JPH10182407A - 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 an iron-chelating agent as essential components. SOLUTION: This preparation for external use for skin capable of sufficiently exhibiting the characteristic skin-aging preventing effect and roughened skin improving effect of a chelating agent 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 kinds of iron-chelating agents (e.g. ethylenediaminetetraacetic acid and/or its salt, phytic acid and/or its salt or o-phenanthroline).

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin, and more particularly, to a method for preparing lipid peroxide due to active oxygen generation in the skin by mixing an extract of Arhat fruit with an iron chelating agent. The present invention relates to an external preparation for skin, such as cosmetics and external medicines, which has an excellent anti-aging effect on the skin and an effect for improving the rough skin, which can prevent skin inflammation, blackening, aging and the like.

[0002]

2. Description of the Related Art Conventionally, external preparations such as emulsions, creams, lotions, packs, detergents, foundations, ointments, and dispersions have been used for the purpose of imparting an effect of preventing skin aging and improving skin roughness. Various medicinal ingredients have been added. In recent years, as one of the causes of skin aging, the adverse effect of active oxygen on living organisms has been cited, and hydroxyl radicals generated via iron derived from living organisms may damage lipid production and proteins, etc. There are reports that there is. Chelation and removal of iron involved in the generation of hydroxy radicals that are toxic to living bodies leads to prevention of skin aging and is very significant.

[0003]

Therefore, there is a demand for the development of an iron chelating agent for the purpose of defense of the living body and prevention of aging. It must be sufficiently satisfactory from the viewpoint of sex. That is, there has been a demand for the development of a medicinal component having excellent effects and suitable for application to biological systems.

[0004]

Means for Solving the Problems The present inventors have conducted intensive studies to improve the effects of the medicinal components incorporated in the external preparation for skin to prevent skin aging and to improve skin roughness. It has been found that when the iron chelating agent is combined with the iron chelating agent, the action inherent to the iron chelating agent is sufficiently exhibited, and the present invention has been completed.

That is, the present invention provides an external preparation for skin containing one or more of the following components (A) and (B): (A) an extract of arhat fruit (B) and an iron chelating agent.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION The component (A) of the present invention, an extract of Arhat fruit, is momordica grosvenorii;
Extract grosnoverii Swingle fruit 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 age for about one week and then filtered again.

[0008] The content of the extract of arhat in the composition of the present invention is preferably 0.0005 to 10 as dry solids.
% (Hereinafter simply referred to as "%"), and more preferably 0.005 to 5%. Within this range, the effect of the iron chelating agent of the component (B) can be synergistically enhanced. When an extract is used, the concentration of the extract is not particularly limited as long as the content of the dry solid content as a solute is within the above range.

On the other hand, the iron chelating agent as the component (B) of the present invention includes, for example, ethylenediaminetetraacetic acid and / or a salt thereof, diethylenetriamine-N, N, N ′, N ″,
N ″ -pentaacetic acid and / or its salt, phytic acid and / or its salt, salicylic acid and / or its salt, citric acid and / or
Or salts thereof, o-phenanthroline, desferrioxamine, transferrin, lactoferrin, hemoglobin, hematin, etc., and these may be used alone or in combination of two or more.

The amount of the iron chelating agent (B) is 0.0001 to 10%, more preferably 0.001 to 5%, in the composition. When the content is within this range, the effect of preventing iron aging and the effect of improving skin roughness that the iron chelating agent originally has are sufficiently exhibited. That is, the production of lipid peroxide due to the production of active oxygen in the skin, the inflammation of the skin,
It is effective in preventing blackening and aging. In addition, these iron chelating agents can be used alone or in combination of two or more.

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

Examples of the form of the external preparation for skin are not particularly limited, and include, for example, milky lotions, creams, lotions, packs, cleansers, makeup cosmetics such as lipsticks / foundations, scalp / hair cosmetics, ointments, It can be used as an external medicine such as a dispersion liquid, and according to the form of these external preparations for skin, within the range not impairing the effects of the present invention, for example, purified water, lower alcohol, polyhydric alcohol, oils and fats, powders ,
Surfactants, ultraviolet absorbers, thickeners, pigments, beauty ingredients,
Preservatives, fragrances and the like can be used.

[0013]

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 grosnoveri
i Swingle fruit dried to 80% water content
(V / v) Ethyl alcohol was added, extraction was performed at room temperature for 3 days, followed by filtration to obtain an extract of Arhat fruit.

Test Example 1 Photoageing Prevention Effect Test Arkan extract and an iron chelating agent listed in Table 1 were used alone or in combination as a sample, and diluted with 50% (v / v) ethanol. The effect of preventing light aging was examined.

[0016]

[Table 1]

The effect of a 6-week-old hairless mouse, which was prepared by irradiating ultraviolet rays to a light-aged model mouse, was measured. That is, 0.105 J / cm2 of ultraviolet light is applied for 3 weeks.
Irradiation was performed for a total of 20 weeks, and the sample was applied to the back of the mouse at 0.1 ml daily (in the case of irradiation, 2 hours before irradiation). One group consisted of 6 animals. The light aging prevention effect of the application was evaluated according to the following criteria for the aging score (evaluated after 10 weeks and 20 weeks) and the yellowing of the skin color (evaluated after 20 weeks) indicating texture and wrinkles.

1) Aging score A texture score and a wrinkle score were added to obtain an aging score.
The aging score increases as the light aging of the mouse progresses.

Texture score: [Score] [State] 0 Texture is in order 1 Texture is slightly disturbed 2 Texture is disturbed 3 Texture is lost

Wrinkle score: [Score] [State] 0 No wrinkles 1 Fine wrinkles 2 Slight coarse wrinkles 3 Coarse wrinkles

2) Yellowing of Skin The skin color tends to increase in yellow color with the aging of mice (b value in the Lab color system). The color of the mouse skin was measured with a color difference meter, and the change in the value of the b value at the end of the test with respect to that before the test was Δb, and the skin color was evaluated. Table 2 shows the evaluation results of the aging score and the yellowing of the skin color.

[0022]

[Table 2]

As shown in Table 2, the combination of the extract of Arhat fruit and the iron chelating agent has the function of suppressing the aging score and the yellowing of the skin color of the light aging model mouse, and prevents the aging of the skin. It turned out to be effective.

Example 1 Emulsion: Emulsions (product 1 of the present invention and comparative products 1 to 3) were prepared according to the composition shown in Table 3 and the following production method, and their beautiful skin effect and skin aging prevention effect were examined. The results are also shown in Table 3.

(Composition and results)

[Table 3]

(Production method) A. Components (6)-(9) and (13) are mixed and heated to 70 ° C. B. Components (1)-(5), (10) and (11) are mixed and heated to 70 ° C. C. B was added to A, mixed, and the component (12) was added to emulsify uniformly, followed by cooling to obtain an emulsion.

(Test method) 25 to 5 per test emulsion
Twenty zero-year-old women are panelized twice a day, morning and night.
After washing the face for two weeks, an appropriate amount of the test emulsion was applied to the face. The skin and skin aging prevention effects of the application were evaluated according to the following criteria.

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

Skin Aging Prevention Effect: <Evaluation> <Contents> Effective Skin peeling and gloss were improved. Slightly effective Skin glue, gloss slightly improved. Ineffective No change from before use.

As shown in the results in Table 3, by applying to the skin a milky lotion containing the lactone extract and lactone extract represented by the product 1 of the present invention, the occurrence of "dullness" and the like on the skin can be prevented and the beautiful skin can be obtained. At the same time, it was revealed that skin abrasion and gloss were improved and that skin aging was prevented.

Example 2 Lotion: A lotion was prepared according to the following formulation and the following method. (Prescription) (%) (1) Glycerin 6.0 (2) 1,3-butylene glycol 5.5 (3) Polyoxyethylene (20EO) sorbitan monolaurate 1.5 (4) Ethyl alcohol 9 0.0 (5) Arhat fruit extract * 1 10.0 (6) Disodium ethylenediaminetetraacetate * 2 0.5 (7) Preservative appropriate amount (8) Flavor appropriate amount (9) Purified water remaining amount * 1 In Reference Example 1 Manufactured * 2 Wako Pure Chemical Industries

(Production method) A. 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 Cream: A cream was prepared according to the following formulation 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) 1,3-butylene glycol 5.0 (8) Arhat extract * 1 1.0 (9) Magnesium potassium phytate * 2 0.1 (10) Preservative appropriate amount (11) Remaining purified water (12) Perfume appropriate amount * 1 Produced in Reference Example 1 * 2 Sigma

A. Ingredients (1) to (6) and (10)
Heat and dissolve at 0 ° C. B. The components (7), (8) and (11) are heated and mixed at 70 ° C. C. Add A to B. D. The components (9) and (12) were added to C, and the mixture was cooled to obtain a cream.

Example 4 Ointment: An ointment was prepared according to the following formulation and the following production method. (Prescription) (%) (1) Stearic acid 18.0 (2) Cetanol 4.0 (3) Triethanolamine 2.0 (4) Glycerin 5.0 (5) Lohan fruit extract * 1 2.0 (6) ) Transferrin * 2 0.02 (7) Hemoglobin * 3 0.02 (8) Remaining amount of purified water * 1 Produced in Reference Example 1 * 2 Sigma * 3 Sigma

(Production method) A. A part of components (3), (4) and (8) are mixed by heating and kept at 75 ° C. B. Heat mix components (1) and (2) and maintain at 75 ° C. C. Add A slowly to B. D. While cooling C, components (5), (6) and (7) dissolved in the rest of component (8) were added to obtain an ointment.

The lotion of Example 2, the cream of Example 3, and the ointment of Example 4 are all excellent in stability over time, and when applied to the skin, the skin is improved in terms of abrasion and luster, and dullness of the skin is improved. It prevented skin aging.

Example 5 Oily foundation: An oily foundation was prepared by the following formulation and the following method. (Prescription) (%) (1) Celesin 5.0 (2) Solid paraffin 6.0 (3) Vaseline 5.0 (4) Macadamian nut oil 15.0 (5) Castor oil Remaining (6) Dimethyl poly Siloxane 15.0 (7) Organically modified clay mineral 1.0 (8) Titanium oxide 10.0 (9) Sericite 5.0 (10) Nylon powder 5.0 (11) Iron oxide 5.0 (12) Rakanka Extract * 1 0.5 (13) Citric acid * 2 0.2 (14) Preservative appropriate amount (15) Flavor appropriate amount * 1 Manufactured in Reference Example 1 * 2 Sigma

(Production method) The components (1) to (6) are mixed by heating. B. Add components (7) to (15) to A and mix uniformly. C. B was cooled and molded to obtain an oily foundation.

Example 6 White powder: White powder was prepared according to the following formulation and the following production method. (Prescription) (%) (1) Remaining amount of talc (2) Sericite 15.0 (3) Kaolin 10.0 (4) Titanium oxide 5.0 (5) Iron oxide 1.5 (6) Calcium carbonate 5. 0 (7) Zinc stearate 5.0 (8) Arhat fruit extract * 1 0.05 (9) Salicylic acid * 2 0.05 (10) Preservative appropriate amount (11) Flavor appropriate amount * 1 * 2 Sigma

(Production method) Components (1) to (11) are mixed. B. A was pulverized, filled in a metal plate, and press-molded to obtain a white powder.

The oil-based foundation of Example 5 and the white powder of Example 6 were excellent in stability over time and, when applied to the skin, suppressed dullness and roughness of the skin and prevented aging of the skin.

Example 7 Lipstick: A lipstick was prepared according to the following formulation and the following method. (Prescription) (%) (1) Candelilla wax 7.0 (2) Solid paraffin 8.0 (3) Beeswax 5.0 (4) Lanolin 10.0 (5) Cetyl ethylhexanoate 15.0 (6) Castor oil Remaining (7) Lohan fruit extract * 1 0.02 (8) Calcium phytate * 2 0.02 (9) Color pigment appropriate amount (10) Fragrance appropriate amount * 1 Manufactured in Reference Example 1 * 2 Sigma Made

(Production Method) A. The components (1) to (6) are heated and dissolved at 100 to 110 ° C. B. A is mixed with the components (7) to (10) at 90 ° C. with stirring. C. B was cooled and molded to obtain a lipstick.

The lipstick of Example 7 was excellent in stability over time, feeling in use and finish, and was applied to the lips to keep the lips smooth and prevent roughening.

[0046]

As described above, by combining the iron chelating agent with the extract of Arhat fruit, the original effects of the iron chelating agent can be sufficiently exhibited. That is, it has an extremely high improvement and prevention effect against lipid peroxide generation, inflammation, blackening, aging and the like caused by active oxygen generation in the skin. Therefore, since the composition of the present invention can sufficiently exhibit the inherent performance of the iron chelating agent, it is 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] 0002

[Correction method] Change

[Correction contents]

[0002]

2. Description of the Related Art Conventionally, external preparations such as emulsions, creams, lotions, packs, detergents, foundations, ointments, and dispersions have been used for the purpose of imparting an effect of preventing skin aging and improving skin roughness. Various medicinal ingredients have been added. In recent years, one of the causes of skin aging is the adverse effect of active oxygen on living organisms. Hydroxyl radicals generated via iron derived from living organisms may damage lipid production and proteins, etc. There are reports that there is. Such chelation and removal of iron involved in the production of hydroxyl radicals that are toxic to living bodies leads to prevention of skin aging and is very significant.

[Procedure amendment 2]

[Document name to be amended] Statement

[Correction target item name] 0006

[Correction method] Change

[Correction contents]

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION An extract of Arhat fruit, which is the component (A) of the present invention, is Momordica Grosvenorii;
The fruit of dica gros venori ri Swingle 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.

[Procedure amendment 3]

[Document name to be amended] Statement

[Correction target item name] 0010

[Correction method] Change

[Correction contents]

The amount of the iron chelating agent (B) is 0.0001 to 10%, more preferably 0.001 to 5%, in the composition. Within this range, the action inherent to the iron chelating agent is sufficiently exhibited.
In other words, it is effective in preventing the generation of lipid peroxide due to the generation of active oxygen in the skin and the prevention of skin inflammation, blackening, aging and the like. In addition, these iron chelating agents can be used alone or in combination of two or more.

[Procedure amendment 4]

[Document name to be amended] Statement

[Correction target item name] 0012

[Correction method] Change

[Correction contents]

Examples of the form of the external preparation for skin are not particularly limited and include, for example, emulsions, creams, lotions, packs, cleansers, makeup cosmetics such as lipsticks / foundations, scalp cosmetics, ointments and dispersions. Can be used as external medicines, etc., and depending on the form of these external preparations for skin, within the range not impairing the effects of the present invention, for example, purified water, lower alcohols, polyhydric alcohols, oils, fats, powders, Activators, ultraviolet absorbers, thickeners, pigments, cosmetic ingredients, preservatives, fragrances and the like can be used.

[Procedure amendment 5]

[Document name to be amended] Statement

[Correction target item name] 0014

[Correction method] Change

[Correction contents]

[0014] Reference Example 1 manufacture of swingle extract momordica gloss Beno Rii; Momordica
Gros venori ri Swingle fruit was dried, to which 80% (v / v) ethyl alcohol in water content was added, extracted at room temperature for 3 days, and then filtered to obtain an extract of Arhat fruit.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁶ Identification code FI A61K 7/035 A61K 7/035

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 an iron chelating agent. 2. The iron chelating agent is ethylenediaminetetraacetic acid and / or a salt thereof, diethylenetriamine-N, N,
N ′, N ″, N ″ -pentaacetic acid and / or its salt, phytic acid and / or its salt, salicylic acid and / or its salt, citric acid and / or its salt, o-phenanthroline, desferrioxamine 2. The external preparation for skin according to claim 1, wherein the external preparation is selected from the group consisting of, transferrin, lactoferrin, hemoglobin, and hematin.