JPH0196109A - Skin-beautifying cosmetic - Google Patents

Abstract

PURPOSE:To provide a skin-beautifying cosmetic containing kojic acid and/or its derivative and phytosterol and/or its derivative, and having improved excel lent skin-beautifying effect and high safety. CONSTITUTION:The objective skin-beautifying cosmetic contains 0.01-10wt.% of kojic acid and/or its derivative and 0.01-25wt.% of phytosterol of formula [R1 is H, 3-22C alkyl, 3-22C alkoxy, polyhydroxylated alkylene (2-3C) residue or sugar residue R2 is decyl, decenyl or nenyl] and/or its derivative. The phytosterol or its derivative is, e.g., beta-sitosterol, stigmasterol, campesterol, their fatty acid ester, aliphatic ether, polyoxyalkylene compound or glucoside. The above cosmetic can be used in the form of various cream, milky lotion, face lotion, pack, lip cream, foundation, etc.

Description

[Detailed description of the invention] [Industrial application field] The present invention relates to cosmetics with excellent whitening effects.

More specifically, the present invention relates to a whitening cosmetic composition in which kojic acid and/or its derivatives and phytosterols and/or its derivatives are blended into a cosmetic base to improve the whitening effect.

[Prior art]

Consumers, especially women in their late twenties, are very interested in cosmetics that have a skin whitening effect, and there has been a long-standing desire for products that are both safe and effective, especially for the improvement of age spots. Therefore, many researchers are searching for whitening ingredients and researching, developing, or providing various whitening cosmetics based on the inhibition of the activity of tyrosinase enzyme and the disappearance of active melanocytes, which are thought to be involved in the generation of age spots.

In the past, hydrogen peroxide, zinc peroxide,
Peroxides such as magnesium peroxide, ascorbic acid, glutathione, colloidal sulfur, and various natural products have been blended as whitening ingredients. but.

Peroxides and ascorbic acid have problems with stability, storage stability, etc., and their effects cannot be said to be sufficient. on the other hand,
Glutathione and colloidal sulfur have a strange odor, which makes it difficult to incorporate them into cosmetics.

Furthermore, in the United States and other countries, hydroquinone is used as a skin bleaching agent, but although it has a whitening effect, it is problematic to incorporate it into cosmetics due to safety (irritancy, allergy).

Therefore, recently, various whitening ingredients or cosmetics that have skin whitening effects without the problems mentioned above have been intensively developed.For example, kojic acid and kojic acid produced from Aspergillus, Penicillium, Acetobacter, etc. Whitening cosmetics using derivatives have been proposed (Special Publication No. 1983-
No. 18569, JP-A No. 53-3538, JP-A No. 61-
No. 60801, Special Publication No. 58-22151, Special Publication No. 1983
-9722), and cosmetics containing quercetin and/or its derivatives as an active ingredient (JP-A-55-92305).
Cosmetics containing catechins as active ingredients (Japanese Patent Application Laid-Open No. 52-44375) have also been developed, but the stability of these whitening ingredients is difficult to find in actual use. At present, various problems remain, such as that it is still insufficient, and that although it is effective at the cellular level, it is not fully effective in animals and humans.

[Problem that the invention seeks to solve]

The present invention aims to solve the above-mentioned problems and provide a cosmetic with excellent whitening effects.

More specifically, the present invention aims to provide a cosmetic containing a concomitant substance that further improves the whitening effect of kojic acid and/or its derivatives, which are known as whitening ingredients.

[Means to solve the problem]

The present inventors have focused on the knowledge obtained from the study of the morphology and physiological properties of age spots, namely that moisture content in the age spot area is lower than in normal areas and the skin is hardened, and we aim to improve the skin condition of the area. We investigated the effects of combining kojic acid and/or its derivatives with intercellular lipids and similar structures that can bring about the It has been found that the whitening effect of kojic acid and/or its derivatives can be further improved by doing so. The present invention was completed based on this knowledge.

That is, the present invention provides a whitening cosmetic composition characterized by containing kojic acid and/or a derivative thereof and a phytosterol represented by the following general formula (RI) and/or a derivative thereof.

○R1 In the above formula, R0 represents a hydrogen atom, an alkyl group having 3 to 22 carbon atoms, an alkoxy group having 3 to 22 carbon atoms, a polyoxylated alkylene (having 2 to 3 carbon atoms) residue, or a sugar residue. R2
represents a decyl group (C10H21-), a decenyl group (C1°Hxs-) or a nonyl group (C, U, S-). In this case, examples of polyoxylated alkylene residues include those represented by the formula -(CJ*0)rr-Hl-(C3R70+r7H).As the sugar residues, examples of the formula -
Examples include those shown by C, Hllo.

The kojic acid used in the present invention has a chemical name of 5-hydroxy-2-hydroxymethyl-4-pyrone, and is produced from fermentation extracts and recrystallizations produced from microorganisms such as Aspergillus, Penicillium, and Acetobacter. or synthetic products obtained by synthetic methods can be used. Kojic acid and its salts are commercially available and can be easily obtained.

The derivatives of kojic acid in the present invention include reaction derivatives of 5- and/or 2-hydroxy groups of kojic acid. Preferred examples of such derivatives include fatty acid esters having 3 to 22 carbon atoms, aliphatic ethers having 3 to 22 carbon atoms, and polyoxyalkylene (2 to 3 carbon atoms) derivatives.

In addition, the phytosterols represented by the above-mentioned general formula (1) used in the present invention belong to steroid alcohols widely distributed in the plant kingdom.2 In addition to existing in free form in vegetable oils, they also exist as esters and glucosides. ,soy,
Separated and purified products from shea butter, carrots, etc. can be used. In addition, Ly-l-sterol is not a single compound, but a mixture consisting of β-l-sterol, stigmasterol, and campesterol, and in the case of soybean phytosterol, the ratio is approximately 2:1:1. .

Furthermore, phytosterol derivatives consisting of phytosterols and their fatty acid esters, aliphatic ethers, polyoxyalkylene derivatives and glycosides.

They themselves have emulsifying, emulsion stabilizing, and solubilizing abilities, and their derivatives are commercially available at low cost and can be used depending on the dosage form of the product. Commercially available products include the Generalol 122 series (manufactured by Henkel Hakusuisha) and the N1kkol BPS series (manufactured by Nikko Chemicals).

In the present invention, it is essential to contain both the above-mentioned kojic acid and/or its derivative (hereinafter also referred to as kojic acid component) and phytosterol and/or its derivative (hereinafter also referred to as phytosterol component), Cosmetics containing only one of them cannot achieve the improvement in whitening effect, which is the objective of the present invention. The improvement in the whitening effect of the present invention is due to the fact that the skin condition is improved due to the skin anti-hardening or skin conditioning effect of phytosterols, and the transdermal absorption of kojic acid, which is a whitening agent, is increased by smoothing the transition to the stratum corneum. This is thought to be due to the mutual effect of preventing the deterioration of kojic acid due to the ultraviolet protection effect of phytosterols and stably retaining it on the skin.

The whitening cosmetic of the present invention includes, for example, cream.

Emulsion, lotion, pack agent, powder, lip balm,
This includes lipstick, under-makeup, foundation, sun care, and many more.

The amounts of the kojic acid and/or its derivatives and phytosterols and/or its derivatives to be added to the cosmetics are arbitrarily selected depending on the dosage form, but usually the kojic acid component is 0% in the cosmetics. .01-10 weight X.

It is preferable to mix the phytosterol component in an amount of 0.01 to 25% by weight. The blending amount is 0.01 weight 2
If the amount is less than that, the preferable effects of the present invention cannot be obtained. There is no particular upper limit on the upper limit, but if a large amount is blended, the stability of the product and the feeling of use such as stickiness will be poor, so it is not desirable for cosmetics. In the case of the phytosterol component, it is preferably 25% by weight. Moreover, the method of blending each component can be carried out in accordance with the conventional method of blending physiologically active ingredients and the like.

In addition to the above-mentioned components, the cosmetic of the present invention may contain additive components commonly used in cosmetics, such as surfactants, oils and fats, alcohols, humectants, thickeners, and preservatives.

Antioxidant, chelating agent, pHtA9Qi agent, fragrance 1 pigment.

Ultraviolet absorbing/scattering agents, water, etc. can be added. Specific examples of these additive components include, for example, as surfactants, lipophilic glycerin monostearate, self-emulsifying glycerin monostearate, polyglycerin monostearate, sorbitan monooleate, polyethylene glycol monostearate, Nonionic surfactants such as polyoxyethylene sorbitan monooleate, polyoxyethylene cetyl ether, polyoxyethylene sterol, polyoxyethylene lanolin, polyoxyethylene beeswax, polyoxyethylene hydrogenated castor oil; sodium stearate, palmitic acid Anionic surfactants such as potassium, sodium cetyl sulfate, sodium lauryl phosphate, triethanolamine palmitate, sodium polyoxyethylene lauryl phosphate, and sodium N-acylglutamate; cationic surfactants such as stearyldimethylbenzylammonium chloride and stearyltrimethylammonium chloride. Surfactant: Examples include amphoteric surfactants such as alkylaminoethylglycine hydrochloride solution and lecithin.

Examples of oils and fats include vegetable oils such as castor oil, olive oil, cacao butter, camellia oil, coconut oil, wood wax, jojoba oil, grapeseed oil, and avocado oil; animal oils and fats such as mink oil and egg yolk oil; beeswax, whale oil, etc. wax, lanolin, carnauba wax,
Waxes such as candelilla wax; hydrocarbons such as liquid paraffin, squalane, microcrystalline wax, ceresin wax, paraffin wax, petrolatum; lauric acid, myristic acid, stearic acid, oleic acid,
Natural and synthetic fatty acids such as isostearic acid and behenic acid; natural and synthetic higher alcohols such as cetanol, stearyl alcohol, hexyldecanol, octyldodecanol, lauryl alcohol; isopropyl myristate, isopropyl palmitate, octyldodecyl myristate, oleic acid Examples include esters such as octyl dedocyl and cholesterol oleate.

Moisturizing agents include polyhydric alcohols such as glycerin, propylene gellicol, 1,3-butylene gellicol, sorbitol, polyethylene glycol, and dipropylene glycol; amino acids, NMF components such as sodium lactate, sodium pyrrolidone carboxylate, and hyaluronic acid. Acid, collagen, mucopolysaccharides.

Examples include water-soluble polymeric substances such as chondroitin sulfate.

Thickeners include natural polymeric substances such as sodium alginate, xanthan gum, aluminum silicate, quince seed extract, tragacanth gum, and starch; semisynthetic substances such as methylcellulose, human-oxyethylcellulose, carboxymethylcellulose, soluble starch, and cationized cellulose. Polymeric substances; synthetic polymeric substances such as carboxyvinyl polymers and polyvinyl alcohol can be exemplified.

Preservatives include benzoate, salicylate, sorbate, dehydroacetate, hydroxybenzoic acid ester,
2,4,4'-trichloro-2'-hydroxydiphenyl ether, 3,4,4'-trichlorocarbanilide,
Benzalkonium chloride, hinokitiol, resorcinol,
Examples include ethanol and the like.

Examples of the antioxidant include dibutylhydroxytoluene, butylhydroxyanisole, propyl gallate, ascorbic acid, and the like. Furthermore, chelating agents include edetate disodium, ethylenediaminetetraacetate, pyrophosphate, hexametaphosphate, citric acid, tartaric acid, gluconic acid, etc., and pH adjusting agents include sodium hydroxide, triethanolamine, citric acid, etc. Examples include acids, sodium citrate, boric acid, borax, potassium hydrogen phosphate, and the like.

For ultraviolet absorbing and scattering agents, 2-hydroxy-4-
Examples include methoxybenzophenone, octyl dimethyl para-aminobenzoate, ethylhexyl para-methoxycynamate, titanium oxide, kaolin, and talc. Note that the optional components are not limited to these. By appropriately blending the above essential ingredients and optional ingredients, it can be used in various product forms such as creams, milky lotions, lotions, packs, powders, lip balms, lipsticks, under makeup, foundations, sun care, etc. .

A specific example of the cosmetic of the present invention will be shown below. For example, as a skin cream: Essential ingredients: 0.02 to 10%.

Oil content: 20-70%, surfactant: 2-7%, humectant:
5~■ part.

Purified water: balance, preservative: trace amount, fragrance: composition containing trace amount; as emulsion; essential ingredients: 0.02-10%
.

Oil content: 10-40%, surfactant: l-5%, humectant:
5-10%.

Purified water: balance, preservative: trace amount, fragrance: composition containing trace amount, as a lotion; essential ingredients: 0.02-10
%, alcohol: 2-50%, surfactant = 0.5
In ~2.

Moisturizer: 2-8%, antioxidant: 0.01-0.05%
, chelating agent: 0.02-0.1%, PU regulator: 0
．． 05-0.2%, purified water: balance, preservative: trace amount,
A composition containing a trace amount of pigment, a trace amount of fragrance, as a pack; Essential ingredients: 0.02-10%, 7/L/l -
/L/ type: 2-30%, moisturizer: 2-10%.

Examples include compositions containing inorganic powder: 0 to 20%, film-forming agent: 10 to 20%, preservative: trace amount, fragrance: trace amount.

〔Effect of the invention〕

According to the present invention, a cosmetic is provided which has a superior whitening effect and is highly safe than conventional products.

Therefore, the cosmetics of the present invention can be used in various product forms such as various cosmetic creams, emulsions, lotions, packs, powders, lip balms, lipsticks, under makeup, foundations, sun care, etc., and are especially suitable as skin cosmetics. 6 Next, the present invention will be explained in more detail with reference to Examples.

〔Example〕

Example 1 In order to prove the whitening effect of the cosmetic of the present invention, C57
Using the backs of black mice, the inhibitory effect on active melanocytes increased by UVB (ultraviolet) irradiation was investigated.

The test method is as follows.

(1) Sample The component composition (weight %) of the sample is as shown in Table-1.

(2) Active melanocyte suppression effect test The backs of C57 black mice (3 mice in each group) were shaved,
After hair removal with wax, 1/2 MEDth1 UVB
(Ultraviolet light) is irradiated once a day for one week. The specimen was applied once a day before or after irradiation. Furthermore, the evaluation was performed on the third day after the end of the test, and the inhibition rate was calculated based on the number of active melanocytes in the specimen that had not been coated. The number of active melanocytes was measured by exfoliating the epidermis with 2N sodium bromide treatment, staining with Dopa, and counting using a microscope6.The results are shown in Table 1.
Shown below.

From the results in Table 1, it can be seen that the products of the present invention containing a kojic acid component and a phytosterol, as well as both, have a clearly improved inhibitory effect on active melanocytes compared to a product containing only a kojic acid component. Furthermore, the effect of using a phytosterol component in combination is more pronounced when applied before ultraviolet irradiation than after irradiation.

Example 2 Furthermore, in order to prove the whitening effect of the cosmetic composition of the present invention, the bleaching effect was investigated using the backs of colored guinea pigs.

The test method is as follows.

(1) A lotion containing the whitening ingredients shown in Sample Table 2 and consisting of ~% ethanol and the balance purified water was prepared.

(2) Depigmentation effect test After shaving the backs of colored guinea pigs (3 animals in each group), 50 μQ'1r of each lotion - once a day, 5 times a week, approximately 4 d
The skin color was measured using a color difference meter on the 4th day after the test was completed. The results are shown in Table-2.

From the results in Table 2, it can be seen that the lotion of the present invention containing both a kojic acid component and a phytosterol component has a better decolorizing effect than a lotion containing only a kojic acid component.

Example 3 Examples of various cosmetics according to the present invention are shown below.

<Cream> A: Oil phase liquid paraffin (#70) 5.0 heavy weight% squalane 15.0 #cetostearyl alcohol 5. O〃Secret wax
2.0 Glyceryl monostearate 2.0 POE (20) Sorbitan monolaurate 2.011 Propyl paraben Q, l
n-phytosterol 1. Q n
B: Aqueous phase Kojic acid 0.5 weight 2 Hyaluronic acid 0.2 Methyl paraben
0.2〃Purified water
Balance C: Fragrance After mixing and dissolving appropriate amounts of ingredients A and B at 70℃, add B.
Add A to the mixture and emulsify it uniformly. Further, add C and cool to prepare cream.

Emulsion liquid〉 A: Oil phase liquid Para 7 in (#70) 10.0 wt ff% isopropyl myristate 2.0 wt%
Glycerin monostearate 0.5 Stearic acid 2.0 POE (20) Stearyl ether 0.7 POE (5) Phytosterol 2. O Glycyrrhetinic acid
0.1 Butylparaben 0.1
〃B: Water phase part Koji @ O, S heavy picture I triethanolamine 0.5〃Glycerin
2.0 Rikiichi Bobball 941
Q, l nethanol
10.0 II Methylparaben
Q, ln Purified water Balance C: Fragrance Mix and dissolve appropriate amounts of the above formulations A and B at 70°C.

Add A and emulsify uniformly. Further, add C and cool to prepare a milky lotion.

<Lotion> A: Ethyl alcohol phase Ethyl alcohol 10.0 weight 2PO
E (80) Hydrogenated castor oil 0.3 Phytosterol palmitate 0. l〃Tocopherol
0.1〃Methylparaben
0.1% by weight fragrance Appropriate amount B: Water phase Kojic acid 0.1% weight + A% glycerin 3.0〃Purified water
Balance After uniformly dissolving the above formulation A, it is gradually added to the aqueous phase of B while stirring to prepare a lotion.

<Pack agent> A: Ethyl alcohol phase Ethyl alcohol 1000 weight 2 Polyvinyl alcohol 15. OIT Propylene Glycol 3.0 Methylparaben
Q, l n-butylparaben
o, os upoc (5) phytosterol
2.5 I+glycyrrhizic acid
0. l〃B: Aqueous phase Sodium kojate 1.0% by weight Sodium carboxymethylcellulose 5.0I POR (15) Oleyl ether 1. O〃Purified water Balance C: Fragrance Appropriate amount The above formulations A and B were mixed and heated and mixed uniformly at 70°C. While further cooling, add Formulation C to characterize the pack.

Claims (3)

[Claims] (1) Kojic acid and/or its derivatives and the following general formula (
A whitening cosmetic containing a phytosterol represented by I) and/or a derivative thereof. General formula (I) ▲ Numerical formulas, chemical formulas, tables, etc. ) residue or sugar residue, R_2
represents a decyl group, decenyl group or nonyl group) (2) The phytosterol represented by the above general formula (I) and/or its derivatives are β-sitosterol, stigmasterol, campesterol and fatty acid esters, aliphatic ethers, polyoxyalkylene compounds or glycosides of these compounds. The whitening cosmetic according to claim (1), comprising one or more selected from the following. (3) The whitening cosmetic contains 0.01 to 10% by weight of kojic acid and/or a derivative thereof, and one of the phytosterols and/or derivatives thereof represented by the above general formula (I). The content of the species or two or more species is 0.01
The whitening cosmetic according to claim (1), wherein the content is 25% by weight.