JP2002121125A - Skin care preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a skin care preparation containing an extract of Agracejo (Berberis vulgaris). SOLUTION: The skin care preparation contains an extract of Agracejo. The Agracejo extract has excellent melanogenesis suppressing action and exhibits excellent safety. The skin care preparation containing the Agracejo extract exhibits safe and excellent bleaching action on the skin.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin which has an excellent skin whitening effect by incorporating an extract of a specific plant.

[0002]

2. Description of the Related Art In general, skin pigmentation, which is observed in spots, freckles, sunburn, etc., is caused by abnormal hormonal activity or ultraviolet light, which causes melanin-producing cells present in the skin to excessively produce melanin pigment. It is thought to be due to deposition within. As one of methods for preventing such pigmentation, a method for suppressing excessive production of melanin is known. Conventionally, treatments for external use of hydroquinone, ascorbic acid (vitamin C) and the like have been performed for the treatment of pigmentation.

[0003]

As a whitening agent, a highly safe natural raw material is desired instead of a chemically synthesized product such as hydroquinone which has a risk of side effects. Also, ascorbic acid is unstable and difficult to formulate.

[0004] In view of the above, there is a demand for a skin external preparation that is safe, has excellent stability, and has a whitening effect.

[Means for Solving the Problems]

[0005] Under such circumstances, the present inventors have conducted intensive studies, and as a result, have found that an extract of aglasefo has an excellent melanin production inhibitory action and is also excellent in stability. Furthermore, they have found that an external preparation for skin containing an extract of aglasefo has a safe and excellent skin whitening effect, and have completed the present invention.

Agrasejo (scientific name: Be) used in the present invention
rberis vulgaris, also known as Agracejo, barberry)
Is a shrub of the barberry family. It is widely distributed from Europe to Central Asia and tropical America, and is widely used as a crude drug.

[0007] The extract of agrasejo used in the present invention is extracted from a part or whole plant such as agrasejo leaf, stem, bark, flower, fruit, root and the like. Preferably,
Those obtained by extracting from the leaves and stems of Agrasejo are preferred. The extraction method is not particularly limited, and may be, for example, the one extracted by heating or the one extracted at room temperature.

Examples of the solvent to be extracted include water, lower alcohols (methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, 2-butanol, etc.) and liquid polyhydric alcohol (1,3-butylene glycol). ,
Propylene glycol, glycerin, etc.), ketones (acetone, methyl ethyl ketone, etc.), acetonitrile, esters (ethyl acetate, butyl acetate, etc.), hydrocarbons (hexane, heptane, liquid paraffin, etc.), ethers (ethyl ether, tetrahydrofuran, Propyl ether). Preferred are polar solvents such as water, lower alcohols and liquid polyhydric alcohols, and particularly preferred are water, ethanol, 1,3-butylene glycol and propylene glycol. These solvents may be used alone or in combination of two or more.

[0009] The extract of agrasejo may be used as it is as an extracted solution, or may be used after being subjected to a treatment such as concentration, dilution, or filtration, if necessary. Further, the extracted solution may be subjected to a treatment such as concentration and drying, spray drying, and freeze drying to be used as a dried product.

The above-mentioned extract may be used as it is in the external preparation for skin of the present invention, and oils, fats and waxes which are components used in ordinary external preparations within a range not to impair the effect of the extract of aglasefo. , Hydrocarbons, fatty acids, alcohols, esters, surfactants, metal soaps, pH adjusters, preservatives, fragrances, humectants, powders, ultraviolet absorbers, thickeners, pigments, antioxidants And components such as a whitening agent and a chelating agent.

The external preparation for skin of the present invention can be used in any of cosmetics, quasi-drugs and pharmaceuticals. Examples of the dosage form include lotions, creams, emulsions, gels,
Aerosol, ointment, poultice, essence, pack,
Those applied to the skin, such as detergents, bath agents, foundations, powders, and lipsticks, may be mentioned.

The amount of the extract of aglasefo used in the present invention is preferably 0.0001% by weight or more, preferably 0.001 to 10% by weight, in terms of solids, based on the total amount of the external preparation for skin of the present invention. If it is less than 0.0001% by weight, a sufficient effect is hardly exhibited. When the content is more than 10% by weight, the effect is hardly enhanced and it is uneconomical. As for the method of addition,
It may be added in advance or may be added during the production, and may be appropriately selected in consideration of workability.

[0013]

EXAMPLES In order to explain the present invention in detail, examples of the production of the extract used in the present invention, prescription examples of the present invention and experimental examples will be given below, but the present invention is not limited to these examples. Absent. Parts in the amounts shown in Examples are parts by weight, and%
Indicates% by weight.

Production Example 1 Hot water extract of agrasejo 400 ml of purified water was added to 20 g of dried agrasejo leaves, and
After extraction at 100 ° C. for 2 hours, the mixture was filtered, and the filtrate was concentrated and freeze-dried to obtain 4.2 g of a hot water extract of Aglasejo.

Production Example 2 50% Ethanol Extract of Agrasejo 1 L of purified water and 1 L of ethanol were added to 100 g of dried agrasejo leaves and stems, extracted at room temperature for 7 days, filtered, and the filtrate was concentrated to dryness. As a result, 21 g of an ethanol extract of agrasejo was obtained.

Production Example 3 1,3-butylene glycol extract of aglasejo To 100 g of dried whole plant of agrasejo, 1.0 kg of 1,3-butylene glycol was added, and the mixture was extracted at room temperature for 7 days. 0.90 kg of 3,3-butylene glycol extract was obtained.

Example 1 Cream Formulation Formulation amount 1. Hot water extract of aglasejo (Production Example 1) 0.05 part 2. Squalane 5.5 3. Olive oil 3.0 4. Stearic acid 2.0 5. Beeswax 2.0 6. Octyldodecyl myristate 3.5 7 Polyoxyethylene cetyl ether (20E.O.) 3.0 8. Behenyl alcohol 1.5 9. Glycerin monostearate 2.5 10. Fragrance 0.1 11. 1,3-butylene glycol 8.5 12. Ethyl parahydroxybenzoate 0.05 13. Methyl paraoxybenzoate 0.2 14. Make the total amount up to 100 with purified water. [Production method] Heat and dissolve components 2 to 9 and mix. Keep at 70 ° C to obtain oil phase. Components 1 and 11 to 14 are dissolved by heating and mixed, and kept at 75 ° C. to obtain an aqueous phase. Add the water phase to the oil phase, emulsify, cool with stirring, add component 10 at 45 ° C,
Cool to 30 ° C to obtain a product.

Comparative Example 1 Conventional Cream The same cream as in Example 1 except that the hot water extract of aglasejo was replaced with purified water was used as a conventional cream.

Example 2 Lotion Formulation Formulation amount 1. 0.1% of a 50% ethanol extract of aglasefo (Production Example 2) 2. 1,3-butylene glycol 8.0 3. Glycerin 2.0 4. Xanthan gum 0.02 5. Citric acid 0.016 Sodium citrate 0.1 7. Ethanol 5.0 8. Methyl parahydroxybenzoate 0.1 9. Polyoxyethylene hydrogenated castor oil (40E.O.) 0.1 10. Appropriate amount of fragrance 11. Make the total amount 100 with purified water [Production method] Components 1 to 6 and 11 and Components 7 to 10 are each dissolved uniformly, and both are mixed and filtered to obtain a product.

Example 3 Emulsion Formulation Formulation amount 1. Agarosefo 50% ethanol extract (Production Example 2) 0.5 part 2. Squalane 5.0 3. Olive oil 5.0 4. Jojoba oil 5.0 5. Cetanol 1.5 6. Glycerin monostearate 2.0 7. Polyoxyethylene cetyl ether (20E.O.) 3.0 8. Polyoxyethylene sorbitan monooleate (20E.O.) 2.0 9. Fragrance 0.1 10. Propylene glycol 1.0 11. Glycerin 2.0 12. Methyl paraoxybenzoate 0.2 13. Make the total amount up to 100 with purified water. [Production method] Heat and dissolve components 2 to 8 and mix them. Components 1 and 10 to 13 are dissolved by heating and mixed, and the mixture is kept at 75 ° C. to form an aqueous phase. Add the water phase to the oil phase, emulsify, cool with stirring, add component 9 at 45 ° C, and add
Cool to 0 ° C to obtain a product.

Example 4 Gel Formulation Formulation Amount 1. Agrasefo 1,3-butylene glycol extract (Preparation Example 3) 0.01 part 2. Ethanol 5.0 3. Methyl parahydroxybenzoate 0.1 4. Polyoxyethylene hydrogenated castor oil ( 60E.O.) 0.1 5. Appropriate amount of perfume 6. 1,3-butylene glycol 5.0 7. Glycerin 5.0 8. Xanthan gum 0.1 9. Carboxyvinyl polymer 0.2 10. Potassium hydroxide 0.2 11. Make the total amount to 100 with purified water [Manufacturing method] Components 2 to 5 and components 1 and 6 to 11 are each dissolved uniformly, and both are mixed to obtain a product.

Example 5 Ointment Prescription Formulation amount 1. Hot water extract of aglasefo (Preparation example 1) 1.0 part 2. 1,3-butylene glycol extract of aglasefo (Preparation example 3) 1.0 3. Polyoxyethylene cetyl ether (30E.O.) 2.0 4. Glycerin monostearate 10.0 5. Liquid paraffin 5.0 6. Cetanol 6.0 7. Methyl paraoxybenzoate 0.1 8. Propylene glycol 10.0 9. Make the total amount to 100 with purified water [Production method] Components 3 to 6 are dissolved by heating and mixed, and kept at 70 ° C. to obtain an oil phase. Components 1, 2 and 7 to 9 are dissolved by heating and mixed. Add the water phase to the oil phase, emulsify and cool to 30 ° C with stirring to obtain the product.

Example 6 Pack Prescription Formulation Amount 1. Hot water extract of aglasejo (Preparation Example 1) 0.1 part 2. 50% ethanol extract of aglasejo (Preparation Example 2) 0.1 3. Polyvinyl alcohol 12.0 4. Ethanol 5.0 5 1,3-butylene glycol 8.0 6. Methyl paraoxybenzoate 0.2 7. Polyoxyethylene hydrogenated castor oil (20E.O.) 0.5 8. Citric acid 0.1 9. Sodium citrate 0.3 10. Perfume qs 11. In purified water [Production method] Components 1 to 11 are uniformly dissolved to give a product.

Example 7 Foundation Formulation Formulation amount 1. Agrasefo 1,3-butylene glycol extract (Preparation Example 3) 1.0 part 2. Stearic acid 2.4 3. Polyoxyethylene sorbitan monostearate (20E.O.) 1.0 4. Polyoxyethylene cetyl ether (20E.O.) 2.0 5. Cetanol 1.0 6. Liquid lanolin 2.0 7. Liquid paraffin 3.0 8. Isopropyl myristate 6.5 9. Butyl paraoxybenzoate 0.1 10. Sodium carboxymethyl cellulose 0.1 11. Bentonite 0.5 12. Propylene glycol 4.0 13. Triethanolamine 1.1 14. Methyl parahydroxybenzoate 0.2 15. Titanium dioxide 8.0 16. Talc 4.0 17. Bengala 1.0 18. Yellow iron oxide 2.0 19. Fragrance qs. 20. Purified water [Production method] Components 2 to 9 are heated and dissolved, and kept at 80 ° C to obtain an oil phase. Swell the ingredient 10 well to the ingredient 20, then add the ingredient 1
And 11 to 14 are added and mixed uniformly. Add the ingredients 15 to 18 crushed and mixed with a crusher to this, and stir with a homomixer for 75
Keep at ℃ and make water phase. Add the oil phase to this aqueous phase with stirring, cool, add component 19 at 45 ° C, and stir with 30
Cool to ℃ to make the product.

Example 8 Bath agent Prescription Formulation amount 1. Hot water extract of agracejo (Production Example 1) 1.0 part 2. Sodium hydrogen carbonate 50.0 3. Yellow 202 (1) qs 4. Fragrance qs 5. Anhydrous sodium sulfate [Production method] Components 1 to 5 are uniformly mixed to give a product.

Next, experimental examples will be described in order to explain the effects of the present invention in detail.

Experimental Example 1 Inhibition test of melanin production using B16 mouse melanoma (whitening effect) Melanoma in the logarithmic growth phase was seeded at 3 × 10 ⁴ cells in a φ60 mm dish, and hot-water extract of agrasejo at various concentrations and ethanol extraction Eagles' MEM containing 10% fetal calf serum containing ascorbic acid or a positive control
The cells were cultured under 5% CO ₂ conditions. In addition, in order to confirm the stability of the sample, the same evaluation was performed using a solution in which an aqueous solution of the sample was left at room temperature for 24 hours. Dish cells after 5 days of culture
After sonication of the cells, a 2N aqueous solution of sodium hydroxide was added thereto, the mixture was treated at 60 ° C. for 2 hours, and OD 475 nm was measured with a spectrophotometer. In addition, the cell lysate after sonication was subjected to Lowry's method (J. Biol. Chem., 193, 265-275, 19
The protein was quantified in 51) and the amount of melanin per protein amount was compared to obtain an index of the melanin production inhibitory effect.

The results of these tests are shown in Table 1. Also,
When ascorbic acid was left for 24 hours, the inhibitory effect of melanin production was reduced, but the effect of agrasefo extract was not changed. As a result, it was confirmed that the extract of aglasefo had a stable and excellent melanin production inhibitory action.

[0029]

[Table 1]

Experimental Example 2 Use Test Using the cream of Example 1 and the conventional cream of Comparative Example 1, a use test for 30 months (30 to 45 years old) was carried out for 30 women each. After use, skin whitening action was determined by a questionnaire survey on improvement of skin spots, freckles and clarity. As a result, the external preparation for skin characterized by containing the extract of aglasefo exhibited excellent skin whitening action (Tables 2 and 3). There was no skin trouble during the test, and there was no problem in safety.
Also, there was no problem with the deterioration of the prescription components.

[0031]

[Table 2]

[0032]

[Table 3]

Also used for the lotion of Example 2, the emulsion of Example 3, the gel of Example 4, the ointment of Example 5, the pack of Example 6, the foundation of Example 7, and the bath agent of Example 8. The test showed safe and excellent skin whitening action.

[0034]

As described above, the extract of agrasefo of the present invention has an excellent melanin production-inhibiting action and exhibits an excellent stability. Furthermore, the external preparation for skin containing the extract of aglasejo showed a safe and excellent skin whitening effect.

Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat II (reference) A61K 7/00 A61K 7/00 U 7/50 7/50 F term (reference) 4C083 AA082 AA111 AA112 AA122 AB032 AB232 AB242 AB312 AB432 AC022 AC072 AC102 AC122 AC182 AC242 AC302 AC352 AC422 AC432 AC442 AC482 AC542 AC842 AD092 AD352 CC04 CC05 CC07 CC12 CC25 DD12 DD23 DD31 DD41

Claims (2)

[Claims] 1. An external preparation for skin, characterized by containing an extract of aglasefo. 2. A whitening agent comprising an extract of aglasejo.