JPH01121206A - Skin beautifying cosmetic - Google Patents

Abstract

PURPOSE:To obtain a cosmetic having improved skin beautifying effect and high safety, by compounding a cosmetic base with kojic acid and/or its derivative and guanosine 3',5'-cyclic monophosphate and/or its derivative. CONSTITUTION:The objective skin beautifying cosmetic having synergistically improved skin beautifying effect and especially suitable as a skin cosmetic (e.g. cream, milky lotion, face lotion, pack, powder, rouge, foundation or sun care) is produced by compounding (A) kojic acid (5-hydroxy-2-hydroxymethyl-4- pyrone) and/or its derivative in combination with (B) a guanosine 3',5'-cyclic monophosphate of formula (R1-R3 are H, 2-22C acyl or 2-22C alkyl; X is H or salt-forming cation) and/or its derivative. The amounts of the components A and B are preferably 0.01-10wt.% and 0.01-15wt.%, respectively.

Description

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

More specifically, kojic acid and/or its derivatives and guanosine 3',5'-cyclic monophosphate and/or
The present invention relates to a whitening cosmetic in which the whitening effect is improved by blending the present invention or a derivative thereof into a cosmetic base.

[Prior art]

Consumers, especially middle-aged women in their late twenties, are extremely interested in cosmetics that have a skin whitening effect, and in particular, cosmetics that can safely and effectively prevent age spots and remove age spots that appear on the skin. has been traditionally requested. 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 order to obtain whitening cosmetics, peroxides such as hydrogen peroxide, zinc peroxide, and magnesium peroxide, ascorbic acid, glutathione, colloidal sulfur, and various natural products have previously been blended as whitening ingredients. However, peroxides and ascorbic acid have problems in 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 not safe. There are problems with incorporating it into cosmetics from the viewpoint of (irritation and allergy).

Therefore, in recent years, various whitening ingredients or cosmetics that have skin whitening effects without the above-mentioned problems have been intensively developed. For example, whitening cosmetics using kojic acid and kojic acid derivatives produced from the genus Aspergillus, Penicillium, Acetobacter, etc. have been proposed (Japanese Patent Publication No. 1973-
No. 18569, Japanese Patent Publication No. 53-3538, Special Publication No. 1856]-
No. 60801, Special Publication No. 58-22151, Special Publication No. 1983
-9722). In addition, cosmetics containing quercetin and/or its derivatives as an active ingredient (Japanese Patent Application Laid-Open No. 55-923'0
5, JP 58431911) and cosmetics containing catechins as active ingredients (JP 52-44375), etc., but the stability of these whitening ingredients is still insufficient in actual use. At present, various problems remain, such as being insufficient, and although effective at the cellular level, the effects cannot be fully demonstrated 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 investigated the morphology and physiological properties of age spots, and found that the age of the age spot has decreased moisture content and hardened skin compared to normal areas. Therefore, with the aim of improving the skin condition, we investigated the effects of coenzymes, vitamins, and other minerals involved in melanin production and skin metabolic functions in combination with kojic acid and/or its derivatives. By combining acid and/or its derivative and guanosine 3',5'-cyclic monophosphate and/or its derivative in cosmetics,
It was found that the whitening effect was synergistically improved. The present invention was completed based on this knowledge.

That is, the present invention relates to kojic acid and/or its derivatives and guanosine 3' represented by the following general formula (1).

The present invention provides a whitening cosmetic containing 5'-cyclic monophosphate and/or a derivative thereof. , General formula (1) In the above formula, R□tR2 and R3 are hydrogen, carbon number 2-2
2 acyl group or an alkyl group having 2 to 22 carbon atoms.

X represents hydrogen or a salt-forming cation. In this case, representative examples of the salt-forming cation include sodium, potassium, and the like.

The chemical name of the kojic acid used in the present invention is 5-hydroxy-2-hydroxymethyl-4-pyrone, and it can be used in fermentation extracts produced from microorganisms such as Aspergillus, Penicillium, and Acetobacter. Purified products such as crystals 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. Such derivatives include fatty acid esters having 3 to 22 carbon atoms and aliphatic ethers having 3 to 22 carbon atoms.

Preferred examples include polyoxyalkylene (having 2 to 3 carbon atoms) derivatives.

Guanosine 3',5'-cyclic monophosphate (hereinafter abbreviated as cGMP), which is used in the present invention, exists in small amounts in living organisms and has recently become important as it has the ability to regulate various hormone actions. It is a substance that is becoming recognized. Currently, cGMP and various derivatives produced by fermentation or synthesis methods are commercially available as biochemical reagents.

Examples of the compound represented by the general formula (1) used in the present invention include cGMP, cGMP sodium salt, c
GMP potassium salt, dibutyryl cGMP sodium salt,
Examples include monobutyryl cGMP sodium salt.

In the present invention, the above-mentioned kojic acid and/or its derivative (hereinafter also referred to as kojic acid component) and guanosine 3',
It is essential to contain both 5'-cyclic monophosphate and/or its derivative (hereinafter also referred to as cGMP component).

Regarding the effects of the present invention, the kojic acid component forms a complex with copper ions necessary for tyrosinase activity and suppresses melanin production, while the cGMP component has a fibroblast proliferation promoting effect, etc. Increases metabolism and activates cells. It is thought that these two different effects work together to achieve a remarkable improvement in the whitening effect.

The whitening cosmetics of the present invention include, for example, creams, emulsions, lotions, packs, powders, lip balms, lipsticks, under-make-up, foundations, sun care, and many others.

The amounts of the kojic acid component and cGMP component incorporated into the cosmetic are arbitrarily selected depending on the dosage form, but usually the kojic acid component is 0.01 to 10% by weight and the cGMP component is 0.01 to 10% by weight in the cosmetic. It is preferable to mix it so that it becomes 0.01-15 weight percent. If the amount of each of the two is less than 0.01 weight, 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. and in the case of the cGMP component, it is preferred to use 15% 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 ingredients, the cosmetic of the present invention may contain additive ingredients that are commonly used in cosmetics, such as surfactants.

Oils and fats, alcohols, humectants, thickeners, preservatives, antioxidants, chelating agents, PH adjusters, fragrances, pigments, 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,
Nonions such as sorbitan monooleate, polyethylene glycol monostearate, polyoxyethylene sorbitan monooleate, polyoxyethylene cetyl ether, polyoxyethylene sterol, polyoxyethylene lanolin, polyoxyethylene beeswax, polyoxyethylene hydrogenated castor oil, etc. Surfactant: Anionic surfactant such as sodium stearate, potassium palmitate, sodium cetyl sulfate, sodium lauryl phosphate, triethanolamine palmitate, polyoxyethylene sodium lauryl phosphate, sodium N-acylglutamate; stearyl dimethyl chloride Examples include cationic surfactants such as benzylammonium and stearyltrimethylammonium chloride; 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, and whale oil. 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, and lauryl alcohol; isopropyl myristate, isopropyl palmitate, octyldodecyl myristate, Examples include esters such as octyldedosyl oleate and cholesterol oleate.

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

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

Thickeners include natural polymers such as sodium alginate, xanthan gum, aluminum silicate, quince seed extract, tragacanth gum, and starch; semisynthetic polymers such as methylcellulose, hydroxyethylcellulose, carboxymethylcellulose, soluble starch, and cationized cellulose. Substances: Examples include synthetic polymeric substances such as carboxyvinyl polymers and polyvinyl alcohol.

Preservatives include benzoates, salicylates, sorbates, dehydroacetates, paraoxybenzoic acid esters,
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. Acid, sodium citrate, boric acid, borax, hydrogen phosphate carton 1
1=Rium, etc. can be exemplified.

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, creams, emulsions, lotions, packs, powders,
It can be used in various product forms such as lip balm, lipstick, under makeup, foundation, and sun care.

To give specific examples of the cosmetics of the present invention, for example, as a skin cream: Essential ingredients: 0.02 to 10%.

Oil content: 20-70%, surfactant: 2-7%, humectant:
5-10%.

Purified water: balance, preservative = vol amount, fragrance: composition containing a trace amount, as an emulsion; essential ingredients: 0.02-10
%, oil content: 10 to 40%, surfactant: 1 to brocade, humectant: 5 to 10, purified water: balance, preservative: trace amount, fragrance: composition containing trace amount, as a lotion: Essential component:
0.02-10%, alcohol: 2-50%, surfactant: 0.5-2%, humectant: 2-8%, anti-aggressive agent:
0.01-0.05%, chelating agent: 0.02-0.1
%, pH adjuster: 0.05 to 0.2%, purified water: Balance, preservative: trace amount 1 Pigment: trace amount, fragrance: composition containing trace amount, as a pack; Essential ingredients: 0.02 to 10
%, alcohol: 2-30%, humectant: 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. Can be used.

〔Example〕 Next, the present invention will be explained in more detail with reference to Examples.

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 and weight) of the specimen 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 MED amount of UVB (ultraviolet rays) is irradiated once a day for one week. The specimen was applied once a day after irradiation. Also, the evaluation period is 3 days after the end of the exam.
The suppression rate was calculated based on the number of active melanocytes in the unapplied sample. The number of active melanocytes was measured by exfoliating the epidermis with 2N sodium bromide treatment, staining with Dopa, and counting using a microscope. The results are shown in Table-1.

From the results in Table 1, it can be seen that the products of the present invention containing both a kojic acid component and a cGMP component contain both a kojic acid component and a cGMP component.
It can be seen that the inhibitory effect on active melanocytes is clearly improved compared to those containing each component alone.

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

The test method is as follows.

(1) Sample Contains the whitening ingredients shown in Table 2 and ethanol.

A lotion was prepared, the remainder of which was purified water.

(2) Depigmentation effect test After the backs of colored guinea pigs (3 animals in each group) were shaved, 50μQ of each lotion was applied to approximately 42 areas once a day, 5 times a week for 3 weeks, and the test was completed. The skin color on the fourth day was measured using a color difference meter. The results are shown in Table-2.

From the results in Table 2, the lotion of the present invention containing both a kojic acid component and an eGMP component has a kojic acid component and a cGM component.
It can be seen that the decolorizing effect is superior to lotions containing each P component alone.

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

<Cream> A: Oil phase liquid paraffin (#70) 5.0 weight mesqualane 15. On cetostearyl alcohol 5.0 wax
2. OI glyceryl monostearate 2.0〃POE (20) Sorbitan monolaurate 2.0〃Propyl paraben 0.
1 Tocopherol acetate 0.1 B: Water phase Kojic acid 0.5% by weight dibutyryl cGMP sodium salt 065 Water-soluble collagen 0.2 Methylparaben
0.2〃Purified water Balance C: Fragrance Appropriate amount After mixing and dissolving the above formulations A and B at 70°C,
Add A to B and emulsify uniformly. Further add C and cool.
Prepare the cream.

<Milk> A: Oil phase Liquid paraffin (#70) 10.0 Weight 2 Isopropyl myristate 2.0 Glycerin monostearate 0.5 Stearic acid 2.0 POE (20) Stearyl ether 0.7 〃Glycyrrhetinic acid
0. l〃□ Butylparaben
0.1〃B: Water phase Kojic acid 0.5% by weight Monobutyryl cGMP potassium salt 0.5 n゛Water-soluble elastin Q, l n Triethanolamine 0.5〃Glycerin
2.0 Carbopol 941
Q, i in ethanol
10.0 /J Methylparaben 0.1 Purified water
Balance C: Fragrance Mix and dissolve appropriate amounts of the above formulations A and B at 70°C,
Add A to the mixture and emulsify it uniformly. Further, add C and cool to prepare a milky lotion.

<Lotion> A: Ethyl alcohol phase Ethyl alcohol 10.0% by weight PO
E (80) Hydrogenated castor oil 0.3 Vitamin A O,05II Methylparaben 0.1 Fragrance Appropriate amount B: Water phase Kojic acid 0.1% by weight cGM
P sodium salt 0.1〃Hyaluronic acid 0.1〃Glycerin
3.0 Purified ice balance After uniformly dissolving the above formulation A, gradually add it to the aqueous phase of B while stirring to prepare a lotion.

<Pack agent> A: Ethyl alcohol phase: Ethyl alcohol 10.0% by weight polyvinyl alcohol 15. OII Propylene Glycol 3.0 Methylparaben
0.1 Butylparaben
0.05 n Glycyrrhizic acid 0.
1.B: Aqueous phase sodium kojate 1.0 weight 2 dibutyl cGMP potassium salt 0.3 sodium pyrrolidone carboxylate 1. O POE (15) Oleyl ether 1.0 Purified water
Balance C: Fragrance Appropriate amounts of the above formulations A and B were mixed and heated and mixed uniformly at 70°C. Formulation C is added while cooling to prepare a pack.

Claims (2)

[Claims] (1) Kojic acid and/or its derivatives and the following general formula (
A whitening cosmetic product characterized by containing a guanosine 3',5'-cyclic monophosphate represented by I) and/or a derivative thereof. General formula (I) ▲There are mathematical formulas, chemical formulas, tables, etc.▼ (In the formula, R_1, R_2 and R_3 are hydrogen, carbon numbers 2 to
22 acyl group or an alkyl group having 2 to 22 carbon atoms, and X represents hydrogen or a salt-forming cation) (2) The whitening cosmetic contains 0.01 to 10% by weight of kojic acid and/or its derivatives, and contains guanosine 3',5'-cytosiloxane represented by the above general formula (I). Claim No. 1, wherein the amount of click monophosphate and/or its derivative is 0.01 to 15% by weight.
Whitening cosmetics described in section 1).