JPH04124118A - Skin external preparation - Google Patents

Abstract

PURPOSE:To obtain a skin external preparation improved in the reduction of skin irritation, having excellent effect capable of providing moisture and gloss to skin with excellent safety and causing no papula, comedo, pustle, erythema, etc., by blending erythritol alone or blending erythritol in combination with epsilon-aminocaproic acid. CONSTITUTION:Erythritol which is a sugar alcohol as a tetrose contained in lichen, Basidiomycetes and fruit, etc., is blended into a skin external preparation at an amount of 0.1-30wt.% preferably 1-20wt.%. As necessary, epsilon-aminocaproic acid is further blended at an amount of 0.1-30wt.%, preferably 1-20wt.%. Increase of a synergistic effect can be expected by combining erythritol with epsilon- aminocaproic acid. The external preparation is applied to outer skin as a cosmetic, medicine, quasi-drug, etc., in a wide agent form of water solution-based, solubilization-based, emulsion-based, powder-based and gel-based agent, etc.

Description

[Detailed Description of the Invention] [Industrial Application Field] The present invention improves rough skin, has an excellent effect of providing moisture and luster to the skin, does not cause papules, acne scars, erythema, etc., and is safe. Concerning excellent external skin preparations.

[Prior Art] One of the major purposes of external skin preparations such as cosmetics is to prevent and improve skin roughness. In order to achieve this purpose, various moisturizing agents such as glycerin, sorbitol, propylene glycol, and polysaccharide have been blended into the composition.

[Problem to be solved by the invention] However, moisturizers, such as polysaccharides, may precipitate if formulated with a high alcohol content, and glycerin, sorbitol, propylene glycol, chondroitin sulfate, etc. may become sticky or give a sticky feeling when added in large amounts. However, amino acids such as DL-threonine have disadvantages such as coloring and odor. In recent years, it has become known that the most commonly used moisturizers, glycerin and propylene glycol, can cause skin complaints such as papules, acne, fading, and erythema when used in large amounts. .

In view of the above circumstances, the present inventors have conducted extensive research and found that a topical skin preparation containing erythritol can prevent rough skin and
We found that erythritol and epsilon aminocaproic acid were not only effective in improving symptoms, but were also less likely to cause the sticky feeling, papules, acne, erythema, etc. seen with other polyhydric alcohols such as glycerin and sorbitol. It was discovered that these effects are even stronger when the external skin preparations are formulated with the above ingredients, and the present invention has been completed.

[Means for Solving the Problems 1] That is, the present invention provides an external skin preparation which is characterized by containing erythritol, and a skin external preparation which is characterized by containing erythritol and epsilon aminocaproic acid. be.

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

Erythritol used in the present invention is also called meso-erythritol, and is a tetramonosaccharide sugar alcohol that is naturally found in lichens, basidiomycetes, fruits, and the like.

The amount of erythritol in the present invention is preferably 0.1 to 30% by weight, more preferably 1% by weight in the skin external preparation.
~20% by weight. If it is less than 0.1%, the effect of the present invention will not be exhibited, and even if it is added in excess of 30%, no increase in the effect can be expected.

Furthermore, epsilon aminocaproic acid used in the present invention is also called epsilon aminocaprolactam, and is a type of epsilon amino acid.

The amount 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 skin preparation. If it is less than 0.1%, the effect of the present invention will not be exhibited, but if it is added in excess of 30%, no increase in the effect can be expected.

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

The skin external preparation of the present invention can be used for cosmetics, pharmaceuticals, quasi-drugs, etc.
This refers to products that are applied to the outer skin, and therefore, its dosage forms include aqueous solutions, solubilized systems, emulsified systems, powder systems, oil liquid systems, gel systems, ointment systems, water-oil two-layer systems, and water-oil-powder systems. It can take a wide range of forms, such as a three-layer system.

In addition to the above-mentioned essential ingredients, the external skin preparation of the present invention may contain other ingredients normally used in external skin preparations such as cosmetics and pharmaceuticals, such as powder components such as titanium dioxide, mica, and talc, avocado oil, and macadamia. Nut oil, corn oil, olive oil, rapeseed oil, evening primrose oil, castor oil, sunflower oil,
Tea seed oil, rice bran oil, jojoba oil, cacao butter, coconut oil, squalene, squalane, beef tallow, Japanese wax, beeswax, cante'lira wax, carnauba wax, spermaceti wax, lanolin,
Oils such as silicone oil, liquid paraffin, ceresin, vaseline, polyoxyethylene (8 mol) oleyl alcohol ether, glyceryl monooleate, caprylic alcohol, lauryl alcohol, myristyl alcohol,
Higher alcohols such as cetyl alcohol, cholesterol, and phytosterols; higher fatty acids such as capric acid, lauric acid, myristic acid, palmitic acid, stearic acid, hebenic acid, lanolin fatty acid, linoleic acid, and lilunic acid;
Para-aminobenzoic acid, homomenthyl-7N-acetyl alanthranilate, butylmethoxybenzoylmethane,
UV absorbers such as di-paramethoxycinnamate-mono-2-ethylhexanoic acid glyceryl, amyl salicylate, octyl cinnamate, 2,4-dihydroxybenzophenone, polyethylene glycol, glycerin, sorbitol, xylitol, maltitol, mucopolysaccharide, hyaluronic acid, Humectants such as chondroitin sulfate and chitosan,
Methylcellulose, ethylcellulose, gum arabic,
Bulking agents such as polyvinyl alcohol, montmorillonite, and laponite, organic solvents such as ethanol, ■,3,-butylene glycol, butylated hydroxytoluene, tocopherol, antioxidants such as phytic acid, benzoic acid, salicylic acid, sorbic acid, and paraoxybenzoic acid. Alkyl esters (ethylparaben, butylparaben, etc.), antibacterial preservatives such as hexachlorophene, glycine, alanine, valine, leucine, serine, threonine, phenylalanine,
Amino acids such as tyrosine, aspartic acid, asparagine, glutamine, taurine, arginine, histidine and their alkali metal salts and hydrochlorides, acylsarcosinates (e.g. sodium lauroylcosinate), glutathione, citric acid, malic acid, tartaric acid, lactic acid, etc. Organic acids, vitamin A and its derivatives, vitamin B6 hydrochloride, vitamin B61-lipalmitate, vitamin B6 dioctanoate, vitamin B2 and its derivatives, vitamin B12, vitamin B10 and its derivatives, ascorbic acid, ascorbic acid sulfate esters (salt), ascorbic acid phosphate ester (salt), vitamin C such as ascorbyl dipalmitate, α-tocopherol, β-
Tocopherol, γ-tocopherol, vitamin E such as vitamin E acetate, vitamin E nicotinate, vitamin D, vitamin H1, pantothenic acid, pantethine and other vitamins, nicotinamide, benzyl nicotinate, γ-oryzanol, allantoin, glycyrrhizinic acid (salt), glycyrrhetinic acid and its derivatives, hinokitiol, mucidin, bisabolol, eucalybutol, thymol, inositol, saponins (saikosaponin,
Various drugs such as carrot saponin, loofah sabonin, mucrodisaponin, etc.), pantothenyl ethyl ether, ethinyl estradiol, tranexamic acid, cephalanthine, placenta extract, Gishigishi, Clara, Kouhone, etc.
Organic solvents, alcohol, such as orange, sage, yarrow, mallow, Japanese stork, Japanese commonweed, thyme, horsetail, spruce, birch, horsetail, loofah, horse chestnut, saxifrage, arnica, lily, mugwort, peony, aloe, gardenia, Spanish mackerel, etc. Natural extracts, pigments extracted with polyhydric alcohol, water, aqueous alcohol, etc., sorbitan monolaurate, sorbitan monopalmidate, sorbitan sesquioleate, sorbitan oleate, polyoxyethylene sorbitan monolaurate, polyoxyethylene monostearate Nonionic surfactants such as sorbitan, polyethylene glycol monooleate, polyoxyethylene alkyl ether, polyglycol diester, lauroyl jetanolamide, fatty acid isopropanolamide, maltitol hydroxy aliphatic ether, alkylated polysaccharide, alkyl glucoside, sugar ester, etc. agents, cationic surfactants such as stearyltrimethylammonium chloride, benzalkonium chloride, laurylamine oxide, sodium palmitate,
Anionic surfactants, amphoteric surfactants such as sodium laurate, sodium lauryl sulfate, potassium lauryl sulfate, alkyl sulfate triethanolamine ether, funnel oil, linear dodecylbenzene sulfate, polyoxyethylene hydrogenated castor oil maleic acid, acylmethyl taurine, etc. ,
Flavors, purified water, etc. can be added. Further, the dosage form of the present invention may be arbitrary, for example, a solubilized system such as a lotion,
Emulsified products such as milky lotions and creams, or foundations,
It can take the form of a dispersion, ointment, etc.

In order to demonstrate that erythritol and epsilon aminocaproic acid have an excellent effect on preventing and improving skin roughness, do not cause erythema, and are highly safe, we measured the moisturizing effect by the rate of water evaporation, and conducted open application of sodium dodecyl sulfate. Tests were conducted on the effect of preventing rough skin against irritation and practical use tests.

(Measurement of moisturizing effect by moisture evaporation rate) As a test for measuring the moisturizing effect of a humectant, measurement of the moisture evaporation rate is suitable. That is, 2. OX2. 1 on Ocm filter paper
After dropping a 0 μm sample solution, the weight decreases by 1 every minute.
The measurement was carried out for 0 minutes, and the weight that decreased per minute was determined. Note that a sample of the humectant was obtained by dissolving the dry residue in water at a ratio of 5%. Distilled water was used as a control.

The determination method is as follows.

Judgment 10: Moisture evaporation rate 0.50 μg/win, below ○: Moisture evaporation rate 0.50 to 0.55 μg/sin.

△: Moisture evaporation rate 0.55-0.60 ug/ai
n.

X: Moisture evaporation rate 0.60 ug/win, the results are shown in Table-1.

Erythritol and glycerin were found to have strong moisturizing effects.

(Skin roughness prevention effect against irritation caused by open application of sodium dodecyl sulfate) Next, we added 7-notol, glycerin, and epsilon aminocaproic acid, which had a high moisturizing effect in the above test.
A mixed sample of erythritol and epsilon aminocaproic acid was tested for its anti-irritation and skin roughening effect due to open application of sodium dodecyl sulfate.

That is, the back skin of Hartley Alpino guinea pig C was treated with a 3% aqueous solution of sodium dodecyl sulfate to create rough skin. After 2 hours, 40 μl of each sample was applied open. This was repeated for 5 days, and the state of rough skin was visually measured on the 68th day.

(Margin below) Rough skin rating - Judgment was made using the average value of 10 animals based on the scores.

-Rough skin determination- 〇: Average score is 4 or more and 5 or less ○: Average score is 3 or more and less than 4 △; Average score is 2 or more and less than 3 ×: Average score is 1 or more and less than 2 The results are shown in Table-2.

Table 2 Effect on preventing rough skin As mentioned above, both glycerin and erythritol have an effect on preventing rough skin, but glycerin is sticky at high concentrations and tends to increase rough skin, perhaps because it blocks the surface of the skin. This effect is thought to be the cause of skin troubles caused by external skin preparations containing high concentrations of glycerin.

On the other hand, erythritol was found to have an anti-skin effect at all concentrations. Furthermore, this effect was strengthened when epsilon aminocaproic acid was added.

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.

(actual use test) The effect of improving rough skin in actual use tests is shown below.

1 Test method 1 A replica of the skin surface of a healthy female person (facial) was taken using a silicone resin replica method and a microscope (1
Observation was made at 7x magnification. In other words, skin roughness rating 1 is based on the criteria shown in Table 3 based on the condition of the skin pattern and the peeling condition of the stratum corneum.
．． The lotions of Prescription Example 1 and Comparative Example 1 were applied to the left and right half of the face of 30 people in one group who were judged to have skin irritation of 2 (rough skin panel).
The lotions (Group 1) and Prescription Example 2 and Comparative Example 1 (Group 2) were applied twice a day. Two weeks later, a replica was taken again and the condition of the skin was observed and evaluated according to the criteria shown in Table 3 as above.

(Margin below) Table-3 Judgment was made using the following criteria based on the scores.

○: The proportion of panels rated as 4 and 5 is 75% or more △: The proportion of panels rated as 4 and 5 is 25% or more and less than 75% ×: The proportion of panels rated as 4 and 5 <25%> Takumi - A lotion having the composition shown in Table 4 was manufactured by a conventional method.

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

Table 5 As is clear from Tables 4 and 5, the skin external preparation of the present invention is a novel skin external preparation excellent in the effect of improving rough skin.

Example 3 Pack A pack was manufactured by a conventional method according to the following recipe.

Kaolin 70.8 Talc 23.0 Propylene Glycol Calcium Acetate Urea Erythritol Flavor 5.0 0.01 0.5 0.3 0.39 Example 4 Nutritional Cream Nourishing was carried out in a conventional manner according to the following formulation.

stearic acid stearyl alcohol reduced lanolin Squalane Octyldodecanol maltitol hydroxylauryl ether glyceryl monostearate Preservative fragrance Propylene glycol manufacture reams 2.0 7.0 2.0 5.0 6.0 3.0 2.0 Appropriate amount Appropriate amount 5.0 erythritol purified water 2.0 remainder Example 5 Lip treat Refill in the usual manner according to the following prescription. manufactured.

candelilla row solid paraffin Beeswax carnauba wax lanolin castor oil erythritol Epsilon aminocabronic acid isopropyl myristate fragrance Antioxidant ment top treatment 9.0 8.0 5.0 5.0 11.0 remainder 18.0 10.0 10.0 Appropriate amount Appropriate amount Example 6 Emulsion A milky lotion was prepared by a conventional method according to the following recipe.

stearic acid Setanol Vaseline lanolin alcohol liquid paraffin Squalane S-power roll 507 erythritol POE (10) monooleate triethanolamine Propylene glycol Preservative fragrance purified water 2.0 1.0 3.0 2.0 8.0 2.0 2.0 10.0 2.5 1.0 5.0 Appropriate amount Appropriate amount remainder Example 7 Emulsion Follow the following recipe and use the usual method. stearic acid Setanol Vaseline A milky lotion was produced.

2.0 1.0 3.0 lanolin alcohol liquid paraffin Squalane S-power roll 507 erythritol POE (10) monooleate triethanolamine Propylene glycol Preservative fragrance purified water 2.0 8.0 2.0 2.0 25.0 2.5 1.0 5.0 Appropriate amount Appropriate amount remainder Example 8 Emulsion Follow the following recipe and use the usual method. stearic acid Setanol Vaseline lanolin alcohol liquid paraffin Squalane A milky lotion was produced.

2.0 1.0 3.0 2.0 8.0 2.0 S-power roll 507 erythritol Ibsilone aminocabronic acid POE (10) monooleate triethanolamine Propylene glycol Preservative fragrance purified water 2.0 5.0 3.0 2.5 1.0 5.0 Appropriate amount Appropriate amount remainder Example 9 Nutritional cream A nutritional cream was produced by a conventional method according to the following recipe.

Stearic acid 2.0 Stearyl alcohol 7.0 Reduced lanolin 2.0 Squalane
5.0 octyldodecanol
6.0 Maltitol hydroxylauryl 3.0 Ether glyceryl monostearate 2.0 Preservatives Appropriate amount Fragrance
Appropriate amount of propylene glycol 5.0 erythritol
1.0 epsilon aminocaproic acid 0.5 purified water
Remaining Example 10 Bag A bag was manufactured by a conventional method according to the following recipe.

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

Candelilla wax 9.0 Solid paraffin 8.0 Beeswax
5.0 carnauba wax
5.0 lanolin
11. O castor oil
residual erythritol
20.0 Epsilon Amino Caprone *
10.0 Isopropyl myristate 10.0 Fragrance Appropriate amount Antioxidant Appropriate amount The skin external preparations of Examples 3 to 11 have excellent effects on preventing and improving rough skin, and are effective against papules,
It was a highly safe topical skin preparation that did not cause skin irritation, red spots, or erythema.

[Effects of the Invention] The external skin preparation of the present invention is a highly safe external skin preparation that improves rough skin, provides moisture and luster to the skin, and does not cause papules, superficial layers, thickening, or erythema. be.

Claims (2)

[Claims] (1) A skin external preparation characterized by containing erythritol. (2) A skin external preparation characterized by containing erythritol and epsilon aminocaproic acid.