JP2008094784A - Hair growing or restoring agent - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a preparation for external use for skin, having excellent safety and stability, developing a therapeutic effect on alopecia and excellent preventive effect on a person unaffected by alopecia by the hair growing or restoring effect caused by a skin function promoting action and further exhibiting a promoting action and an antiaging action on the skin. <P>SOLUTION: The hair growing or restoring agent contains an extract of a plant of the genus Euonymus such as Euonymus alata Sieb. and Euonymus japonica Thunb. and a vitamin A compound as essential components in a base of the preparation for external use for skin and, as necessary, a compounding component to be added to such external agents. <P>COPYRIGHT: (C)2008,JPO&INPIT

Description

  The present invention relates to an extract of a plant belonging to the genus Euonymus that does not have significant side effects on a living body, such as hormone agents, and has an excellent skin function improving action and hair growth / hair-restoration effect by enhancing skin function and hair root cells. The present invention relates to a hair growth and hair nourishing agent comprising an A compound (vitamin A1, vitamin A2, and provitamin A) as an essential component.

Numerous studies on hormonal agents, blood flow promoters, various cell activation components, etc. have been conducted on hair growth and hair restoration for alopecia caused by aging skin and male hormones. Ingredients have been tried and formulated. However, there are still only a few that are particularly effective and highly safe, and most of the ingredients that are said to have medicinal properties remain effective in the prevention if they are evaluated objectively. The current situation is.
To date, there are known hair growth and hair nourishing ingredients using plant extracts (Patent Document 1) and hair nourishing agents using vitamin A compounds (Patent Document 2). Is not given.
JP-A-7-126146 JP 2001-199843 A

  The present invention is excellent in safety and stability, has a therapeutic effect on alopecia due to hair growth / hair restoration effect by promoting the function of skin, and has an excellent preventive effect for those who have not developed alopecia, It was also conducted for the purpose of developing an external preparation for skin having an promoting action and an anti-aging action on the skin.

The hair growth / hair nourishing agent of the present invention comprises an extract for the genus Nishikigi, such as Nishikigi, Masaki, Shirasaki and the like, and vitamin A1, vitamin A2, and vitamin A compounds of provitamin A, as essential ingredients. It is a feature.
The hair growth / hair nourishing agent of the second aspect of the present invention is characterized in that a substance having an anti-androgenic action and a blood circulation / blood flow promoter are further blended with a plant extract of the genus Euonymus and a vitamin A compound.

  The hair growth / hair restoration action of the genus plant extract is already known, but by using it in combination with a vitamin A compound, a more stable and superior hair growth / hair restoration effect can be obtained. The present invention can further enhance the hair-growth / hair-growth effect by the extract of the genus Euonymus and vitamin A compound by adding a substance having an anti-androgenic action and a blood circulation / blood flow promoter. Can respond to the symptoms.

The Euonymus genus plant is a member of the order of the genus Euphoridae, and is widely distributed in Japan and China, and some of them are planted as garden trees and hedges. It is a distributed woody plant. Representative species of the genus Euonymus used in the present invention include typical euonymus (Euonymus alata Sieb.), Shirasaki (Euonymus japonica Thunb.), Shirasaki (Euonymus radicons Sieb.) And its variant, Filimasaki,
Examples include Nakabasaki, Obamasaki, Himemasaki, Kawachimasaki, Kobamasaki, Otsurumasaki.

  For the extraction of the genus Euonymus plant extract of the present invention, any of the leaves, stems and roots of the genus Euonymus can be used, and these may be used alone or in combination as raw materials for extraction, and each may be separately rooted. In addition, components extracted from stems and the like may be used together as necessary. Similarly, the extracted plant which is a raw material does not need to be a single plant, and two or more kinds thereof may be used in combination such as Nishikigi and Masaki. As an extraction method, for example, it is possible to chop the whole of the stem portion of onyokigi into a semi-fluid liquid with a homogenizer and use the juice as it is or after concentrating the juice. Preferably, extract by adding a suitable solvent to a semi-fluid liquid by a plant shredded product or homogenizer, evaporate the supernatant with a freeze-dryer, and mix this component with the skin external preparation base. It is recommended to prepare hair growth and hair nourishing agents.

  As the extraction solvent, one selected from hydrophilic solvents such as water, ethanol, n-propanol, t-butanol, propylene glycol and 1,3-butylene glycol, and hydrophobic solvents such as chloroform and diethyl ether, or Two or more kinds thereof may be used alone or as a mixed solvent. Extraction may be performed at room temperature, or may be performed under heating or heating. When using the solvent extraction method, the plant body may be not only a raw plant body but also a dry body or a semi-dry body. In order to facilitate subsequent operations, the solvent extract is used after being concentrated or concentrated to dryness as necessary, but at that time, it does not affect the activity of starch and the like contained in the solvent extract as necessary. The components that appear to be precipitated may be removed by ordinary methods.

  The extract of the genus Euonymus is a weight (W) converted to a dry solid, and is blended in the hair growth / hair nourishing agent of the present invention in an amount of 0.001 to 10% (W / W), preferably 0.01 to 5% (W / W) can do.

As the vitamin A compound of the present invention,
(1) Vitamin A1 group (retinol acetate, retinol palmitate, retinol / retinal / retinoic acid and its fatty acid ester, fatty acid ether or glycoside derivative, retinoic acid tocopherol, etc.)
(2) Vitamin A2 group (dehydroretinol, dehydroretinal, dehydroretinoic acid and its fatty acid ester, fatty acid ether, glycoside derivatives, etc.)
(3) Provitamin A group (Carotenes such as β-carotene, lycopenes, cryptoxanthine, ecainenone, astaxanthin, carotenol, carotenal, carotic acid and its fatty acid esters, fatty acid ethers or derivatives such as glycosides)
Can be mentioned.
Among these, retinol acetate, retinol, and retinoic acid of vitamin A1 group are particularly effective, and each substance has the same effect as the retinol acetate of the examples. Similarly, vitamin A2 group dehydroretinol acetate, dehydroretinal and dehydroretinoic acid have the same effect. In addition, the action of provitamin A group is moderate, but as a real problem, when it is used in the long-term expectation of hair growth / hair-restoring effect in humans, it changes to active form in the skin and exhibits the same hair-growth effect. It is thought to do.

The compounding amount of vitamin A compound is a weight (W) converted to a pure component, and 0.001 to 10% (W / W), preferably 0.01 to 5% (W / W) is incorporated into the hair growth / hair nourishing agent of the present invention. Can do.
The compounding ratio of the genus Euonymus plant extract and the vitamin A compound is not particularly limited, but the compounding ratio of the genus Euonymus plant extract: vitamin A compound may be appropriately selected and used within the range of 1: 1 to 1: 500.

Although the details of the active ingredient contained in the plant extract belonging to the genus Euonymus that act as an essential component in the hair growth and hair nourishing agent of the present invention are currently unknown, sterols, flavonoids, alkaloids contained in the plant extract It is speculated that some organic compounds such as saponins, organic acids and coumarin compounds exhibit the excellent cell function promoting action of the present invention.

  It is known as a known fact that the vitamin A compound acting as an essential component in the hair restoration / hair nourishing agent of the present invention already exhibits an excellent hair restoration effect, but its action mechanism has not yet been clarified.

  As a result of many years of research and development on the action on hair root cells and skin cells in combination with various components in order to further enhance the effect of the genus plant extract, the present inventors have completed the present invention. It is a thing. The action and effect of the hair growth and hair nourishing agent of the present invention was examined on the action on skin cells and hair matrix cells using cultured cells and experimental animals. One of the experimental examples is shown below.

Experimental example The hair of the back of a C3H mouse cage (6 weeks old), which is widely used as an experimental animal for evaluating the effectiveness of hair growth, was shaved with a hair clipper and an electric shaver (area approximately 4 cm ² ). The test solution was applied 5 times a week, and the hair growth action was compared with the negative control group (after testosterone treatment, only 50% ethanol solution of the solvent was applied) as a recovery rate from hair growth inhibition by testosterone. Ten mice per group were subjected to the test (Table 1). The hair growth rate was measured about 3 times a week from the day after cutting with a digital camera (total 13 times). Print the image taken from the 15th day after haircutting on which the hair growth began to appear on the copy paper, measure the weight of the paper on the haircut portion and the weight of the paper on the haircut portion with an electronic balance, The hair growth rate (hair growth area) was calculated by obtaining the area of the hair growth portion relative to the area.
The breeding environment for evaluating the effectiveness of this hair-growth action is fluorescent lighting (AM8: 00 ~ PM20: 00) for 12 hours a day, temperature 24 ± 2 ℃, humidity 45 ± 15%. They were raised in two cages and allowed free intake of food and water. Feeding operation and water supply operation were performed once every two days, and flooring was changed twice a week.

１群は陽性対照群、２群は陰性対照群とする。２〜５群の各マウスの毛刈部位全面に、シリンジ(テルモ(株)）を用いて0.05％テストステロン溶液0.2mL塗布した。その３０分後に各試験液を0.2mL塗布した。 塗布は１日１回、原則的に午前9:00に行った。

Group 1 is a positive control group and group 2 is a negative control group. 0.2 mL of 0.05% testosterone solution was applied to the entire surface of the hair cutting site of each mouse in groups 2 to 5 using a syringe (Terumo Corp.). After 30 minutes, 0.2 mL of each test solution was applied. Application was performed once a day in principle at 9:00 am.

As a result of comparison with the negative control group (T + 50% ethanol aqueous solution) on the same day, T + 1% Masaki extract and T + 0.016% retinol acetate (BASF) showed a promoting effect, and the hair growth recovery rate was not so large. Both groups showed hair regeneration at about the same rate.
However, with T + 1% Masaki Extract + 0.016% Retinol Acetate (BASF), hair regeneration is clearly increased from the hair growth from the 15th day to the 20th day compared to the case of individual components alone. The hair growth rate was superior to the sum of both groups.

From the results of this experimental example, it is understood that the composite of both components according to the present invention has a hair growth / hair growth effect by an excellent skin function enhancing action that promotes the growth of skin and hair of the living body. The details of the mechanism of these actions are unknown, but certain active ingredients and vitamin A compounds in the plant extract of the present invention penetrate into the skin, activate skin and hair root cells, and grow hair. Promotes the development of capillaries that are greatly involved in hair follicles, or restores the function of hair follicles that have been suppressed by some male hormones by some mechanism of action, directly enhances the function of hair follicle cells, and This is thought to be due to keeping the state healthy.

In order to further enhance the hair growth / hair growth promoting effect of a hair growth / hair restoration agent comprising the plant extract of the present invention of the present invention and a vitamin A compound, the anti-male is a substance whose hair restoration effect is already known. Studies were also made on the combined action of a substance having a hormonal action and / or a blood circulation / blood flow promoter, a plant extract of the genus Euonymus and a vitamin A compound. As a result, the present inventors have shown that these known hair growth / hair restoration components have a synergistic effect of promoting hair growth / hair growth by promoting skin function, which is superior to the combination of the plant extract and vitamin A alone. As a result, the second invention was completed.
The following are exemplified as these substances.
(1) Substances having anti-androgenic activity (β-glycyrrhetinic acid and its glycosides, female hormones such as estradiol and derivatives thereof, saponin extract, etc.)
(2) Blood circulation / blood flow promoting agent (cephalanthin, cucumber extract, enamel extract, cattail extract, red pepper tincture, menthol, photosensitizer T198, etc.)
Among these, (1) β-glycyrrhetinic acid and (2) cephalanthin have particularly high synergistic effects. The effect of β-glycyrrhetinic acid is a test method in which the hair growth evaluation method itself shown in the Examples targets male pattern baldness, and it is considered that the anti-androgenic effect of β-glycyrrhetinic acid has emerged as a synergistic effect. On the other hand, the effect of cephalanthin may be to secure nutrient supply by increasing blood flow to the hair root, but since this drug itself has a variety of actions such as activation of the immune system and reticuloendothelial system, it has a true effect on hair growth. Although the mechanism of action is not yet clear, it has now been clarified that the effect of the extract of onygi and vitamin A is further enhanced by the addition.

  In addition to the above-mentioned hair growth / hair-restoring components, there are further known skin irritation mechanism components, cholinergic activity mechanism components, adrenergic inhibitory mechanism components, and vascular smooth muscle relaxation mechanism mechanisms. As a result of examining the effects of external preparations such as hair growth promotion by combining the components and the like with the plant extract of the present invention, higher effectiveness was confirmed for these components. In addition, for the purpose of increasing the transdermal absorption rate of the plant extract of the genus Euonymus, it is incorporated into the skin by combining a moisturizer, a keratin softener and a surfactant frequently used in cosmetics in the external preparation of the present invention. An increase in the effect, which seems to be due to an increase in the absorption rate, was observed.

The blending concentration of the genus Euonymus plant extract used as a hair growth and hair nourishing agent in the present invention is preferably about 0.01 to 5.0%. The blending concentration of the vitamin A compound used as a hair restoration / hair nourishing agent in the present invention is preferably about 0.001 to 5.0%. The concentration of “β-glycyrrhetinic acid” to be blended in the hair growth / hair nourishing agent in the present invention is preferably about 0.01 to 1.0%. Similarly, the blending concentration of “dipotassium glycyrrhizinate” is preferably 0.01 to 5.0%, the blending concentration of “cephalanthin” is 0.001 to 1.0%, and the blending concentration of “menthol” is desirably about 0.001 to 5.0%. The blending concentration of the “assembly extract (dry weight 1 g corresponds to 1 g of extract)” is preferably about 0.01 to 5%. The blending concentration of “ethynylestradiol” is preferably about 0.001 to 0.1%. The blending concentration of the “life-prolonging grass extract (1 g of dry weight corresponds to 1 g of extract)” is preferably 0.01 to 10.0%. The blending concentration of “bitter extract (1 g of dry weight is equivalent to 1 g of extract)” is preferably about 0.01 to 10.0%.

  As for the compounding concentration of the component known to have the effect of preventing skin aging by inhibiting the production of lipid peroxide, for example, Augon extract 0.01 to 10.0%, Vitamin E 0.1 to 5%, and Aloe extract 0.01 to 10.0% are preferable. Examples of skin moisturizers include glycerin, propylene glycol, 1,3-butylene glycol, ethylene glycol, diethylene glycol, PEG (polyethylene glycol) s, ethyl hexanediol, sugar alcohols (for example, sorbitol), mucopolysaccharides (for example, Hyaluronic acid salt, chondroitin sulfate, PCA salt, etc.) used in this type of field can be used, and the blending concentration can be in the normal range, but is preferably in the range of 0.1 to 10%. As the keratin softener, salicylic acid, urea and the like are used at a blending concentration of 0.1 to 10%. Examples of the anionic surfactant include N-lauroylglutamine hydrochloride, and examples of the nonionic surfactant include decaglyceryl monolaurate, polyoxyethylene sorbitans, polyoxyethylene hydrogenated castor oil, and the like. % Is desirable. As a base used for the hair growth / hair growth promoter of the present invention, a base cream, gel cream, ointment as well as an aqueous agent and an alcohol solvent which are bases generally used for external preparations are used. In addition to bases such as makeup cosmetics such as foundations and lipsticks, bases such as cleaning agents such as shampoos, rinses, soaps and bathing agents can be used. The excellent effect was fully recognized.

  Some examples of the present invention are shown below, but the present invention is not limited to these examples. In addition to the ingredients fried in the following examples, the external preparation of the present invention may further contain ingredients conventionally useful for skin and hair.

Example 1
A gel hair nourishing cosmetic having an excellent hair nourishing effect was prepared by a conventional method according to the following formulation.
Euonymus plant extract 1.0 (unit: g)
Retinol acetate 0.16
Dipotassium glycyrrhizinate 0.2
7-Chloro-3-methyl-2H-1,2,4-benzo 1.0
Thiadian-1,1-dioxide Life-extending herb extract 5.0
D-pantothenyl alcohol 0.2
Concentrated glycerin 2.0
Ethylhexanediol 2.0
Decaglyceryl monolaurate 0.5
Carboxy vinyl polymer 0.5
Triethanolamine appropriate amount
Perfume appropriate amount
Antioxidant Suitable amount Alcohol 30.0
Water (add water to make 100g in total) Total 100.0g

Example 2
According to the following prescription, a lotion hair nourishing cosmetic having an excellent hair nourishing effect was prepared by a conventional method.
Masaki plant extract 1.5 (unit: g)
Retinol acetate 0.16
Concentrated glycerin 5.0
Dipotassium glycyrrhizinate 0.2
Salicylic acid 0.1
Pyridoxine hydrochloride 0.1
POE hydrogenated castor oil (50 EO) 0.5
Alcohol 30.0
Perfume
Buffer amount
Antioxidant Appropriate amount Water (Add water to make a total amount of 100 ml: Same applies below) Total amount 100.0 ml
In the above, POE represents polyoxyethylene and EO represents ethylene oxide.

Example 3
According to the following prescription, a lotion hair nourishing cosmetic having an excellent hair nourishing effect was prepared by a conventional method.
Euonymus plant 1,3-butylene glycol extract 2.0 (unit: g)
Retinoic acid 0.01
Bitter extract 5.0
Urine 1.0
β-glycyrrhetinic acid 0.1
Sodium N-lauroyl glutamate 0.5
Allantoin 0.1
Perfume
Buffer amount
Antioxidant Suitable amount Alcohol 50.0
Phenoxytanol 1.0
Total amount of water 100.0ml

Example 4
Shirumasaki plant extract 0.5 (Unit: g)
Retinol 0.16
Prolonging herbal extract 5.0
(3-Carboxypropyl) -trimethylammonium
Chloride methyl ester 1.0
Concentrated glycerin 3.0
Isopropyl methyl ferryl 0.3
Decaglyceryl monolaurate 0.5
Salicylic acid 0.5
Perfume
Buffer amount
Antioxidant Suitable amount Alcohol 40.0
Total amount of water 100.0ml

Example 5
Masaki plant extract 1.0 (Unit: g)
Retinol palmitate 0.16
6-amino acid-1,2-dihydrohydroxyimino-4 1.0
-Piperidinopyrimidine
β-glycyrrhetinic acid 0.1
D-pantothenyl alcohol 0.2
Concentrated glycerin 25.0
Salicylic acid 0.5
Polyoxyethylene hydrogenated castor oil (50E.O.) 0.5
Isopropylmethylphenol 0.3
Tocopherol acetate 0.1
Perfume
Buffer amount
Antioxidant Suitable amount Alcohol 60.0
Total amount of water 1 00.0ml

Claims (6)

A hair-growth / hair-restoring agent characterized by comprising an extract of genus Euonymus and a vitamin A compound as essential ingredients in a skin external preparation base.   The hair-growth / hair-restoring agent according to claim 1, further comprising a substance having an anti-androgenic action and / or a blood circulation / blood flow promoter in the plant extract and vitamin A compound.   The hair growth / hair growth agent according to claim 1, wherein the vitamin A compound is one or more compounds selected from vitamin A1, vitamin A2, and provitamin A.   Vitamin A1 is one or more compounds selected from the group consisting of retinol acetate, retinol palmitate, retinol / retinal / retinoic acid and fatty acid esters thereof, fatty acid ethers or glycoside derivatives, and tocopherol retinoic acid The hair growth and hair nourishing agent according to claim 2.   The hair-growth / hair nourishing agent according to claim 1, wherein the plant extract of the genus Euonymus is one or more of the extract of onykigi, masaki, or shirasaki.   The hair-growth / hair-growth agent according to claim 1, wherein the mixing ratio of the genus plant extract: vitamin A compound is 1: 1 to 1: 500.