JP4402278B2 - Whitening cosmetics - Google Patents

Description

【００２８】
（長期連用試験）
試験方法
しみ、色黒、そばかすに悩む女性モニター４０名（１８〜５８歳）を被験者として、１グループ１０名ずつ実施例−３、比較例−４、比較例−５、比較例−６の乳液を３ヵ月間、一日一回毎日使用させた。３ヵ月後の、しみ、色黒、そばかすの改善度合いについて、他覚所見、自覚所見にて美白効果を判定した。
【００２９】
比較例−４：乳液
実施例−３の乳液の（１０）田七ＢＧ抽出物を除き、他は同様に調製した。
比較例−５：乳液
実施例−３の乳液の（１１）Ｌ−アスコルビン酸りん酸マグネシウムをコウジ酸として、他は同様に調製した。
比較例−６：乳液
実施例−１の乳液の（１１）Ｌ−アスコルビン酸りん酸マグネシウムを胎盤抽出液として、他は同様に調製した。
【００３０】
試験結果
長期連用試験結果を表２に示す。表２から明らかな様に、本発明の田七人参抽出物とＬ−アスコルビン酸りん酸塩を併用した化粧料、実施例−３は、比較例−４、比較例−５、比較例−６と比較して美白効果に優れた新規化粧料である。なお、実施例−１、実施例−２、実施例−４についても同様に優れた美白効果の結果が得られた。
【００３１】
【表２】

【００３２】
（経時安定性試験）
試験方法
実施例−２及び比較例−７、比較例−８のクリームについて経時安定性試験を実施した。試験としては、常温、保温（４０℃）、冷温（５℃）でのクリームの経時的状態変化として、変色度と匂いの変化を観察した。
【００３３】
比較例−７：クリーム
実施例−２のクリームの（１３）Ｌ−アスコルビン酸りん酸マグネシウムと（１４）Ｌ−アスコルビン酸りん酸ナトリウムをカミツレエキスとし、他は同様に調製した。
比較例−８：クリーム
実施例−２のクリームの（１２）田七熱水抽出物（ＢＧ）を胎盤抽出液として、他は同様に調製した。
【００３４】
試験結果
各クリームの経時的状態変化を表３に示す。表３に示した様に、実施例−２のクリームは経時安定性に優れたものであった。比較例−７及び比較例−８の化粧料は褐色に変色し、変臭も認められ、経時的に状態が変化した。なお、実施例−１、実施例−３、実施例−４の化粧料についても 同様に経時安定性に優れていた。
【００３５】
【表３】

【００３６】
【発明の効果】
本発明によれば、上記で明らかのように、田七人参抽出物及びL−アスコルビン酸及びその誘導体の一種又は二種以上を有効成分として併用することにより、しみ、色黒、そばかすを著しく改善し、美白効果が相乗的に増大され、また、経時的安定性も飛躍的に改良された。[0001]
BACKGROUND OF THE INVENTION
The present invention relates to a novel whitening cosmetic. More specifically, the present invention relates to a whitening cosmetic having an excellent whitening effect, which contains as an active ingredient one or more of a ginseng extract, L-ascorbic acid and derivatives thereof.
[0002]
[Prior art]
It is considered that melanin pigments are formed due to abnormalities in hormones and the stimulation of ultraviolet rays from sunlight, and this is abnormally deposited in the skin. ing. Such compounds effective in the treatment and improvement of spots, dark blacks and freckles are classified into three types according to their whitening mechanism. The first type is a type that fades darkness by reducing melanin, which is mainly black, as represented by ascorbic acid and ascorbic acid derivatives. The second type, represented by kojic acid, works directly on melanin-producing cells, inhibits the activity of tyrosinase enzyme, inhibits the production of melanin, and suppresses darkness. The third type, like placenta extract, promotes metabolism and discharges black melanin pigments outside the body. In conventional whitening cosmetics, these three types of compounds have been used alone or in combination.
[0003]
[Problems to be solved by the invention]
Ascorbic acid and its derivatives, kojic acid, lucinol, arbutin, hydroquinone and the like are known as those used in conventional whitening cosmetics, but there were no satisfactory preparations from the viewpoint of stability and whitening effect.
[0004]
[Means for Solving the Problems]
In view of such a situation, as a result of intensive research, the present inventors are excellent in stability over time by using one or two or more of ginseng extract and L-ascorbic acid and its derivatives, It has been found that the stain, color blackness and freckles are remarkably improved and the whitening effect is synergistically increased, and the present invention has been completed. That is, the present invention is a whitening cosmetic characterized by containing one or two or more of ginseng extract, L-ascorbic acid and derivatives thereof.
[0005]
The seven ginsengs used in the present invention are also known as the three ginsengs, and are perennial herbs belonging to the family ginseng, a special product of Wenshan County, Yunnan Province, China. The active ingredient saponin is also contained 7-12%. In addition, it contains many flavone glycosides effective for heart disease, dentistin having hemostatic action, acetylene compound having anticancer action, various essential amino acids, other minerals, etc., and the effect is said to be great. JP-A-61-115013 also describes that a cosmetic containing a specific polysaccharide contained in ginseng such as ginseng as an active ingredient has an excellent cosmetic effect.
[0006]
The amount of the ginseng extract used in the present invention is 0.000005 to 10.0% by weight as a solid content in the entire cosmetic. Preferably it is 0.00001 to 5.0 weight%. If it is 0.000005% by weight or less, the effects referred to in the present invention may not be sufficiently exerted, which is not preferable. A blending amount of 10.0% by weight or more is possible, but a significant increase in the effect is not recognized and it is not economical.
[0007]
There is no particular limitation on the ginseng extract used in the present invention as long as it is an extract of ginseng. The preparation method is not particularly limited, and for example, it may be one extracted by heating or one extracted at room temperature, but one extracted at low temperature is desirable.
[0008]
The solvent used for the extraction is not particularly limited. For example, water, alcohols such as ethanol and methanol, ketones such as acetone and methyl ethyl ketone, ethers such as diethyl ether and tetrahydrofuran, and halogenation such as dichloromethane and chloroform. Examples thereof include one or more solvents selected from hydrocarbons, nitriles such as acetonitrile, and polyhydric alcohols such as 1-3 butylene glycol. According to these solvents, the components desired for the whitening cosmetic composition of the present invention are extracted from the ginseng. Of these, water or alcohol is preferred, and water or ethanol is particularly preferred from the viewpoint of the toxicity of the solvent.
[0009]
Further, the extract of the ginseng may be used as it is, or may be used after being subjected to treatments such as concentration, purification, dilution and filtration, if necessary. In addition, when dissolving the extract of ginseng, liquid polyhydric alcohols such as 1,3-butylene glycol, propylene glycol, diglycerin, glycerin, dipropylene glycol and the like are suitable. 1,3-butylene glycol, propylene glycol and diglycerin are preferable, and 1,3-butylene glycol is more preferable. These solvents may be used alone or in combination of two or more.
[0010]
The ginseng extract contains various substances, but the main component is saponin, and it contains other proteins and neutral sugars.
[0011]
The 1-3 butylene glycol solution of hot water extract of ginseng was crushed 1 kg of ginseng, added 3.3 kg of purified water, heated at 80 ° C. for 5 hours, and then allowed to stand at room temperature for 10 days. . A concentrate obtained by filtering and concentrating under reduced pressure was prepared by adding 50 wt% 1-3 butylene glycol aqueous solution so that the dry component became 2.5%. By this method, an extract of about 5 kg can be obtained from 1 kg of the ginseng (hereinafter referred to as “Tanachi hot water extract (BG)”).
[0012]
For the ethanol extract of ginseng, 1 kg of ginseng was pulverized, 3.3 kg of 90% ethanol aqueous solution was added to the ginseng, allowed to stand at room temperature for 24 hours, filtered, and concentrated under reduced pressure. Manufactured. By this method, it is possible to obtain about 100 g of extract from 1 kg of the ginseng (hereinafter referred to as “Tanachi Et extract”).
[0013]
1-3 butylene glycol extract of ginseng is crushed 1 kg of ginseng, added 5 kg of 50 wt% 1-3 butylene glycol aqueous solution, left at room temperature for 10 days, filtered and concentrated under reduced pressure. The obtained concentrate was prepared by adding 50% 1-3 butylene glycol aqueous solution so that the dry component was 2.5%. By this method, an extract of about 4 kg can be obtained from 1 kg of the ginseng (hereinafter, this extract is referred to as “tabuchi BG extract”).
[0014]
The compounding quantity of L-ascorbic acid and its derivative used for this invention is 0.001 to 20.0 weight% in the whole cosmetics, Preferably, it is 0.01 to 10.0 weight%. If it is 0.001% by weight or less, the effects referred to in the present invention are not sufficiently exhibited, which is not preferable. Moreover, although 20.0 weight% or more of mixing | blending is also possible, the remarkable increase in an effect is not recognized but it is not economical.
[0015]
L-ascorbic acid and its derivatives used in the present invention are, for example, L-ascorbic acid phosphate, L-ascorbic acid sulfate, L-ascorbic acid glucoside, L-ascorbic acid higher fatty acid ester, etc. Any of those produced by the method, enzyme method, fermentation method and the like can be used, and one or more of them can be used alone or in combination. Examples of the salt of L-ascorbic acid phosphate and L-ascorbic acid sulfate include sodium and potassium as metal salts, and magnesium and calcium as alkaline earth metal salts.
[0016]
In addition, the cosmetics of this invention can be implemented according to a normal manufacturing method. The cosmetics of the present invention, in addition to the essential components described above, are various components generally used in cosmetics, that is, fats, waxes, hydrocarbons, fatty acids, as long as the effects of the present invention are not impaired as required. , Alcohols, synthetic esters, surfactants, moisturizers, thickeners, inorganic substances, fragrances, drugs, purified water, and the like.
[0017]
【Example】
Next, although an Example is given and this invention is demonstrated further in detail, this invention is not limited by this. Note that the ginseng extract blended in the following examples was prepared according to the production method described above, and the blending amount indicates the solid content in the extract obtained by each extraction method.
[0018]
Example-1: Toner preparation Formulation amount (%)
(1) Ethyl alcohol 8.0
(2) Perfume appropriate amount (3) Polyoxyethylene (20) hydrogenated castor oil 0.4
(4) Glycerin 5.0
(5) 1,3 butylene glycol 3.0
(6) Tabuchi Et extract 2.0
(7) L-ascorbic acid magnesium phosphate 3.0
(8) Citric acid 0.5
(9) Sodium citrate 1.0
(10) Add purified water to bring the total amount to 100. Add (2) to (5) to (1) and dissolve to make A. Next, (6) to (9) are dissolved in (10) to obtain B. After adding A to B, no. Filter through 5C filter paper.
[0019]
Example-2: Cream formulation Formulation amount (%)
(1) Squalane 5.0
(2) Stearyl alcohol 1.5
(3) Cetyl alcohol 0.5
(4) Polyoxyethylene (20) sorbitan monostearate 1.2
(5) Sorbitan monostearate 0.8
(6) Polyoxyethylene (20) cetyl ether 2.5
(7) Adsorption purified lanolin 4.0
(8) Isops opil myristate 8.0
(9) Stearic acid 1.2
(10) 1,3-butylene glycol 6.0
(11) Methyl paraoxybenzoate 0.2
(12) Tanachi Hot Water Extract (BG) 0.5
(13) Magnesium L-ascorbate phosphate 0.5
(14) Sodium L-ascorbate phosphate 1.0
(15) Fragrance Appropriate amount (16) Add purified water to bring the total amount to 100. Dissolve (1) to (9) at 80 ° C. to give A. Next, (10) and (11) are dissolved in (16) at 80 ° C. to obtain B. Emulsify B with stirring, add (15) at 70 ° C., add (12), (13) and (14) at 40 ° C., and cool to 30 ° C. with stirring.
[0020]
Example-3: emulsion formulation blending amount (%)
(1) Squalane 3.0
(2) Microcrystalline wax 2.0
(3) Vaseline 1.0
(4) Behenyl alcohol 0.7
(5) Sorbitan monostearate ester 1.2
(6) Sorbitan sesquioleate 1.3
(7) Polyoxyethylene (20)
Sorbitan monooleate ester 2.2
(8) 1,3-butylene glycol 5.0
(9) Methyl paraoxybenzoate 0.2
(10) Tabuchi BG extract 0.001
(11) Magnesium L-ascorbate phosphate 5.0
(12) Perfume appropriate amount (13) Add purified water to bring the total amount to 100. Dissolve (1) to (7) at 80 ° C. Next, (8) and (9) are dissolved in (13) at 80 ° C. to obtain B. Emulsify B with stirring, add (12) at 70 ° C., add (10) and (11) at 40 ° C., and cool to 30 ° C. with stirring.
[0021]
Example-4: Pack formulation Formulation amount (%)
(1) Carboxymethylcellulose 3.0
(2) 1,3-butylene glycol 5.0
(3) Glycerin 4.0
(4) Ethyl alcohol 5.0
(5) Polyoxyethylene (20) lauryl ether 0.5
(6) Fragrance appropriate amount (7) Rice field hot water extract (BG) 0.2
(8) Magnesium L-ascorbate phosphate 8.0
(9) L-ascorbic acid glucoside 0.5
(10) Purified water is added to bring the total amount to 100. (1) to (6) are dissolved in (10) at 60 ° C, and (7), (8), (9) are added to 30 ° C. Cool with stirring.
[0022]
【The invention's effect】
The cosmetics of the present invention are superior in stability over time by using a combination of Tannin ginseng extract and magnesium L-ascorbate phosphate, significantly improving stains, darkness and freckles, and synergistically increasing the whitening effect. It is a glazed cosmetic. Next, about the effect of this invention, the result in a melanin production suppression test (in vitro whitening test), a long-term continuous test (in vivo whitening test), and a time-dependent stability test is shown.
[0023]
(Melanin production inhibition test)
Test Method To a dish (Falcon 3002) having a diameter of 60 mm, 3 ml of the skin lotion of Example-1 and Example-1a to Example-1e, Comparative Example-1, Comparative Example-2, and Comparative Example-3 was added, and B16 mouse melanoma was further added. 1.0 ml of the cell suspension was added and cultured. B16 mouse melanoma cells were thawed from a stock frozen at −85 ° C. and cultured in a culture solution at 37 ° C. under 5% CO ₂ conditions. In the test, cells in the logarithmic growth phase were subjected to the test. After 3 days of culture, the culture medium containing the sample substance was replaced, and after 6 days, the cells were detached with PBS (−) containing 0.25% trypsin and 0.02% EDTA, and the number of cells per dish was calculated. The pellet was collected by centrifugation, then treated with 10% TCA, and 0.1N NaOH containing 10% DMSO was added to the pellet obtained by centrifugation to 1 × 10 ⁶ cells / ml, and OD475 nm was measured. . Next, the inhibition rate of melanin production was calculated from the OD475 nm of each sample with respect to the blank OD475 nm.
[0024]
Example-1a to Example-1e: Toner lotion In the lotion of Example-1, the blending amount of (6) Tabashi Et extract and the blending amount of (7) magnesium L-ascorbate phosphate are as follows. Toner lotion.
Tabuchi Et Extract (%) Magnesium Ascorbate Phosphate (%) Example-1a 0.000005 0.005
Example-1b 0.0002 0.02
Example-1c 0.05 2.0
Example-1d 5.0 10.0
Example-1e 10.0 20.0
[0025]
Comparative example-1: lotion The lotion of Example-1 was prepared in the same manner except for the (6) Tabuchi Et extract.
Comparative Example-2: Lotion Toner lotion of Example-1 (7) Magnesium L-ascorbate was used as kojic acid, and the others were similarly prepared.
Comparative Example-3: Lotion Toner lotion of Example-1 (7) Magnesium L-ascorbate was prepared in the same manner as the placenta extract.
[0026]
Test results Table 1 shows the results of the melanin production inhibition test. As is apparent from the results in Table 1, Example-1, Example-1b, Example-1c, Example-1d, and Example in which the ginseng extract and L-ascorbic acid phosphate were used in combination were combined. -1e lotion, compared with the lotions of Example-1a, Comparative Example-1, Comparative Example-2, and Comparative Example-3, a novel makeup that is very excellent in whitening effect with melanin production inhibitory action It is a fee. In addition, also about Example-2, Example-3, and Example-4, the result of the excellent melanin production inhibitory effect was obtained similarly.
[0027]
[Table 1]

[0028]
(Long-term continuous test)
Test method: 40 female monitors (18-58 years old) who are bothered with darkness and freckles (18-58 years old) as subjects, 10 emulsions per group in Example-3, Comparative Example-4, Comparative Example-5, and Comparative Example-6 Was used once a day for 3 months. After 3 months, the whitening effect was determined based on objective findings and subjective findings on the degree of improvement in spots, dark blacks and freckles.
[0029]
Comparative Example-4: Emulsion Other than the (10) Tabuchi BG extract of the emulsion of Example-3, the others were prepared in the same manner.
Comparative Example-5: Emulsion The emulsion of Example-3 was prepared in the same manner except that (11) magnesium L-ascorbate phosphate was used as kojic acid.
Comparative Example-6: Emulsion The emulsion of Example 1 was prepared in the same manner except that (11) magnesium L-ascorbate phosphate was used as the placenta extract.
[0030]
Test results Table 2 shows the long-term continuous test results. As is apparent from Table 2, the cosmetic composition using Example 7 ginseng extract and L-ascorbic acid phosphate in combination, Example-3, Comparative Example-4, Comparative Example-5, and Comparative Example-6. It is a new cosmetic with an excellent whitening effect compared to In addition, the result of the excellent whitening effect was similarly obtained about Example-1, Example-2, and Example-4.
[0031]
[Table 2]

[0032]
(Aging stability test)
Test Method A time-dependent stability test was performed on the creams of Example-2, Comparative Example-7, and Comparative Example-8. As a test, changes in discoloration and odor were observed as changes over time in the cream at normal temperature, heat retention (40 ° C.), and cold temperature (5 ° C.).
[0033]
Comparative Example-7: Cream The cream of Example-2 was prepared in the same manner except that (13) magnesium L-ascorbate phosphate and (14) sodium L-ascorbate phosphate were used as the chamomile extract.
Comparative Example -8: Cream The cream of Example-2 was prepared in the same manner except that the (12) Tanachi hot water extract (BG) was used as the placenta extract.
[0034]
Test results Table 3 shows changes in the state of each cream over time. As shown in Table 3, the cream of Example-2 was excellent in stability over time. The cosmetics of Comparative Example-7 and Comparative Example-8 turned brown, odors were observed, and the state changed over time. The cosmetics of Example-1, Example-3, and Example-4 were similarly excellent in stability over time.
[0035]
[Table 3]

[0036]
【The invention's effect】
According to the present invention, as apparent from the above, the use of one or more of ginseng extract and L-ascorbic acid and its derivatives as an active ingredient significantly improves stains, color blackness and freckles. However, the whitening effect was synergistically increased, and the stability over time was dramatically improved.

Claims (1)

A whitening cosmetic characterized by containing an ethanol extract of a ginseng and a magnesium L-ascorbate phosphate.