JPH04270212A - Skin external agent - Google Patents

Abstract

PURPOSE:To provide a skin external agent preventing the dryness of skin and having a good skin-stimulating action. CONSTITUTION:A skin external agent contains L-arginine-L-asparaginic acid salt, DL-alpha-tocopherol-L-ascorbic acid phosphoric acid diester and/or a salt thereof and a pharmacologically acceptable carrier.

Description

[Detailed description of the invention]

0001

[Industrial Application Field] The present invention provides an external skin preparation for preventing skin dryness, which contains L-arginine-L-aspartate and DL-α-tocopherol-L-ascorbic acid phosphate diester and/or its salt. Regarding.

0002

[Prior Art] Conventionally, there have been products that contain various moisturizing agents to prevent skin dryness, and products that contain various vitamins and biological extracts to revitalize aging skin. Nothing that combines these effects has yet been developed.

0003

SUMMARY OF THE INVENTION Accordingly, an object of the present invention is to provide an external preparation for skin that has the effect of preventing skin dryness and revitalizing the skin. Other objects and features of the present invention will be apparent from the following description.

0004

[Means for Solving the Problems] According to the present invention, L-arginine-L-aspartate, DL-α-tocopherol-L-ascorbic acid phosphodiester and/or
or a salt thereof, and a pharmacologically harmless carrier.

[0005] As a result of intensive research into whether there is anything that can prevent skin dryness, the present inventors found that L-arginine-L-aspartate and DL-α-tocopherol-L-ascorbic acid phosphate diester (hereinafter referred to as EPC) The present inventors have discovered that a combination with EPC salt (abbreviated as EPC salt) and/or its salt (hereinafter abbreviated as EPC salt) has the effect of preventing drying, and has completed the present invention.

L-arginine-L- used in the present invention
Aspartate is a 1:1 salt of L-arginine biosynthesized by chemical synthesis or microorganisms, and L-aspartic acid synthesized in the same way. L- used in the present invention
The amount of arginine-L-aspartate is 0.0001 to 10% by weight, preferably 0.0% by weight based on the total amount of the skin external preparation.
1 to 1% by weight is desirable.

EPC or EPC salt used in the present invention contains vitamin E (DL-α-tocopherol) and vitamin C.
(L-ascorbic acid) is ester-bonded with phosphoric acid. The amount of EPC or EPC salt used in the present invention is 0.0001 to 10% by weight in the amount of the external skin preparation.
It is preferably 0.01 to 1% by weight.

[0008] As a pharmacologically harmless carrier to be incorporated into the external skin preparation of the present invention, any carrier commonly used in external skin preparations can be used. For example, the carrier may include water, lower alcohols, higher alcohols, etc. , polyhydric alcohols, monosaccharides,
Disaccharides, polysaccharides, hydrocarbon oils, fats and oils, waxes, fatty acids, silicone oils, nonionic surfactants, ionic surfactants, silicone surfactants, polymer compounds, and any of the above. Examples include selected aqueous mixtures and emulsified mixtures.

[0009] The external skin preparation of the present invention may optionally contain various ingredients commonly used in cosmetics, pharmaceuticals, etc., such as vitamin oil, retinol, and retinol acetate, to the extent that the effects of the present invention are not impaired. Type A, riboflavin, riboflavin butyrate, vitamin B2 such as flavin adenine dinucleotide, pyridoxine hydrochloride,
Vitamin B6 such as pyridoxine dioctanoate,
Vitamin C such as L-ascorbic acid, L-ascorbyl dipalmitate, sodium L-ascorbic acid 2-sulfate, L-ascorbic acid phosphate, calcium pantothenate, D-pantothenyl alcohol, pantothenyl ethyl Ether, pantothenic acids such as acetyl pantothenyl ethyl ether, vitamin Ds such as ergocalciphenol and cholecalciferol, nicotinic acids such as nicotinic acid, nicotinamide, and benzyl nicotinate, α-tocopherol, tocopherol acetate, nicotinic acid DL -α-tocopherol, succinic acid D
Vitamin E such as L-α-tocopherol, vitamin P
, vitamins such as biotin, avocado oil, palm oil, peanut oil, beef tallow, rice bran oil, jojoba oil, evening primrose oil,
Carnauba wax, lanolin, liquid paraffin, squalane, isostearyl palmitate, isostearyl alcohol, oils such as glycerin tri-2-ethylhexanoate, glycerin, sorbitol, polyethylene glycol, 1,3-butylene glycol, collagen, hyaluronic acid, chondroitin Moisturizing agents such as sulfuric acid, sodium dextran sulfate, amyl paradimethylaminobenzoate, octyl methoxycinnamate, 4-tert-butyl-4-
Methoxy-dibenzoylmethane, diparamethoxycinnamate mono-2-ethylhexanoic acid glyceryl, 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-
Ultraviolet absorbers such as sodium 4-methoxybenzophenone-5-sulfonate, urocanic acid, ethyl diisopropylcinnamate, sodium erythorbate, antioxidants such as parahydroxyanisole, sodium stearyl sulfate, diethanolamine cetyl sulfate, cetyl trimethylammonium saccharin. , polyethylene glycol isostearate, polyoxyethylene octyldodecyl alcohol, sorbitan monoisostearate, polyoxyethylene hydrogenated castor oil, glyceryl arachiate, diglycerine diisostearate, phospholipids and other surfactants, methyl paraoxybenzoate, Preservatives such as ethyl paraoxybenzoate and butyl paraoxybenzoate, anti-inflammatory agents such as glycyrrhizic acid derivatives, glycyrrhetinic acid derivatives, salicylic acid derivatives, hinokitiol, zinc oxide, and allantoin, whitening agents such as placenta extract, glutathione, saxifrage extract, Extraction of oilseed buttercup, orensis, citrus, peony, Japanese japonica, birch, sage, loquat, carrot, aloe, mallow, iris, grape, saffron, loofah, lily, saffron, nebula, ginger, hypericum, hypericum, rosemary, garlic, etc. royal jelly, photosensitizers, cholesterol derivatives, activators such as calf blood extract, blood circulation promoters such as γ-oryzanol, antiseborrheic agents such as sulfur and thianthol, carboxyvinyl polymer, carboxymethylcellulose, carboxyhydroxypropylcellulose Thickeners, fragrances, water, etc.
Colorants such as alcohol, titanium yellow, cursamine, and safflower red, resin powders such as polyethylene and nylon, etc. can be appropriately blended as needed.

[0010] The external preparation for skin of the present invention may be in any form; for example, it may be in the form of an oily preparation, a solubilized lotion, an emulsion such as a milky lotion, a cream, an ointment, a dispersion powder product, or the like. be able to.

[0011] There is no particular limit to the amount of the skin external preparation of the present invention applied, but preferably 1.5 to 1.5 to 1.5 per application for lotions.
Apply 2 ml twice a day, 1 to 1.5 ml for emulsions, and approximately 0.2 g for creams.

0012

EXAMPLES Next, the present invention will be explained in more detail with reference to Examples. Note that the present invention is not limited to this. The blending amount is in weight%.

Example 1: Lotion (1) L-arginine-L-aspartate 5.
0 (2) DL-α-tocopherol-
L-ascorbic acid phosphoric acid diester dipotassium salt 5.0 (3
) tocopherol acetate

0.01 (4) Glycerin

4.0 (
5) 1,3-butylene glycol
4
．． 0 (6) Ethanol

7.0 (7)
Polyoxyethylene (50 moles) oleyl alcohol ether 0.5 (8) Methyl paraben
0.2
(9) Citric acid

0.05 (10) Sodium citrate
0.
1 (11) Flavoring

0.05 (12
) purified water

remainder

(Production method) Citric acid, sodium citrate, glycerin, 1,3-butylene glycol, L-arginine-L-aspartate, and DL-α-tocopherol-L-ascorbic acid phosphate diester dipotassium salt in purified water. was dissolved. Separately, polyoxyethylene oleyl alcohol ether, tocopherol acetate, fragrance, and methylparaben were dissolved in ethanol, and this was added to the above-mentioned purified aqueous solution to solubilize and filtered to obtain a lotion.

Example 2: Cream (1) Cetostearyl alcohol

3.5 (2) Squalane

40.0
(3) Beeswax

3.0 (4) Reduced lanolin
5
．． 0 (5) Ethylparaben

0.3 (6) Polyoxyethylene (20 mol) Sorbitan monopalmitate ester
2.0 (7)
Storic acid monoglyceride
2.0
(8) Sodium N-stearoylglutamate 0.5
(9) 2-hydroxy-4-methoxybenzophenone 1.0
(10) Retinol acetate

2.0 (11) Evening primrose oil

0
．． 05 (12) Fragrance

0.03 (1
3) L-arginine-L-aspartate
0.01
(14) DL-α-tocopherol-
L-ascorbic acid phosphoric acid diester dipotassium salt 1.0 (15) 1
,3-butylene glycol
5.0
(16) Polyethylene glycol 1500

5.0 (17) Purified water

remainder

00
16] (Production method) Ingredients (1) (2) (3) (4) (5) (
6)(7)(8)(9)(10)(11)(12) were dissolved by heating and heated to 75°C to obtain components (13)(14)(
15) Added to (16) and (17) with stirring. After processing with a homomixer to make emulsified particles fine, the mixture was rapidly cooled while stirring to obtain cream.

Example 3: Emulsion (1) Stearic acid

1.5 (2) Cetyl alcohol
0.5
(3) Beeswax

2.0 (4)
Polyoxyethylene (10 mol) monooleate ester 1.0 (5) Octyl methoxycinnamate
2.0 (
6) DL-α-tocopherol-
L-ascorbic acid phosphoric acid diester dipotassium salt 0.2 (7) L-arginine-L-aspartate
1.0 (8) Sodium hyaluronate
0.1
(9) Triethanolamine

0.75 (10) Glycerin

7.0
(11) Ethanol

3.0 (12) Ethylparaben
0
．． 3 (13) Flavorings

0.03 (1
4) Purified water

remainder

(Production method) A fragrance was added and dissolved in ethanol (alcohol phase). Glycerin, triethanolamine, sodium hyaluronate, DL-α-tocopherol-L-ascorbic acid phosphoric acid diester dipotassium salt, L-arginine-L in purified water
- Aspartate was added, dissolved and kept at 70°C (aqueous phase). The other ingredients were mixed and heated to melt and kept at 70°C (
oil phase). Preliminary emulsification was performed by adding the oil phase to the water phase, and the mixture was uniformly emulsified using a homomixer. Add the alcohol phase to this while stirring. Thereafter, the mixture was cooled to 30° C. while stirring to obtain a milky lotion.

Example 4: Foam Mask (1) L-Arginine-L-Aspartate 0.
5 (2) DL-α-tocopherol-
L-ascorbic acid phosphoric acid diester disodium salt 0.01 (3)
1,3-butylene glycol
5.0
(4) Glycerin

7.0 (5) Methylparaben

0.1 (6) Potassium hydroxide

0.15 (7)
stearic acid

0.5 (8) Myristic acid

1.0 (9
) batyl alcohol

1.5 (10) Polyoxyethylene (
60 mole) hydrogenated castor oil
3.0 (11) Flavorings

0.0
5 (12) Liquefied petroleum gas

6.0 (13) Dimethyl ether
3.
0 (14) Purified water

remainder

(Production method) Ingredients (1) (2) (3) (4) (5) are added to component (14).
)(6), heat and melt at 70℃, and add the ingredients (6) into it.
A solution obtained by heating and dissolving 7)(8)(9)(10)(11) at 75°C was added, stirred thoroughly, and then cooled. This was filled into a container, and finally components (12) and (13) were filled as a propellant to obtain a foam mask.

Example 5: Ointment (1) L-arginine-L-aspartate 0.
5 (2) DL-α-tocopherol-
L-ascorbic acid phosphoric acid diester dipotassium salt 0.5 (3
) tocopherol acetate

1.0 (4) Retinol palmitate
0.5 (5) Stearyl alcohol
18.0
(6) Mokuro

20.0 (7) Polyoxyethylene (20 mol) monooleate 0.25 (8) Glycerin monostearate
0.3 (9) Vaseline

40.0 (10) Purified water

remainder

002
2] (Production method) Add L-arginine-L-aspartate and DL-α-tocopherol-L-ascorbic acid phosphoric acid diester dipotassium salt to purified water and dissolve at 70°C.
(aqueous phase). The remaining components were mixed and dissolved at 70°C (oil phase). The oil phase was added to the water phase, uniformly emulsified using a homomixer, and then cooled to obtain an ointment.

Evaluation Example 1 The moisturizing ability of L-arginine-L-aspartate and EPC was evaluated by calculating the water evaporation rate constant. That is, a 10% aqueous solution of L-arginine-L-aspartate or EPC and a 1:1 mixture thereof were dropped onto a filter paper, and the weight change was measured over time using a precision balance and a personal computer. The water evaporation rate constant was calculated. The results are shown in Table 1. The smaller this value is, the more difficult it is for water to evaporate and the more effective the moisturizing effect is.

[0024]

[Table 1]

[0025] From the above results, it was found that L-arginine-L-aspartate and EPC have a moisturizing ability, and that when they are combined, the moisturizing effect is further enhanced.

Evaluation Example 2 A three-week test was conducted using the cream formulation of Example 2 on women with dry skin. Then, the moisturizing effect of L-arginine-L-aspartate and EPC on the skin was evaluated using the amount of water in the stratum corneum of the skin before and after continuous use as an index of electrical conductivity. The results are shown in Table 2. As shown in Table 2, the higher the electrical conductivity, the greater the amount of water in the stratum corneum.

[0027]

[Table 2]

From the above results, it was confirmed that L-arginine-L-aspartate and EPC have a high moisturizing effect on the skin even in the product system.

Claims (3)

[Claims] Claim 1: Skin comprising L-arginine-L-aspartate, DL-α-tocopherol-L-ascorbic acid phosphodiester and/or its salt, and a pharmacologically harmless carrier. Topical preparation. Claim 2: Claim 1, wherein the content of L-arginine-L-aspartate is 0.0001 to 10% by weight.
External skin preparations listed. 3. The skin external preparation according to claim 1, wherein the content of DL-α-tocopherol-L-ascorbic acid phosphodiester and/or its salt is 0.0001 to 10% by weight.