JPH0460446B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a hair growth composition containing a linoleic acid component and an oleic acid component, which is effective in promoting hair growth, preventing hair loss, suppressing dandruff, itching, and the like. It is a common desire of all human beings to have thick hair throughout their lives. Although various hair nourishing compositions have been used to prevent and treat hair loss, suppress dandruff, and itching, the causes and mechanisms behind these symptoms are not fully understood. It suppresses hair loss and promotes hair growth and nourishment.
Furthermore, no drug has yet been found that is truly effective in suppressing dandruff and itching. As a result of intensive research to develop a truly effective hair nourishing composition, the inventors discovered that oleic acid or a salt thereof acceptable as a hair nourishing composition (hereinafter referred to as the oleic acid component) and linoleic acid or its salt. Salts acceptable as hair nourishing compositions (hereinafter referred to as linoleic acid components)
The present inventors have discovered the surprising fact that a mixed fatty acid component comprising the following has an extremely effective hair-nourishing and hair-growth effect, and also suppresses dandruff and itching, and based on this knowledge, they have completed this invention. In other words, in order to develop a hair nourishing composition based on truly scientific evidence, the inventors first focused on those with healthy hair, and those with less-than-healthy hair, such as those with dandruff, itching, or abnormal hair loss. As a result of a detailed comparison of the microbiota in the scalps of individuals with the former's scalp, we obtained a completely new finding that Staphylococcus capitia alone accounts for the majority of the scalp of the former. When applied to the scalp, the bacterial cells of the bacterial species, the treated bacterial cells, etc. have a remarkable hair-nourishing effect, and this effect is due to the lipase activity and testosterone-5α-reductase (reducing testosterone to 5α-dihydrotestosterone) of the bacteria. 5α-reductase (hereinafter abbreviated as 5α-reductase) has a close relationship with the inhibitory activity of 5α-reductase (Patent Application No. 110395, 1982). The inventors have discovered that the lipase activity and 5α-reductase inhibitory activity, hair growth,
While examining in detail the relationship with the hair-nourishing effect, we found that a substance whose main component is fatty acids produced when the lipase of Staphylococcus capitis acts on fats and oils has a strong 5α-reductase inhibitory activity. It was discovered that the fatty acid-containing substance itself also exerts a hair-nurturing effect (1981).
7463 patent application specification). In addition, as a result of pursuing the active ingredients in fatty acids, we found that linoleic acid, oleic acid, arachidonic acid, n-capric acid, n-caprylic acid, lauric acid, myristic acid, palmitic acid, stearic acid, linolenic acid,
It has been revealed that parinaric acid, petroselic acid, palmitoleic acid, or salts thereof that are acceptable as hair-growth compositions have strong 5α-reductase inhibitory activity and exhibit hair-growth effects. (1981 No. 14555, 58-24687, 58-
No. 24686, No. 58-45292, and No. 58-45293 patent application specifications). The inventors further considered that since fatty acids are effective in preventing or alleviating dandruff and itching, fatty acids act effectively against inflammation that causes dandruff and itching in the scalp. Certain fatty acids are said to have an inhibitory effect on cyclooxygenase, which is said to be involved in inflammation.
Regarding various fatty acids and mixtures thereof,
As a result of research on 5α-reductase inhibitory activity, cyclooxygenase inhibitory activity, hair growth effect, dandruff, and anti-itch effect, we found that the amount of oleic acid or its salt (oleic acid component) is 80 to 99.9%.
A mixture of two types of fatty acids or their salts in which the amount of linoleic acid or its salt (linoleic acid component) is 0.1 to 20% by weight, and a mixture of this mixture and other types of fatty acids or their salts are most effective. The present invention was completed based on the discovery that it inhibits the activities of 5α-reductase and cyclooxygenase, and is effective in preventing or alleviating dandruff and itching, and in promoting hair growth. In addition, JP-A-56-61308 discloses a commonly used dandruff, which is made of zinc pyrithione and a cationic surfactant.
An anti-dandruff and itch-preventing hair treatment composition is described in which a specific carboxylic acid compound is blended into the itch-preventing hair treatment composition, and the active ingredient for preventing dandruff and itch is zinc pyrithione;
Cationic surfactants have the effect of making hair soft and supple, and carboxylic acid compounds are only described as having the effect of alleviating the strong irritation to the eyes and skin caused by the above substances, and fatty acids are It not only has 5α-reductase inhibitory activity and cyclooxygenase inhibitory activity, but also
There is no suggestion that it has a hair-nourishing effect. Further, JP-A-57-502166 describes a hair treatment containing a combination of betaine and an aliphatic organic acid, but the fatty acid of this invention is not mentioned as the aliphatic organic acid. Moreover, it is only stated that this hair treatment agent has the effect of imparting good brushing properties to the hair without damaging the hair (that has already been formed), and there is no mention of any effect on hair growth. do not have. In addition to the above-mentioned oleic acid component and linoleic acid component, the mixed fatty acid component that is the active component of the hair nourishing composition of this invention includes other fatty acids that have 5α-reductase inhibitory activity and cyclooxygenase activity, such as n- Capric acid, n-caprylic acid, lauric acid, myristic acid, palmitic acid,
Linolenic acid, parinaric acid, petroselic acid, palmitoleic acid or eicosenoic acid, or salts thereof, etc. can be optionally contained. Since the mixed fatty acid component which is the active ingredient of the hair nourishing composition of this invention is not toxic to the human body, the amount to be added to the hair nourishing composition is not particularly limited and can be selected from a wide range. for the total amount of
It is preferably in the range of 0.01 to 10% by weight. As the base material used in the hair growth composition of this invention, any base material commonly used in cosmetic compositions can be used, such as distilled water, monohydric alcohols such as ethanol, glycerin, ethylene glycol, etc. Polyhydric alcohols, oils and fats, surfactants, etc. can be used. The hair nourishing composition of the present invention may contain various known ingredients used in conventional hair nourishing compositions and hair styling compositions, as long as the effects of the composition of the present invention are not impaired. Examples of the ingredients include hormones, vitamins, amino acids, crude drug extracts, photosensitive pigments, resorcinol, menthol, humectants, fragrances, and the like. The hair nourishing composition of this invention includes hair tonic, hair lotion, hair cream, shampoo,
It can be in conventional dosage forms such as rinses, pomades, aerosols, etc. Next, the effects of this invention will be explained together with the estimated mechanism of action. The mechanisms of occurrence of dandruff, itching, hair loss, etc., and the hair growth mechanism of the hair growth composition of this invention, which will be briefly described below, are estimates based on experimental evidence. Even if the hair growth effect of the hair growth composition of this invention is due to other mechanisms, this does not negate the effects of this invention. The technical scope of the invention is not limited. There are various theories regarding the causes of hair loss, hair loss, dandruff, and itching, including hormonal imbalance theory, nutrition-related theory, prolapse theory, and genetic theory.Although it is not confirmed, in any case, it is related to the development of sebaceous glands. [Masumi Inaba, Mainichi Life, November 1981 issue, pp. 26-35; Latest Cosmetic Science,
130 pages (published by Yakuji Nippo), 1981; Kenji Adachi et al., Biochemical and Biophysical Research
Communication 41 (4) 884-890 (1970); Susumu Takayasu et al., Journal of Investigative
Dermatology 74 pp. 187-191 (1980)]. In other words, when the sebaceous glands on the head become enlarged due to nutrients, hormones, etc., the 5α-reductase present in the glands converts testosterone into the more powerful 5α-dihydrotestosterone, which is then transferred to the dermal papilla via blood vessels. It inhibits the activity of adenyl cyclase in hair matrix cells and delays the division of hair matrix cells, resulting in gradual regression of hair follicles, which causes the hair to become fine and unkempt, leading to baldness. has been done. Furthermore, it is thought that inflammation occurs due to some kind of irritation, resulting in dandruff and itching, and the accumulation of sebum secreted by sebaceous glands on the scalp is also thought to be a cause of irritation. Inflammation is thought to involve substances produced by the arachidonic acid cascade. In the cell, arachidonic acid released from the cell membrane due to stimulation is converted to prostaglandin _G2 by cyclooxygenase, and further converted to prostaglandin G2 by endoperoxidase.
The hydroxyl radicals generated at this _time are considered to be the cause of inflammation. In addition, prostaglandin _G2 itself is said to be a cause of inflammation (Hajime Fujimura, Recent Medicine, Vol. 38).
Vol., pp. 2226-2232, 1983). Considering the mechanisms of occurrence of dandruff, itching, hair loss, etc., 5α-reductase inhibitory activity and cyclooxygenase inhibitory activity are important attributes that a hair nourishing composition should have. It serves as a standard for scientifically evaluating the effects of The hair nourishing composition of this invention, which is a mixture of two types of fatty acids, oleic acid and linoleic acid, or their salts, or a mixture of this with other types of fatty acids or their salts has a strong 5α-reductase inhibitory effect as described above. The hair-growth composition of the present invention has a strong dandruff and itch-suppressing effect and a hair-growth effect, which is thought to be due to the above-mentioned mechanism. A mixture of two fatty acids or their salts according to the invention,
Alternatively, a mixture of this and other types of fatty acids or their salts can control the microflora of the scalp in a good condition, and when these are combined or synergized, they exert a strong dandruff and itch control effect and a hair-nourishing effect. it is conceivable that. When the hair growth composition of this invention is applied to human scalp or animal skin, it exhibits a strong hair growth effect. That is, when the composition of the present invention is applied to the scalp, hair pulling and hair loss are suppressed, downy hair becomes healthy, and the rate of hair growth is significantly increased. Also, the occurrence of dandruff is suppressed and itching is prevented. Furthermore, when the cosmetic of the present invention is applied to animals, the rate of hair growth increases significantly. The hair growth composition of this invention has no safety problems for humans and animals. That is, the fatty acid and its plurality of salts of the present invention were each dispersed in separate base materials (aqueous alcohol solutions), and these were applied to five domestic rabbits once a day for three days, and only the base material was applied. As a result of comparison with the control, no abnormalities were observed. In the present invention, 5α-reductase inhibitory activity and cyclooxygenase inhibitory activity were measured by the following method. 1 Measurement of 5α-reductase inhibitory activity Rat prostate cells are disrupted and microsomes are separated from the disrupted solution to prepare a specimen of testosterone 5α-reductase. The conversion of testosterone to 5α-dihydrotestosterone by this enzyme preparation is monitored using radioisotope-labeled testosterone. After the reaction is complete,
Extract with ethyl acetate, double develop using silica gel thin layer chromatography (solvent system dichloromethane: cyclohexane: acetone = 15:4:1),
The amounts of 5α-dihydrotestosterone and 5α-androstane-3,17-diol (hereinafter abbreviated as Adeol) are determined from the radioactivity intensity. (Reaction) 0.05M phosphate buffer (PH6.6) 30μ, enzyme preparation
1.6 unit (1 unit is the amount of enzyme that reduces 1 pmol of testosterone per hour), labeled testosterone
Mix 8.5 pmol, reduced NADP, 50 nmol, and the measurement sample to make a total volume of 50μ. This at 25℃
Allow to react for 60 minutes. After the reaction is completed, 100 μl of ethyl acetate is added to the reaction solution for extraction, the extract is developed as described above, and the amount of 5α-dihydrotestosterone and adéol produced is determined by measuring the amount of radioisotope using a scintillation counter. The above measurements are performed on various concentrations of two fatty acid mixture samples of oleic acid and linoleic acid at various mixing ratios, and the 5α-reductase inhibitory activity is determined as ID ₅₀ . 2 Measurement of cyclooxygenase inhibitory activity As the enzyme, sheep seminal vesicle gland microsomal enzyme (manufacturer code: A-3, RAN Chemical Company, Israel) was used. Cyclooxygenase activity was measured by the oxygen absorption method described below. Enzyme absorption of the reaction solution is
The measurement was carried out using a 3.2 ml reaction tank (Ishikawa Seisakusho, Tokyo) equipped with a DG-G-5 type enzyme electrode (Ishikawa Seisakusho, Tokyo). The reaction tank is maintained at 30°C using a constant temperature circulation tank (Neslab, Endocal RTE-9). The reaction solution (3.2ml) was Tris-HCl buffer (0.1M, PH8.0)
3.1 ml, containing 1 mg of ovine seminal vesicle microsomes, hemoglobin (0.25 μM), L-tryptophan (10 mM) and arachidonic acid (21.8 μM).
The reaction is initiated by the addition of arachidonic acid. The test preparation was dissolved in 50μ of ethanol and added 5 minutes before the start of the reaction. The initial velocity is determined from the straight line part of the oxygen absorption curve on the recording paper. The above measurements were performed on various concentrations of two types of fatty acid mixture samples with various mixing ratios, and the cyclooxygenase inhibitory activity was determined as _ID50 .

[Table] As is clear from the above results, when oleic acid and linoleic acid are mixed within the above ratio range, the inhibition of 5α-reductase is equal to or greater than when these fatty acids are used alone. Inhibition of cyclooxygenase is most potent with linoleic acid alone and weaker with oleic acid alone.
However, since linoleic acid is a polyunsaturated fatty acid, it is easily oxidized, and if it is used alone as a fatty acid component, it may be difficult to store the hair nourishing composition for a long period of time. Therefore, it is preferable to mix this with oleic acid so that the amount of linoleic acid is 20% by weight or less based on the entire mixed fatty acid composition. Further, as mentioned above, since the cyclooxygenase inhibitory activity of oleic acid is weak, it is preferable that the amount of linoleic acid is 0.1% or more based on the entire mixed fatty acid composition. Next, Examples will be described to explain the hair growth composition of the present invention and its effects. Example 1 (Example of formulation of hair nourishing composition) A hair nourishing composition having the following composition was prepared. (1) Hair lotion ingredients Contents Oleic acid 98% by weight Linoleic acid 2 Mixture 0.5g L-menthol 0.1g 95% ethanol 74ml Distilled water Total volume is 100ml (2) Hair lotion ingredients Contents Oleic acid Linoleic acid Palmitic acid 98% by weight 2 〃 1 〃 Mixture 0.2g Propylene glycol 3g Tocopherol 0.05g Flavor Appropriate amount 95% ethanol 50ml Distilled water Make the total volume 100ml. (3) Hair cream ingredients Contents Oleic acid 99% by weight Linoleic acid 1 Mixture 0.5g Liquid paraffin 45g Beeswax 5g Lanolin 3g Vaseline 5g Emulsifier (polyoxyethylene sorbitan sesquiolate) 2g Propylene glycol 5g Fragrance Appropriate amount of distilled water The volume should be 100ml. (4) Pomade ingredients Contents Oleic acid Linoleic acid Palmitic acid 98% by weight 1 〃 1 〃 Mixture 0.5g Japanese wax 12g Castor oil 87.5g Tocopherol 0.1g Fragrance Appropriate amount (5) Rinse ingredients Content Oleic acid 99% by weight Linole Acid 1 Mixture 0.2g Stearyltrimethylammonium chloride 2g Cetyl alcohol 1g Glyceryl monostearate 0.5g Propylene glycol 5.5g Fragrance/preservative Appropriate amount of distilled water 80ml Example 2 (Example of use) Use the hair tonic prepared in Example 1 to treat dandruff and itching. , boys with unhealthy hair that pulls out a lot (age
24 years old to 49 years old) 1 to 2 times per day for each 11 people
When an appropriate amount of the product was rubbed on the head twice for 4 weeks, the following results were obtained.

[Table] Example 3 (Effect on domestic rabbits) The hair on the back of a male rabbit (2 months old) was shaved off,
Twice a day, drop a small amount of a 0.2% ethanol solution of a mixture of 98% oleic acid, 1% linoleic acid, and 1% palmitic acid in this area and rub it in with your fingertips. The length was measured. An ethanol solution containing no fatty acids was used as a control. The results are shown in the table below. The numbers in the table are a: Average hair length on the control side (mm) ± standard deviation a': Average hair length on the test side (mm) ± standard deviation b: Average hair length on the test side - Hair length on the control side Average value (mm) *1: Average of the average hair length on the control side *2: Means the average hair length on the test side.

【table】

【table】

Claims (1)

[Scope of Claims] 1. A mixed fatty acid component comprising oleic acid or a salt thereof acceptable as a hair nourishing composition and linoleic acid or a salt thereof acceptable as a hair nourishing composition; The blending amount of the oleic acid or its salt is 80 to 99.9% by weight, and the blending amount of linoleic acid or its salt is 0.1 to 20% by weight.
A hair nourishing composition characterized by: 2. The hair nourishing composition according to claim 1, wherein the total amount of the mixed fatty acid component is 0.01 to 10% by weight based on the total amount of the hair nourishing composition.