JP4370221B2 - Skin external composition - Google Patents

Description

  The present invention relates to a composition for external application to skin, and in particular, contains an extract obtained from a flower bud of Honkan elephant, in particular, an extract obtained using water, a water-soluble organic solvent or a mixed solvent thereof as an extraction solvent, The present invention relates to an external composition for skin having excellent antioxidant ability, anti-inflammatory effect and whitening effect.

  The human body is affected in various ways by exposure to ultraviolet rays. When active oxygen, lipid peroxide, and the like are generated, they cause inflammation and cause great damage to tissues such as skin. Further, these inflammations and skin damage cause rough skin, which causes loss of moisture and gloss of the skin, texture, etc., and when the effect reaches the dermis, it causes photoaging such as wrinkles. In addition, active oxygen generated by ultraviolet rays and various factors released from epidermal cells activate tyrosinase of melanocytes and overproduce melanin. Excess melanin is delivered to epidermal cells, changing the skin tone and leading to skin darkening. Other ultraviolet rays may cause skin cancer through DNA damage.

  For the purpose of preventing and improving various skin problems such as rough skin, photoaging, pigmentation, etc. caused by ultraviolet rays, conventionally, cosmetics, pharmaceuticals, foods, etc. have been used for dibutylhydroxytoluene (BHT), butylhydroxyanisole. Synthetic antioxidants such as (BHA) and various antioxidants such as naturally derived α-tocopherol and ascorbic acid are used (for example, see Patent Documents 1 and 2). However, the effect of preventing and improving skin troubles caused by exposure to ultraviolet rays is not sufficient, and there is a current situation that the antioxidant property does not necessarily lead to improvement of skin troubles caused by ultraviolet rays. Furthermore, the former synthetic antioxidant has a concern in terms of safety, and the latter has many problems in terms of stability.

  In addition, various antioxidant substances extracted from plant seeds have been manufactured and tried to be formulated into cosmetics, pharmaceuticals, foods, etc. When using plants as raw materials, procurement of the raw materials, production costs, etc. From the standpoint of production, the production amount is limited, and the production cost is expensive. Therefore, it is difficult to blend an effective amount substantially.

JP-A-5-320036 JP-A-9-263513

  Under such circumstances, the object of the present invention is to provide a safe, stable and inexpensive external composition for skin that is excellent in the effect of improving rough skin and skin blackening caused by oxidation reaction and inflammation reaction caused by ultraviolet rays and the like. Is to provide.

  As a result of intensive studies in view of the above circumstances, the present inventors have found that various extracts having an antioxidant effect and an anti-inflammatory effect are contained in the extract obtained from the flower bud of Honkan elephant. When blended in a composition for external use on the skin, it has been found that it has a remarkable effect in terms of improving rough skin and skin blackening caused by ultraviolet rays. Moreover, they are naturally derived substances, have no safety problems, and have excellent stability.

  That is, the first invention of the present application lies in an external composition for skin characterized by blending an extract obtained by solvent extraction from the licorice of Honkan elephant. 2nd invention exists in said skin external composition characterized by the extraction solvent being chosen from water, a water-soluble organic solvent, or these mixed solvents.

  In the present invention, by blending an extract obtained from the licorice of licorice into a composition for external use of the skin, it is excellent in the effect of improving rough skin and skin blackening caused by skin damage caused by ultraviolet rays etc. Thus, a stable and inexpensive composition for external use on the skin can be provided.

Hereinafter, embodiments of the present invention will be described in detail. Honkan elephant ( Hemerocallis fulva Linn.) Is a lily family plant native to China and is widely cultivated in various parts of China. The flower buds are effective for antipyretic and the roots and leaves are effective for diuresis and swelling. In addition, boiled and dried flower buds are general-purpose foods in the Greater China region and are generally used as gold needle vegetables, dried lily buds, and the like. Therefore, the licorice florets dried raw or boiled can be obtained at low cost. In addition, the external application to the skin of the floret or its extract is not performed.

  In the present invention, the extraction solvent used for solvent extraction can be any known extraction solvent used for solvent extraction from plant materials. As the extraction solvent, a solvent having a relatively high hydrophilicity is preferably used because an effective extract that meets the object of the present invention can be obtained. As such a solvent, in the present invention, a solvent selected from water, a water-soluble organic solvent or a mixed solvent thereof is particularly preferably used. The water-soluble organic solvent refers to a solvent having some compatibility with water, specifically, lower alcohols such as methanol, ethanol, propanol, isopropanol, butanol, polyhydric alcohols such as butylene glycol, propylene glycol, Examples thereof include aliphatic carboxylic acid esters such as methyl acetate and ethyl acetate, and other relatively polar organic solvents such as acetone. Among the extraction solvents, an aqueous ethanol solution is preferable.

  In the extraction, firstly the licorice florets are shredded and crushed by a known appropriate means. Extraction with a solvent may be performed according to a known method. For example, when water, a water-soluble organic solvent or a mixed solvent thereof is used as an extraction solvent, the extraction solvent amount is 1 to 50 times, preferably 3 to 10 times, 0 to 100 ° C. What is necessary is just to extract for 0.1 to 50 hours, preferably 0.5 to 24 hours under the temperature conditions in the range of ° C and lower than the boiling point of the extraction solvent. The extraction may be in a stationary state, but it is desirable to perform the extraction with moderate stirring for more efficient extraction.

  The licorice floret extract thus obtained may be blended into the composition for external use as it is, or may be blended after being concentrated or dried. Moreover, you may use what re-extracted what was extracted with the other organic solvent etc. Furthermore, a fraction obtained by fractionating and purifying the extract by a known fractionation means or purification means may be used.

The composition for external application of skin containing the licorice flower extract of the present invention can be various pharmaceuticals, quasi drugs, cosmetics, cosmetics and the like. The dosage form is not particularly limited, and various forms can be used. Specifically, ointments, lotions, emulsions, creams, packs, granules, cataplasms, and the like can be used. Cosmetics are not particularly limited as long as they are applied to the human skin, and are cosmetics such as skin cosmetics, foundations, makeup cosmetics such as lipsticks, hair cosmetics such as shampoos, rinses and treatments, bath preparations, facial cleansers. However, skin cosmetics and whitening cosmetics intended to improve rough skin are particularly preferable.

  The amount of licorice floret extract blended in the composition for external use of the skin according to the present invention is not particularly limited, and since it varies depending on the purpose and the target, it cannot be specified unconditionally. Generally, it can be used at 0.00001 to 5.0% by mass, preferably 0.001 to 1.0% by mass in terms of dry matter.

  Moreover, the composition for external use of this invention can be mix | blended combining the various components normally used in the range which does not impair the effect as needed. For example, in the case of cosmetics, oils, surfactants, humectants, thickeners, preservatives, antioxidants, ultraviolet absorbers, ultraviolet scattering agents, fragrances, dyes, pigments and the like.

  EXAMPLES Hereinafter, although this invention is explained in full detail based on an Example and a comparative example, this invention is not limited by these. Moreover, unless otherwise specified,% shown in an Example and a comparative example means the mass%.

Production Example 100.4 g of dried lily bud dried in boiled water was chopped with a knife. 500 mL of 50% ethanol aqueous solution was added to the shredded florets, extracted as it was with stirring for 24 hours at room temperature, and then filtered to obtain honkanzo florets extract (348 g, 46.3 g in terms of solid content). It was.

[Measurement of antioxidant power]
According to the following method, the antioxidant power of the licorice flower extract was measured.
Liquid A: 0.5 mmol / L DPPH (1,1-Diphenyl-2-picrylhydrazyl, Wako Pure Chemical Industries) ethanol solution B liquid: 100 mmol / L Tris-HCl aqueous solution (pH 7.4)
C liquid (sample): Honkan elephant flower extract in production example Procedure: Take 1.0 mL of A liquid, 0.8 mL of B liquid and 0.2 mL of C liquid respectively in a test tube, and stir with a vortex mixer for about 10 seconds, then at room temperature And then left to stand for 20 minutes in the dark, and then the absorbance A517 at ₅₁₇ nm was measured with a spectrophotometer. As a control, the same amount of 75% ethanol solution was added instead of liquid C, and the same amount of ethanol was added instead of liquid A for the purpose of correcting the absorbance derived from the measurement sample itself, The antioxidant power value was determined according to the following equation. As a comparison of the antioxidant power, a 1 mmol / L ascorbic acid solution prepared with a 75% ethanol solution was used instead of the C solution.
Formula: [A ₅₁₇ (control)-{A ₅₁₇ (sample) -A ₅₁₇ (correction)}] / A ₅₁₇ (control) × 100 (%)

  The measurement results are shown in Table 1. The antioxidant power of the licorice flower extract of the present invention was comparable to that of ascorbic acid.

[Table 1]
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Sample Antioxidant power (%)
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94.19 Extract of Honkan elephant flower of production example
Ascorbic acid (control) 75.99
――――――――――――――――――――――――

[Tyrosinase activity inhibitory effect]
The activity inhibitory effect on mushroom tyrosinase of the licorice flower extract of the present invention was evaluated as follows.

1. Activity Evaluation System An L-tyrosine solution (pH 6.8) was used as a substrate solution, mushroom tyrosinase was allowed to act on this at 37 ° C., and the resulting dopachrome was evaluated by measuring the absorbance at 475 nm.
2. Inhibition test A sample solution appropriately diluted with a 50% ethanol aqueous solution was added to the substrate solution of the activity evaluation system, and tyrosinase was allowed to act on this solution to measure the absorbance.
3. Inhibitory effect Based on the increase in absorbance in the control using 50% aqueous ethanol instead of the sample, the inhibition rate (%) was calculated from the absorbance, and this was used as the activity inhibition rate as an index of the tyrosinase activity inhibition effect. .

  The evaluation results are shown in Table 2. It was found that the licorice flower extract of the present invention has an inhibitory effect on mushroom tyrosinase activity.

[Table 2]
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Concentration Activity inhibition rate
(Mass%) (%)
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Honkan Elephant Flower Extract 0.02 18.2
0.05 31.1
0.10 46.3
―――――――――――――――――――――――

[Melanin synthesis inhibitory effect]
The melanin synthesis inhibitory effect of the licorice flower extract of the present invention was evaluated by the following test using B16 melanoma cells.

1. Cell culture conditions B16 melanoma cells were seeded in 12-well culture plates at 10 ⁴ cells / well and pre-cultured for 24 hours at 37 ° C. in a 5% (v / v) CO ₂ atmosphere. The medium was replaced with a theophylline-added (2 mmol / L) medium containing the honkanzo flower extract of the production example at various concentrations, followed by melanin-induced culture for 72 hours.
2. Melanin quantification After culturing, cells were treated with 10% trichloroacetic acid followed by ethanol / diethyl ether (1: 1, v / v) and then dissolved in 1 mol / L NaOH aqueous solution containing 10% dimethyl sulfoxide. I let you. Absorbance at 475 nm was measured and used as an indicator of the amount of melanin synthesis.
3. Synthesis Inhibitory Effect Relative values of absorbance when the licorice floret extract was added at various concentrations were calculated based on the absorbance value when the licorice floret extract was not added. An inhibition curve was created based on the relative values of the extract concentration and absorbance, and from this, the concentration at which melanin synthesis was inhibited by 50% (IC ₅₀ value) was calculated and used as an index of the melanin synthesis inhibitory effect.

As a result of the test, the IC ₅₀ of the Honkan elephant flower bud extract of Production Example was 0.2% (corresponding to 0.027% in terms of solid content), and it was found that the Honkan elephant flower bud extract of the present invention has a high melanin synthesis inhibitory effect. It was. Incidentally, _{IC 50} of the ascorbic acid is known to be about 60 [mu] g / mL.

Example 1 [Rough skin improvement effect]
The effect of the composition for external use containing the licorice flower extract of the present invention on the rough skin of ultraviolet rays was evaluated by the following test using hairless mice. The animals were 5 groups of 9 hairless mice aged 9 weeks at the start of the test.

1. Ultraviolet irradiation and rough skin evaluation method Ultraviolet irradiation was performed by irradiating UVB region ultraviolet rays in an amount of about 7 times the minimum amount of erythema. The degree of rough skin caused by ultraviolet irradiation was evaluated by the fluctuation of transdermal moisture transpiration (TEWL). TEWL was measured using a hydrograph before sample application, before ultraviolet irradiation, after 3 days and after 4 days of irradiation. A value obtained by dividing the values after 3 days and 4 days after irradiation by the value before the sample application was calculated as the TEWL fluctuation rate, and this value was used as an index of the degree of rough skin.
2. Sample and Experimental Method Using a 50% aqueous ethanol solution as a base, a sample (Example 1) was prepared by blending the licorice flower extract obtained in Production Example at a concentration of 1%. First, 0.05 mL of these samples were applied to the skin of the back test site of hairless mice once a day for 7 days (preliminary application). The day after the final pre-application, UV irradiation was performed, and the sample was also applied the next day after irradiation and 2 days after the irradiation. Table 3 shows the effect of the sample application on the rough skin of the hairless mouse. In addition, the sample of only the base was used as Comparative Example 1.

[Table 3]
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Sample TEWL fluctuation rate ―――――――――――――――――――――――――――――――――――
Example 1 (Hangzhou elephant flower extract 1.0%) 5.92 (3 days after irradiation)
4.87 (4 days after irradiation)
Comparative Example 1 (base only) 7.27 (3 days after irradiation)
8.17 (4 days after irradiation)
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  In this test system, the smaller the TEWL fluctuation rate is, the more the UV rough skin is suppressed. From the comparison between the Examples and Comparative Examples in Table 3, it was found that rough skin caused by ultraviolet rays was improved by applying the composition for external application of skin containing the licorice flower extract. In addition, the fluctuation | variation of TEWL by prior application was not seen.

Example 2 [Evaluation of safety and stability]
A lotion of Example 2 was prepared with the composition shown in Table 4 below, and applied as a test sample to human skin continuously for 1 month.

[Table 4]
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Compounding amount Component name (% by mass)
―――――――――――――――――――――
Ethanol 5.0
Polyoxyethylene monolaurate 0.3
Sorbitan (20E.O.)
Methyl paraoxybenzoate 0.1
Honkan Elephant Flower Extract (Production Example) 1.0
Purified water residual amount ―――――――――――――――――――――

  As a result of the test, no side effects such as itching and dryness were observed. Further, this test sample was placed in a constant temperature bath at 40 ° C. and left for one month, but no precipitate was formed or discolored, and the stability was excellent.

  The present invention can provide cosmetics and the like as an external composition for skin. Examples are given below, but the present invention is not limited to these examples. In addition, a compounding quantity is the mass%.

Example 3 (skin lotion)
Ingredient name Blending amount A component (1) Olive oil 10.0
(2) Isopropyl myristate 1.0
(3) Monolauric acid 0.5
Polyoxyethylene (20) sorbitan (4) Propylene glycol 1.0
(5) Glycerin 2.0
B component (6) Honkan elephant flower extract of production example 5.0
(7) Methyl paraben 0.1
(8) Ethanol 7.0
(9) Purified water remaining amount After each component A and component B were uniformly dissolved, the components A and component B were mixed, stirred and dispersed, and then filled into a container. In use, the contents are uniformly shaken and dispersed.

Example 4 (skin cream)
Ingredient name Compounding amount A component (1) dense wax 25.0
(2) Stearic acid 5.0
(3) Stearyl alcohol 5.0
(4) Reduced lanolin 2.0
(5) Squalene 2.0
(6) Monostearate sorbitan 3.0
Monostearate (7) Polyoxyethylenesorbitan 3.0
(8) Propylene glycol 5.0
B component (9) Honkan elephant flower extract of production example 5.0
(10) Methylparaben 0.2
(11) Remaining amount of purified water After each component A and component B were heated and dissolved, the mixture was stirred and cooled to 30 ° C. to produce a skin cream.

According to the present invention, a safe, stable, and inexpensive skin external composition containing an extract of licorice florets is provided, and rough skin and black skin caused by oxidative reaction, inflammatory reaction, etc. caused by ultraviolet rays and the like are provided. Can be improved.

Claims (2)

A skin whitening composition for whitening , characterized in that it contains an extract obtained by solvent extraction from a flower of Honkan elephant with an extraction solvent selected from water, a water-soluble organic solvent or a mixed solvent thereof. The whitening skin composition for external use according to claim 1, wherein the extraction solvent is an aqueous ethanol solution .