-Japanese Pharmacopoeia non-standardized processed bush powder 50
g in 500 ml of 40% ethanol at room temperature (20 to 2).
(5 ° C.) for 10 hours, and the supernatant was collected by filtration, concentrated at 45 ° C. under reduced pressure for 3 hours, and the solvent was distilled off to obtain 6.1 g of a brown extract.

Examples 1 to 10 and Comparative Examples 1 to 13 (Heart Tonic) In the following component composition, the extract of batsumi prepared in Production Example 1 was mixed with a hyaluronic acid having a molecular weight of 55,000 (hereinafter referred to as HA). Abbreviated), hyaluronic acid having a molecular weight of 1,000,000 (hereinafter abbreviated as HAL), molecular weight of 4,8
00 sodium hyaluronate (hereinafter abbreviated as HAN), dermatan sulfate having a molecular weight of 6,500 (hereinafter DS)
, A molecular weight of 7,000 potassium dermatan sulfate (hereinafter abbreviated as DSK), a molecular weight of 5,000 chondroitin 4 sulfate (hereinafter abbreviated as C4S), and a molecular weight of 30,000 chondroitin 4 sulfate (hereinafter, abbreviated as C4S). C4
SL), chondroitin 6 sulfate having a molecular weight of 5,500 (hereinafter abbreviated as C6S), molecular weight of 5,000
Chondroitin tetrasulfate L-lysine (hereinafter abbreviated as C4SL), heparin having a molecular weight of 4,300 (hereinafter He)
p) and low-molecular-weight acidic mucopolysaccharides such as heparan sulfate (hereinafter abbreviated as HS) having a molecular weight of 5,400 as shown in Tables 1 and 2, respectively. Prepared and performed the tests described above.

(1) Composition Ingredient Blending Amount (wt%) Ethanol 60.0 Batsumi extract, acidic mucopolysaccharides, etc. See Tables 1 and 2 Propylene glycol 1.0 Fragrance 0.1 Purified water ──────────────────────────

(2) Preparation Method The extract of Fuzi and the flavoring agent are dissolved in ethanol, and the acidic mucopolysaccharides and propylene glycol are dissolved in purified water. Was prepared.

(3) Characteristics As shown in Tables 1 and 2, the results of various tests conducted for each hair tonic are shown in Comparative Examples 1 to 7 in which the low-molecular-weight acidic mucopolysaccharide of the present invention is used alone, and Comparative Examples 8 to 11 in which the extract alone was used, or Comparative Examples 12 and 13 in which the high-molecular-weight acidic mucopolysaccharide was used in combination with the extract of Fuzi had a low hair growth promoting effect, and also exhibited a hair nourishing and anti-dandruff effect. I was not able to admit. The hair restorer of the present invention of Examples 1 to 10 in which the low-molecular-weight acidic mucopolysaccharide of the present invention and the extract of Fuzi were simultaneously mixed showed a high hair growth promoting effect in mice and humans, and the results of practical tests were also good. Results were shown. Examples 1 to 10 did not cause skin irritation in various tests on human skin.

[0034]

[Table 1]

[0035]

[Table 2]

[0036]

As described above, it is apparent that the present invention provides a hair restorer which exhibits a remarkable hair growth promoting effect and is excellent in hair growth effect, hair loss prevention and dandruff prevention effects.

Continuation of the front page (56) References JP-A-3-271213 (JP, A) JP-A-63-238717 (JP, A) JP-A-3-123722 (JP, A) JP-A-3-66606 (JP) JP-A-1-197422 (JP, A) JP-A-63-150210 (JP, A) JP-A-63-215617 (JP, A) International publication 90/12561 (WO, A1) (58) Survey Field (Int.Cl. ⁷ , DB name) A61K 7/06

Claims (1)

(57) [Claims] (1) a molecular weight of 1,000 or more and less than 100,000;
A hair restorer comprising a mixture of hyaluronic acid and / or a salt thereof and an extract of Fuzi.