JPH10182404A - Preparation for external use for skin - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a preparation for external use for skin useful for cosmetic and external drug by using extract of Rakanka (fruit of Momordica grosvenorii) and a tyrosinase inhibiting agent as essential components. SOLUTION: This preparation for external use for skin exhibiting high effect of suppressing pigmentation and effective, e.g., for preventing and improving spots and freckles caused by sunburn, etc., is produced by using preferably 0.0005-10wt.%, especially 0.005-5wt.% (in terms of dried solid component) of Rakanka extract produced by extracting dried fruit of Momordica grosvenorii Swingle with one or more extractants such as water, a lower monohydric alcohol, a liquid polyhydric alcohol, etc., in combination with 0.0001-10wt.%, especially 0.001-5wt.% of one or more tyrosinase inhibiting agents (e.g. ascorbic acid, its derivative, cysteine or its derivative), thereby sufficiently developing the effect of the tyrosinase inhibitor.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for the skin, and more particularly, to a cosmetic, an external preparation and the like having an excellent skin-whitening effect on the skin by blending an extract of Arhat fruit and an inhibitor of tyrosinase activity. Skin external preparation.

[0002]

2. Description of the Related Art Conventionally, skin external preparations such as emulsions, creams, lotions, packs, detergents, foundations, dispersions, ointments and the like have been used for blackening of the skin caused by sunburn and the like, spots and freckles caused by pigmentation. To prevent phenomena such as calamine, ascorbic acids, glutathione,
It contains colloidal sulfur, hydroquinone, cinamic aldehyde, placenta extract and the like.

[0003]

However, in a skin external preparation containing these whitening ingredients, the effect of the whitening ingredients is not sufficient, or the desired medicinal effect is obtained due to deterioration in the preparation. In many cases, no improvement was desired.

[0004]

Means for Solving the Problems The present inventors have conducted intensive studies to improve the effect of the whitening component of the external preparation for skin. As a result, the combination of an extract of Arhat fruit and an inhibitor of tyrosinase activity originally required tyrosinase. The present inventors have found that the action of the activity inhibitor is sufficiently exerted, and completed the present invention.

[0005] That is, the present invention provides an external preparation for skin containing the following components (A) and (B): (A) an extract of arhat fruit (B) and a tyrosinase activity inhibitor.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION The component (A) of the present invention, an extract of Arhat fruit, is momordica grosvenorii;
Grosvenorii Swingle fruit is extracted from the dried fruit 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 a preferred example of the extraction method, extraction was performed at room temperature for 1 to 5 days using ethyl alcohol or 1,3-butylene glycol having a water content of 20 to 80% (v / v), followed by filtration. There is a method in which the filtrate is left to mature for about one week and then filtered again.

[0008] The content of the extract of Rakan fruit in the external preparation for skin of the present invention is preferably 0.0005 as dry solids.
To 10% by weight (hereinafter simply referred to as "%"), and more preferably 0.005 to 5%. Within this range, the tyrosinase activity inhibitor can be stably compounded, and the effect of the tyrosinase activity inhibitor can be synergistically enhanced. When an extract is used, the concentration of the extract is not limited at all, as long as the content of dry solids as a solute is within the above range.

On the other hand, examples of the tyrosinase activity inhibitor which is the component (B) of the present invention include the following.

That is, ascorbic acid and its derivatives and salts thereof (for example, magnesium L-ascorbyl phosphate), cysteine and its derivatives (for example, N,
N′-diacetylcystine dimethyl, etc.) and salts thereof,
Placenta extract, Aloe extract, Ibukitrano extract, chamomile extract, Clara extract, Calyptium extract, Hawthorn extract, Sampens extract, Shirahuri extract, Sempukuka extract, Sohakuhi extract, Touki extract, Neubara Examples include flavonoids such as an extract, a hop extract, a yokunin extract, glabridine, glabrene, liquiritin, isoliquiritin, and a licorice extract containing these flavonoids.

The content of the tyrosinase activity inhibitor in the external preparation for skin of the present invention is preferably 0.0001 to 10% by weight (hereinafter simply referred to as "%") as a dry solid content, and more preferably 0.001 to 10% by weight. From 5%. Within this range, the effect originally possessed by the tyrosinase activity inhibitor can be sufficiently obtained. In other words, it has a high inhibitory effect on pigmentation and is effective in preventing and improving skin darkening, spots and freckles due to sunburn and the like. These can be used alone or in combination of two or more tyrosinase activity inhibitors.

The skin external preparation of the present invention is prepared by blending the essential components (A) and (B) with various types of bases known as ordinary skin external preparations according to a conventional method. be able to.

Examples of the form of the external preparation for skin are not particularly limited, and include, for example, cosmetics such as emulsions, creams, lotions, packs, cleansers, make-up cosmetics, dispersions, ointments, and external medicines. And as a base,
Depending on the form of these skin external preparations, within the range not impairing the effects of the present invention, for example, purified water, lower alcohols, polyhydric alcohols, fats and oils, powders, surfactants, ultraviolet absorbers, thickeners, pigments, Beauty ingredients, preservatives, fragrances and the like can be used.

[0014]

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 Arhat Fruit Extract Momordica grosvenori
i Swingle dried fruit, 50% water content
(V / v) Ethyl alcohol was added, extraction was performed at room temperature for 3 days, and then filtration was performed to obtain an extract of Arhat fruit.

REFERENCE EXAMPLE 2 Production of Plant Extracts 10 g of Licorice (JP), Sohakuhi (JP), Kujin (Clara) (JP), and Touki (JP) each have a water content of 50% (v / v). ) 100 ml of ethyl alcohol was added, extracted at room temperature with occasional stirring for 3 days, and filtered to obtain each plant extract.

Test Example 1 Tyrosinase Activity Inhibition Test The tyrosinase activity inhibition rate of a sample of the arhat extract obtained in Reference Example 1 and the plant extract obtained in Reference Example 2 singly or in combination was examined by the following method. . That is, an enzyme solution [28,000, manufactured by Sigma] was added to each sample.
Dissolving 10 mg of tyrosinase in 20 ml of 0.1 M phosphate buffer (pH 6.8)], adding 0.1 ml, and further adding 0.1 M phosphate buffer (pH 6.8) to make 4.0 ml. Was incubated at 25 ° C. for 10 minutes.

Next, a substrate solution [L-DOPA (manufactured by Tokyo Chemical Industry Co., Ltd.) 198.
0 mg in 0.1 M phosphate buffer (pH 6.8) 100 m
dissolved in 1], and reacted for 10 minutes. After the reaction, absorbance at 475 nm (OD _S )
Was measured. Similarly, the absorbance (OD _HE ) and the absorbance (OD _B ) when the reaction was performed using the enzyme inactivated by heating and when no sample was added were calculated, and the activity inhibition rate of tyrosinase activity was calculated from the following equation. did.

[0019]

(Equation 1)

(Results)

[Table 1]

As is evident from the results in Table 1, when arhat extract and tyrosinase activity inhibitor were combined, the tyrosinase activity inhibitory effect was higher than when arhat extract or tyrosinase activity inhibitor was used alone, and the synergistic effect was higher. Showed a natural whitening effect. Therefore, the composition of the present invention in which the arhat extract and the tyrosinase activity inhibitor are combined, by applying the composition to the skin, exerts an extremely excellent tyrosinase activity inhibitory action, such as skin blackening due to sunburn, spots, freckles, etc. Is effectively suppressed.

Example 1 Cream: Creams (products 1 and 2 of the present invention and comparative products 1 to 4) were prepared according to the composition shown in Table 2 and the following production method, and their skin effects were examined. The results are also shown in Table 2.

(Composition and results)

[Table 2]

(Production method) A. Components (1) to (6), (10) and (11) are mixed and heated to 70 ° C. B. Components (7)-(9) and (12) are mixed and heated to 70 ° C. C. B was added to A, mixed, and cooled to obtain a cream.

(Test Method) 27 per test cream
A panel consisting of 15 women aged 54 to 54
After washing the face for 12 weeks, an appropriate amount of the test cream was applied to the face. The beautiful skin effect of the application was evaluated according to the following criteria.

(Evaluation Criteria) <Evaluation> <Contents> Effective Skin dullness became inconspicuous. Slightly effective The dullness of the skin became less noticeable. Ineffective No change from before use.

As shown in the results in Table 2, the composition of the present invention obtained by combining the arhat extract represented by the present invention 1 with magnesium L-ascorbyl phosphate and the arhat extract represented by the present invention 2 It has been clarified that the composition of the present invention, which is obtained by combining the present invention with licorice extract, can prevent and improve the occurrence of "dullness" in the skin by applying these compositions to the skin, resulting in beautiful skin.

Example 2 Lotion: A lotion was prepared according to the following formulation and the following method. (Prescription) (%) (1) Glycerin 5.0 (2) 1,3-butylene glycol 6.5 (3) Polyoxyethylene (20EO) sorbitan 1.2 Monolaurate (4) Ethyl alcohol 8 0.0 (5) Lohan fruit extract * 1 10.0 (6) Kujin extract * 2 0.5 (7) Preservatives proper amount (8) Flavor proper amount (9) Purified water balance * 1 Produced in Reference Example 1. * 2 manufactured in Reference Example 2

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

Example 3 Emulsion: An emulsion was prepared according to the following formulation and the following production method. (Prescription) (%) (1) Polyoxyethylene (10EO) sorbitan 1.0 monostearate (2) Polyoxyethylene (60EO) sorbit 0.5 tetraoleate (3) Glyceryl monostea Rate 1.0 (4) Stearic acid 0.5 (5) Behenyl alcohol 0.5 (6) Squalane 8.0 (7) Arhat fruit extract * 1 0.1 (8) Cysteine * 2 0.1 (9) Preservative Agent 0.1 (10) Carboxyvinyl polymer 0.1 (11) Sodium hydroxide 0.05 (12) Ethyl alcohol 5.0 (13) Purified water Remaining amount (14) Perfume appropriate amount * 1 Produced in Reference Example 1. * 2 Cysteine (manufactured by Wako Pure Chemical Industries, Ltd.) diluted to 1.0 mg / ml with water

(Production method) A. The components (8) to (13) are mixed by heating and maintained at 70 ° C. B. The components (1) to (6) are mixed by heating and kept at 70 ° C. C. Add A to B, mix and emulsify uniformly. D. After cooling C, components (7) and (14) were added and mixed uniformly to obtain an emulsion.

Example 4 Cream: A cream was prepared according to the following recipe and the following method. (Prescription) (%) (1) Polyoxyethylene (40EO) monostearate 2.0 (2) Glycerin monostearate (self-emulsifying type) 5.0 (3) Stearic acid 5.0 (4) Behenyl alcohol 0.5 (5) squalane 15.0 (6) cetyl isooctanoate 5.0 (7) butyl paraben 0.1 (8) methyl paraben 0.1 (9) 1,3-butylene glycol 5.0 (10) Arhat fruit extract * 1 0.2 (11) Neubara extract * 2 0.5 (12) Remaining purified water (13) Perfume appropriate amount * 1 Produced in Reference Example 1 * 2 Manufactured by Maruzen Pharmaceutical Co., Ltd.

(Production method) A. The components (1) to (7) are heated and dissolved at 70 ° C. B. Heat components (8)-(12) to 70 ° C. C. Add A to B, add component (13) with cooling,
Get the cream.

Each of the lotion of Example 2, the lotion of Example 3, and the cream of Example 4 is excellent in stability over time, and can be applied to the skin to prevent the occurrence of "dullness" on the skin. Pigmentation such as spots can also be improved,
It was intended to make the skin transparent and beautiful.

Example 5 Pack: A pack was prepared according to the following formulation and the following production method. (Prescription) (%) (1) Polyvinyl alcohol 20.0 (2) Ethyl alcohol 20.0 (3) Glycerin 5.0 (4) Kaolin 6.0 (5) Arhat fruit extract * 1 1.0 (6) Hop extract * 2 1.0 (7) Preservative 0.2 (8) Perfume 0.1 (9) Remaining purified water * 1 Produced in Reference Example 1 * 2 Koei Kogyo Co., Ltd.

(Production method) A. Mixing components (1), (3), (4) and (9),
Heat to 70 ° C. and stir. B. Mix components (2), (7) and (8). C. The above B was added to the above A, mixed, cooled, and the components (5) and (6) were uniformly dispersed to obtain a pack.

The pack of Example 5 has excellent stability over time,
By applying it to the skin, the texture of the skin can be adjusted, the "dullness" of the skin can be prevented, and the pigmentation such as spots can be improved, resulting in a beautiful skin with a transparent feeling.

Example 6 Liquid foundation: A liquid foundation was prepared according to the following formulation and the following production method. (Prescription) (%) (1) Lanolin 7.0 (2) Liquid paraffin 5.0 (3) Stearic acid 2.0 (4) Cetanol 1.0 (5) Glycerin 5.0 (6) Triethanolamine 1 0.0 (7) Carboxymethylcellulose 0.7 (8) Remaining purified water (9) Mica 15.0 (10) Talc 6.0 (11) Titanium oxide 3.0 (12) Color pigment 6.0 (13) Arhat extract * 1 0.05 (14) Licorice extract * 2 0.05 (15) Suitable amount of UV absorber (16) Suitable amount of fragrance * 1 Manufactured in Reference Example 1 * 2 Manufactured in Reference Example 2

(Production method) The components (1) to (4) are mixed and dissolved. B. Add components (9) to (12) to A, mix uniformly,
Keep at 70 ° C. C. Components (5) to (8) are uniformly dissolved and kept at 70 ° C. D. Add C to B and emulsify uniformly. E. FIG. After cooling D, components (13) to (16) were added to obtain a liquid foundation.

Example 7 Sunscreen emulsion: A sunscreen emulsion was prepared according to the following formulation and the following method. (Prescription) (%) (1) stearic acid 2.0 (2) cetanol 1.0 (3) polyoxyethylene sorbitan monooleate (20EO) 0.5 (4) sorbitan sesquioleate 0.5 ( 5) 2-Ethylhexyl paramethoxycinnamate 8.0 (6) Cetyl 2-ethylhexanoate 12.0 (7) 1,3-butylene glycol 10.0 (8) Carboxyvinyl polymer 0.2 (9) Triethanolamine 0.5 (10) Lohan fruit extract * 1 0.5 (11) Sorrel extract * 2 0.1 (12) Remaining purified water (13) Preservative appropriate amount (14) Titanium oxide 3.0 ( 15) Appropriate amount of fragrance * 1 manufactured in Reference Example 1 * 2 manufactured in Reference Example 2

(Production method) The components (1) to (6) and (14) are mixed by heating.
Keep at 5 ° C. B. Heat and mix components (7)-(13) and maintain at 75 ° C. C. Add A slowly to B. D. While cooling C, the component (15) was added to obtain a sunscreen emulsion.

The liquid foundation of Example 6 and the sunscreen emulsion of Example 7 are both excellent in stability over time, and can be applied to the skin to prevent darkening and spots on the skin due to sunburn and the like. Was.

Example 8 Gel ointment: A gel ointment was prepared according to the following formulation and the following production method. (Prescription) (%) (1) Carboxyvinyl polymer 1.0 (2) Triethanolamine 1.0 (3) 1,3-butylene glycol 10.0 (4) Arhat extract * 1 0.01 (5) Yokuinin extract * 2 0.01 (6) Remaining purified water * 1 Produced in Reference Example 1 * 2 Maruzen Pharmaceutical Co., Ltd.

(Production Method) A. Components (1) and (3) to (6) are mixed and dissolved. B. Component (2) was added to A and mixed to make a uniform, and a gel ointment was obtained.

The gel ointment of Example 8 has excellent stability over time, and can be applied to the skin to regulate the texture of the skin, prevent the skin from dulling, and improve pigmentation such as spots. The result was a clear and beautiful skin.

[0046]

According to the present invention, the inherent performance of the tyrosinase activity inhibitor can be sufficiently exhibited.
In other words, it has a high inhibitory effect on pigmentation and is effective in preventing and improving skin darkening, spots and freckles due to sunburn and the like. As described above, the skin external preparation of the present invention can sufficiently exhibit the intrinsic performance of the tyrosinase activity inhibitor, and is therefore extremely useful in beauty and medicine.

────────────────────────────────────────────────── ───

[Procedure amendment]

[Submission date] July 28, 1997

[Procedure amendment 1]

[Document name to be amended] Statement

[Correction target item name] 0046

[Correction method] Change

[Correction contents]

[0046]

According to the present invention, tyrosinase activity inhibition
By combining the agent with the extract of Arhat fruit extract, the intrinsic performance of the tyrosinase activity inhibitor can be sufficiently exhibited. In other words, it has a high inhibitory effect on pigmentation and is effective in preventing and improving skin darkening, spots and freckles due to sunburn and the like. As described above, the skin external preparation of the present invention can sufficiently exhibit the intrinsic performance of the tyrosinase activity inhibitor, and is therefore extremely useful in beauty and medicine.

Claims (2)

[Claims] 1. An external preparation for skin, characterized by containing one or more of the following components (A) and (B): (A) an extract of arhat fruit (B) and a tyrosinase activity inhibitor. 2. The method according to claim 1, wherein the tyrosinase activity inhibitor is ascorbic acid or a derivative thereof and a salt thereof, cysteine and a derivative thereof and a salt thereof, a placenta extract, an aloe extract, an Ibukitranoo extract, a chamomile extract, a Clara extract, and a coconut tree. Extract, hawthorn extract, sampens extract, white lily extract, Sempukuka extract, soybean extract, touuki extract, Neubara extract, hop extract,
The external preparation for skin according to claim 1, which is selected from flavonoids such as yokuinin extract, glabridine, glabrene, liquiritin, isoliquiritin, and a liquorice extract containing these flavonoids.