JP2780805B2 - New skin external preparation composition - Google Patents

Description

Description: FIELD OF THE INVENTION The present invention relates to a novel skin external preparation composition,
The present invention relates to a composition for external use on the skin which has an excellent effect of imparting a moist feeling and a luster to the skin, and has good stability and high safety.

2. Description of the Related Art The stratum corneum that covers the surface of the skin functions as a barrier to prevent the loss of substances necessary for living organisms, including water, and to prevent harmful substances from entering the living tissue from outside the body. It is known to be fulfilled.

Generally, it is said that the water in the stratum corneum is ideally in a state of 10 to 15% and gives the skin a moist feeling and a glossy state. Excessive moisture pushes the structure of the stratum corneum as free water, not only making it brittle, but also giving the skin a greasy and unpleasant feel. Conversely, if the water content is too low, it will become bulky, and in some cases, it will produce chips and cracks.

Conventionally, in order to solve the problem that occurs when the water content of the stratum corneum is too low, skin lotions, creams, emulsions and other skin external preparations include moisturizing agents such as glycerin, propylene glycol, and 1,3-butylene glycol. Polyhydric alcohols are relatively large (5-
10%), and amino acids and their derivatives may be used in hopes of restoring hydration to aged skin.

Furthermore, recently, attention has been paid to collagen and elastin, which are dermis components, and these fibrous proteins obtained from animals are made soluble by chemical or oxygen treatment, or a soluble portion is extracted from these fibrous proteins. Attempts have been made to mix collagen or elastin or a hydrolyzate thereof obtained by such a method as a humectant in an external preparation for skin. Furthermore, blending of proteins such as gelatin, casein, soybean protein, and their hydrolysates has also been proposed as a humectant.

However, among these humectants, skin external preparations containing polyhydric alcohols have a large stickiness to the skin, and when used at low temperatures, water is taken up from the skin in reverse and the skin is dried. There are drawbacks such as getting lost.

In addition, skin external preparations containing amino acids and derivatives thereof have few disadvantages such as those containing polyhydric alcohols that have a large stickiness, but have a disadvantage that deterioration of odor over time is large. On the other hand, skin external preparations containing a protein or a hydrolyzate thereof have the disadvantage that their effects are not sufficient and, therefore, stickiness is unavoidable if the amount is increased.

Problem to be Solved by the Invention The present invention overcomes the drawbacks of such a conventional external preparation for skin containing a moisturizing agent, and has an excellent effect of giving a moist feeling and luster to the skin, and also has stability. The object of the present invention is to provide a good and highly safe skin external preparation composition.

Means for Solving the Problems The present inventors have enthusiastically developed a skin external preparation composition that has good stability and does not give stickiness to the skin and effectively gives the skin a moist feeling and gloss. As a result of repeated studies, a skin external preparation composition comprising at least one selected from amino acids and derivatives thereof, and proteins and hydrolysates thereof, and an ellagic acid compound or an alkali metal salt thereof, It has an excellent effect on the moist feeling and the effect of giving gloss, shows good stability without deterioration of odor, and finds no irritation or sensitization. It was completed.

That is, the present invention relates to (A) at least one selected from amino acids and derivatives thereof, and proteins and hydrolysates thereof; (Wherein R ₁ , R ₂ , R ₃ and R ₄ are a hydrogen atom, an alkyl group having 1 to 20 carbon atoms, a polyoxyethylene or polyoxypropylene residue or a compound represented by the formula Which may be the same or different, and R ₅ is a hydrogen atom, a hydroxyl group or an alkoxy group having 1 to 8 carbon atoms. An object of the present invention is to provide a skin external preparation composition comprising an acid compound and at least one selected from alkali metal salts thereof.

 Hereinafter, the present invention will be described in detail.

In the composition of the present invention, the amino acid used as the component (A) not only constitutes a protein that is a basic component of all cells but also plays an important role in substance metabolism. From a dermatological standpoint, some amino acids are known to have a moisturizing effect as NMF components and are used as cosmetic raw materials. Furthermore, it is widely used as food and medicine. Specific examples of such amino acids include neutral amino acids such as alanine, glycine, serine, cystine, cysteine, tyrosine, threonine, tryptophan, valine, proline, hydroxyproline, phenylalanine, methionine, leucine, isoleucine, aspartic acid, glutamic acid. Acidic amino acids such as, asparagine, glutamine,
Basic amino acids such as histidine and lysine are exemplified.

Examples of amino acid derivatives include, for example, acyl-β
-Alanine and its salts, acyl glutamic acid and its salts, acyl sarcosine and its salts such as acyl salts and glutathione, pyrrolidone carboxylic acid and its salts, in addition to glutatine, carnosine, gramshigin S, tyrosidine A, tyrosidine B, etc. Of oligopeptides.

In the composition of the present invention, the protein also used as the component (A) is a component of every cell, and forms an element essential for contraction movement and an enzyme required for a biological reaction, and has a transport function in blood. Play an important role. On the other hand, from a dermatological standpoint, it is known to have a moisturizing effect, and is used as a raw material for cosmetics. Furthermore, it is indispensable as a raw material for various processed foods. Specific examples of such proteins include soy protein, fish protein, wheat protein, corn protein, casein, gelatin, plasma protein, serum protein, egg white, collagen, elastin, myosin, globulin, lysozyme, fibrinogen,
Gluten, glucagon, glutelin, avidin, histone, chymotrypsinogen, albumin, keratin, succinylated casein and salts thereof.

In addition, protein hydrolyzate is obtained by hydrolyzing protein enzymatically or by acid or alkali treatment, and is known to have a moisturizing effect and adsorptivity to hair, as well as skin cosmetics such as creams and shampoos. It is also used as an external preparation for the skin of the hair, such as a hair rinse and a hair cream. Specifically, the above-mentioned various types such as collagen hydrolyzate and its salt, elastin hydrolyzate and its salt, gelatin hydrolyzate and its salt, soy protein hydrolyzate and its salt, fish protein hydrolyzate and its salt, etc. Examples include protein hydrolysates and salts thereof. Further, acylated or quaternized derivatives of protein hydrolysates such as acylated or quaternized derivatives of collagen hydrolysates can also be used.

In the composition of the present invention, as the component (A), one kind of the above-mentioned amino acids and derivatives thereof may be used, or two or more kinds thereof may be used in combination. May be used alone, or two or more may be used in combination, or one or more amino acids or derivatives thereof may be used in combination with one or more proteins or hydrolysates thereof. The content of the component (A) is usually 0.01 to 20% by weight, preferably 0.05 to 10% by weight, based on the total amount of the composition, although it depends on the product form and the frequency of use.
Is selected in the range.

In the composition of the present invention, as the component (B), at least one selected from the ellagic acid-based compounds represented by the general formula (I) and alkali metal salts thereof is used. Examples of the ellagic acid-based compound include ellagic acid in which R ₁ , R ₂ , R ₃ , R ₄ and R _{5 in the} general formula (I) are all hydrogen atoms, and R ₁ , R ₂ , R ₃ and R ₄ is preferably a hydrogen atom, a methyl group or an ethyl group, and R ₅ is preferably a hydrogen atom, a hydroxyl group or a methoxy group. Examples of the alkali metal salts of these ellagic acid compounds include, for example, sodium salts and potassium salts, and those in which some of the phenolic hydroxyl groups of ellagic acid have become sodium or potassium salts have poor solubility. It is preferable in that it is good.

The ellagic acid-based compound and the alkali metal salt thereof may be used in the preparation of the composition for external preparation for skin to adjust the lipophilicity or hydrophilicity of R ₁ , R ₂ , R ₃ and R in the general formula (I). ₄ is substituted with an arbitrary group selected from a long-chain alkyl group having up to 20 carbon atoms, a polyoxyethylene residue, a polyoxypropylene residue and a sugar residue represented by the formula (II). it may be, for R ₅ may be substituted by long-chain alkoxy group having up to 8 carbon atoms.

Specific examples of the ellagic acid-based compound and an alkali metal salt thereof include ellagic acid, 3,4-di-o-methylellagic acid,
3,3'-di-o-methylellagic acid, 3,3 ', 4-tri-o-
Methylellagic acid, 3,3 ', 4,4'-tetra-o-methyl-
5-methoxyellagic acid, 3-ethyl-4-methyl-5
Examples thereof include hydroxyellagic acid, amritoside, and alkali metal salts of these compounds.

These ellagic acid compounds are eucalyptus wood (Eucalypt
us), poisonous azalea (Koriaria japonica), radiata pine, bearberry, pomegranate, anmarok, ukyuyou, enfuyou, gaijicha, kakojuyou, miko,
Kiki, Kenjin, Kounaka, Sankyukon, Sankyuyou, Shufuboku, Senkusai, Sougenroukansou, Daihyosou, Doumouanyou, Haouben, Banseki Ryukan, Banseki Ryuh, Bossah, Moshoku, Yutaka, Kanto, Kanto, Kanto From natural products such as sokon, bansekiryuuyou, ukyubokumpi, sidokon, chinshuso, gennoshoko,
For example, it can be easily obtained by the method described in JP-B-53-14605.

The ellagic acid compound used in the composition of the present invention is widely present in natural products as described above and is considered to be extremely high in safety. No practical problems were observed in terms of skin irritation, skin sensitization, mutagenicity, etc., and the safety was confirmed to be high.

In the composition of the present invention, the ellagic acid-based compound or an alkali metal salt thereof may be used singly or in combination of two or more. Depending on the total amount of the composition, usually 0.001
-20% by weight, preferably 0.005-5% by weight.

In order to better disperse the ellagic acid compound and the alkali metal salt thereof, the composition of the present invention contains a monosaccharide such as glucose, preferably 0.001 to 30% by weight, more preferably 0.005 to 20% by weight. %, And, if desired, various components commonly used in external preparations for the skin, such as oils, water, surfactants, as well as humectants, lower alcohols, thickeners, and the like. Antioxidants, chelating agents, pH adjusters, preservatives, fragrances, dyes, ultraviolet absorbers, ultraviolet scattering agents, vitamins, and the like can be added.

Examples of the oil component include oils and fats such as olive oil, jojoba oil, cacao butter, camellia oil, palm oil, wood wax, grape seed oil, avocado oil, mink oil, egg yolk oil, and hardened oil, whale wax, beeswax, lanolin , Waxes such as carnauba wax and candelilla wax, liquid paraffin, ceresin, squalane, microcrystalline wax, paraffin wax, hydrocarbons such as petrolatum, stearic acid, oleic acid, lauric acid, myristic acid, isostearic acid, behenic acid, etc. Fatty acids, alcohols such as cetanol, stearyl alcohol, lanolin alcohol, octyldodecanol, hexyldecanol, isopropyl myristate, butyl stearate, isopropyl palmitate, octyldodecyl myristate, octyldode oleate Le, and the like esters such as cholesterol oleate.

Examples of the surfactant include anionic surfactants such as sodium stearate, sodium cetyl sulfate, polyoxyethylene lauryl ether phosphate, sodium lauryl phosphate, triethanol palmitate, sodium N-acylglutamate, and stearyl dimethylbenzyl chloride Ammonium, cationic surfactants such as stearyltrimethylammonium chloride, alkylaminoethylglycine hydrochloride solution, amphoteric surfactants such as lecithin, glyceryl monostearate, sorbitan monostearate, sucrose fatty acid ester, propylene glycol monostearate, Polyoxyethylene oleyl ether, polyethylene glycol monostearate, polyoxyethylene sorbitan monopalmitate, polyoxyethylene coconut fat Monoethanolamide, polyoxyethylene polyoxypropylene glycol, polyoxyethylene castor oil, such as non-ionic surfactants such as polyoxyethylene lanolin.

Examples of the humectant include polyhydric alcohols such as glycerin, 1,3-butylene glycol, propylene glycol, sorbitol, polyethylene glycol, and dipropylene glycol, hyaluronic acid, mucopolysaccharides, and water-soluble polymer substances such as chondroitin sulfate. Examples of the lower alcohol include ethanol and isopropanol, and examples of the thickener include sodium alginate,
Natural polymer substances such as xanthan gum, aluminum silicate, quince seed extract, tragacanth gum, starch, methylcellulose, hydroxyethylcellulose,
Semi-synthetic polymer substances such as carboxymethyl cellulose, soluble starch, and cationized cellulose; and synthetic polymer substances such as carboxyvinyl polymer and polyvinyl alcohol.

Examples of the antioxidant include dibutylhydroxytoluene, butylhydroxyanisole, dl-α-tocopherol, dl-α-tocopherol acetate, propyl gallate, ascorbic acid, and the like.As the chelating agent, for example, disodium edetate , Ethane hydroxy diphosphate, pyrophosphate, hexametaphosphate, citric acid, tartaric acid, gluconic acid, etc., as pH adjusters, for example, sodium hydroxide, triethanolamine,
Citric acid, sodium citrate, boric acid, borax, sodium monohydrogen phosphate, and the like, as preservatives, for example, methyl parahydroxybenzoate, ethyl paraoxybenzoate,
Dehydroacetic acid, salicylic acid, benzoic acid, sorbic acid, benzalkonium chloride and the like.

Further, as an ultraviolet absorber, for example, 2-hydroxy-4-methoxybenzophenone, octyldimethylparaaminobenzoate, ethylhexylparamethoxycinnamate, and the like, and as an ultraviolet scattering agent, for example, titanium oxide, kaolin, talc, and the like, as vitamins Is, for example, vitamin A, vitamin B, vitamin C, vitamin D, vitamin E, vitamin F, vitamin K, vitamin P, vitamin U, carnitine, ferulic acid, γ-oryzanol, α-lipoic acid, orotic acid and derivatives thereof Is mentioned. The optional components are not limited to these.

The composition of the present invention can be prepared by appropriately blending the essential components (A) and (B) with these optional components, for example, creams such as hand cream, nutritional cream, massage cream, lotion, It can be used as various product forms such as lotions, skin milks, emulsions, packs, and solvents.

Specifically, as a lotion, (A)
Component 0.01 to 5% by weight and component (B) 0.01 to 2% by weight, and optionally 2 to 10% by weight of lower alcohol, 0 to 1% by weight of surfactant, 2 to 7% by weight of humectant, pH
A composition containing 0 to 0.2% by weight of an adjusting agent, 77 to 94% by weight of purified water, and trace amounts of a preservative, a pigment, and a fragrance is used as a skin cream, as an essential component, component (A) 0.01 to 5% by weight.
And (B) 0.01 to 2% by weight of an ingredient, and 20 to 70% by weight of an oil component, 1 to 7% by weight of a surfactant, 0.1 to 10% by weight of a humectant, 8 to 73% by weight of purified water, and A composition containing a trace amount of preservatives and fragrances, as a lotion,
It contains 0.01 to 5% by weight of component (A) and 0.01 to 2% by weight of component (B) as essential components, and 5 to 10% by weight of lower alcohol, 0.5 to 2% by weight of surfactant, and humectant 2 as optional components. -8% by weight, 0.01-0.05% by weight of antioxidant, 0.02-0.1% by weight of chelating agent, 0.1-1% by weight of pH adjuster, 77-94% by weight of purified water, and trace amounts of preservatives, pigments and fragrances The composition contains, as skin milk, 0.01 to 5% by weight of component (A) and 0.01 to 2% by weight of component (B) as essential components, and 20 to 40% by weight of oil as an optional component. A composition containing ５5% by weight, purified water 53-78% by weight, and trace amounts of preservatives and fragrances, as an emulsion, essential components (A) are 0.01 to 5% by weight and (B) 0.01 to 5% by weight.
It contains 2% by weight, and oils 10 to 30% by weight, surfactants 1 to 5% by weight, humectants 2 to 10% by weight, purified water 54 to 86% by weight and trace amounts of preservatives and fragrances as optional components. Compositions containing the same.

Effect of the Invention The skin external preparation composition of the present invention contains, as essential components, at least one selected from amino acids and derivatives thereof and proteins and hydrolysates thereof, and an ellagic acid compound or an alkali metal salt thereof. It has an excellent effect of giving a moist feeling and luster to the skin, and is also excellent in safety and stability, as compared with conventional ones.

Therefore, the composition of the present invention is, for example, various cosmetic creams, lotions, lotions, serums, emulsions, packs,
It is suitably used as various product forms such as powder, lip balm, lipstick, under makeup, foundation, sun care, bath salt, body shampoo and body rinse.

EXAMPLES Next, the present invention will be described in more detail with reference to examples, but the present invention is not limited to these examples.

Example 1, Comparative Examples 1 and 2 Emulsions having the compositions shown in Table 1 were prepared, and the moisturizing effect and the effect on the gloss of the skin were evaluated by use tests shown below. That is, the test was carried out by applying a suitable amount of emulsion after washing the face twice a day for 2 weeks twice a day using 15 female panelists in each group (45 in total 3 groups). Table 2 summarizes the results.

As is clear from Table 2, the emulsion containing collagen and ellagic acid (the present invention, Example 1) was compared with the emulsion containing only collagen (Comparative Example 2) or only ellagic acid (Comparative Example 1). Thus, it can be seen that the effect of improving skin moistness and gloss is excellent. During and after use of the emulsion, no skin irritation or allergic reaction was observed, confirming that the safety was extremely high. It was also confirmed that the emulsion had no discoloration over time and had high stability.

Example 2, Comparative Examples 3 and 4 10.0 g of commercially available ellagic acid (manufactured by Tokyo Chemical Industry Co., Ltd.) was added to 200 g of purified water, and the mixture was stirred and dispersed.
Was added and dissolved, and 2.5 g of activated carbon was further added, followed by stirring at room temperature for 30 minutes. Next, the suspension was filtered under reduced pressure to obtain a reddish brown filtrate, and concentrated hydrochloric acid was added dropwise thereto to adjust the pH to 7.0, thereby depositing a precipitate. After centrifugation (8000 rpm, 10 minutes), the precipitate was collected, washed with water and ethanol, and dried to obtain 9.8 g of sodium salt of ellagic acid.

Then, using the thus obtained potassium ellagate (treatment pH 7.0), a cream having the composition shown in Table 3 was prepared (the cream pH was adjusted to 0.5 to 5.5 with citric acid). Then, a use test was performed in the same manner as in Example 1 to evaluate the effect on the moist feeling and the luster of the skin. Also,
At the same time, a storage test at 45 ° C. for one month was performed, and the stability, especially the change in odor, was evaluated according to the following criteria. Table 4 shows the results.

Judgment criteria ◎: No deterioration odor ○: Almost no deterioration odor △: Slightly deterioration odor ×: Remarkable deterioration odor As is clear from the results in Table 4, the cream containing the aspartic acid and potassium ellagate (the present invention, Example 2) contained only aspartic acid (Comparative Example 4) or only potassium ellagate (Comparative Example 3). It can be seen that the moisturizing effect of the skin and the effect of improving the gloss are excellent as compared with the cream containing the same. Further, the odor stability of aspartic acid was significantly improved as compared with the case of using only aspartic acid, and it was confirmed that the cream had high stability.

Example 3 Various skin external preparation compositions of the present invention are shown below.

Essence 1 Sodium salt of ellagic acid (treatment pH 5) 0.5 wt% Elastin 0.1 Isopropyl palmitate 1.0 POE (40) hydrogenated castor oil 1.0 Propylene glycol 5.0 Ethanol 5.0 Xanthan gum 0.2 Disodium edetate 0.05 Fragrance Fine volume Purified water Balance Beauty serum 2 3,4-di-o-methylellagic acid 0.3 wt% sodium piperidone carboxylate 5.0 squalane 1.5 liquid paraffin 1.0 POE (10) octyl phenyl ether 1.0 glycerin 5.0 ethanol 8.0 Carbopol 940 0.2 Perfume Fine amount Purified water Balance Lotion 1 3,3 ', 4-Tri-o-methylellagic acid 0.2 wt% Gelatin 1.5 Propylene glycol 5.0 Ethanol 8.0 Methylparaben 0.1 Sodium citrate 0.02 Ethanehydroxydiphosphate 0.03 Perfume Fine amount Purified water Balance Lotion 2 A. Ethyl alcohol phase Ethyl alcohol 10.0 wt% hexyldecanol 0.5 POE (15) oleyl ether 0.2 dl-α-tocopherol acetate 0.2 methylparaben 0.1 flavor appropriate amount B. aqueous phase potassium ellagic acid salt (treatment pH 7) 0.5 wt% cysteine 2.0 glycerin 5.0 sodium citrate 0.05 purified water Balance The above formulation A was uniformly dissolved, and gradually added to the aqueous phase of B with stirring to prepare a lotion.

Emulsion 1 A. Oil phase Silicone KF56 2.0 wt% Isopropyl myristate 3.0 POE (20) POP (4) Cetyl ether 1.0 Ethyl paraben 0.1 B. Water phase Ellagate sodium salt (treatment pH 6.5) 1.0 wt% Elastin Decomposed product (average molecular weight: 1000) 0.5 Glycerin 3.0 Hibiswako 105 0.2 Ethanol 5.0 Purified water Balance C. Perfume Appropriate amount The above formulations A and B were mixed and dissolved at 70 ° C. respectively, and A was added to B and emulsified uniformly. Add more C, cool,
An emulsion was prepared.

Emulsion 2 Ellagic acid 0.25wt% Glycine 5.0 Stearic acid 1.5 Cetanol 2.0 Vaseline 2.0 Squalane 5.0 Glucose 1.0 Lipophilic glyceryl monostearate 1.0 Glycerin 3.0 Triethanolamine 0.2 Preservatives Fine amount Perfume Fine amount Purified water Balance pack A.Ethyl Alcohol phase Ethyl alcohol 10.0wt% POE (15) stearyl ether 1.0 Ethyl paraben 0.15 Monoammonium glycyrrhizinate 0.05 B. Aqueous phase Elagic acid potassium salt (treatment pH 6) 1.0wt% Collagen hydrolyzate (average molecular weight 1000) 0.5 Polyvinyl Alcohol 15.0 Propylene glycol 3.0 Polyethylene glycol 1500 1.0 Purified water Balance C. Perfume Appropriate amount The above formulations A and B were mixed and uniformly heated and mixed at 70 ° C. With further cooling, C was added to prepare a pack.

Cosmetic cream A. Oil phase Liquid paraffin (# 70) 5.0 wt% Squalane 5.0 Cetostearyl alcohol 5.0 Reduced lanolin 3.0 Beeswax 2.0 Glycerin monostearate 1.5 POE (20) Sorbitan monolaurate 2.0 Pyridoxine dioctanoate 0.02 Propyl Paraben 0.1 B. Aqueous phase Sodium ellagate (treatment pH 6) 0.2 wt% Soluble collagen 1.0 1,3-butylene glycol 5.0 Tetrasodium edetate 0.05 Methylparaben 0.2 Purified water Balance C. Fragrance Minor amount After mixing and dissolving each of them at a temperature of C, A was added to B and emulsified uniformly. Add more C,
Upon cooling, a cream was prepared. Each of the compositions was excellent in the effect of giving a moist feeling and luster to the skin, and was good in both stability and safety.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁶ identification code FI A61K 7/48 A61K 7/48 (58) Fields investigated (Int.Cl. ⁶ , DB name) A61K 7/00-7/50

Claims (1)

(57) [Claims] (1) at least one selected from the group consisting of (A) an amino acid and a derivative thereof, and a protein and a hydrolyzate thereof;
Seed and (B) general formula (Wherein R ₁ , R ₂ , R ₃ and R ₄ are a hydrogen atom, an alkyl group having 1 to 20 carbon atoms, a polyoxyethylene or polyoxypropylene residue or a compound represented by the formula Which may be the same or different, and R ₅ is a hydrogen atom, a hydroxyl group or an alkoxy group having 1 to 8 carbon atoms. A novel skin external preparation composition comprising an acid compound and at least one selected from alkali metal salts thereof.