JP2013173735A - Topical skin preparation for skin-lightening or cosmetic for skin-lightening - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a novel skin-lightening agent, and a topical skin preparation for skin-lightening or a cosmetic for skin-lightening.SOLUTION: A skin-lightening agent includes Echinacea extract as an effective ingredient. A topical skin preparation for skin-lightening or a cosmetic for skin-lightening contains Echinacea extract.

Description

  The present invention relates to a whitening skin external preparation or a whitening cosmetic containing an echinacea extract, and further relates to a whitening agent and a melanin production inhibitor.

  Conventionally, various plant-derived components have been used as active ingredients such as external preparations for skin and cosmetics. As for the extract obtained from Echinacea purpurea, the antioxidant effect and the anti-inflammatory effect (Patent Document 1), the unwanted hair growth inhibitory effect (Patent Document 2), the sebum secretion effect (Patent Document 3). ), Hair-growth effect (Patent Document 4), etc. are known, and various uses for cosmetics, foods, pharmaceuticals and the like have been proposed. However, none of the above patent documents describes the whitening effect of the extract.

JP 2001-098263 A Japanese Patent No. 04102500 Japanese Patent No. 03819126 JP-A-11-092339

Conventionally, various plant extracts having a whitening effect are known, but from the viewpoint of obtaining a sufficient whitening effect, whitening agents such as arbutin, ascorbic acid and derivatives thereof, kojic acid, and ellagic acid are generally used. Has been. However, although these widely used whitening agents are excellent in whitening effect, there are many restrictions on blending into a skin external preparation or cosmetic, and skin external preparations or cosmetics containing these whitening agents are Various problems such as discoloration or coloring, separation, and crystal precipitation are likely to occur.
The present invention has been made in view of the above problems, and can be easily blended into a skin external preparation or cosmetic (including quasi-drugs and medicinal cosmetics), and contains a whitening agent having a high whitening effect and the same. It is an object of the present invention to provide a whitening skin external preparation or a whitening cosmetic that has good stability and safety and has a high whitening effect.

  As a result of intensive studies to solve the above problems, the present invention has found an excellent whitening effect in an extract of Echinacea purpurea, and has completed the present invention based on this finding. That is, the present invention relates to a whitening agent and a melanin production inhibitor containing an extract of Echinacea purpurea as an active ingredient, and a whitening skin external preparation or a whitening cosmetic containing these.

  According to the present invention, by using an extract of Echinacea (Echinacea purpurea) as an active ingredient, a plant-derived melanin production inhibitor having good stability and safety, a whitening agent, and a whitening containing the same as an active ingredient An external preparation for skin or a cosmetic for whitening can be provided. Furthermore, a whitening skin external preparation or whitening cosmetic that can be easily blended into a wide range of skin external preparations or cosmetics, regardless of the dosage form, such as an aqueous type or an emulsifier type, has a good skin feel and a high whitening effect. Can be provided.

Hereinafter, the present invention will be described in detail. In the present specification, “to” is used to mean that the numerical values described before and after it are included as a lower limit value and an upper limit value.
Echinacea is a plant belonging to the genus Muraceki Barenkiku, and its scientific name is Echinacea purpurea. Echinacea is cultivated mainly in the United States and is used for health foods. The production area of echinacea used in the present invention is not particularly limited.

Examples of plant parts of Echinacea that can be used in the present invention include flowers, flower spikes, pericarp, fruits, stems, leaves, branches, branches and leaves, stems, bark, rhizomes, root barks, roots, whole plants, etc. The fruit includes all of the fruit, pulp including the skin, and seed. In the present invention, when the above-ground part (flower, leaf, or stem) is used as the extraction site, an extract having good storage stability can be obtained.

The extract of the present invention can be obtained by extracting echinacea using various extraction solvents. The extraction method is not particularly limited, but the extraction is performed at a low temperature or at room temperature or under heating using a suitable solvent. Examples of the extraction solvent include water; lower monohydric alcohols such as methanol, ethanol, propanol and isopropanol; liquid polyhydric alcohols such as glycerin, propylene glycol and 1,3-butylene glycol; ketones such as acetone; ethyl ether and propyl Examples include ethers such as ether; esters such as ethyl acetate, and one or more of these can be selected and used. Further, physiological saline, phosphate buffer, phosphate buffered saline, or the like may be used. From the viewpoint of the whitening effect, the storage stability of the extract, and the cytotoxicity, it is preferable to use a lower monohydric alcohol or an aqueous solution of a lower monohydric alcohol, or hot water of 80 ° C. or more, and particularly preferably an ethanol aqueous solution. . Further, from the viewpoint of storage stability of the extract and cytotoxicity, the ethanol concentration of the aqueous ethanol solution is preferably 60% or less, particularly preferably 30% or less.

  The extraction method is not particularly limited in the set temperature, time, etc. For example, using an aqueous ethanol solution at low temperature or room temperature, or after heating for 1 to 5 days, filtering and obtaining A method may be mentioned in which the obtained filtrate is further left to mature for about one week and then filtered again. It is preferable to stir the system during extraction. In addition, pretreatment such as pulverization, chopping, pressing, or fermentation can be performed on echinacea before the extraction operation.

  The obtained extract may be in the form of a solution, paste, gel, solid, powder or the like. In other words, the extract can be used as it is after preparation, but it may be used after being concentrated, dried, spray-dried or freeze-dried, dissolved again in water or a polar solvent.

  As the solvent for redissolving the extract, for example, water; lower monohydric alcohols such as methanol and ethanol; liquid polyhydric alcohols such as glycerin, propylene glycol, and 1,3-butylene glycol are used. be able to. Alternatively, for preserving, one or more preservatives such as paraoxybenzoic acid ester and phenoxyethanol may be added and used.

  Furthermore, if necessary, it can be used after being subjected to treatment such as decolorization, deodorization, and desalting with filtration or ion exchange resin within a range that does not affect the effect of the present invention. Moreover, it can also fractionate and use by methods, such as ultrafiltration, ion-exchange chromatography, and gel filtration chromatography.

  A whitening agent containing the thus obtained Echinacea purpurea extract as an active ingredient suppresses melanin production and exhibits an excellent whitening effect for preventing skin spots and freckles.

  The content of the echinacea extract in the skin whitening external preparation or whitening cosmetic of the present invention is preferably 0.0001 to 0.1% by mass (hereinafter simply referred to as “%”) in terms of dry matter. 0.0001 to 0.01% is more preferable. When it is in the above range, a high whitening effect can be obtained, and it can be stably blended into a skin external preparation or cosmetic.

  The whitening skin external preparation or whitening cosmetic of the present invention may contain other whitening agents in addition to the whitening agent of the present invention. Examples of other whitening agents include ascorbic acid or derivatives thereof, arbutin, linoleic acid, tranexamic acid and derivatives thereof, chamomile extract and the like. Other whitening agents are preferably one or more selected from ascorbic acid or a derivative thereof and arbutin. Although these whitening agents have a high whitening effect, high concentration blending is difficult in terms of stability over time and usability. By using together with the whitening agent of the present invention, it is possible to obtain a whitening effect more than that of a conventional whitening skin external preparation or whitening cosmetic without impairing the stability over time and the feeling of use.

  In preparing the skin whitening preparation or skin whitening cosmetic of the present invention, the components usually used in the manufacture of skin external preparations, cosmetics and the like, that is, water (purified water, hot spring water, deep water, etc.) , Alcohols, oils, surfactants, thickeners, metal soaps, gelling agents, powders, chelating agents, water-soluble polymers, film forming agents, resins, inclusion compounds, antibacterial agents, deodorants, salts , PH adjusters, UV absorbers, extracts from animals, plants and microorganisms, keratolytic agents, enzymes, hormones, other vitamins, moisturizers, active oxygen removers, blood circulation promoters, astringents, antiseborrheic agents -Various medicinal agents such as anti-inflammatory agents, cell activators, and refreshing agents, fragrances, and the like can be appropriately added within a range that does not impair the effects of the present invention, but are not limited thereto.

There are no particular restrictions on the form of the whitening skin external preparation or whitening cosmetic of the present invention, such as an ointment, external liquid, patch, milky lotion, cream, lotion, cosmetic liquid, pack, face wash, makeup cosmetic, etc. It may be prepared as any form of external preparation for skin or cosmetic.
Examples of the dosage form of the skin whitening external preparation or whitening cosmetic of the present invention include liquids, powders, solids, sticks, oil-in-water / water-in-oil emulsions, creams, gels, and the like. Can do. Moreover, it can be used parenterally or orally depending on the therapeutic purpose.

The melanin production inhibitory activity in the melanin production inhibitor of the present invention is not particularly limited as long as it is an activity that suppresses the action of causing darkening of the body color of the skin and the like accompanying the production and accumulation of melanin. The whitening effect of the whitening agent and the skin external preparation for whitening includes not only an active whitening effect to whiten the skin but also a passive whitening effect to suppress the blackening of the skin, such as stains, buckwheat etc. This includes not only a whitening effect that improves pigmentation of the skin, but also a whitening effect that suppresses pigmentation.

EXAMPLES Hereinafter, although an Example demonstrates this invention further more concretely, the scope of the present invention is not limited to the following Example.
[Production Example 1] Production of Echinacea extract 1 10 g of dried Echinacea aerial parts (flowers, leaves, stems) were pulverized, and 100 mL of 20% (v / v) aqueous ethanol solution was added and stirred at room temperature for 24 hours. Extracted. The obtained extract was filtered to remove insolubles, and then filtered again with a Vacuum Driven Disposable Filteration System (IWAKI). This was concentrated under reduced pressure and freeze-dried to obtain an extract. The yield was 0.72g.
[Production Example 2] Production of Echinacea extract 2 10 g of dried Echinacea aerial parts (flowers, leaves, stems) were pulverized, and 100 mL of 50% (v / v) aqueous ethanol solution was added and stirred at room temperature for 24 hours. Extracted. The obtained extract was filtered to remove insolubles, and then filtered again with a Vacuum Driven Disposable Filteration System (IWAKI). This was concentrated under reduced pressure and freeze-dried to obtain an extract. The yield was 0.68g.
[Production Example 3] Production of Echinacea extract 3 10 g of dried Echinacea aerial part (flowers, leaves, stems) was pulverized, and 100 mL of 80% (v / v) aqueous ethanol solution was added and stirred at room temperature for 24 hours. Extracted. The obtained extract was filtered to remove insolubles, and then filtered again with a Vacuum Driven Disposable Filteration System (IWAKI). This was concentrated under reduced pressure and freeze-dried to obtain an extract. The yield was 0.75g.

Example 1
<Evaluation of whitening effect>
B16 melanoma cultured cells derived from mice were used, and the melanin production inhibitory effects of Echinacea extract 1, Extract 2 and Extract 3 of Production Examples were examined. Specifically, it was performed as follows. An appropriate amount of 10% FBS-containing MEM medium was taken in two 6-well plates, seeded with B16 melanoma cells, and allowed to stand at 37 ° C. in a carbon dioxide concentration of 5%. The next day, echinacea extract 1, extract 2 or extract 3 so that their final concentrations are 0 μg / mL (control), 10 μg / mL, 30 μg / mL, 100 μg / mL, 300 μg / mL, 1000 μg / mL It was dissolved in water, added and mixed. On day 5 of the culture, the medium was changed, and the sample preparation solution was added again. On the next day, the medium was removed and the cells were collected after washing with phosphate buffer on one plate, and the degree of whiteness of the cultured B16 melanoma cells was evaluated according to the following criteria. As a control, a sample to which no specimen was added was prepared.
(Criteria)
++: A whitening effect comparable to that of the sample to which 200 μg / mL kojic acid was added is shown.
+: A whitening effect comparable to that of the sample added with 100 μg / mL kojic acid is shown.
±: A whitening effect comparable to that of the sample added with 50 μg / mL kojic acid is shown.
-: Shows the same black color as the control.
For the remaining one plate, cells were fixed with formalin, added to a 1% crystal violet solution and stained. The cell viability (%) with respect to each sample concentration was measured with a monocerator (Olympus).
The results are shown in Table 1 below.

  From the results of Table 1, it can be seen that Echinacea extracts 1 to 3 show a high whitening effect of ++. In addition, the cell growth rate is higher in the order of the extract 1, the extract 2 and the extract 3, and it is understood that the echinacea extract extracted with hydrous ethanol having a low ethanol content is superior in safety. Therefore, the Echinacea extract has good safety and can be used as a whitening agent having a high whitening effect. Moreover, the skin external preparation or cosmetics which suppress a melanin production | generation and prevent skin spots and freckles can be created by mix | blending an echinacea extract with a skin external preparation and cosmetics.

Example 2: Lotion (Ingredient)
(mass%)
1 Glycerin 5
2 1,3-butylene glycol 6.5
3 Polyoxyethylene (20E.O.) sorbitan 1.2
Monolaurate 4 Ethanol 12
5 Lactic acid 0.05
6 Sodium lactate 0.1
7 Ascorbic acid glucoside 2
8 Echinacea extract of Production Example 1 0.0001
9 Methyl paraoxybenzoate 0.1
10 Perfume appropriate amount 11 Purified water remaining

(Production method)
A: Components 3, 4 and 9, 10 are mixed and dissolved.
B: Components 1, 2, 5-8 and 11 are mixed and dissolved.
C: A and B were mixed and uniformed to obtain a skin lotion.

Example 3: Latex (oil-in-water type)
(Ingredient) (mass%)
1 Polyoxyethylene (10E.O.) sorbitan 1
Monostearate 2 Polyoxyethylene (60EO) Sorbit 0.5
Tetraoleate 3 Glyceryl monostearate 1
4 Stearic acid 0.5
5 Behenyl alcohol 0.5
6 Squalane 8
7 Arbutin 3
8 Ethanol 10
9 Echinacea extract of Production Example 2 0.001
10 Purified water remaining amount 11 Carboxyvinyl polymer 0.2
12 Sodium hydroxide 0.1
13 Hyaluronic acid 0.1
14 perfume appropriate amount

(Production method)
A: Component 10 is heated and maintained at 70 ° C.
B: Components 1 to 6 are heated and mixed and kept at 70 ° C.
C: A is added to B, mixed and uniformly emulsified.
D: After cooling C, components 7-9 and 11-14 were added and mixed uniformly to obtain an emulsion.

Example 4: Liquid foundation (oil-in-water cream)
(Ingredient) (mass%)
1 Acrylic acid / alkyl methacrylate copolymer (Note 1) 0.5
2 Triethanolamine 1.5
3 Remaining purified water 4 Glycerin 5
5 Ethyl paraoxybenzoate 0.1
6 1,3-butylene glycol 5
7 Hydrogenated soybean phospholipid 0.5
8 Titanium oxide 5
9 Bengala 0.1
10 Yellow iron oxide 1
11 Black iron oxide 0.05
12 Stearic acid 0.9
13 Glycerol monostearate 0.3
14 cetostearyl alcohol 0.4
15 Polyoxyethylene (20E.O.) sorbitan monooleate 0.2
16 Polyoxyethylene trioleate (20E.O.) sorbitan 0.2
17 2-methoxyhexyl paramethoxycinnamate 5
18 Echinacea extract of Production Example 3 0.001
19 Perfume 0.02
(Note 1) Pemulen TR-2 (manufactured by NOVEON)

(Production method)
A: Components 6 to 11 are dispersed.
B: Components 12 to 17 are mixed uniformly at 70 ° C.
C: Components 1 to 5 are mixed uniformly at 70 ° C.
D: B is added to C to emulsify, and cooled to room temperature.
E: A and components 18 and 19 were added to D and mixed uniformly to obtain an oil-in-water cream liquid foundation.

Example 5: Sunscreen cosmetic (water-in-oil cream)
(Ingredient) (mass%)
1 Polyoxyethylene (20E.O.) sorbitan monolaurate 0.2
2 Polyoxyethylene (60E.O.) hydrogenated castor oil 0.1
3 Remaining purified water 4 Dipropylene glycol 10
5 Magnesium sulfate 0.5
6 Ascorbic acid glucoside 2
7 Silicone compound (Note 2) 3
8 Decamethylcyclopentasiloxane 20
9 Isotridecyl isononanoate 5
10 2-Ethylhexyl paramethoxycinnamate 8
11 Echinacea extract of Production Example 2 0.001
12 Dimethylstearyl ammonium hectorite 1.2
(Note 2) KF-6028 (manufactured by Shin-Etsu Chemical Co., Ltd.)

(Production method)
A: Components 1 to 6 are uniformly dispersed.
B: Components 7 to 12 are uniformly dispersed.
C: While stirring B, A was gradually added to emulsify to obtain a water-in-oil cream sunscreen cosmetic.

Example 6: Ointment (component) (mass%)
1 Stearic acid 18
2 Cetanol 4
3 DL-α-Tocopherol acetate (Note 3) 0.2
4 Methyl paraoxybenzoate 0.1
5 Echinacea extract of Production Example 1 0.1
6 Triethanolamine 2
7 Glycerin 5
8 Remaining purified water (Note 3) Made by Eisai

(Production method)
A. Ingredients 6-8 are heat mixed and maintained at 75 ° C.
B. Ingredients 1-5 are heat mixed and maintained at 75 ° C.
C. B was gradually added to A and mixed while cooling to obtain an ointment.

Example 7: Lotion agent (ingredient) (mass%)
1 Polyoxyethylene (20E.O.) sorbitan 1.2
Monolaurate 2 Ethanol 8
3 Methyl paraoxybenzoate 0.2
4 Echinacea extract of Production Example 1 0.1
5 1,3-butylene glycol 6.5
6 Glycerin 20
7 Allantoin (Note 4) 0.2
8 Remaining purified water (Note 4) Merck

(Production method)
A. Components 1 to 4 are mixed and dissolved.
B. Components 5 to 8 are mixed and dissolved.
C. A and B were mixed and homogenized to obtain a lotion preparation.

Example 8: Pack cosmetic (component) (mass%)
1 Polyvinyl alcohol 15
2 Glycerin 10
3 Polyoxyethylene (10E.O.) methyl glucoside 3
4 Glyceryl trioctanoate 5
5 Dipotassium glycyrrhizinate 0.1
6 Polyoxyethylene (4EO)
Cetyl ether sodium phosphate 1
7 Ethanol 20
8 Kaolin 2
9 Titanium oxide 2
10 Lactic acid (50% aqueous solution) 0.5
11 Sodium lactate (50% aqueous solution) 0.5
12 Preservative Appropriate amount 13 Fragrance Appropriate amount 14 Echinacea extract of Production Example 1 0.1
15 Remaining amount of purified water

(Production method)
A. Ingredients 1-6 and 15 are heated and mixed at 70 ° C. and cooled to room temperature.
B. Ingredients 7 to 14 were added to A and mixed to obtain a pack cosmetic.

  The lotions, emulsions, liquid foundations, sunscreen cosmetics, ointments, lotions, and pack cosmetics prepared in each of the above examples are all excellent in the whitening effect. It exhibits excellent effects such as prevention of precipitation, does not generate precipitates, has good stability, and is excellent in touch.

  According to the present invention, a whitening agent that can be easily blended into a skin external preparation or cosmetic and has a high whitening effect, and a skin external preparation or cosmetic that contains the same, has good stability and safety, and has a high whitening effect. Can be provided.

Claims (4)

A skin whitening external preparation for whitening comprising an echinacea extract as an active ingredient. A whitening cosmetic comprising an echinacea extract as an active ingredient. A whitening agent comprising an echinacea extract as an active ingredient. A melanin production inhibitor comprising an echinacea extract as an active ingredient.