JP2001270820A - Skin care preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a skin care preparation capable of synergistically enhancing whitening effect of an extract of Arctostaphylos uva-ursi by including an extract of Arctostaphylos uva-ursi, an oil soluble extract of Glycyrrhiza and extract of Gentiana lutes, which has a stable and anexcellent whitening effect, exhibits a high suppressing effect on pigmentation caused by sunburn, effective for prevention/improvement of melanization caused by sunburn, mark and freckles. SOLUTION: This skin care preparation includes (A) 0.0001-5 mass. % of the extract of Arctostaphylos uva-ursi, (B) 0.0001-5 mass. % of the oil soluble extract of Glycyrrhiza and (C) 0.0001-5 mass. % of the extract of Gentiana lutea.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin containing a bearberry extract, an oil-soluble licorice extract and a gentian extract, and more particularly to a bearberry berry extract, an oil-soluble licorice extract and a gentian extract. The present invention relates to an external preparation for skin having an excellent skin-whitening effect on the skin, such as by preventing pigmentation from occurring when combined with a product.

[0002]

2. Description of the Related Art Conventionally, medicinal ingredients have been added to skin external preparations such as emulsions, creams, lotions, packs, detergents, dispersions, ointments, and external preparations for the purpose of imparting a predetermined medicinal effect to them. Have been. For example, whitening agents such as ascorbic acid, glutathione, and hydroquinone have been added to prevent phenomena such as darkening of the skin caused by sunburn, pigmentation, and spots and freckles caused by pigmentation. In addition, the extract of bearberry leaves (Uwaurushi) stains,
It is known that pigmentation such as freckles is prevented and has a whitening effect (JP-A-6-166609).

[0003]

However, skin external preparations containing these whitening agents, such as cosmetics and external medicines, are not effective enough for the whitening agent or may be deteriorated in the preparation. In some cases, the medicinal effect of the first stage may not be obtained, and improvement has been desired. An object of the present invention is to provide a skin external preparation having a stable and excellent whitening effect.

[0004]

Means for Solving the Problems The present inventors have conducted intensive studies to improve the effect of the medicinal component of the external preparation for skin. As a result, the extract of the bearberry extract, the oil-soluble licorice extract and the gentian extract were combined. For example, the present inventors have found that the whitening effect of the bearberry extract can be enhanced synergistically, and completed the present invention.

That is, the present invention provides the following component (A):
(B) and (C) A skin external preparation characterized by containing (A) a bear berry extract (B) an oil-soluble licorice extract (C) a gentian extract.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION The Bearberry extract, which is the component (A) of the present invention, is a plant belonging to the family Azaleaaceae, and uses an extraction solvent from stems and leaves (Uwaurushi) of Bearberry (Arctostaphylos uva ursi). To extract. The preparation method is not particularly limited, but, for example, extraction is performed at low temperature or at room temperature to heating using various suitable solvents.

As the extraction solvent, for example, one or more of water; lower monohydric alcohols such as methyl alcohol and ethyl alcohol; and liquid polyhydric alcohols such as glycerin, propylene glycol and 1,3-butylene glycol are used. be able to. As an example of a preferable extraction method, after performing extraction for 2 to 3 days while heating using purified water, a part of the tannin is removed, filtered, and the obtained filtrate is further left for about 5 days. A method of aging and filtering again.

The content of the bearberry extract, which is the component (A) of the present invention, is preferably 0.000 as a dry solid content.
01 to 5% by mass (hereinafter simply referred to as "%"), and more preferably 0.001 to 3%. When the content of the bearberry extract is within this range, the effects of the present invention are more effectively exhibited.

The oil-soluble licorice extract (B) of the present invention is a perennial herb belonging to the legume family, and is a licorice (scientific name: Glycyr).
rhiza glabra linne) using an extraction solvent.
The preparation method is not particularly limited, but, for example, extraction is performed at low temperature or at room temperature to heating using various suitable solvents.

As the extraction solvent, one or more of lower monohydric alcohols such as methyl alcohol and ethyl alcohol; and liquid polyhydric alcohols such as glycerin, propylene glycol and 1,3-butylene glycol may be used. it can. Examples of preferred extraction methods include:
Extraction is performed for 2 to 10 hours using ethyl alcohol while heating, followed by filtration, and the obtained filtrate is left to mature for about 2 to 3 days, followed by filtration again.

The content of the oil-soluble licorice extract as the component (B) of the present invention is preferably 0.000 as a dry solid content.
1 to 5%, more preferably 0.001 to 3%. When the content of the oil-soluble licorice extract is within this range, the effects of the present invention are more effectively exhibited.

The gentian extract, which is the component (C) of the present invention, is a plant belonging to the family Gentian and is extracted from roots and rhizomes of gentian (Gentiana lutea linne (Gentianaceae)) using an extraction solvent. The preparation method is not particularly limited, but, for example, extraction is performed at low temperature or at room temperature to heating using various suitable solvents.

As the extraction solvent, for example, one or more of water; lower monohydric alcohols such as methyl alcohol and ethyl alcohol; and liquid polyhydric alcohols such as glycerin, propylene glycol and 1,3-butylene glycol are used. be able to. As an example of a preferable extraction method, a 50% 1,3-butylene glycol aqueous solution is used,
After performing extraction for 2 to 10 hours while heating, filtration was performed, and the obtained filtrate was left to mature for about 2 to 3 days,
There is a method of performing filtration again.

The content of the gentian extract which is the component (C) of the present invention is preferably 0.000 as a dry solid content.
1 to 5%, more preferably 0.001 to 3%. When the content of the gentian extract is within this range, the effects of the present invention are better exhibited.

In addition to the components (A), (B) and (C), the external preparation for skin of the present invention usually contains cosmetics and pharmaceuticals, if necessary, as long as the effects of the present invention are not impaired. Ingredients used in the preparation of quasi-drugs, topical medicines, etc., i.e., water (purified water, hot spring water, deep water, etc.), oils, surfactants, metal soaps, gelling agents, powders, alcohols, water-soluble Polymer, film forming agent, resin, ultraviolet ray protective agent, clathrate compound, antibacterial agent, fragrance, deodorant, salt, pH regulator, freshener, animal / microorganism-derived extract, plant extract, blood circulation promoter , Astringent, antiseborrheic, active oxygen scavenger, cell activator,
Moisturizers, keratolytic agents, enzymes, hormones, vitamins and the like can be added.

The external preparation for skin of the present invention comprises the component (A)
The components (B) and (C) are blended as essential components, and can be prepared according to a conventional method. Examples of the form of the external preparation for skin are not particularly limited and include, for example, emulsions, creams, lotions, packs, skin care cosmetics such as lipsticks, makeup cosmetics such as lipsticks, foundations, ointments, dispersions,
It can be a pharmaceutical such as a liquid for external use, etc., and there is no particular limitation on the form of the drug. Solid, paste, mousse, gel, powder, solution, solubilization, emulsification, powder dispersion The system can be in a multilayer form.

[0017]

EXAMPLES Next, the present invention will be described in more detail with reference to Reference Examples, Test Examples and Examples, but the present invention is not limited thereto.

REFERENCE EXAMPLE 1 Production of Bearberry Extract (30 g) The dried leaves of Bearberry (Arctostaphylos uva ursi) were added to 30 g of dried leaves at a concentration of 80 vol% ethyl alcohol (100 mL), extracted at room temperature for 3 days, and filtered. Thus, a bearberry extract was obtained (dry solid content: 3.0%).

Reference Example 2 Production of Bearberry extract (30 g of dried leaves of Bearberry) (scientific name: Arctostaphylos uva ursi) was added to 30 g of dried leaf containing 80 vol% of 1,3-
After adding 100 mL of butylene glycol, extraction was performed at room temperature for 3 days, and filtration was performed to obtain a bearberry extract (2.50% dry solid content).

Reference Example 3 Production of oil-soluble licorice extract To 20 g of dried licorice (Glycyrrhiza glabra linne) root, 100 mL of ethyl alcohol was added, and the mixture was extracted at room temperature for 5 days. A soluble licorice extract was obtained (dry solid content: 5.0%).

Reference Example 4 Gentian extract Gentian (scientific name: Gentiana lutea linne (Gentianacea
e)) 20 vol% to 10 g of coarse powder of root and rhizome
100 mL of ethyl alcohol was added, and the mixture was extracted for 3 days with occasional stirring at room temperature, followed by filtration to obtain a gentian extract (dry solid content: 3.0% each).

Test Example 1 Tyrosinase activity inhibition test The bearberry extract obtained in Reference Example 1 was obtained by the following method.
Regarding the oil-soluble licorice extract obtained in Reference Example 2 and the gentian extract obtained in Reference Example 3, the tyrosinase activity inhibition rate of a sample alone or in combination thereof was examined. That is, 0.1 mL of an enzyme solution [10 mg of tyrosinase (28,000 units, manufactured by Sigma) dissolved in 20 mL of 0.1 mol / L phosphate buffer (pH 6.8)] was added to each sample.
Was added, and 0.1 M phosphate buffer (pH 6.8) was further added to make 4.0 mL, which was incubated at 25 ° C. for 10 minutes.

Next, a substrate solution [L-DOPA (manufactured by Tokyo Chemical Industry Co., Ltd.) 19
8.0 mg of 0.1 mol / L phosphate buffer (pH 6.0)
8) Dissolved in 100 mL] and added 1.0 mL
It was allowed to react for 0 minutes. After the reaction, the absorbance at 475 nm (OD _S ) was measured. Similarly, the absorbance (OD _HE ) when the enzyme was reacted with the heat-inactivated enzyme, the absorbance (OD _B ) when the enzyme was added and the sample was not added, and the sample and the inactivated enzyme were added. Absorbance (OD _{S HE} )
Was measured, and the activity inhibition rate of tyrosinase activity was calculated from Formula 1 and the results are shown in Table 1.

[0024]

(Equation 1)

[0025] In the formula, OD _S absorbance upon addition Samples and enzymes, OD _B is the absorbance in the case without addition of the sample enzyme addition, OD _HE absorbance at enzyme inactivation, OD _SHE samples and inactivation This is the absorbance when the added enzyme is added.

[0026]

[Table 1]

As is evident from Table 1, when the bearberry extract, oil-soluble licorice extract and gentian extract are combined, when the bearberry extract, oil-soluble licorice extract and gentian extract are used alone, respectively. Tyrosinase activity was significantly higher than that of tyrosinase.

Test Example 2 Melanin Production Inhibition Test by Cell Culture The bearberry extract obtained in Reference Example 1 was obtained by the following method.
With respect to the oil-soluble licorice extract obtained in Reference Example 2 and the gentian extract obtained in Reference Example 3, a melanin production inhibitory effect of a sample alone or in combination thereof was examined. For cultured cells, mouse-derived B16 melanoma cultured cells were used.
An appropriate amount of the medium was taken in two 6-well dishes, and B16 melanoma cells were inoculated and allowed to stand at 37 ° C. in a carbon dioxide concentration of 5%. On the next day, each sample was tested at a final concentration of 0 (control), 1, 1
A sample preparation solution was added and mixed so as to be 0 and 100 μg / mL. On the fifth day of the culture, the medium was replaced, and the sample preparation solution was added again. On the next day, the medium was removed, and the cells were washed with a phosphate buffer in one petri dish and collected.
The whitening degree of the melanoma cultured cells was evaluated based on the following criteria.

(Criterion) ++: extremely white with respect to the control. +: Clearly white with respect to the control. ±: slightly white with respect to the control. -: The same black color as the control.

For the remaining one petri dish, the cells were fixed in formalin and added to a 1% crystal violet solution for staining. The viable cell ratio for each sample concentration was measured with a monocerator (Olympus). Table 2 shows the above results.

[0031]

[Table 2]

As is evident from Table 2, when the bearberry extract, the oil-soluble licorice extract and the gentian extract are combined, when the bearberry extract, the oil-soluble licorice extract and the gentian extract are used alone, respectively. It showed a much higher whitening effect than the above, and was found to be less toxic to cultured B16 melanoma cells.

Test Example 3 Pigmentation Inhibition Test The back of a colored guinea pig (15 animals in each group) was shaved and irradiated with ultraviolet light under anesthesia. UV irradiation is performed by FL2 manufactured by Toshiba Corporation.
Irradiate three 0S • BLB lamps and three FL20S • E30 lamps at the same time, and the amount of ultraviolet rays is 4.8 × 10 ⁶ erg /
cm ² . Twenty-four hours before, immediately after, and 12 hours after and 24 hours after the irradiation with ultraviolet rays, 0.2 g each of the composition shown in Table 3 and the sample prepared by the following method were applied to four places on the back of the guinea pig. However, before irradiation, the application site was thoroughly washed with warm water. Seven days after irradiation, the degree of pigmentation was observed and evaluated according to the following criteria. Table 3 shows the results.

[0034]

[Table 3]

(Production method) Components (1) to (6), (1
0) is mixed and heated to 70 ° C. B. Heat (12) and keep at 70 ° C. C. Add B to A, mix and cool (7)
(8), (9) and (11) were added and mixed to obtain a cream.

(Evaluation Criteria for Pigmentation Inhibition Effect) <Evaluation> <Contents> Excellent Effect No pigmentation was observed at all. Effective Very slight pigmentation is observed. Slightly effective pigmentation is observed, but the boundary with the non-irradiated part is unclear. Ineffective Pigmentation was observed, and the boundary with the non-irradiated part was clear.

As shown in the results in Table 3 (the numbers in the column of the effect of inhibiting pigmentation are the number of guinea pigs corresponding to each), the bearberry extract, the oil-soluble licorice extract and the gentian extract were combined. It has been clarified that the skin external preparation of the present invention product 1 effectively suppresses pigmentation due to ultraviolet rays by applying them to the skin.

Example 1 Lotion (Formulation) (%) (1) Glycerin 5.0 (2) 1,3-butylene glycol 6.5 (3) Polyoxyethylene (20EO) 1.2 Sorbitan monolaurin Acid ester (4) Ethyl alcohol 8.0 (5) Bearberry extract * 1 0.5 (6) Oil-soluble licorice extract * 2 0.1 (7) Gentian extract * 3 0.2 (8) Preservative Appropriate amount (9) Perfume Appropriate amount (10) Remaining purified water * 1 Produced in Reference Example 1 * 2 Produced in Reference Example 3 * 3 Produced in Reference Example 4

(Production method) Components (3), (4), (8) and (9) are mixed and dissolved. B. Components (1), (2), (5), (6), (7) and (10) are mixed and dissolved. C. A and B were mixed and made uniform to obtain a lotion.

Example 2 Emulsion (Formulation) (%) (1) Polyoxyethylene (10EO) 1.0 Sorbitan monostearate (2) Polyoxyethylene (60EO) 0.5 Sorbit tetraole Eate (3) Glyceryl monostearate 1.0 (4) Stearic acid 0.5 (5) Behenyl alcohol 0.5 (6) Squalane 8.0 (7) Bearberry extract * 1 0.3 (8) Oil-soluble licorice Extract * 2 0.1 (9) Gentian extract * 3 0.3 (10) Preservative 0.1 (11) Carboxyvinyl polymer 0.1 (12) Sodium hydroxide 0.05 (13) 1,3 -Butylene glycol 5.0 (14) Remaining amount of purified water (15) Appropriate amount of fragrance * 1 Manufactured in Reference Example 1 * 2 Manufactured in Reference Example 3 * 3 Manufactured in Reference Example

(Production method) Heat and mix components (12) and (13) with a portion of (14) and maintain at 70 ° C. B. Components (1) to (6) and (10) are mixed by heating.
Keep at 0 ° C. C. Add A to B, mix and emulsify uniformly. D. After cooling C, (7) to (9) and (11) were mixed and dissolved in the remainder of (14), (15) was added, and the mixture was uniformly mixed to obtain an emulsion.

Each of Examples 1 and 2 has excellent stability over time, and when applied to the skin, prevents "dullness" of the skin due to sunburn, spots and freckles, and makes the skin beautiful and transparent. Water and emulsion.

Example 3 Ointment (Formulation) (%) (1) Stearic acid 18.0 (2) Cetanol 4.0 (3) Triethanolamine 2.0 (4) Glycerin 5.0 (5) Bearberry extract * 1 0.2 (6) Oil-soluble licorice extract * 2 0.1 (7) Gentian extract * 3 0.3 (8) Remaining amount of purified water * 1 Produced in Reference Example 2 * 2 Reference Example 3 * 3 Manufactured in Reference Example 4

(Production Method) A. Heat-mix components (3), (4) and (8) and mix
Keep at ° C. B. Heat mix components (1) and (2) and maintain at 75 ° C. C. Add A slowly to B. D. While cooling C, add (5), (6) and (7)
An ointment was obtained.

Example 3 was an ointment which was excellent in stability over time and applied to the skin to prevent "dullness", spots and freckles on the skin, and to give a clear and beautiful skin.

Example 4 Pack (Formulation) (%) (1) Polyvinyl alcohol 20.0 (2) Ethyl alcohol 20.0 (3) Glycerin 5.0 (4) Kaolin 6.0 (5) Bearberry extract * 1 0.1 (6) Oil-soluble licorice extract * 2 0.1 (7) Gentian extract * 3 0.2 (8) Preservative 0.2 (9) Fragrance 0.1 (10) Purified water * 1 Manufactured in Reference Example 2 * 2 Manufactured in Reference Example 3 * 3 Manufactured in Reference Example 4

(Production method) Mix components (1)-(4), (8) and (10), heat to 70 ° C. and stir. B. After cooling A,
(5) to (7) and (9) were added and stirred uniformly to obtain a pack.

Example 4 was a pack which was excellent in stability over time and applied to the skin to prevent the skin from dulling and spotting, and to make the skin transparent and beautiful.

Example 5 Liquid Foundation (Formulation) (%) (1) Lanolin 7.0 (2) Liquid Paraffin 5.0 (3) Stearic Acid 2.0 (4) Cetanol 1.0 (5) Paramethoxy Silicate Cinnamic acid 3.0-2-ethylhexyl (6) 4-t-butyl-4'-methoxy 1.0 dibenzoylmethane (7) glycerin 5.0 (8) triethanolamine 1.0 (9) carboxymethylcellulose 0 0.7 (10) Remaining purified water (11) Mica 15.0 (12) Talc 6.0 (13) Color pigment 6.0 (14) Bearberry extract * 1 0.1 (15) Oil-soluble licorice extract * 2 0.1 (16) Gentian extract * 3 0.2 (17) Perfume appropriate amount * 1 Manufactured in Reference Example 1 * 2 Manufactured in Reference Example 3 * 3 Manufactured in Reference Example 4

(Production method) Components (1) to (6) are mixed and dissolved. B. Add components (11) to (13) to A, mix uniformly, and keep at 70 ° C. C. Components (7) to (10) are uniformly dissolved and kept at 70 ° C. D. Add C to B and emulsify uniformly. E. FIG. After cooling D, components (14) to (17) were added to obtain a liquid foundation.

Example 5 was a liquid foundation which was excellent in stability over time and applied to the skin to prevent darkening of the skin due to sunburn, spots and freckles.

[0052]

According to the present invention, bearberry extract,
By containing the oil-soluble licorice extract and the gentian extract, the whitening effect originally possessed by the bearberry extract can be synergistically enhanced. That is, since it has a stable and excellent whitening effect, it exerts a high inhibitory effect on pigmentation due to sunburn, and is effective in preventing / improving skin blackening, spots and freckles due to sunburn. As described above, the skin external preparation of the present invention can sufficiently exhibit the inherent performance of a whitening agent, and is therefore extremely useful in beauty and medicine.

 ──────────────────────────────────────────────────続 き Continuing on the front page (72) Inventor Yuki Hata 48-18, Sakaemachi, Kita-ku, Tokyo Inside Kose Research Laboratory (72) Inventor Hiroki Nakayama 8-5-1 Nishishinjuku, Shinjuku-ku, Tokyo T-farm Japan Co., Ltd.

Claims (4)

[Claims] 1. An external preparation for skin comprising the following components (A), (B) and (C): (A) a bearberry extract; (B) an oil-soluble licorice extract; and (C) a gentian extract. . 2. The content of the bearberry extract is 0.000.
The external preparation for skin according to claim 1, which is 1 to 5% by mass. 3. The oil-soluble licorice extract content of 0.0001.
The external preparation for skin according to claim 1, wherein the amount is from 5 to 5% by mass. 4. A gentian extract having a content of 0.0001.
The external preparation for skin according to claim 1, wherein the amount is from 5 to 5% by mass.