JP2594173B2 - External preparation for skin - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Application Field] The present invention has an excellent effect of improving rough skin, moisturizing and glossing the skin, and does not generate papules, facial blisters, blisters, erythema, etc., and is safe. It relates to an excellent external preparation for skin.

[Prior Art] One of the major purposes of skin external preparations such as cosmetics is prevention and improvement of rough skin. In order to achieve this object, various humectants such as glycerin, sorbitol, propylene glycol, and polysaccharide have been conventionally blended.

[Problems to be Solved by the Invention] However, humectants, for example, polysaccharides cause precipitation in a prescription system containing a large amount of alcohol, and glycerin, sorbitol, propylene glycol, chondroitin sulfate, etc. have a sticky or hot feel when mixed in large amounts. In addition, amino acids such as DL-threonine have disadvantages such as coloring and unpleasant odor. Furthermore, it has recently been known that glycerin and propylene glycol, which are the most commonly used moisturizers, cause skin complaints of products such as papules, vesicles, blisters, and erythema when incorporated in large amounts.

In view of the above circumstances, the inventors of the present invention have conducted intensive studies, and as a result, skin external preparations containing erythritol are not only excellent in preventing rough skin and improving, but also found in many polyhydric alcohols such as glycerin and sorbitol. It has been found that the occurrence of stickiness and papules, blisters, blisters, erythema, etc. is small, and that an external preparation for skin containing erythritol and epsilon aminocaproic acid together shows that these effects become stronger, and that the present invention It was completed.

[Means for Solving the Problems] That is, the present invention is a highly safe external skin preparation for improving rough skin, comprising erythritol and epsilon aminocaproic acid as active ingredients.

 Hereinafter, the configuration of the present invention will be described in detail.

Erythritol used in the present invention is also called meso-erythritol, and is a monosaccharide sugar alcohol contained in lichens, basidiomycetes, fruits and the like in the natural world.

The amount of erythritol in the present invention is preferably 0.1 to 30% by weight, more preferably 1 to 2% by weight, in the external preparation for skin.
0% by weight. If it is less than 0.1%, the effect of the present invention is hardly exhibited, and even if it exceeds 30%, the effect cannot be expected to increase.

Epsilon aminocaproic acid used in the present invention is also called epsilon aminocaprolactam and is a kind of epsilon amino acid.

The content of epsilon aminocaproic acid in the present invention is preferably 0.1 to 30% by weight, more preferably 1 to 20% by weight, in the external preparation for skin. If it is less than 0.1%, the effect of the present invention is hardly exhibited, and even if it exceeds 30%, the effect cannot be expected to increase.

Erythritol is effective even when used alone, but a synergistic effect can be expected by combining it with epsilon aminocaproic acid.

The external preparation for the skin of the present invention refers to cosmetics, pharmaceuticals, quasi-drugs, and the like, which are applied to the outer skin. It can take a wide range of forms, such as a gel system, an ointment system, a water-oil two-layer system, and a water-oil-powder three-layer system.

In the skin external preparation of the present invention, usually, in addition to the above essential components,
Other ingredients used in skin external preparations such as cosmetics and pharmaceuticals,
For example, powder components such as titanium dioxide, mica, and talc,
Avocado oil, macadamia nut oil, corn oil, olive oil, rapeseed oil, evening primrose oil, castor oil, sunflower oil, teaseed oil, rice bran oil, jojoba oil, cocoa butter, coconut oil, squalene, squalane, beef tallow, mokurou, beeswax, can Delila wax, carnauba wax, whale wax, lanolin, silicone oil, liquid paraffin, ceresin, petrolatum, oils such as polyoxyethylene (8 mol) oleyl alcohol ether, glyceryl monooleate, caprylic alcohol, lauryl alcohol, myristyl alcohol, cetyl alcohol , Cholesterol, higher alcohols such as phytosterols, capric acid, lauric acid,
Higher fatty acids such as myristic acid, palmitic acid, stearic acid, behenic acid, lanolin fatty acid, linoleic acid, linolenic acid, paraaminobenzoic acid, homomenthyl-7N-acetylarantranilate, butylmethoxybenzoylmethane, and di-paramethoxycinnamic acid UV absorbers such as glyceryl mono-2-ethylhexanoate, amyl salicylate, octyl cinnanate, 2,4-dihydroxybenzophenone, polyethylene glycol, glycerin, sorbitol, xylitol, maltitol, mucopolysaccharide,
Hyaluronic acid, chondroitin sulfate, humectants such as chitosan, methylcellulose, ethylcellulose, gum arabic, polyvinyl alcohol, montmorillonite, thickeners such as laponite, ethanol, organic solvents such as 1,3-butylene glycol, butylhydroxytoluene, tocopherol, Antioxidants such as phytic acid, benzoic acid, salicylic acid, sorbic acid, alkyl esters of parahydroxybenzoic acid (ethylparaben, butylparaben, etc.), antibacterial preservatives such as hexachlorophene, glycine, alanine, valine, leucine, serine, threonine, Amino acids such as phenylalanine, tyrosine, aspartic acid, asparagine, glutamine, taurine, arginine, histidine and the like, and alkali metal salts and hydrochlorides thereof, acyl sarcosine acids (eg, lauroyl) Thin sodium), glutathione, citric acid, malic acid, tartaric acid, organic acids such as lactic acid,
Vitamin A and its derivatives, vitamin B ₆ hydrochloride, vitamin B ₆ tripalmitate, vitamin B ₆ dioctanoate,
Vitamin B ₂ and its derivatives, vitamin B _12, vitamin B ₁₅
And vitamin Cs such as ascorbic acid, ascorbic acid sulfate (salt), ascorbic acid phosphate (salt), ascorbic acid dipalmitate, α-tocopherol, β-tocopherol, γ-tocopherol; Vitamin E such as vitamin E acetate, vitamin E nicotinate, vitamin D,
Vitamins such as vitamin H, pantothenic acid, pantethine, nicotinamide, benzyl nicotinate, γ-oryzanol, allantoin, glycyrrhizic acid (salt), glycyrrhetinic acid and its derivatives, hinokitiol, mucidin, bisabolol, eucalyptol, thymol, Inositol, saponins (saikosaponin, carrot saponin, luffimasaponin, muclodisaponin, etc.), pantothenyl ethyl ether, ethinyl estradiol,
Various drugs such as tranexamic acid, cepharanthin, and placenta extract, Rumex japonicus, Clara, Kouhone, orange,
Sage, yarrow, mallow, senkyu, assembly, thyme, touki, spruce, birch, horsetail, loofah, marronnier, yukinoshita, arnica, lily, mugwort,
Organic solvents such as peonies, aloe, gardenia and sawara,
Natural extracts, pigments, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monosesquioleate, sorbitan trioleate, polyoxyethylene sorbitan monolaurate, polyoxyethylene monostearate Non-ionic surfactants such as sorbitan, polyethylene glycol monooleate, polyoxyethylene alkyl ether, polyglycol diester, lauroyl diethanolamide, fatty acid isopropanol amide, maltitol hydroxy aliphatic ether, alkylated polysaccharide, alkyl glucoside, sugar ester, etc. Cationic surfactants such as stearyltrimethylammonium chloride, benzalkonium chloride, laurylamine oxide; Anionic surfactants such as sodium mitinate, sodium laurate, sodium lauryl nitrate, potassium lauryl nitrate, alkyl triethanolamine ether, funnel oil, linear dodecylbenzene sulfate, polyoxyethylene hydrogenated castor oil, maleic acid, acylmethyl taurine, etc. Surfactants, fragrances,
Purified water or the like can be added. The dosage form of the present invention is optional, for example, a solubilizing system such as cosmetics, an emulsion,
Formulations such as emulsified systems such as creams, foundations, dispersion systems, ointments and the like can be taken.

Erythritol and epsilon aminocaproic acid prevent rough skin, improve rough skin, do not cause erythema, etc.
In order to show that it is excellent in safety, the following measurements of the moisturizing effect by the water evaporation rate, a test of the effect of preventing rough skin against the stimulus of sodium dodecyl sulfate open application, and a practical use test were performed.

(Measurement of Moisturizing Effect by Moisture Evaporation Rate) As a test for measuring the moisturizing effect of the humectant, measurement of the moisture evaporation rate is suitable. That is, after dropping 10 μl of the sample solution onto a 2.0 × 2.0 cm filter paper, the weight loss was measured every minute for 10 minutes, and the weight loss per minute was determined.
The humectant was used as a sample by dissolving the dried residue in water at a rate of 5%. Distilled water was used as a control.

 The determination method is as follows.

-Judgment-◎: Water evaporation rate 0.50μg / min or less ○: Water evaporation rate 0.50 to 0.55μg / min. △: Water evaporation rate 0.55 to 0.60μg / min. ×: Water evaporation rate 0.60μg / min or more Result Are shown in Table 1.

Erythritol and glycerin exhibited strong moisturizing effects.

(Effect of preventing rough skin against irritation of open application of sodium dodecyl sulfate) Next, erythritol, glycerin, and epsilon aminocaproic acid, which have a high moisturizing effect in the above test,
With respect to a mixed sample of erythritol and epsilon aminocaproic acid, the effect of preventing rough skin against irritation caused by sodium dodecyl sulfate open application was tested.

That is, the back skin of a Hartley albino guinea pig is treated with a 3% aqueous solution of sodium dodecyl sulfate,
Skin roughness was produced. Two hours later, 40 μl of each concentration of the sample was open-coated. This was repeated for 5 days, and on the 6th day, the skin roughness was measured visually.

As described above, glycerin and erythritol both have the effect of preventing rough skin. However, when glycerin is used at a high concentration, the glycerin tends to block the skin surface, or tends to enhance the rough skin. This effect is considered to be a cause of skin trouble of the high-concentration glycerin-containing skin external preparation.

On the other hand, erythritol exhibited an effect of preventing rough skin at all concentrations. When epsilon aminocaproic acid was added thereto, the effect became stronger.

[Examples] Next, the present invention will be described in more detail with reference to Examples.
Note that the present invention is not limited to this.

(Actual use test) The effect of improving skin roughness by the actual use test is shown below.

-Test method- The skin surface morphology of a healthy female person (face) was sampled using a replica method with a silicone resin, and a replica of the skin was taken and observed with a microscope (17x). That is, a group of 30 persons (rough panel) whose skin roughness was judged to be 1 or 2 based on the criteria shown in Table 3 based on the state of the skin pattern and the peeling state of the stratum corneum was used. And the lotion of Comparative Example 1 (first group) was applied twice a day. Two weeks later, a replica was again taken to observe the state of the skin, and evaluated in accordance with the criteria shown in Table 3 in the same manner as described above.

Example 1 A lotion having the composition shown in Table 4 was produced by a conventional method.

Comparative Example 1 A lotion having the composition shown in Table 5 was produced by a conventional method.

As is clear from Tables 4 and 5, the skin external preparation of the present invention is a novel skin external preparation having an excellent skin roughness improving effect.

Example 2 Lip treatment A lip treatment was produced according to the following formulation by a conventional method.

Candelilla wax 9.0 Fixed paraffin 8.0 Beeswax 5.0 Carnauba wax 5.0 Lanolin 11.0 Castor oil Residue Erythritol 18.0 Epsilon aminocaproic acid 10.0 Isopropyl myristate 10.0 Perfume Appropriate amount Antioxidant Appropriate amount Example 3 Emulsion An emulsion was prepared by a conventional method according to the following formulation.

Stearic acid 2.0 Cetanol 1.0 Vaseline 3.0 Lanolin alcohol 2.0 Liquid paraffin 8.0 Squalane 2.0 Escalol 507 2.0 Erythritol 5.0 Epsilon aminocaproic acid 3.0 POE (10) monooleate 2.5 Triethanolamine 1.0 Propylene glycol 5.0 Preservatives Appropriate amount Perfume Appropriate amount Purified water Residue Example 4 Nutrition Cream Nourishing cream was produced according to the following formula by a conventional method.

Stearic acid 2.0 stearyl alcohol 7.0 reduced lanolin 2.0 squalane 5.0 octyldodecanol 6.0 maltitol hydroxylauryl ether 3.0 glyceryl monostearate 2.0 preservatives qs perfume qs propylene glycol 5.0 erythritol 1.0 epsilon aminocaproic acid 0.5 purified water residue Example 5 pack In accordance with the standard method.

Kaolin 65.0 Talc 19.0 Propylene glycol 5.0 Calcium acetate 0.01 Urea 0.5 Erythritol 0.5 Epsilon aminocaproic acid 0.1 Fragrance 0.39 Example 6 Lip treatment A lip treatment was produced by a conventional method according to the following formulation.

Candelilla wax 9.0 Fixed paraffin 8.0 Beeswax 5.0 Carnauba wax 5.0 Lanolin 11.0 Castor oil Residue Erythritol 20.0 Epsilon aminocaproic acid 10.0 Isopropyl myristate 10.0 Perfume Appropriate amount Antioxidant Appropriate amount The external preparations of Examples 2 to 6 are effective for preventing rough skin and improving rough skin. It was an excellent topical skin preparation that was excellent and did not generate papules, blisters, blisters, erythema, etc., and was excellent in safety.

[Effects of the Invention] The external preparation for skin of the present invention is an excellent external preparation for skin which is excellent in improving skin roughness, moisturizing and glossing the skin, and not causing papules, face blisters, blisters, erythema and the like. is there.

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Claims (1)

(57) [Claims] 1. A highly safe external preparation for skin roughening, comprising erythritol and epsilon aminocaproic acid as active ingredients.