JP2003012509A - Ski care preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a skin care preparation capable of expressing no remarkable adverse effects to living bodies, expressing excellent promotion of skin functions by advance action of skin function and hair root cells and excellent hair raising and growing effects. SOLUTION: This skin care preparation contains friedelin and/or an extract of a friedelin-containing plant, e.g. the extract obtained from one or more species of plants selected from cork, apple, grape fruit lemon, lime and the like.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to friedelin, which has no significant side effects on the living body such as hormone preparations, and has excellent skin function-improving action and hair-growing / hair-promoting effect by promoting skin function and hair root cells. And / or a skin-containing external preparation in which an extract obtained from a plant containing friedelin, for example, a plant such as cork, apple, grapefruit, lime, and lemon is distributed as an essential component.

[0002]

2. Description of the Related Art Skin aging prevention, whitening action for the prevention and treatment of spots and freckles, and hair growth and nourishing action by maintaining and enhancing the functions of the scalp and hair root. Many researches have been conducted on various cell active ingredients such as flow enhancers, and various medicinal ingredients have been tried and blended. However, there are still few that are particularly effective and highly safe,
At present, most of the ingredients that are said to have a medicinal effect are only expected to have a preventive effect if the effectiveness is objectively evaluated.

[0003]

DISCLOSURE OF THE INVENTION The present invention is excellent in safety and stability, and has a whitening effect by promoting the function of the skin and a therapeutic effect for alopecia due to hair-growth and hair-growth effects and no hair loss. It was carried out for the purpose of developing an external preparation for skin which has an excellent preventive effect on humans and also has an promoting effect and a skin aging preventing effect.

[0004]

The external skin preparation of the present invention comprises
Extracts obtained from one or more plants selected from plants containing friedelin and / or friedelin as a skin external preparation base, for example, plants such as cork, apple, grapefruit, lime and lemon (plant extract) The external preparation for skin is characterized by containing as an essential component. In addition, the external preparation for skin of the second aspect of the present invention comprises, in addition to friedelin and / or a plant extract containing friedelin, other ingredients known to be further compounded in the external preparation for skin. It is characterized by. Friedelin is a colorless crystalline substance, which is a compound widely belonging to the plant kingdom and belonging to the triterpenoids. Examples of the plant containing a large amount of friedelin include cork layers of beech plants such as cork oaks and abemakis, citrus peels such as grapefruit, lime and lemon, and leaves.

[0005]

DETAILED DESCRIPTION OF THE INVENTION Friedelin used in the present invention may be commercially available. Alternatively, it may be extracted and purified from a plant containing friedelin,
Furthermore, an extract containing friedelin from a plant can be used as it is, or an appropriately purified or concentrated extract can be used. Examples of plants used for the extraction of friedelin include plants containing friedelin, for example, bark such as cork oak or abemaki with developed cork or cork layer, or leaves such as lime, lemon, grapefruit, fruits, etc. It is not limited to these. Further, when Friedelin is added to the hair-growth base, it is not always necessary to purify Friedelin,
The extract may be directly added to the hair-growth base. In addition, if necessary, an extract that is obtained by concentrating the extract may be added. Furthermore, when blending friedelin or an extract containing friedelin into a skin external preparation base, it does not necessarily have to be a single plant, and two or more plants may be used in combination as an extracted plant raw material, and each plant You may use together the extract from if necessary.

Friedelin, which is a component of the present invention, has never been used in medicines, quasi drugs or cosmetics, and the action of Friedelin is not known. Friedelin is a colorless crystal, has almost no odor, and is hardly soluble in water, but soluble in ethanol, ether, and chloroform. Friedelin is also soluble in propylene glycol, 1,3-butylene glycol, ethanol, liquid paraffin, higher alcohols, oils and fats, which are base components used in medicines, quasi-drugs or cosmetics, and liquids, creams and emulsions. It is possible to make various dosage forms such as. Friedelin used in the present invention may be chemically not Friedelin itself but a derivative such as Friedelin benzoate, or may be a sugar-bound form.

Solvents used to extract friedelin from plants containing friedelin include lower alcohols such as methanol, ethanol, isopropanol and butanol, polyhydric alcohols such as propylene glycol and 1,3-butylene glycol, chloroform, benzene, and the like.
Hydrocarbon solvents such as diethyl ether and toluene may be mentioned, but two or more kinds selected from these may be mixed and used. Although these solvents are used as the extraction solvent, the obtained extract may be directly used as the extract of the present invention, or a concentrate obtained by distilling the extraction solvent may be used, and if necessary. You may use the extract obtained by refine | purifying with methanol, ethanol, etc. Extraction at room temperature,
Moreover, you may heat and heat and may extract. When the plant is extracted with these solvents, the plant may be in a raw state, but a semi-dried or dried form is preferable.

The blending amount of friedelin in the present invention is
The amount used as an external preparation for skin is 0.00 based on the total amount of the composition, although it depends on the base used, the dosage form and other components.
001 to 10% (% by weight, the same applies hereinafter), preferably 0.
It can be added in a proportion of 0001 to 1%. Friedelin used in the present invention can also be used in a state of freederin or an extract containing friedelin obtained by extracting from a commercial reagent or a plant containing friedelin. When used in the state of an extract containing friedelin, the blending amount is 0.000 as friedelin.
It is possible to use an amount of the extract which results in a blending concentration of 01 to 10%, preferably 0.0001 to 1%.

Next, an extraction example of the present invention will be given, but the extraction example is not limited to this. Extraction Example 1 A new cork stopper to be used as a stopper for a container such as a bottle is crushed, washed with water and dried, and then about 2 L of benzene is added to 1000 g of the cork, followed by extraction for 5 hours by a conventional method in a hot water bath. Benzene is distilled off from the obtained extract to obtain a cork extract. Ethanol was added to this extract, and the resulting crystal was collected by filtration, washed with water to remove water-soluble components, and suction filtered. The obtained crystallized product was recrystallized from ethanol and had a melting point of about 263.
Needle crystals of Friedelin at ℃ are obtained.

Extraction Example 2 The peel of grapefruit is washed with water, dried in the shade,
Chloroform is added to the obtained dried fruit skin, and the mixture is allowed to stand at room temperature for 3 days to obtain a chloroform extract. Chloroform was distilled off under reduced pressure, and ethanol was added to the remaining substance and the mixture was filtered to obtain a Friedelin-containing extract.

The details of the action of friedelin, which is contained as an essential component in the external preparation for skin of the present invention, are unknown, but it is presumed that it affects some sort of action of enhancing skin cell / tissue function. As a result, It is presumed that it has a whitening effect and a hair growth effect.

While studying various glycosides which are one of the triterpenoids known in the pharmaceutical field, the present inventors have found that most of the Friderin group, which is one of the triterpenoids, is a drug, a quasi drug or a quasi drug. Focusing on the fact that it has not been applied or used in the cosmetics field, we have extracted and separated Friedelin from cork containing a relatively large amount of Friedelin, and as a result of further studying its effect on hair growth, as a result, it has an action of promoting skin tissue function. As a result, they have an excellent hair growth promoting action and have completed the present invention. Next, some of the experimental examples will be shown below, but the present invention is not limited to these examples.

Experimental Example 1 C which is widely used as an experimental animal for evaluating the effectiveness of hair growth action
3H mouse ♂ (6 weeks old) was completely hand pluced on the back hair.
Hair was removed by the king method (area: about 4 cm), and a 0.1 mg solution of freederin (research reagent) 0.1 mg dissolved in a 60% alcohol aqueous solution as a test solution was used as a test solution and a 60% alcohol aqueous solution as a control. Group total 1
Until hair regrowth is completed for 0 animals (5 animals per group)
200 μl was applied once a day for 25 days continuously. Twenty hairs were collected from each animal on the 13th, 15th, and 19th days from the start of application of the test solution, and the length was measured by the expansion measurement method, and the total calculation and the statistical calculation were performed. The effectiveness was examined by analysis. The results are shown in Table 1. ．

[0014] Test of difference in mean value between both groups by statistical analysis (t-test) (comparison between 1 group and 2 groups at the same time point) * indicates a significant difference at a risk rate of 5%, and ** indicates a significant difference at a risk rate of 1%.

From the results of this experimental example, it can be seen that the component according to the present invention has excellent hair growth and hair-growth effects. Although the details of the mechanism of this action are unknown, it is considered that friedelin penetrates into the skin and activates the cells of the skin and hair roots, thereby promoting hair growth.

The present inventors have generally known in the field of external skin preparations that the hair growth and hair growth effects of compositions containing friedelin or a plant extract containing friedelin, which is the active ingredient of the present invention, as essential ingredients. We examined the possibility that the effect of friedelin could be hindered by the combined use of active ingredients. That is, a substance known to have already been known to have hair-growth, hair-growth, and hair-growth effects, Sembri extract, Enmeisou extract, Kujin extract, ethinyl estradiol, 3-carboxypropyl) -trimethylammonium chloride methyl ester, 6-amino -1,2-Dihydroxy-imino-4-piperidinopyrimidine, 7-chloro-3-methyl-2H-benzo-1,2,4-thiadiazine-1,1-
The combined action with diazoxide, 2,4-diamino-6-piperidinopyrimidine-3-oxide, etc. was examined. As a result, the action of reducing the hair-growth and hair-growth effect of friedelin or friedelin-containing extract by these active ingredients is not seen, but rather a synergistic effect of enhancing the action and effect of the commonly known active ingredients is exhibited. The present invention has been completed. Further, in addition to the above-mentioned hair-growth ingredients, various vitamins, skin stimulants, anti-inflammatory agents, peripheral vasodilators and other agents commonly used in this field were also investigated, and as a result, it was found that The effect of friedelin was not diminished, and higher efficacy was observed.

Also in the second aspect of the present invention, the blending amount of friedelin is 0.0001 to 1% with respect to the total amount of the composition.
The degree is desirable, and when it is used in the state of an extract containing friedelin, the compounding amount as friedelin is 0.
It is desirable to use an amount of extract which results in a blending concentration of 0001 to 1%. 0.0001-1 as Freederin
% Extract for the external application to the skin for the external application of skin, Enmeizo extract, Kujin extract, (3-carboxypropyl) -trimethylammonium chloride methyl ester, 6-amino-1,2-dihydroxy-imino-4-
Piperidinopyrimidine, 7-chloro-3-methyl-2H
The compounding amount of -benzo-1,2,4-thiadiazine-1,1-diazoxide, 2,4-diamino-6-piperidinopyrimidine-3-oxide and the like may be 0.01 to 10%, preferably 0. 1 to 5%, and 0.001 to 0. 0 for female hormone-like components such as ethinyl estradiol.
About 1% is desirable, but not limited to these. In addition, vitamin E, vitamin B group, vitamin H and other vitamins, organic acids such as salicylic acid and lactic acid, polyhydric alcohols such as glycerin and butylene glycol, and chondroitin, which are components known to be mixed in the field of external preparations for skin. , Mucopolysaccharides such as hyaluronic acid can be used.

As a base for the external preparation for skin, it is used for aerosols, emulsions, gels, two-layer liquids, creams, etc. in addition to general alcoholic liquids usually used in this kind of field. A base can be used, and a liquid agent, an aerosol agent, an emulsion, a gel agent, a cream agent or the like can be used. In particular, a dosage form that can be applied to the head, which is the use site of the product of the present invention, is more preferable, but the dosage form is not limited to these dosage forms.

[0019]

EXAMPLES The present invention will be described in more detail with reference to Examples and Comparative Examples, but the present invention is not limited thereto. In the following examples,% indicates% by weight.

Example 1 A lotion-type external preparation for skin having excellent hair-growth and hair-restoring effects was prepared by a conventional method according to the following formulation. Cork extract obtained in Extraction Example 1 0.01% 1,3-butylene glycol 2.0% ethanol 60.0% fragrance trace water balance 100.0% in total

Example 2 A gel-type external preparation for skin having excellent hair-growth and hair-restoring effects was prepared by a conventional method according to the following formulation. Cork extract obtained in Extraction Example 1 2.0% 2,4-Diamino-6-piperidino pyrimidine-3-oxide 1.0% Pantothenyl alcohol 0.5% Glycyrrhetinic acid 0.1% Polyoxyethylene hydrogenated castor oil 1.0% Ethanol 50.0% Carboxyvinyl polymer 0.2% Aminomethylpropanediol 0.005% Water Appropriate amount Total 100.0%

Example 3 A gel-type external preparation for skin having excellent hair-growth-promoting effect was prepared by a conventional method according to the following formulation. Grapefruit extract obtained in Extraction Example 2 3.0% (3-carboxypropyl) -trimethyl ammonium chloride methyl ester 1.0% Glycyrrhetinic acid 0.1% Polyoxyethylene hydrogenated castor oil 1.0% Ethanol 30.0% Water proper amount 100.0%

Example 4: A milky liquid type external preparation for skin having an excellent hair-nourishing effect was prepared by a conventional method according to the following formulation. Grapefruit extract obtained in Extraction Example 1.0 1.0% Panthenol 0.5% Kujin extract 1.0% Glycerin 3.0% Self-emulsifying monoglycerin stearate 5.0% Oleyl alcohol 2.0% Cetanol 0 .3% Methylcellulose 0.2% Preservative Suitable amount Perfume Suitable amount Water Suitable amount Total 100.0%

Test Example A group of 5 healthy males aged 30 to 49 exhibiting the symptoms of alopecia areata is used as a group, and each skin external preparation of the following composition is administered 2 times a day.
About 3 mL each was applied once to the head for 3 months, and the results of the hair growth effect shown below were obtained. (Judgment Criteria) Three months later, the SCORE judgment method is used to measure the number of hair shafts of terminal hairs per unit area for the occurrence of new hair on the applied part, hair growth, etc. evaluated. The SCORE criteria were as follows. SCORE1: Almost no hair and only slight vellus. SCORE2: Many vellus hairs and slightly bristles are found at the hair loss site. SCORE3: There is dense vellus hair at the hair loss site, and bristles are seen in about half. SCORE4: The whole is covered with bristles, but the scalp can be seen through. SCORE5: No bald area or thinning hair is observed. The case where the rank is improved by one rank or more by the SCORE judgment is valid.

(Results) 1) The effective rate of the external preparation for skin of the present invention containing 0.01% Friedelin in the base 1 was 63.5%. 2) The effective rate of promoting hair growth of a composition containing 1.0% of (3-carboxypropyl) -trimethylammonium chloride methyl ester and 0.01% of friedelin in the base 1 is (3-carboxypropyl). From the effective rate of promoting hair growth and hair growth of a composition containing only 1.0% of trimethylammonium chloride methyl ester, 6.0
%, And the synergistic effect of Friedelin was observed.

3) The cork extract of Extraction Example 1 was added to the base material 2.
01% (as Freederin amount, the same below) and 2,4
-Diamino-6-piperidinopyrimidine-3-oxide 1.0% is effective in promoting hair growth and hair growth in a composition containing 2,4-diamino-6-piperidinopyrimidine-3.
-It was 7.2% higher than the effective rate of the hair growth promoter of the composition containing 1.0% of oxide, and the synergistic effect of the cork extract was observed. 4) Extraction liquids 3.0 and 2, which were obtained in Extraction Example 2, in the base material 3
The effective rate of promoting hair growth of a composition containing 1.0% of 4-diamino-6-piperidinopyrimidine-3-oxide is 2,4-diamino-6-piperidinopyrimidine-.
It was 7.3% higher than the effective rate of the hair nourishing / hair growth promoting agent of the composition containing 1.0% of 3-oxide, and a synergistic effect of the extract was observed.

The composition of each base used for the preparation of the hair growth-promoting agent used in the test is shown below. Base 1 unit: g Concentrated glycerin 3.0 Isopropylmethylphenol 0.3 Decaglyceryl monolaurate 0.5 Salicylic acid 0.5 Perfume Trace alcohol 40.0 Water total amount 100.0

[0028]     Base 2 units: g             Concentrated glycerin 25.0             Isopropyl methylphenol 0.3             Polyoxyethylene hydrogenated castor oil (50E.O.) 0.7             Salicylic acid 0.5             Fragrance             Alcohol 60.0             Total amount of water 100.0

[0029]     Base 3 units: g             Concentrated glycerin 2.0             Isopropyl methylphenol 0.3             Decaglyceryl monolaurate 0.5             Carboxy vinyl polymer 0.5             Triethanolamine Trace amount             Hexanediol 2.0             Fragrance             Alcohol 30.0             Total amount of water 100.0

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61P 17/14 A61P 17/14 17/16 17/16 43/00 107 43/00 107 F term (reference) 4C083 AA111 AA112 AC072 AC102 AC122 AC422 AC432 AC542 AC642 AC692 AC852 AD092 AD262 AD531 AD532 CC37 DD23 DD31 DD41 EE22 4C088 AB12 AB51 AB62 AC04 AC05 BA08 MA01 MA02 MA63 NA14 ZA89 ZA92 MA04 ZA92 MA04 ZA92 MA04 MA04 MA04 ZA04 MA04 MA04 ZA24 MA04

Claims (3)

[Claims] 1. An extract from a plant containing friedelin and / or friedelin as a skin external base, for example, obtained from one or more plants selected from plants such as cork, apple, grapefruit, lemon and lime. An external preparation for skin, which comprises the extract as defined above. 2. The external preparation for skin according to claim 1, which has hair-growth and hair-growth effects. 3. The external preparation for skin according to claim 1, wherein the external preparation for skin according to claim 1 is combined with one or more components known to be mixed in this external preparation. .