JPS59141514A - Hair tonic composition containing linoleic acid - Google Patents

Abstract

PURPOSE:A hair tonic composition, containing linoleic acid or a salt thereof, and effective for promotion of hair growth, prevention of depilation and inhibition of dandruff, itching etc. CONSTITUTION:A hair tonic composition containing lineleic acid or a salt thereof, e.g. ammonium salt, alkali metallic salt or organic amine salt, or a mixture thereof in an amount of 0.01-10wt% based on the total weight of the composition. The linoleic acid (salt) has powerful inhibitory action on testosterone-5alpha- reductase, and the depilation and fallen hair are inhibited by applying the above- mentioned composition to the human scalp or animal skin. The downy hair becomes healthy, and the growth speed of the hair is remarkably increased.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a hair nourishing composition which entirely contains a linoleic acid compound and is effective in promoting hair growth, preventing hair loss, suppressing dandruff, itching, and the like.

Bushy hair all your life? , is a common desire of humankind. Although various hair nourishing compositions have traditionally been used to prevent and treat hair loss, suppress dandruff, and itching, the causes and mechanisms of these symptoms have not been fully elucidated. Is it possible to suppress hair loss and grow hair? No drug has yet been found that is truly effective in promoting dandruff and suppressing dandruff and itching.

Did the inventors create a truly effective hair growth composition? As a result of extensive research aimed at developing linoleic acid, its salts, or a mixture thereof, it has been found that linoleic acid, its salts, or a mixture thereof has extremely effective hair nourishing and hair growing effects.
Furthermore, he discovered the surprising fact that it also suppresses dandruff and itching, and based on this knowledge he invented this invention. completed.

In other words, in order to develop a hair nourishing composition based on truly scientific grounds, the inventors aimed to, first of all, achieve healthy hair. Who has it and who has unhealthy hair such as dandruff, itching, and abnormal hair loss? As a result of a detailed comparison of the microflora in the scalps of those with the disease and those with the disease, it was found that in the scalp of those with the disease, Staphylococcus cavitis
Capiti! i) alone for the most part? We obtained a completely new finding that the bacterial cells of this species, the treated bacterial cells, etc., were applied to the scalp, and a remarkable hair-nourishing effect was obtained, and this effect was caused by the lipase activity and testosterone-5α of the bacteria. −
It has been revealed that there is a close relationship with the inhibitory activity of reductase (an enzyme that reduces testosterone to 5α-dihydrotestosterone, hereinafter abbreviated as 5α-reductase). , the inventors have determined that the lipase activity and 5α-
While examining in detail the relationship between reductase inhibitory activity, hair growth, and hair-nourishing effects, we looked at the fatty acids produced when the lipase of Staphylococcus cavitis is applied to fats and oils. Does the product have strong 5α-reductase inhibitory activity? It has been found that the fatty acid-containing substance itself also exhibits a hair-nourishing effect. The inventors further investigated the active ingredients in fatty acids? As a result of their pursuit, they obtained the surprising finding that linoleic acid, a type of fatty acid, or its salt has a strong 5α-reductase inhibitory activity and also exhibits a hair-nourishing effect, leading to the completion of this invention.

In addition, JP-A-56-61308 describes zinc pyrithione and specific carboxylic acid compounds. A hair treatment composition for preventing dandruff and itching is described, but there is no mention of linoleic acid, and the specific carboxylic acid has an extremely mild effect on the human body.
It is only stated that the fatty acid has 5α-reductase inhibitory activity and does not cause any harmful irritation to the eyes or skin. There is no suggestion that it has. Also, Special Table 57-50216
No. 6 Vcfl, a hair treatment agent containing a combination of betaine and an aliphatic organic acid is described, but linoleic acid is not mentioned as the aliphatic organic acid, and furthermore, this hair treatment agent (already fC) Good brushability for hair without damaging the hair? It is only described that it has effects such as hair growth, but there is no mention of a hair-nourishing effect.

As an active ingredient of this invention, linoleic acid can be mentioned. However, not only linoleic acid itself, but also various acceptable salts thereof can be used in hair nourishing compositions. These salts include salts with inorganic substances and salts with organic bases. Included are salts with inorganic substances, ammonium salts, alkali metal salts such as lithium salts, potassium salts, sodium salts, and salts with alkaline earth metals such as aluminum salts. Salts with organic bases include salts with various organic amines. These linoleic acid and its various salts can be used alone or in any combination of two or more. or,
Other compounds having 5α-reductase inhibitory activity, such as arachidonic acid, n-caprylic acid, n-capric acid, lauric acid, noglumitic acid, palmitoleic acid, lylunic acid, stearic acid or eicosenoic acid or their salts, etc. They can also be used in combination.

Since linoleic acid and its salt, which are the active ingredients of this invention, are not toxic to the human body, the amount added to the hair growth composition is not particularly limited and can be selected from a wide range. It is preferably in the range of 0.01 to 10% by weight based on tIc. When using linoleic acid and its salts of class 2α or higher, or a combination of these and other active acids, such as the aforementioned fatty acids or salts thereof, the total amount should be 0.0% relative to the total amount of the composition. It is preferable to set it as 01-10 weight t%.

As the base material used in the hair nourishing composition of this invention, any base material commonly used in cosmetic compositions can be used, such as distilled water, ethanol, etc. Polyhydric alcohols such as ethylene IJ:71, 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 side-lighting hormones, vitamins, amino acids, herbal medicine extracts, photosensitive pigments, resorcinol, menthol, humectants, and numbering agents. In particular, fatty acids such as linoleic acid are easily oxidized, so add oxidizing fat inhibitors such as tocopherol to 1 to 1
It is preferable to contain 0 times the amount.

The hair nourishing composition of the present invention can be in the form of commonly used dosage forms such as hair tonics, hair lotions, hair creams, shampoos, conditioners, pomades, and aerosols.

Next, the effects of this invention will be explained together with the estimated mechanism of action.In addition, the mechanism of occurrence of hair loss etc. and the hair growth mechanism of the hair growth composition of this invention, which will be briefly described below, are based on experimental grounds. This is an accompanying assumption, but even if hair loss, etc. is due to other mechanisms, and 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, nor does it limit the technical scope of this invention.

There are various theories regarding the causes of hair loss, hair loss, dandruff, and itching, including hormonal imbalance theory, nutrition-related theory, seborrhea theory, and genetic theory. It is probably certain that there is a high correlation with development [
Masumi Inaba, Mainichi Life, November 1981 issue, 26-3
5 pages; Latest Cosmetic Science, 130 pages (published by Yakuji Nipposha), 1981; Kenji Adachi et al., Biochemical
andBiophysical Re5each C
communication 41(4) 884-8
90 (1970); Susumu Takayasu et al., Journal
of InvestigativeDermotol
ogy 24 pp. 187-189 (1980)].

In other words, when the sebaceous glands in the head become enlarged due to nutrients, hormones, etc., the 5α-1 noductase present in these glands converts testosterone into the more powerful 5α-dihydrotestosterone, which is then transferred to the blood vessels. It then transfers to the dermal papilla through the hair follicle, suppresses the activity of adenine cyclase in the hair matrix cell, and delays the division of the hair matrix cell.As a result, the hair follicle gradually regresses, and the hair becomes finely thickened in this hole, leading to baldness. It is believed that this has occurred.

Considering the mechanism of hair pulling, hair loss, etc. as a basis, 5α-reductase inhibitory activity is an important attribute that hair nourishing compositions should have, and it is important to scientifically evaluate the effects of hair nourishing compositions. This serves as one standard for evaluation.

Linoleic acid and its salts, which are the active ingredients of the hair nourishing composition of this invention, have a strong 5α-reductase inhibitory effect as described above, and the hair nourishing composition of this invention exhibits a strong hair nourishing effect. This is thought to be due to the mechanism described above, but linoleic acid and its salts actually control the microflora of the scalp in a favorable state, and these act together or synergistically to promote strong hair growth. It is considered to be effective.

The hair nourishing composition of this invention? Does it have a strong hair growth effect when applied to human scalp or animal skin? Demonstrate.

Namely, the composition of this invention? When applied to the scalp, hair pulling and hair loss are suppressed, downy hair becomes healthy, and the growth rate of the father's hair increases markedly. It also suppresses the occurrence of dandruff and prevents itching. When the cosmetics of this invention are applied to animals, the rate of hair growth increases significantly. The hair growth product of this invention has no safety problems for humans and animals. That is, linoleic acid and its multiple salts were each dispersed in a separate base (alcoholic water bath solution) and applied to each of these 25 domestic rabbits once a day for 3 days, and a control in which only the base material was applied. As a result of comparison, no abnormalities were observed.

In the present invention, 5α-reductase inhibitory activity was measured by the following method.

A specimen of testosterone 5α-reductase is prepared by crushing rat statutornic gland cells and isolating all microsomes from the crushed liquid. 5α from testosterone by this enzyme specimen
- Conversion to dihydrotestosterone is followed using radioeitope-labeled testosterone.

After the reaction was completed, it was extracted with ethyl acetate, and subjected to silica gel thin layer chromatography (solvent system: dichloromethane: cyclohexane: acetonate 5:4:1) and double development using TLC to determine the amount of testosterone and 5α-dihydrotestosterone.
Determined from radioactivity intensity.

(Reaction) 0.05M phosphate buffer (0, containing IMBSA, pH 6,
6) 10μt of 3oμt1 enzyme preparation, Label Tothystste+:+Na, 5pmol, Reduced NADP 50nm
ol, and 10 μtf of the measurement sample to make a total volume of 50 μL.
shall be. This was allowed to react at 25°C for 60 minutes. After the reaction was completed, 200 μtf of ethyl acetate was added to the reaction solution for extraction, and the extraction was carried out as described above.
The measurement of radioisotope 1 is determined by VC.

The above measurements are performed on samples at various concentrations, and the 5α-reductase inhibitory activity is determined as 1IC5o (concentration that inhibits 5α-reductase activity by 250%).

In this measurement, the 5α-reductase inhibitory activity I Cso of linoleic acid was 0.16 mM.

EXAMPLES 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 tonic ingredient content (weight%) 95
%ethanol 50 castor
Oil 2 tocopherols 0.1 fragrance
0.5 linoleic acid
0.05 Distilled water The total value is 100.

(2) Hair loss: φ-tearic acid 5 Secnor 0.5 Glycerin 5 95% ethanol 10 Tocopherol 0.1 Fragrance
Monosodium linoleate
0.5 distilled water
The whole number is 100.

(3) Hair cream liquid paraffin 36 nuts
Row
5 Lanolin
3waseli
5 Ammonium linoleate 0.5 Polyethylene glycol 1 Tocopherol 0.1 Distilled water The total is 100.

(4) Sodium shampoo alkyl ether sulfate 16 Lauric acid jetanolamide 4 Propylene glycol 2 Cetyl alcohol 1 Preservative 9 Colors and fragrances
1 phosphoric acid

0.05 arachidonic acid 0.
05 Distilled water The total value is 100.

(5) Aerosol polyoxyethylene lanolin 1.
0 Lanolin alcohol 2.5 Glycerin fatty acid ester 0.5 Tocopherol 0.1 Fragrance
Material 0.2 Linoleic acid 0.05 Denatured alcohol (anhydrous) 25.7
'5 (6) Pomade Mori Row
12 castor oil
84.6 hardening
Oil 2 tocopherol 0.2 linole acid
1.0 fragrance
0.2 Example 2. (Usage example) Example 1. The bear tonic prepared in (1) is used for boys (ages 28-4) who have unhealthy hair with a lot of dandruff or hair loss.
0) When 2 to 4 doses of the drug were administered to each of 10 people once a day for 6 months, the results shown in Table 1 below were obtained.

Table 1 Examples & Use on domestic rabbits The hair on the back of a male rabbit (10 weeks old) was shaved, and the hair was applied to this area twice a day.Example 1. One coat of (1) Artonic was applied to the hair, and the length of the hair elongated over two weeks was measured. As a control, linoleic acid was replaced with distilled water.

The results are shown in the table below.

a: Control side hair length average value (frrIn) standard deviation a':
Test side hair length average value (inertia) Standard deviation: Test side hair length average value - control side hair length average value (厘) *1: Average of control side hair length average value *2: Test side hair length average value Average patent applicant Suntory Ltd. Patent agent Akira Aoki Patent attorney Kazuyuki Nishidate Patent attorney Fukumoto Akira Yamaguchi Procedural amendment (voluntary) March 23, 1980 Commissioner of the Japan Patent Office Young Kazuo Sugi 1, Indication of the case Patent Application No. 14555 of 1982, 2 Name of the invention: Linoleic acid-containing hair nourishing composition 3, Relationship with the Ministry case making the amendment Name of patent applicant (190) Suntory Shares Company 4, agent address Seiko Toranomon Building, 8-10 Toranomon-chome, Minato-ku, Tokyo 105 Phone number 504-07215 Column 6 of "Detailed Description of the Invention" of the specification to be amended, Contents of the amendment■ Details 6th page, lines 18-19, "1 to 10 times amount" is corrected to "1 to 1/10 times amount".

■ Page 8, line 1 rReach J f lr
Correct to Re5search Jl.

■ Page 8, line 4 [Dermotolog] r 2
Pages 4187-189” Dermalogy 7
4 pages 187-191”.

■ On page 8, line 13, "It is said to be complete." is corrected to "It is determined to be complete."

■ Page 10, line 12 r5:4:IJ is “15:4
:1”.

■ Delete "testosterone and" on page 10, line 13.

of page 10, line 16 r 0. Correct "I M BSA Contains" to "0°1% BSA Contains".

■ On page 11, line 3, amend "dihydrotestosterone J to j5α-dihydrotestosterone."

■ Page 12, line 9 [Tokofue'P-R0. Delete "l".

[Phase] Page 13, lines 12-13 [(po-1-oxyethylene rubitan hisquioleate) i "(po-1-oxyethylene sorbicun sesquioleate)" IICW
A Correct.

■ On page 14, line 8, "Lyl acid" is corrected to "1 nonoleic acid J'.

■ Page 14, line 17 [tocopherol 0.1Jl "Correct to tocopherol 0.01Jl.

[Phase] Page 16, line 5 from the bottom [Example 1. (1)
NOHEARTNIC JKLRO, z% linoleic content 80
Correct to chetanol solution J.

[Phase] In the table on page 17, set r9.55j in the second line from the bottom (column for average A straightness) to "*1) 9.55Jl, r 9
．． Correct 98 to ``*2) 9.98.j.

Claims (1)

[Scope of Claims] 1. A hair nourishing composition comprising all of linoleic acid, a salt thereof acceptable as a hair nourishing composition, or a mixture thereof. 2. The content of linoleic acid or a salt thereof acceptable as a hair nourishing mg product, or a mixture thereof is 0.01 to 10% by weight based on the total amount of the hair nourishing composition, according to claim 1. Hair nourishing composition.