JPH11335229A - Skin lotion - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject lotion capable of suppressing the activity of elastase and recovering and maintaining the tensity and elasticity of skin and thereby having effects on the prevention of skin aging and maintenance of a young skin state by formulating an extract from Bergenia ciliata. SOLUTION: This skin lotion is obtained by including an extract from Bergenia ciliata in an amount of preferably 0.0001-10.0 wt.% expressed in terms of a dried substance in the total amount of the lotion. The extract is preferably prepared by using a rhizome, dipping the rhizome in an extracting solvent (e.g. methanol or acetone) or refluxing the rhizome together with the extracting solvent under heating, then filtering and concentrating the resultant extract solution. A bleaching ingredient, a humectant, an antioxidant, an oily ingredient, an ultraviolet light absorber, a sequestering agent such as disodium edetate, caffeine, vitamin C, magnesium ascorbate phosphate, etc., as necessary, can be formulated with the skin lotion. The resultant skin lotion can preferably be applied to cosmetics.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin containing a plant extract, and more particularly, to prevent aging of the skin by suppressing the activity of elastase and maintaining the firmness and elasticity of the skin. The present invention relates to a skin external preparation capable of maintaining a youthful skin condition.

[0002]

2. Description of the Related Art Conventionally, the necessity of a skin external preparation having an anti-aging effect has been considered, but the mechanism and definition of aging have not been clarified. The skin moisture has been measured by measuring the moisturizing state and the elasticity of the skin, and the skin color has been visually observed to make a judgment. However, in recent years, research on aging has been advanced, and aging is an important factor as a cause of skin aging, and the effects of dryness, oxidation, sunlight (ultraviolet rays), etc. are directly related to skin aging. Has been cited as an important factor. As specific phenomena of skin aging, reduction of collagen and elastin in skin dermis, reduction of mucopolysaccharides such as hyaluronic acid, damage of cells by ultraviolet rays, and the like are known. Of these, elastin forms crosslinks and contributes to the elasticity of tissues.However, elastin, which is an elastin-disrupting enzyme, is overexpressed by UV exposure and aging, and elastin is denatured and destroyed. However, it is thought to lead to a decrease in skin elasticity. Therefore, it is important to prevent the aging of the skin by suppressing the action of elastase and preventing denaturation / destruction of elastin which gives the skin elasticity and firmness.

[0003] Therefore, the present invention suppresses the activity of elastase to restore and maintain the firmness and elasticity of the skin,
It is an object of the present invention to provide a skin external preparation that has an effect of preventing skin aging and maintaining a youthful skin condition.

[0004]

Means for Solving the Problems The present inventors have made intensive studies to solve the above-mentioned problems, and as a result,
The present inventors have found that a solvent extract of A. ciliata has excellent elastase inhibitory activity, and have completed the present invention. There is no report on the elastase inhibitory effect of this plant extract, and let alone application to anti-aging agent,
There is no known application to skin external preparations.

That is, the present invention relates to Bergenia cil
An external preparation for skin characterized by incorporating an iata extract. Further, according to the present invention, there are provided an anti-aging agent, an elastase inhibitor, and a cosmetic, comprising the extract of Aspergillus niger.

Hereinafter, the configuration of the present invention will be described in detail. Bergenia cili used in the present invention
The solvent extract of ata comprises leaves, flowers, stems, rhizomes,
Any site such as a root may be used, but it is preferably obtained by using a rhizome and immersing or refluxing with an extraction solvent, followed by filtration and concentration. The extraction solvent used in the present invention may be any solvent as long as it is a solvent usually used for extraction. Particularly, alcohols such as methanol, ethanol, and 1,3-butylene glycol, aqueous alcohols, and organic solvents such as acetone and ethyl acetate are used. Can be used alone or in combination.

[0007] Bergenia cil in the present invention
The amount of the extract of iata is 0.00001 to 20.0% by weight, preferably 0.1% by weight, as a dry matter in the total amount of the external preparation.
0001 to 10.0% by weight. If the amount is less than 0.00001% by weight, the effects of the present invention cannot be sufficiently exhibited, and if it exceeds 20.0% by weight, it is difficult to formulate the composition, which is not preferable. Further, even if the content is 10.0% by weight or more, the effect is not so much improved.

[0008] Bergeniac used in the present invention
Since the extract of iliata exhibits excellent elastase inhibitory activity on human skin,
An external preparation for skin containing an extract of Enia ciliata can prevent and improve aging of the skin and maintain a youthful and healthy skin condition.

[0009] In addition to the above essential components, the skin external preparation of the present invention contains components usually used in skin external preparations such as cosmetics and pharmaceuticals, for example, whitening agents, moisturizing agents, antioxidants, oily components, ultraviolet absorbers. Surfactants, thickeners, alcohols, powder components, coloring materials, aqueous components, water, various skin nutrition agents, and the like can be appropriately compounded as necessary.

In addition, sequestering agents such as disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, gluconic acid, caffeine, tannin, verapamil, tranexamic acid and derivatives thereof, and licorice extract Products, glabridine, hot water extract of fire thorn fruit, various crude drugs, tocopherol acetate,
Drugs such as glycyrrhizic acid and its derivatives or salts thereof, vitamin C, magnesium ascorbate phosphate,
Whitening agents such as ascorbic acid glucoside, arbutin and kojic acid, and sugars such as glucose, fructose, mannose, sucrose, trehalose and the like can also be appropriately blended.

The present invention can be widely applied to cosmetics and quasi-drugs applied to the outer skin, particularly preferably cosmetics, and its dosage form can be aqueous solution type, solubilizing type, emulsifying type. A wide range of dosage forms can be used, such as powder, oil-liquid, gel, ointment, aerosol, water-oil two-layer systems, water-oil-powder three-layer systems, and the like. That is, if it is a basic cosmetic, face wash, lotion,
It can be widely applied to various forms such as emulsions, creams, gels, essences (packs, masks), etc. Also, if it is a makeup cosmetic,
As a toiletry product such as a foundation, it can be widely applied to forms such as body soap and soap. Furthermore, quasi-drugs can be widely applied to various ointments and the like. The form and form of the external preparation for skin of the present invention are not limited to these dosage forms and forms.

[0012]

The present invention will be further described below with reference to examples and the like. However, the technical scope of the present invention is not limited by these examples and the like. The compounding amount is% by weight. Prior to the examples, a test method for the elastase inhibitory activity of the plant extract of the present invention and the results thereof will be described.

(1) Preparation of sample To 200 g of Rhizome of Bergenia ciliata, 600 g of purified water and 600 g of ethanol were added, and 50 ° C.
And heat to dissolve. After cooling, filter, concentrate and dry to
20 g of an extract of R. iliata were obtained.
This extract was dissolved in DMSO at 2%, the concentration was adjusted by diluting this solution, and the following experiment was performed using this.

(2) Test method for elastase inhibitory activity and its results Elastase activity was measured according to the method of Fujie et al. As follows. As a reaction buffer, 0.1 M
This was performed using HEPES, 0.5 M NaCl (pH 7.4). Methoxy-succinyl as an elastase substrate
-alanyl-alanyl-prolyl-valine-p-nitroanilide (BA
CHEMFEINCHEMIKALIENAG) to 8
It was dissolved in DMSO to 0 mM, dispensed in 20 μl aliquots, and stored frozen (−80 ° C.). At the time of use, it was used after being diluted to 8 mM with a reaction buffer. Elastase is elastase derived from human leukocytes (ELASTI).
N PRODUCT CO., INC.)
Dissolve in the reaction buffer to a concentration of 10 μg / ml.
Each was dispensed and stored frozen (-80 ° C). In use,
The solution was diluted to 5 μg / ml with a reaction buffer and used. As the inhibitor sample, a 2% solution of DMSO diluted 10-fold, 100-fold, and 1000-fold with a reaction buffer was used.

96-well plate (CORNING 25860)
In each case, 25 μl of 8 mM elastase substrate was dispensed, and 50 μl of the inhibitor was further added. next,
Add 25 μl of 5 μg / ml elastase on ice,
Immediately incubated at 37 ° C. for 20 minutes. Thereafter, the absorbance was measured at 415 nm. However, the inhibition rate is based on the following function.

[0016]

## EQU1 ## Inhibition rate (%) = 100- (presence of inhibitor / no inhibitor) × 100

The results are shown in FIG. In addition, as a reference example, a test similar to the above was performed on fetal bovine serum (manufactured by GIBCO), which is an in vivo substance already known to have elastase inhibitory activity. Fetal bovine serum is 10-fold, 100-fold and 1000-fold (V
/ V). Fig. 1 shows the results.
Shown in FIG. 1 also shows the results.

Hereinafter, examples of the formulation of the external preparation for skin according to the present invention in various dosage forms will be described as examples. In the following examples, the extract obtained by the above-mentioned sample preparation was used as the extract of Bergenia ciliata.

Example 1 Cream (Formulation) Stearic acid 3.0% by weight Stearyl alcohol 5.0 Isopropyl myristate 18.0 Glycerin monostearate 3.0 Propylene glycol 10.0 Bergenia ciliata extract 0.01 Caustic potash 0 .2 Sodium bisulfite 0.01 Preservatives Appropriate amount Fragrance Appropriate amount Ion-exchange water residue (Production method) Propylene glycol and Bergen in ion-exchange water
Add ia ciliata extract and caustic potash to dissolve and heat to 7
Keep at 0 ° C. (aqueous phase). Mix other ingredients, heat and melt.
Keep at 0 ° C. (oil phase). The oil phase is gradually added to the water phase, and after the addition is completed, the temperature is maintained for a while to cause a reaction. Thereafter, the mixture is uniformly emulsified with a homomixer and cooled to 30 ° C. while stirring well.

Example 2 Cream (Formulation) Stearic acid 2.0% by weight Stearyl alcohol 7.0 Hydrogenated lanolin 3.0 Squalane 4.0 2-Octyldodecyl alcohol 6.0 Polyoxyethylene (25 mol) Cetyl alcohol ether 3.0 Glycerin monostearate 2.0 Propylene glycol 6.0 Bergenia ciliata extract 0.05 Sodium bisulfite 0.03 Ethyl paraben 0.3 Appropriate amount Ion-exchanged water Residue (Production method) Propylene glycol in ion-exchanged water In addition,
Heat and maintain at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is added to the water phase, pre-emulsified, homogenized with a homomixer, and cooled to 30 ° C. with good stirring.

Example 3 Cream (Formulation) Solid paraffin 5.0% by weight Beeswax 10.0 Vaseline 15.0 Liquid paraffin 41.0 Glycerin monostearate 2.0 Polyoxyethylene (20 mol) Sorbitan monolaurate 2 0.0 Soap powder 0.1 Borax 0.2 Bergenia ciliata extract 0.1 Sodium bisulfite 0.03 Ethyl paraben 0.3 Appropriate amount Ion-exchanged water Residue (Production method) Add soap powder and borax to ion-exchanged water and heat Dissolve and maintain at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is gradually added to the aqueous phase while stirring to carry out the reaction. After completion of the reaction, the mixture is uniformly emulsified with a homomixer, and cooled to 30 ° C. while stirring well after emulsification.

Example 4 Emulsion (Formulation) 2.5% by weight of stearic acid Cetyl alcohol 1.5 Vaseline 5.0 Liquid paraffin 10.0 Polyoxyethylene (10 mol) Monooleate 2.0 Polyethylene glycol 1500 0 Triethanolamine 1.0 Carboxyvinyl polymer 0.05 (trade name: Carbopol 941, BFGoodrich Chemical company) Bergenia ciliata extract 3.0 Sodium bisulfite 0.01 Ethyl paraben 0.3 Perfume Appropriate amount Ion-exchange water residue ( Production method) A carboxyvinyl polymer is dissolved in a small amount of ion-exchanged water (phase A). Polyethylene glycol 1500 and triethanolamine are added to the remaining ion-exchanged water, dissolved by heating, and kept at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is added to the water phase, pre-emulsification is performed, the phase A is added, and the mixture is uniformly emulsified with a homomixer.

Example 5 Emulsion (Formulation) Microcrystalline wax 1.0% by weight Beeswax 2.0 Lanolin 20.0 Liquid paraffin 10.0 Squalane 5.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 mol) ) Sorbitan monooleate 1.0 Propylene glycol 7.0 Bergenia ciliata extract 10.0 Sodium bisulfite 0.01 Ethyl paraben 0.3 Perfume Appropriate amount Ion exchange water Residue (Production method) Add propylene glycol to ion exchange water,
Heat and maintain at 70 ° C. (aqueous phase). The other components are mixed, heated and melted and kept at 70 ° C. (oil phase). While stirring the oil phase, the aqueous phase is gradually added thereto, and the mixture is uniformly emulsified with a homomixer. After emulsification, cool to 30 ° C with good stirring.

Example 6 Jelly (formulation) 95% ethyl alcohol 10.0% by weight dipropylene glycol 15.0 polyoxyethylene (50 mol) oleyl alcohol ether 2.0 carboxyvinyl polymer 1.0 (trade name: Carbopol) 940, BFGoodrich Chemical company) Caustic soda 0.15 L-arginine 0.1 Bergenia ciliata extract 7.0 Sodium 2-hydroxy-4-methoxybenzophenonesulfonate 0.05 Ethylenediaminetetraacetate 3 sodium 2 water 0.05 Methylparaben 0.2 Perfume Appropriate amount Ion-exchanged water Residue (Preparation method) Carbopol 940 is uniformly dissolved in ion-exchanged water, while Bergenia ciliata extract and polyoxyethylene (50 mol) oleyl alcohol ether are dissolved in 95% ethanol. To the aqueous phase. Next, after adding other components, the mixture is neutralized with caustic soda and L-arginine to increase the viscosity.

Example 7 Essence (Formulation) (A phase) Ethyl alcohol (95%) 10.0% by weight Polyoxyethylene (20 mol) Octyldodecanol 1.0 Pantothenyl ethyl ether 0.1 Bergenia ciliata extract 1.5 Methylparaben 0.15 (B phase) Potassium hydroxide 0.1 (C phase) Glycerin 5.0 Dipropylene glycol 10.0 Sodium bisulfite 0.03 Carboxyvinyl polymer 0.2 (Product name: Carbopol 940) BF Goodrich Chemical company) Purified water Residue (Preparation method) Dissolve A phase and C phase uniformly, and add A to C phase
Add phases and solubilize. Next, after adding the phase B, filling is performed.

Example 8 Pack (Formulation) (A phase) Dipropylene glycol 5.0% by weight Polyoxyethylene (60 mol) hydrogenated castor oil 5.0 (B phase) Bergenia ciliata extract 0.01 Olive oil 5.0 Tocopherol acetate 0.2 Ethylparaben 0.2 Fragrance 0.2 (Phase C) Sodium bisulfite 0.03 Polyvinyl alcohol 13.0 (Saponification degree 90, Degree of polymerization 2,000) Ethanol 7.0 Purified water residue (Production method) ) A phase, B phase and C phase are each dissolved uniformly,
Add phase B to phase and solubilize. Next, this is added to the C phase and then filled.

Example 9 Solid foundation (formulation) Talc 43.1% by weight Kaolin 15.0 Sericite 10.0 Zinc white 7.0 Titanium dioxide 3.8 Yellow iron oxide 2.9 Black iron oxide 0.2 Squalane 8 0.0 Isostearic acid 4.0 POE sorbitan monooleate 3.0 Isocetyl octoate 2.0 Bergenia ciliata extract 1.0 Preservatives Appropriate amount Perfume Appropriate amount (Production method) Mix talc and black iron oxide powder components in a blender. The oily components of squalane-isocetyl octanoate, Bergenia ciliata extract, preservatives, and fragrances are added to the mixture, kneaded well, and the mixture is filled into a container and molded.

Example 10 Emulsion type foundation (cream type) (Prescription) (Powder part) Titanium dioxide 10.3% by weight Sericite 5.4 Kaolin 3.0 Yellow iron oxide 0.8 Bengala 0.3 Black iron oxide 0.2 (oil phase) Decamethylcyclopentasiloxane 11.5 Liquid paraffin 4.5 Polyoxyethylene-modified dimethylpolysiloxane 4.0 (aqueous phase) Purified water 50.0 1,3-butylene glycol 4.5 Bergenia ciliata extract 1.5 Sorbitan sesquioleate 3.0 Preservatives Appropriate amount Flavors Appropriate amount (Preparation method) After heating and stirring the aqueous phase, a well-mixed and pulverized powder portion is added, followed by homomixer treatment. Further, the oil phase mixed by heating is added, and the mixture is treated with a homomixer. Then, a fragrance is added with stirring, and the mixture is cooled to room temperature.

Comparative Example 1 Comparative Example 1 was prepared by replacing the Bergenia ciliata extract in the formulation of Example 10 with water.

Each of the cosmetics obtained in Example 10 and Comparative Example 1 was subjected to the following monitor tests. Table 1 shows the results.

Monitor test: A healthy adult woman 1 randomly selected from the ages of 25 to 57 years
With 00 subjects as subjects, the improvement effect on wrinkles and fine wrinkles after using each cosmetic on the facial skin for one month every day was examined.

(A) Effect on wrinkles and fine wrinkles The condition of the skin was visually observed and evaluated based on the following evaluation criteria. (Evaluation criteria) A: Disappeared cleanly. B: Slightly less noticeable. C: No change. D: Increased a little. E: Increased.

(B) Effect of skin on firmness and tarmi Skin condition was visually observed and evaluated based on the following evaluation criteria. (Evaluation criteria) A: Very improved. B: Improved. C: No change. D: It became somewhat noticeable. E: It became noticeable.

In this monitor test, none of the subjects had skin abnormalities when using the cosmetics obtained in Example 10 and Comparative Example 1.

[0035]

[Table 1] ──────────────────────────── Effects on wrinkles and small wrinkles (Hari) ) ───────── ────────── ABCDCEABCDE ──────────────────── ──────── Example 10 18 38 25 19 0 40 32 18 8 2 Comparative Example 1 0 32 45 3 20 7 4 62 17 10 ──────────────── ────────────

As is clear from the results shown in Table 1, when the cosmetic obtained in Example 10 was used, Comparative Example 1 was used.
It is recognized that wrinkles and fine wrinkles and skin firmness and skin thinning were improved as compared with the case where the cosmetic obtained in the above was used. This indicates that blending the Bergeniaciliata extract as an active ingredient is a very useful formulation.

[0037]

As described above, according to the present invention,
By blending the Bergenia ciliata extract as an active ingredient, a skin external preparation exhibiting excellent anti-aging and improving effects is provided. In other words, the Bergenia ciliata extract exerts elastase inhibitory activity, thereby suppressing the degeneration of elastin, which is an elastic fiber, and can maintain elastic, wrinkle-free and sagging skin, and improves skin aging. A skin external preparation is provided which has excellent effects of preventing and maintaining a youthful skin condition.

[Brief description of the drawings]

FIG. 1 is a diagram showing the elastase inhibitory activity of Bergenia ciliata in comparison with the elastase inhibitory activity of fetal calf serum.

Claims (4)

[Claims] 1. An external preparation for skin, comprising an extract of Bergenia cliata. 2. An anti-aging agent comprising an extract of Bergenia cliata as an active ingredient. 3. An elastase inhibitor comprising an extract of Bergenia cliata as an active ingredient. 4. A cosmetic comprising an extract of Bergenia cliata.