JP2002234828A - Skin whitening cosmetic preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a skin whitening cosmetic preparation effective for prevention and improvement of pigmentation caused after sunburn or acne, pigmentation caused in young generation, liver spot frequently generated in a menopause woman, senile pigment macule generated with aging and the like, safe and having an excellent skin whitening effect. SOLUTION: Two kinds or more selected from a group consisting of an L-ascorbic acid derivative, an oil-soluble glycyrrhiza extract and a bearberry leaf fluid extract, and a polyethylene glycol, and a yeast and/or a yeast extract are included.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a whitening cosmetic. More specifically, it suppresses the production of melanin and is effective in preventing and improving pigmentation that occurs after sunburn or acne, pigmentation that occurs in the young age group, liver spots that frequently occur in menopausal women, senile pigmentation that appears with aging, etc. A safe and whitening cosmetic having an excellent skin whitening effect.

[0002]

2. Description of the Related Art Although most people who use whitening cosmetics have high expectations as a stain remover including liver spots and senile pigment spots, the biological mechanisms of these pigment disorders are clear. However, at present, the mechanism of pigmentation caused by ultraviolet irradiation has not been sufficiently elucidated. Even under such circumstances, tyrosinase inhibitors, which are melanin synthases directly involved in enhancement of melanin synthesis in pigment cells, which is a fundamental phenomenon of the pigmentation mechanism, are being searched. Agents for preventing skin spots, pigmentation such as freckles, ascorbic acid and its derivatives, placenta extract, arbutin, kojic acid,
There are ellagic acid, licorice extract, euphorma flow extract, hydroquinone, etc., and a method of topically applying the composition to various cosmetics such as creams and expecting its effects is known. For example, in order to improve the stability and moisturizing effect of the L-ascorbic acid derivative, xanthan gum and sodium hyaluronate were blended (Japanese Patent Application Laid-Open No. 5-34571).
No. 4), hydroxyethanediphosphonate and diethylenetriaminepentaacetate (JP-A-10-1).
No. 47512) is well known. It is also disclosed that a licorice flavonoid is blended to provide an excellent whitening effect and safety (JP-A-5-186324 and JP-A-5-186324).
-201847, JP-A-6-271453). In addition, a whitening agent containing awaurushi or its extract as an active ingredient has been disclosed (JP-A-6-166609).

As a cosmetic, a whitening cosmetic, an external preparation for the skin, a whitening agent, etc. containing polyethylene glycol, 7.0% by weight of awaurushi and polyethylene glycol, awaurushi 1
0% by weight, polyethylene glycol, and Uwaurushi 5
Skin external preparation containing 1% by weight and polyethylene glycol 1500 (JP-A-2000-281555), a transdermal absorption enhancer containing a lipophilic flavonoid and a polymer compound, and efficiently exhibiting effects such as skin whitening and anti-aging, and Cosmetic (JP-A-11-79931), whitening cosmetic containing 2% by weight of sodium L-ascorbate and polyethylene glycol (JP-A-5-229927), 0.1% by weight of glabrene, L-ascorbyl phosphate An external preparation for skin containing 0.5% by weight of magnesium, 0.01% by weight of polyethylene glycol and glabrene, 1.5% by weight of arbutin and polyethylene glycol (JP-A-6-2714)
No. 53), ascorbic acid triphosphate3.
0% by weight and polyethylene glycol 4000 (Japanese Unexamined Patent Publication No.
JP-A-3-267709), an external preparation for skin containing 1.0% by weight of arbutin and polyethylene glycol 1500 (JP-A-11-246339), glutathione 3.0
Skin external preparation containing 1% by weight of arbutin, 1.0% by weight of arbutin and polyethylene glycol 1500 (JP-A-11-9232).
No. 6), a whitening agent containing 1.0% by weight of arbutin and polyethylene glycol 1500 (JP-A-2000-281)
557) and the like. Further, as a cosmetic using polyethylene glycol, a cosmetic having an improved effect of improving rough skin containing polyethylene glycol 1500 in 1.0% by weight, 0.1% by weight and 0.5% by weight of L-ascorbic acid ester, respectively. Kaisho 60-11
No. 6,618, JP-A-60-116616) and cosmetics containing 0.5% by weight of sodium salt of L-ascorbic acid sulfate and polyethylene glycol and excellent in stability over time and feeling of use (JP-A-11-236310) No.)
Is also known.

On the other hand, as a cosmetic utilizing yeast, a cosmetic containing a fermented liquid obtained from a yeast culture of the genus Saccharomyces as an active ingredient (Japanese Patent Application Laid-Open No. 7-107334), the epidermal cell itself inside the skin surface layer. Ceramide synthesis accelerator (JP-A-8-217658) for stimulating ceramide synthesis and improving skin barrier function, glycosides such as raspberry ketone-D-glucoside (β-form) and yeast extract or culture of bacteria containing the same It is uncertain whether the whitening cosmetic (Japanese Patent Laid-Open No. 2000-109408) containing the product can be expected to have a whitening effect such as a tyrosinase activity inhibitory effect or a melanin production inhibitory effect of the yeast extract alone or the yeast extract and the glycoside. . 150 L bathtub as bath agent
The composition for use in L-ascorbic acid 1 g and yeast extract 10 g (JP-A-5-229932)
Gazette). As a composition containing a yeast extract and polyethylene glycol, JP-A-7-30040
No. 9, JP-A-9-124438, JP-A-9-124438
-4953 is disclosed.

[0005]

However, as a whitening agent, ascorbic acid and its derivatives, placenta extract, arbutin, kojic acid, ellagic acid, licorice extract, euphoric acid extract, hydroquinone, etc., and a whitening agent only containing yeast extract. Many of the cosmetics were not satisfactory because the expected effects were weak and there were insufficient safety aspects such as formulation stability and skin irritation.

[0006] Therefore, there is no problem in safety and stability, the skin whitening effect is excellent, the production of melanin is suppressed,
There has been a need for the development of a whitening cosmetic that is effective in preventing and improving pigmentation that occurs after sunburn or acne, pigmentation that occurs in the young age group, liver spots that frequently occur in menopausal women, and senile pigment spots that appear with aging. .

[0007]

In view of such circumstances, the present inventors have conducted intensive studies to obtain a whitening cosmetic having an excellent whitening effect. As a result, an L-ascorbic acid derivative, an oil-soluble licorice extract, Two or more selected from the group consisting of fluid extract, polyethylene glycol, and yeast and / or yeast extract and found that the whitening effect can be synergistically enhanced to solve the above problems,
The present invention has been completed.

That is, the present invention comprises two or more selected from the group consisting of an L-ascorbic acid derivative, an oil-soluble licorice extract, and a saccharomyces cerevisiae extract, polyethylene glycol, and yeast and / or yeast extract. It is a whitening cosmetic characterized by the above.

[0009]

Embodiments of the present invention will be described below in detail.

The L-ascorbic acid derivatives used in the present invention include, for example, L-ascorbate such as sodium L-ascorbate, potassium L-ascorbate, magnesium L-ascorbate, calcium L-ascorbate and aluminum L-ascorbate. -Ascorbate,
L-ascorbic acid such as sodium L-ascorbate, potassium L-ascorbate, magnesium L-ascorbate, calcium L-ascorbate, and aluminum L-ascorbate L-ascorbic acid such as phosphate salt, sodium L-ascorbate sulfate, potassium L-ascorbate sulfate, magnesium L-ascorbate sulfate, calcium L-ascorbate sulfate, and aluminum L-ascorbate sulfate Sulfate, L-ascorbyl palmitate, L-ascorbyl isopalmitate, L-tetraisopalmitate
Ascorbyl, L-ascorbyl dipalmitate, L-ascorbyl diisopalmitate, L-ascorbyl stearate, L-ascorbyl isostearate, L-ascorbyl distearate, L-diisostearate
L such as ascorbyl, L-ascorbyl myristate, L-ascorbyl isomyristate, L-ascorbyl dimyristate, and L-ascorbyl diisomyristate
-Ascorbic acid alkyl ether and the like. In the present invention, one or a combination of two or more of these L-ascorbic acid derivatives can be used as appropriate according to the purpose.

The compounding amount of the L-ascorbic acid derivative used in the present invention is 0.5 to 10.0% by weight, more preferably 1.0 to 7.5% by weight. If the amount of the L-ascorbic acid derivative is less than 0.5% by weight, a sufficient whitening effect cannot be obtained, and if the amount exceeds 10.0% by weight, no improvement in the whitening effect can be expected. Formulation stability becomes difficult.

The oil-soluble licorice extract used in the present invention comprises:
An oil-soluble extract of the roots of licorice or other congeners may be used as an extract extracted with a solvent such as ethanol, or a powder obtained by removing the solvent from the extract may be used. Further, it may be obtained by synthesis.

The amount of the oil-soluble licorice extract used in the present invention is 0.001 to 0.25% by weight, more preferably 0.005 to 0.2% by weight. When the amount of the oil-soluble licorice extract is less than 0.001% by weight, a sufficient whitening effect is not exerted. When the amount exceeds 0.25% by weight, a unique odor becomes uncomfortable to use, and particularly safety. This is a problem.

[0014] The extract of Pleurotus terrestris used in the present invention is an aqueous extract of the bear berry, which is a plant of the family Azalea.
Examples thereof include those extracted using a solvent commonly used for extracting crude drug extracts such as water and ethanol, and powders obtained by removing the solvent from the extract by freeze-drying or the like.

[0015] The blending amount of the eucalyptus flow extract used in the present invention is 0.1 to 25.0% by weight, more preferably 0.5 to 20.0% by weight. If the blending amount of the extract of Ouarushi is less than 0.1% by weight, a sufficient whitening effect cannot be obtained, and if it exceeds 25.0% by weight, no improvement in the whitening effect can be expected.

The polyethylene glycol used in the present invention is known as a cosmetic raw material, and is a HOCH as a condensation polymer of ethylene oxide and water.
₂ (CH ₂ OCH ₂ ) nCH ₂ OH. In cosmetics, it is used as a moisturizer in creams, lotions, serums, etc., and in pharmaceuticals, it is used as an ointment base or tablet base. Specific examples of polyethylene glycol include polyethylene glycol 1000, 1500, 15
40, 4000 and the like. In the present invention, one or more of these polyethylene glycols can be used in an appropriate combination according to the purpose.

The amount of the polyethylene glycol used in the present invention is 0.01 to 5.0% by weight, more preferably 0.1 to 3.0% by weight. If the blending amount of polyethylene glycol is less than 0.01% by weight, the moisturizing effect is insufficient, and if the blending amount exceeds 5.0% by weight, disadvantages such as stickiness may occur.

The yeast and yeast extract used in the present invention include:
Yeast viable cells themselves, dried and powdered yeast cells and yeast cells were subjected to solubilization, extraction, purification, etc. under appropriate conditions such as autolysis, hot water extraction, acid hydrolysis, and enzymatic decomposition. There are yeast extract etc., especially yeast extract, extract Saccharomyces Cerevisiae as a raw material from yeast,
A concentrated and deodorized water-soluble extract having a physiological activity is preferable because it contains abundant nucleic acids and nucleic acid-related substances involved in skin cell activation. The yeast extract can be used arbitrarily regardless of a production method such as an extraction method, a purification method, and a treatment method, and is not particularly limited.

The amount of the yeast and / or yeast extract is not particularly limited, but is preferably 0.001-2% based on the total amount of the whitening cosmetic.
It is 5.0% by weight, preferably 0.1 to 21.0% by weight. When the amount is less than 0.001% by weight, a whitening effect and a skin irritation suppressing effect cannot be obtained, and 25.0%.
Even if it is added in excess of weight%, no improvement in the whitening effect can be expected, and the stability of the preparation as a whitening cosmetic becomes difficult.

In addition to the above-mentioned essential components, the whitening cosmetic of the present invention may contain other components as required, such as humectants, oily components, drugs, and thickeners, which are usually used in cosmetics, pharmaceuticals, and quasi-drugs. An agent, a surfactant, a pH adjuster, a preservative, an antioxidant, a pigment, a dye, an ultraviolet scattering agent, an ultraviolet absorber, a fragrance, alcohol, purified water and the like can be appropriately blended.

The whitening cosmetics of the present invention refer to those applied as cosmetics, pharmaceuticals and quasi-drugs for the purpose of preventing and improving pigmentation, such as creams, ointments, emulsions, serums, and lotions. , Packs, bath preparations, makeup cosmetics, etc., and the dosage form is not particularly limited.

Next, the present invention will be described in more detail with reference to examples, but the technical scope of the present invention is not limited by these examples. In addition, the unit of the compounding amount in the following examples is all weight% with respect to the total amount.

Examples 1 to 4 and Comparative Examples 1 to 4 Cosmetics Cosmetics having the compositions shown in Tables 1 and 2 below were produced, and were evaluated for stickiness, discomfort, and skin irritation using the evaluation methods described below. And the whitening effect was evaluated.

[0024]

[Table 1]

[0025]

[Table 2]

[Production Method] A: Components 1 to 13 are dissolved in Component 19. B. Dissolve components 15 to 18 in component 14. B was added to C A and mixed uniformly to obtain a lotion.

[Usability] (Evaluation method) The usability was evaluated for stickiness, discomfort and irritation during use. According to the method, stickiness, discomfort and irritation when applied to the skin were evaluated by the following criteria based on sensory evaluation by 25 evaluation panels having troubles such as spots and freckles. (Evaluation criteria for stickiness) ○ 20 or more out of 25 people evaluated that they were not sticky. △ 10 to less than 20 out of 25 were evaluated as non-sticky. X: Less than 10 out of 25 people evaluated that they were not sticky.

(Evaluation criteria for discomfort and irritation) ○ Out of the 25 subjects, 0 to 2 recognized discomfort and irritation. △ 3 to 5 out of 25 subjects felt discomfort and irritation. × Six or more of the 25 subjects felt discomfort and irritation.

[Whitening Effect] (Test Method) The skin was applied to the face twice a day for 3 months by 25 evaluation panels having troubles such as spots and freckles, and the whitening effect was evaluated after 3 months. . (Evaluation Criteria) ２０ 20 or more out of 25 subjects clearly showed a whitening effect as compared with the uncoated site. Δ 10 or more and less than 20 out of 25 subjects clearly showed a whitening effect as compared with the uncoated site. × Less than 10 out of 25 subjects clearly showed a whitening effect as compared with the uncoated site.

As is clear from the results shown in Tables 1 and 2, it was recognized that the whitening cosmetics of Examples 1 to 4 according to the present invention had an excellent whitening effect as compared with Comparative Examples.

Example 5 Cream (Ingredient) (% by weight) 1 Behenyl alcohol 4.0 2 Celesin 3.0 3 Adsorbed and purified lanolin 3.0 4 Pentaglyceryl monostearate 3.5 5 Pentaglyceryl hexastearate 1.06 Glyceryl trioctanoate 5.0 7 Liquid paraffin 9.0 8 Neopentyl glycol dicaprate 5.0 9 L-ascorbic acid sodium phosphate 3.0 10 Tetrasodium hydroxyethanediphosphonate 0.1 11 Citric acid 0.01 12 Sodium citrate 0.5 13 Triethanolamine 0.114 1,3-butylene glycol 3.015 Polyethylene glycol 4000 0.316 Xanthan gum 0.217 Preservatives Appropriate amount 18 Uwaurushi flow extract 3.0 19 Yeast extract 3 0.0 20 Sodium copper chlorophyllin proper amount 21 perfume proper amount 22 purified water balance

[Production Method] A Components 1 to 8 are heated to 80 ° C. and dissolved. B. Dissolve components 9 to 17 in component 22 at 80 ° C. Add A to CB and emulsify. Cool DC, add components 18-21, mix homogeneously with a homomixer, and cool to 30 ° C.

Example 6 Lotion (Ingredient) (% by weight) 1 L-ascorbic acid phosphate magnesium 3.0 2 Citric acid 0.05 3 Sodium citrate 0.64 Trisodium edetate 0.15 Propylene Glycol 3.0 6 Polyethylene glycol 4000 0.17 Uwaurushi flow extract 5.0 8 Yeast extract 5.0 9 Sodium copper chlorophyllin qs 10 Triethanolamine 0.2 11 Ethanol 3.0 12 Polyoxyethylene oleyl ether 1.0 13 Appropriate amount of preservatives 14 Appropriate amount of fragrance 15 Purified water balance

[Production Method] A After heating the component 15 to 70 ° C., the component 1 is added and completely dissolved. Cool BA to 30 ° C., add components 2 to 10, and dissolve uniformly. C Add components 12 to 14 to component 11 and dissolve uniformly. Add C to DB and mix uniformly.

Example 7 Essence (Component) (% by weight) 1 L-ascorbic acid sodium phosphate ester 3.0 2 Citric acid 0.01 3 Sodium citrate 0.74 Tetrasodium hydroxyethanediphosphonate 0.04 15 L-Arginine 0.26 Xanthan gum 0.57 Polyethylene glycol 4000 1.08 Concentrated glycerin 3.0 9 1,3-butylene glycol 3.0 10 Polyoxyethylene hydrogenated castor oil 0.311 Polyoxyethylene coconut Oil fatty acid sorbitan 0.1 12 Methyl phenyl polysiloxane 2.0 13 Ethanol 3.0 14 Oil-soluble licorice extract 0.05 15 Preservatives proper amount 16 flavors proper amount 17 Uwaurushi flow extract 10.0 18 Yeast extract 3.0 19 Copper chlorophyllin Sodium suitable amount 20 purified water balance

[Production Method] A: Components 1 to 5 are dissolved in Component 20. Add component 6 to B A and mix uniformly. C. Components 7 to 12 are dissolved by heating to 45 ° C. Add C to DB and mix uniformly. E Add components 14 to 16 to component 13 and dissolve. Add E and components 17 to 19 to FD, and mix uniformly with a homomixer.

Example 8 Pack (ingredient) (% by weight) 1 Magnesium phosphate L-ascorbate 3.0 2 Trisodium edetate 0.05 3 Citric acid 0.014 Sodium citrate 1.05 Polyethylene Glycol 4000 0.26 1,3-butylene glycol 4.5 7 Preservative suitable amount 8 hydroxyethylcellulose 0.59 Titanium mica 3.5 10 Bentonite 16.0 11 Titanium oxide 1.5 12 Talc 0.5 13 Uwaurushi flow Extract 3.014 Yeast extract 3.015 Sodium copper chlorophyllin qs 16 ethanol 4.5 17 polyoxyethylene sorbitan monolaurate 0.3 18 perfume qs 19 purified water balance

[Production Method] A Component 19 is heated to 70 ° C. to completely dissolve Component 1. Add components 2 to 7 to B A and dissolve uniformly. Add components 8 to 12 to CB and mix uniformly. Cool the DC to 35 ° C, add ingredients 13-18 and homogenize in a colloid mill.

Example 9 Cream Foundation (Components) (% by weight) 1 stearic acid 4.0 2 behenyl alcohol 1.0 3 self-emulsifying glyceryl monostearate 2.5 4 polyglyceryl tetraisostearate 3.0 5 sorbitan monooleate 1.56 polyoxyethylene glyceryl tristearate 1.57 adsorbed and purified lanolin 5.0 8 petrolatum 2.5 9 methylphenylpolysiloxane 1.0 10 L-ascorbyl tetraisopalmitate 0.5 11 preservative suitable amount 12 Concentrated glycerin 5.0 13 Bentonite 0.514 Titanium oxide proper amount 15 Talc 0.516 Bengala proper amount 17 Yellow iron oxide proper amount 18 Black iron oxide proper amount 19 Triethanolamine 1.3 20 Oil soluble licorice extract 0.02 21 1,1 3-butylene Recall 5.0 22 bearberry liquid extract 7.5 23 Yeast Extract 3.0 24 sodium copper chlorophyllin qs 25 Perfume qs 26 Purified water Balance

[Production Method] A Component 26 is heated to 80 ° C., and components 12 to 19 are added and uniformly dispersed with an ultra mixer. B Components 1 to 11 are heated to 80 ° C. and uniformly dissolved. Add B to CA and emulsify. Cool DC and add components 20-25 to make it uniform.

The cream of Example 5, the lotion of Example 6,
The essence of Example 7, the pack of Example 8, and the cream foundation of Example 9 showed excellent effects when applied to the skin in all of the usability and whitening effect tests by the above evaluation methods.

[0042]

As described above, the present invention suppresses the production of melanin, pigmentation that occurs after sunburn or acne,
It is possible to provide a whitening cosmetic which is effective for preventing and improving pigmentation occurring in a young age group, liver spots frequently occurring in menopausal women, senile pigment spots appearing with aging, and the like, and having a safe and excellent skin whitening effect. .

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[Procedure amendment]

[Submission date] March 8, 2001 (2001.3.8)

[Procedure amendment 1]

[Document name to be amended] Statement

[Correction target item name] 0024

[Correction method] Change

[Correction contents]

[0024]

[Table 1]

[Procedure amendment 2]

[Document name to be amended] Statement

[Correction target item name] 0025

[Correction method] Change

[Correction contents]

[0025]

[Table 2]

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61K 7/00 A61K 7/00 NU X 7/021 7/021 (72) Inventor Yuki Sakurai Shita Shizuoka 65-1 Irino, Koriokabe-cho Nikko Pharmaceutical Co., Ltd. AD532 AD641 AD642 CC02 CC04 CC05 CC07 CC12 DD23 DD27 DD31 EE16 FF05

Claims (1)

[Claims] 1. A method comprising: containing at least two members selected from the group consisting of an L-ascorbic acid derivative, an oil-soluble licorice extract, and a luxury lux, a polyethylene glycol, and a yeast and / or a yeast extract. Whitening cosmetics.