JPH02292208A - Skin cosmetic composition - Google Patents

Abstract

PURPOSE:To obtain a skin cosmetic composition which is especially effective in prophylaxis and treatment for blots and freckles by using leaves of Gymnema, leaves of Zizyphus, trunk barks, root barks, or leaves of rose trees, leaves of Pieris or Symplocos as active ingredients. CONSTITUTION:One or more components in leaves of Gymnema sylvester R. Br., and Zizyphus jujuba M.v.i.R.), trunk and root barks of Rosaceae such as apple, cherry, pear or peach tree, leaves of apple or leaves of Pieris japonica D. Don and Symplocos microca lyx), or extract therefrom with a solvent, preferably water, alcohol or their mixture, thus containing gymnemic acid, zizyphine, phlorizin, phloretic acid, asebotin or trilobatin or the like, are used as an essential component to give the subject skin cosmetic composition having excellent effect for roughened skin, itching and dandruff of scalp as well as the above- stated effects.

Description

Detailed Description of the Invention (Field of Industrial Application) This invention relates to a skin cosmetic composition, and its purpose is to create a new skin cosmetic composition (quasi-drug product) that is effective in normalizing human skin. A skin cosmetic composition that is particularly effective for the prevention or treatment of age spots, freckles, etc., including medicinal cosmetics and external skin preparations that are pharmaceuticals. The present invention relates to a skin cosmetic composition containing as an active ingredient ingredients such as the stem bark, root bark or leaves of plants of the same family, or the leaves of Asebifolia and Amashiba.

(Prior Art) Conventionally, it has been proposed to incorporate various drugs into skin cosmetics to prevent or treat age spots, freckles, etc. There are few things that are satisfying.

Until now, it has been known that hydroquinone and its derivatives are somewhat effective in preventing or treating these diseases in biological tests.

However, this sometimes causes irreproducible pigmentation as a side effect and is currently not used.

Therefore, at present, vitamin C or its derivatives, aloe extract, placenta extract, glutathione, etc., which have milder effects, are used for this purpose, but these are still not satisfactory.

In other words, these have extremely weak effects, and they also have vitamin C,
Placenta extract and glutathione had problems with stability after preparation, and aloe extract had drawbacks such as browning over time.

(Means for Solving the Problems) This invention was developed as a result of intensive research to develop a skin cosmetic composition that is effective against spots, freckles, etc. Gymnema sylvestre R.B.
r) leaves, jujube (Zixyphus jujuba)
M. v. i. R. ) leaves or apple (Malus p.
umila m. v. d. s. ), Sakura (Pru
nus glandulosa T. ), pear (Py
rus serotinaRehd. ), or stem bark or root bark of peach (Prunus persica Batsch), or apple (Malus pumila M).
．． v. d. s. ) leaves, Pieris
japonica D. Don) or Amashiba (Sy)
We have completed a skin cosmetic composition characterized by containing at least one type of leaves of Mplocos microcalyx, and discovered that it has an extremely effective effect on the prevention or treatment of age spots, freckles, etc. did.

(Structure of the invention) Gymnemasyl used in this invention
vesLre R. Br) is Gymnema sylvesta, a plant of the Asclepiadaceae family native to India.
vestreR. Br. ) and is a vegetation distributed in the tropics to subtropics from India to China.

In India, it has been used as a diabetes treatment for about 2,000 years, as described in medical texts by Ayur Beko-Ida and others.

Gymnema (Gymnema sylvestre R.
A characteristic property of Br) is that it has the property of suppressing sweetness, a fact that has been well known in India for over 2,000 years.

At the end of the 19th century, it was discovered that its main component was a substance called gymnemic acid.

Gymnemic acid is sabonin, a gluconate glycoside of hexaoxyoleanene (triterpene) that has been acylated with various acids, and many homologs exist due to differences in the type and position of the acylated acid. Are known.

Also, jujube is a plant of the buckthorn family, jujube (Ziz).
yphus jujuba M. v. i. R. ), and its seeds are widely used in Chinese medicine as the herbal medicine Dajuju to relieve acute symptoms.

This jujube (Zizyphus jujuba M.v.
．． i. R. ) leaves also contain a substance that has a sweet taste-inhibiting effect similar to gymnemic acid, and its main component is known to be zizyfin, a steroidal sabonin.

Also, Rosaceae (Rosacea I) plants, especially apple (Malus pumila M.v.i.R.),
Sakura (Prunus glandulosa T.)
, Pear (Pyrus serotinaRehd.)
, or peach (Prunus persica Bats)
It is said that there is a substance that suppresses the absorption of sugar from the intestinal tract in the stem bark, root bark, and even in the leaves of apples.The main component is phlorizin (Ph), a derivative of dihydrochalcone.
lorizin) or phloretin (phloreLi)
n) is known.

Acebi (Pieris ja
ponica D. Don), Amashiba (Symp l
ocosmicrocalyx leaves can also be effectively used in this invention. However, these have conventionally been used exclusively orally, and there have been no examples of their use as external preparations such as skin cosmetic compositions.

The inventors have conducted a series of studies to provide a new material that is effective and safe for preventing or treating age spots and freckles by incorporating these plant-derived substances into skin cosmetic compositions. He discovered this during the process and completed this invention.

To prepare skin cosmetic compositions from these plants,
It is possible to use the stem bark, root bark, or leaves as they are, either dried or without drying, but since they contain a large amount of insoluble solids such as fibers, it is possible to use the leaves after sweating or solvent extraction. If liquids are used, their concentrates can also be used more effectively.

In the case of squeezed juice, since a large amount of active ingredients may remain in the residue, it is more preferable to use it after extraction with an appropriate solvent.

The solvent to be used is not particularly limited as long as it can effectively extract components having preventive or therapeutic effects against spots, freckles, etc. from plant leaves, but more preferably,
Water or ethanol or a mixture thereof.

Furthermore, glucose absorption substances from the intestinal tract, such as gymnemic acid, dizyfin, phlorizin, phloretin, acebotin,
Those that have been adjusted or processed to contain trilobatin or the like at a higher concentration may also be used.

Of course, it is a matter of course that gymnemic acid, zydyfin, heptad lysine, phloretin, acebotine, and trilobatin can be isolated and purified and used to produce a skin cosmetic composition.

The product obtained in this way can be blended into ordinary cosmetic forms such as lotions, milky lotions, creams, etc. as raw materials for cosmetic preparations.

It has been found that the skin cosmetic composition thus obtained has an extremely effective effect on the prevention or treatment of age spots, freckles, etc., and revitalizes the skin with vigor.

Although this mechanism of action is not yet clear and is currently under intensive research, the inventors estimate as follows.

That is, the effects of these plants on preventing or treating age spots, freckles, etc. have a parallel relationship with their sweet taste suppressing effects or their sugar absorption suppressing effects from the intestinal tract.

From this, it is thought that sugar absorption inhibitors, ie, gymnemic acid, zizyfin, etc., suppress the uptake of sugar into cells even in melanin pigment-producing cells of the skin. On the other hand, it is known that in melanin pigment-producing cells, tyrosinase, which is involved in melanin production, is produced in liposomes of rough vesicles, and is then activated by modification of sugar chains in the endoplasmic reticulum associated with the Golgi organ. It is being From the above points, it is thought that gymnemic acid, zydyfin, heptad lysine, phloretin, and the like similarly suppress the absorption of sugar into melanin-producing cells. As a result, there is a shortage of sugar in melanin-producing cells, and it is thought that activation of tyrosinase due to modification of sugar chains is suppressed. In addition, it was discovered during research that these substances not only have an effect on preventing or treating age spots and freckles, but also have excellent effects on rough skin, acne, scalp dandruff, itching, and the like.

In particular, regarding effects on rough skin, gymnemic acid,
Crude extracts tend to be more effective than refined products such as Jijifin. This means that it is difficult to attribute the effect on rough skin etc. solely to the presence of gymnemic acid, dizyfin, phlorizin, phloretin, acebotin, trilobatin, etc., but in any case, the effects of gymnema leaves or jujube leaves It contains many other unknown compounds, and it is thought that they act additively or synergistically to exert their effects. Therefore, when used in skin cosmetic compositions, it is not always necessary to isolate the active ingredient and use it, depending on the purpose, and it may be preferable in some cases.

(Examples and Experimental Examples) The present invention will be described in detail below based on Examples and Experimental Examples.

Example 1 (Preparation of crude aqueous extract of Gymnema leaves) 200 g of dried leaves of Gymnema sylvestre (produced in India) were soaked in warm water at 60° C. for about 5 hours and filtered, and this process was repeated several times.

The resulting hot water extracts were combined, concentrated under reduced pressure, and filtered again to obtain 1.000 cc of crude extract.

Example 2 (Preparation of aqueous crude extract of jujube leaves) After drying jujube leaves with hot air, 200g of them were heated at 60°C.
The sample was soaked in warm water for about 5 hours and filtered, and this process was repeated several times. The obtained warm water extracts were combined and concentrated under reduced pressure, and filtered again to obtain crude extract 1. OOOcc was obtained.

Example 3 (Preparation of aqueous crude extract of cherry trunk skin) 200 g of dried cherry trunk skin was soaked in warm water at 60° C. for about 5 hours and filtered, and this process was repeated several times. The obtained warm water extracts were combined and concentrated under reduced pressure, and filtered again to obtain 1,000 c of crude extract.
I got c.

Example 4 (200 g of apple leaves was soaked in hot water at 60°C for about 5 hours and filtered, and this was repeated several times. The resulting hot water extracts were combined and condensed under reduced pressure, and filtered again to obtain a crude extraction. Liquid 1,OO
Got Occ.

Example 5 (Preparation of crude gymnemic acid from gymnema leaves) Soak 200 g of dried gymnema leaves in warm water at 60°C for about 5 hours.
This was filtered to obtain an aqueous extract. This was repeated several times. The resulting hot water extract was adjusted to pH 3 with 2N sulfuric acid, and the resulting precipitate was collected by centrifugation at 15.00 rpm for 20 minutes, thoroughly washed with water, and then extracted several times with ethanol. The ethanol extract was concentrated under reduced pressure, and twice the amount of acetone was added thereto, followed by centrifugation. The supernatant was concentrated to dryness under reduced pressure, diethyl carbonate was added thereto, and extraction was repeated several times at boiling point. Thereafter, the extract was concentrated, and after cooling, the precipitated crude gymnemic acid was collected and dried. 1.4 g of crude gymnemic acid was obtained.

Example 6 (Preparation of crude Jijifin from jujube leaves) 200 g of dried jujube leaves were immersed in warm water at 60°C for about 5 hours, and filtered to obtain a water extract. This was repeated several times.

The obtained hot water extract was concentrated to dryness under reduced pressure, and extracted several times with methanol.

The methanol extract was condensed to dryness under reduced pressure, and this was dissolved in distilled water to obtain Sephadex G-10 (Pharmacia).
column and eluted with a sufficient amount of distilled water. After concentrating this eluate under reduced pressure, it was extracted several times with a mixture of chloroform and ethanol, and this product was condensed and dried to give a crude ciidifin with a concentration of 0.5%. 9g was obtained.

Experimental Example 1 (Melanin production suppression test) Eagle MEM medium containing 10% fetal bovine serum4.
Add 0.0cc of sample liquid to 0.0cc. 1 cc and culture solution containing B-16 melanoma cells tol5. Add 1cc, 5%C
Incubate for 5 days at 37°C under O2 air. During this time, the medium was replaced once. After culturing for 5 days, the cells were collected in a centrifuge tube, and the degree of whitening of the B-16 melanoma cells was visually observed. However, the sample liquids were 10 times diluted and 100 times diluted for the samples of Examples 1, 2.3 and 4, respectively, and 0.1 mg for the samples of Examples 5 and 6, respectively.
/cc, 0.01mg/cc, and phlorizin and phloretin (manufactured by Sigma) were each 0.01mg/cc.
, 0.001 mg/cc. Note that purified water was used as a control.

In all cases, the cells proliferated well, and the macroscopic findings of whitening were as follows.

Adjustment solution of Example 1 10 times diluted solution 100 times diluted solution Adjustment solution of Example 2 10 times diluted solution 100 times diluted solution Adjustment solution of Example 3 10 times diluted solution 100 times diluted solution Adjustment solution of Example 4 10 times Diluted solution 100 times diluted solution Example 5 crude gymnemic acid 0. 1 mg/cc liquid 0.01 mg/cc liquid Jizy Fin 0.01 mg/cc liquid Example 6 1 mg/cc liquid +++ + ++ +++ ++ + + + + + ++ + O, Of mg/cc liquid Phlorizin 0.01 mg/cc liquid 0. 001mg/cc liquid Phloretin 0.01 mg/cc liquid 0. OO1mg/cc liquid control +++: Large whitening ++: Whitening normal +: Slight whitening: No whitening + +++ + + ++ Example 7 (Containing the crude gynunemic acid and flozin obtained in Example 5) Prescription example of lotion) Prescription (1) (2) Weight% Weight% Crude gymnemic acid phlorizin 0.2 0. 05 Ethanol 3.0 3.0
Propylene glycol 4.5 4.5
Glycerin 0.5 0.5 Methyl p-oxybenzoate 0.2 0.2 Ethyl p-oxybenzoate 0.02 0.0
2 Purified water Appropriate amount Appropriate amount A lotion was prepared according to the above recipe.

Experimental Example 2 (Effects of skin cosmetic compositions containing crude gymnemic acid and phlorizin) Eight types of lotions were prepared as follows, and their effects on age spots and freckles were tested.

For formulations a to d, the amount of crude gymnemic acid in the formulation of Example 7 was as follows.

Prescription a O. 01% by weight Prescription b 0.1% by weight Prescription c1, 0% by weight Prescription d 2.0% by weight For formulations e-h, the amount of phlorizin in the formulation of Example 7 was as follows.

Prescription e O. 005% by weight Prescription f O. 05 Weight% prescription g
o. 5% by weight Formula h i. o Weight % The evaluation method and results are as follows.

(1) Subjects with stains: 45 women with stains (33 to 61 years old)
Age) Freckles: 36 girls who are recognized as having freckles (from 17 years old)
(52 years old) (2) Test method For each symptom, subjects were divided into 9 groups, and the 8 groups were asked to apply lotion twice a day in the morning and evening after washing their faces with soap and warm water, and the improvement effect was evaluated 28 and 56 days later. . The remaining group served as a control.

(3) Evaluation Shi Mi 1: The color is quite dark and the border is clear.

2: The color is not very dark, but the border is quite sharp.

3: The color is extremely pale and the border is not clear.

4: No stain symptoms observed.

Freckles L: Blackish spots spread across the cheeks, sometimes extending to the forehead.

2: Brown to grayish spots are spreading on the cheeks.

3: Light brown spots are observed on the cheeks, but they are not noticeable.

4: No symptoms of freckles observed.

The symptoms were evaluated as follows according to the classification of symptoms.

Effective: Symptoms improved from 1 to 3.4 and from 2 to 4.

Moderately effective 2 symptoms from 1 to 2, from 2 to 3, and from 3 to 4
improved on.

Ineffective: There is little change in symptoms or symptoms have worsened.

The evaluation results are shown in Tables 1 and 2. As is clear from the results, all of the lotions containing the aqueous crude extract obtained in Example 1 have superior effects compared to the control.

Table (blank below) Evaluation results of lotion containing gymnemic acid or 7-mouth lysine after 28 days Evaluation results of lotion containing crude gymnemic acid or phlorizin after 56 days Example 8 (Example 1, 2.3 and Preparation of cream containing the aqueous extract obtained in 4) Formula Weight % Stearic acid 2.0 Stearyl alcohol 6.0 Squalane
60 reduction lanolin
2.0 year old cutyldodecanol
6.0 Polyoxyethylene cetyl ether (20E.O) 4.0 Lipophilic glycerin monostearate 1.5 Preservative
0.3 IO times concentrated solution of the extract of Example 1, 2.3 or 4 IO,0 Fragrance Micro-purified water
The rest of the cream was prepared according to the above recipe.

Example 9 (Preparation of emulsion containing the aqueous extract obtained in Example 1 or 4) Formula Weight % squalane
5.0 Vaseline
2. 0 Sorbitan sesquioleate 0. 8 Polyoxyethylene oleyl (20E.O.) 1.2 Propisine glycol 5.0 Ethanol
3.0 Carboxy vinyl polymer (1% aqueous solution) 18.0 Potassium hydroxide 0. 10 times concentrated solution of the extract of Example 1 or 4 10.0 Preservative 0.3 Flavor
micro purified water
The rest of the emulsion was prepared according to the above-mentioned formula in a conventional manner.

Example 1O (Preparation of shampoo containing the aqueous extract obtained in Example 1) Formulation Weight % 10-fold concentrate of the extract of Example 1 10.0 Sodium polyoxyethylene lauryl ether sulfate (2E.0 .) 8.5 lauryl dimerylaminosulfate betaine 5,0 1,3-butylene glycol 4. 0 Lauric acid diethanolamide 2.0 Edetate disodium 0. 1 preservative
Appropriate amount of fragrance
Appropriate amount of purified water
The rest of the shampoo was prepared using the above formulation in a conventional manner.

Experimental Example 3 (Effect of the cream obtained in Example 8) Of the cream obtained in Example 8, 1 of the extract of Example 1
A cream using an O-fold concentrate was tested as follows.

15 subjects (females 24 to 57 years old) with age spots.
The cream of Example 8 was applied to 15 other people (females 31 to 59 years old).
The cream of Comparative Example was applied to the face twice a day in the morning and evening for 5 weeks, and the age spot improvement effect was tested according to the evaluation criteria of Experimental Example 2. At the same time, the rough skin improving effect and moist feeling were tested according to the evaluation criteria of Experimental Example 2. At the same time, effectiveness or ineffectiveness was determined based on the degree of improvement regarding rough skin improvement effect and moisturizing feeling. However, in the cream of the comparative example, purified water was used instead of the extract used in Example 8.

Cream of Example 8 (stain improvement effect) Effective 9/l5 Slightly effective 2/l5 Ineffective 4/l5 (Skin improvement effect) Effective 7/lO Ineffective 3/lO (Moist feeling) Effective 9/10 Ineffective 1/1 0 Comparative cream (stain improvement effect) Effective 1/l 5 Slightly effective 5/l5 Ineffective 9/l5 (Skin improvement effect) Effective 3/lO Ineffective 7/lO (Moist feeling) Effective 4/lO Ineffective 6/l0 Experiment Example 4 (Test using the shampoo obtained in Example 1O) The shampoo of Example 10 was compared to 10 test subjects (males 17 to 48 years old) with a lot of dandruff and itching to other IO subjects (males 22 to 51 years old) The shampoo in this example was used three times a week for one month, and tested for improvement in moisturized hair, dandruff, and itching.

However, the shampoo of Comparative Example used purified water instead of the extract of the shampoo of Example 10.

Shampoo of Example 5 Shampoo of Comparative Example (dandruff/
Itching) (dandruff and itching) Effective 7/1
0 valid 2/1o invalid 3/10
Ineffective 8/1 0 Experimental Example 5 (Melanin production inhibition test of 7 loretin derivatives) Type of adjustment solution Acebot in 0. O
IX liquid trilobatin (trilobatin) 0
．． 01! When the degree of whitening of B-16 melanoma cells was observed for both solutions, the cells proliferated well, and the macroscopic findings of whitening were as follows.

Acebotine ++ Trilobatin +

Claims (1)

[Claims] 1) Gymnema sylvestre
R. Br. ) leaves, jujube (Zizyphus juj
uba M. v. i. R. ) leaves or apple (Malu
s pumila M. v. d. s. ), Sakura (Pr
unus glandulosa T. ), pear (Py
rus serotinaRehd. ), or peach (P
stem bark or root bark of Malus persica Batsch) or apple (Malus pumila M.v
．． d. s. ) leaves, Pieris japon
ica D. Don) or Symploco
A skin cosmetic composition comprising at least one component of the leaves of S. microcalyx or a solvent extract thereof. (2) The skin cosmetic composition according to claim 1, wherein the solvent for the extract is water, alcohol, or a mixture thereof. (3) The extract may contain Gymnemasyl
vestre R. Br. ) for the leaves of gymnemic acid, jujube (Zizyphus jujuba M.v.).
i. R. ) Leaves of Gigifin, Rosaceae (R
phlorizin or phloretin for the stem bark, root bark or leaves of Pieris ja
ponica D. For leaves of Don), acebotine, Symplocos microcalyx
3. The skin cosmetic composition according to claim 2, wherein the leaves of the following are adjusted or processed to contain trilobatin. (4) A skin cosmetic composition containing one or more selected from gymnemic acid, zydyfin, phlorizin, phloretin, acebotin, or trilobatin.