JPH07215839A - Skin external agent - Google Patents

Abstract

PURPOSE:To obtain a skin external agent having an excellent skin roughness- improving effect and an excellent using touch and high in safety. CONSTITUTION:A skin external agent is compounded with erythritol, tranexamic acid and a skin-covering component. The skin external agent is further compounded with epsilon-aminocaproic acid. The skin external agent contains one or more kinds of fats and oils, a wax, a hydrocarbon or silicone oil, a fatty acid, a higher alcohol, an ester Oil, a gum, a polymer having a mol.wt. of >=3000 and a clay mineral as the skin-covering component.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a skin external preparation, and more particularly to a skin external preparation having a high skin roughening improving effect and a good feeling in use.

[0002]

BACKGROUND OF THE INVENTION A major purpose of external preparations for skin is to maintain a beautiful skin condition. In order to maintain a beautiful skin condition, it is important to prevent and improve skin roughness, smooth the skin's groove and crest, and smooth the turnover of epidermal cells. Creams and emulsions for replenishing the skin have been used, and various moisturizers and agents such as hydrocortisone have been blended.

[0003]

However, moisturizers such as polysaccharides cause precipitation in a formulation system containing a large amount of alcohol, and glycerin, sorbitol, propylene glycol, chondroitin sulfate and the like have a sticky or hot feeling when mixed in a large amount. In addition, amino acids such as DL-threonine have drawbacks such as coloring and odor. Furthermore, it has become known in recent years that glycerin and propylene glycol, which are the most widely used moisturizers, cause papules, pimples, erythema and the like when mixed in large amounts.

Although drugs such as hydrocortisone exert remarkable effects, side effects such as moon face and fragility of bones have been reported, and their use is limited. The present invention has been made in view of the above-mentioned problems of the prior art, and an object thereof is to provide an excellent preparation for preventing rough skin, having an improving effect, and having an excellent feeling in use, and having less skin trouble. To do.

[0005]

Means for Solving the Problems As a result of intensive studies for achieving the above-mentioned object, the present inventors have found that an external preparation for the skin containing erythritol and tranexamic acid and a skin-covering component prevents and improves skin roughness. It was found that not only the effect is excellent, but also the occurrence of sticky feeling, papules, comedones, and erythema, which are found in other polyhydric alcohols such as glycerin and sorbitol, are small. Further, they have found that the combined use of epsilon aminocaproic acid with the above-mentioned external preparation for skin further enhances these effects, and completed the present invention.

That is, the external preparation for skin according to claim 1 of the present invention is characterized in that erythritol and tranexamic acid are mixed with a skin-covering component. The external preparation for skin according to claim 2 of the present invention is characterized in that epsilon aminocaproic acid is added to the external preparation for skin according to claim 1. Furthermore, the external preparation for skin according to claim 3 of the present invention comprises
The external skin preparation according to claim 1 or 2, wherein oils, waxes, hydrocarbon-based or silicone-based oils, fatty acids, higher alcohols, ester oils, gums, polymers having a molecular weight of 3,000 or more or clay are used as skin-covering ingredients. One of the minerals or two or more of them are blended.

The structure of the present invention will be described in detail below. Erythritol used in the present invention is also called meso-erythritol, and is a sugar alcohol of 4 carbon sugars contained in lichens, basidiomycetes, fruits and the like in the natural world. The compounding amount of erythritol in the present invention is 0.1 to 30 in the total amount of the skin external preparation.
Weight% is preferable, and 1 to 20 weight% is more preferable. If it is less than 0.1% by weight, the effect of the present invention is not sufficiently exerted, and if it exceeds 30% by weight, the effect corresponding to the increase of the compounding amount cannot be expected.

The tranexamic acid used in the present invention is represented by the following chemical formula 1.

[Chemical 1] The content of tranexamic acid in the present invention is preferably 0.1 to 15% by weight, more preferably 1 to 10% by weight, based on the total amount of the skin external preparation. If it is less than 0.1% by weight, the effect of the present invention is not sufficiently exhibited, and if it exceeds 15% by weight, skin trouble may occur.

[0009] In the present invention, the skin-covering component may be one that temporarily thickens as a pack specification when it is applied on the skin, but in general, it covers the skin surface in a thin film form, Expected to have the same effect as the above sebum, it prevents the skin from drying due to water evaporation, imparts flexibility and elasticity, and further prevents rough skin and improves the skin. For example,
Fats and oils, waxes, hydrocarbon-based or silicone-based oils, fatty acids, higher alcohols, ester oils, gums, polymers or clay minerals, and the like, specifically, avocado oil, corn oil, olive oil, Rapeseed oil, evening primrose oil, castor oil, sunflower oil, tea seed oil, rice bran oil, jojoba oil, cacao oil, coconut oil, squalene, squalane,
Beef tallow, owl, beeswax, candelilla wax, carnauba wax, whale wax, lanolin, silicone oil, liquid paraffin, ceresin, vaseline, polyoxyethylene (8 mol) oleyl alcohol ether, glyceryl monooleate, etc., capryl alcohol, lauryl Alcohol, higher alcohols such as myristyl alcohol and cetyl alcohol, sterols such as cholesterol and phytosterol, capric acid, lauric acid, myristic acid,
Higher fatty acids such as palmitic acid, stearic acid, behenic acid, lanolin fatty acid, linoleic acid and linolenic acid, polymers having a molecular weight of 3000 or more such as methyl cellulose, ethyl cellulose and polyvinyl alcohol, clay minerals such as montmorillonite and laponite, gum arabic and vigum , Gums such as guar gum, and the like.

In the external preparation for skin of the present invention, the combined use of the above-mentioned erythritol and tranexamic acid and the skin-covering component synergistically improves the rough skin improving effect as compared with the case where they are used alone. Further, in the present invention, by adding epsilon aminocaproic acid to a skin external preparation containing erythritol and tranexamic acid and a skin-covering component, the effect of improving skin roughness is further improved.

The 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 15% by weight, more preferably 1 to 10% by weight, based on the total amount of the skin external preparation. If the amount is less than 0.1% by weight, the effect is not sufficiently increased. If the amount is more than 15% by weight,
It may cause skin troubles and may worsen the skin condition.

The external preparation for skin of the present invention refers to those applied to the outer skin such as cosmetics, pharmaceuticals, quasi drugs, etc., and its dosage form is an aqueous solution type, a solubilizing type, an emulsifying type, a powder type, an oil liquid type. , A gel system, an ointment system, a water-oil two-layer system, a water-oil-powder three-layer system, and the like.

In addition to the above-mentioned essential components, the external preparation for skin of the present invention may contain other components which are usually used in external preparations for skin such as cosmetics and pharmaceuticals within a range that does not impair the effects of the present invention. For example, powder components such as titanium dioxide, mica, talc, para-aminobenzoic acid, homomenthyl-7N-acetylalanthranilate, butylmethoxybenzoylmethane, di-paramethoxycinnamic acid-glyceryl mono-2-ethylhexanoate, amyl salicylate. UV absorbers such as octyl cinnamate and 2,4-dihydroxybenzophenone, moisturizers such as polyethylene glycol, glycerin, sorbitol, xylitol and maltitol, organic solvents such as ethanol and 1,3-butylene glycol, butylhydroxytoluene, Tocopherol,
Antioxidants such as phytic acid, benzoic acid, salicylic acid, sorbic acid, alkyl esters of paraoxybenzoic acid (ethyl paraben, butyl paraben, etc.), antibacterial preservatives such as hexachlorophene, glycine, alanine, valine, leucine, serine, threonine, Amino acids such as phenylalanine, tyrosine, aspartic acid, asparagine, glutamine, taurine, arginine and histidine, and their alkali metal salts and hydrochlorides, acylsarcosine acid (eg sodium lauroylmethylsarcosinate), 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 its derivatives such as vitamin B, ascorbic acid, ascorbic acid sulfate (salt), ascorbic acid phosphate (salt), ascorbic acid dipalmitate and other vitamin Cs, α-tocopherol, β-
Vitamin Es such as tocopherol, γ-tocopherol, vitamin E acetate, vitamin E nicotinate, vitamins D, vitamin H, pantothenic acid, vitamins such as pantethine, nicotinamide, benzyl nicotinate, γ-oryzanol, allantoin, glycyrrhizin Acid (salt), glycyrrhetinic acid and its derivatives, hinokitiol, mucidin, bisabolol, eucalyptol,
Thymol, inositol, saponins (saikosaponin, carrot saponin, hemimasaponin, muclodisaponin, etc.), pantothenyl ethyl ether, ethinyl estradiol, cepharantin, placenta extract, and other drugs, crepe, clara, kohone, orange, sage, sawtooth, Mallow, senkyu, senburi, thyme, touki, spruce, birch, horsetail, loofah, horse chestnut, yukinoshita, arnica, lily, mugwort,
Natural extracts extracted with organic solvents of plants such as peony, aloe, gardenia, and mackerel, alcohol, polyhydric alcohol, water, aqueous alcohol, pigments, sorbitan monolaurate, sorbitan monopalmitate, sorbitan sesquioleate, trioleate Sorbitan, polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan monostearate, polyethylene glycol monooleate, polyoxyethylene alkyl ether, polyglycol diester, lauroyl diethanol amide, fatty acid isopropanol amide, maltitol hydroxy aliphatic ether, alkylation Nonionic surfactants such as polysaccharides, alkyl glucosides, sugar esters, stearyl trimethyl ammonium chloride, benzal chloride Chloride, cationic surfactants such as lauryl amine oxide, sodium palmitate,
Sodium laurate, sodium lauryl sulphate, potassium lauryl sulphate, alkylsulfuric acid triethanolamine ether, funnel oil, linear dodecyl benzene sulphate, polyoxyethylene hydrogenated castor oil maleic acid, anionic surfactants such as acylmethyltaurine, amphoteric surfactant Agent,
Fragrances, purified water and the like can be added.

[0014]

The present invention will be described in more detail with reference to the following examples, but the present invention is not limited thereto.
In addition, the compounding amount is expressed in% by weight unless otherwise specified. [Rough skin improvement test] The back skin of a healthy man was treated with a 3% sodium dodecyl sulfate aqueous solution to prepare rough skin. After 2 hours, 20 μl of each sample was applied in an open manner. This was repeated for 5 days, and on the 6th day, the state of rough skin was visually observed and scored according to the criteria in Table 1. The higher the score, the higher the effect of improving rough skin.

[0015]

[Table 1] ─────────────────────────────────── Scores Standards of scores ───── ────────────────────────────── 1 A wide range of horny layer dryness, swelling, and strong erythema are observed. 2 Dry, swelling and moderate erythema on the stratum corneum. 3 Dryness of the stratum corneum is observed, but no curling is observed. Weak erythema. 4 Dryness and turning of the stratum corneum are not observed, but some erythema is observed. 5 Dryness, swelling and erythema of the stratum corneum are not observed. ───────────────────────────────────

The male panel was made up of 10 persons in each group, and the rough skin improving effect of each sample was judged based on the average value of the scores of 10 persons. Judgment ◎: Average score is 4 or more ○: Average score is 3 or more and less than 4 Δ: Average score is 2 or more and less than 3 ×: Average score is less than 2

[0017]

[Table 2] ──────────────────────────────────── Sample 1 2 3 4 5 6 6 ─── ───────────────────────────────── Erythritol 10% 8 6 4 2 0 Tranexamic acid 0% 2 4 6 8 10 Carboxymethyl cellulose sodium 1% 1 1 1 1 1 1 Hydrogenated lanolin 0.5% 0.5 0.5 0.5 0.5 0.5 Purified water Residue ─────────────────────────── ────────── Evaluation △ ○ ○ ○ ○ × ───────────────────────────────── ───

It can be seen from Table 2 that the skin-roughening ingredient (sodium carboxymethyl cellulose, hydrogenated lanolin) and erythritol or tranexamic acid are not effective in improving rough skin, but the combination of these three improves the rough skin. It is understood that the effect is synergistically increased.

Next, a skin external preparation was prepared according to the formulation shown in Table 3 below, and the same rough skin improvement test as described above was conducted. At the same time, the usability was also investigated. The evaluation criteria for the feeling of use are as follows. ◎: No sticky feeling ○: Almost no sticky feeling △: Slightly sticky ×: Sticky

[0020]

[Table 3] ──────────────────────────────────── Sample 7 8 9 9 10 11 12 12 13 14 ─ ─────────────────────────────────── Glycerin 5 10 20 30 30 − − − − Erythritol − − − − 5 10 20 30 Tranexamic Acid 2 5 10 15 2 5 5 10 15 Veegum 2 2 2 2 2 2 2 2 2 Hydrogenated Olive Oil 1 1 1 1 1 1 1 1 1 POE (20) Glycerin Monooleate 2 2 2 2 2 2 2 2 Talc 2 2 2 2 2 2 2 2 Purified water Residue ──────────────────────────────────── Skin roughening prevention effect △ ○ ◎ ◎ ○ ◎ ◎ ◎ ◎ Usability ◎ ○ △ × ◎ ◎ ◎ ○ ──────────────────────────── ────────

As shown in Table 3, when the conventional moisturizer (glycerin) was used, it had an effect of improving rough skin, but it had a sticky feeling at high concentrations. On the other hand, the system in which erythritol and tranexamic acid were used in combination with the skin-covering component did not have a sticky feeling even at a high concentration and was excellent in the effect of improving rough skin.

[0022]

[Table 4] ──────────────────────────────────── Sample 15 16 16 17 18 19 20 20 ─── ───────────────────────────────── Erythritol 5 5 5 5 3 20 Tranexamic acid 5 5 5 5 5 3 10 Epsilon aminocapron Acid 0 1 3 10 3 10 Veegum 2 2 2 2 2 2 2 Hydrogenated olive oil 1 1 1 1 1 1 POE (20) Glycerin monooleate 2 2 2 2 2 2 2 Talc 2 2 2 2 2 2 Purified water Residual ── ────────────────────────────────── Skin roughening prevention effect ○ ◎ ◎ ◎ ◎ ◎ ◎ ─────── ─────────────────────────────

From Table 4, it is understood that the combined use of epsilon aminocaproic acid and the external preparation for skin containing erythritol and tranexamic acid and the skin-covering component further enhances the rough skin improving effect.

[Actual Use Test by Replica Method] The skin surface morphology of the face of a healthy female panelist is replicated using a silicone resin replica method, and a microscope (1
7 times). Rough skin was evaluated based on the criteria shown in Table 5 from the state of the skin pattern and the peeling state of the stratum corneum, and the panelists judged to have a score of 1 or 2 were set to 20 people per group, and Table 6 is shown on the right half of the face. Lotion of Formulation Example 1 or Formulation 2 of Comparative Example 1 was applied to the left half for 2 days each.
It was applied twice. Two weeks later, a replica was taken again and the skin condition was observed and evaluated in the same manner as above.

[0025]

[Table 5] ─────────────────────────────────── Scores Standards of scores ───── ────────────────────────────── 1 Skin clefts, disappearance of cuticles, and wide skin keratinization 2 skins Grooves and crusts are unclear, and horny layer is turned up. 3 Crusts and crusts are observed, but flat 4 Crusts, crusts are clear 5 Crusts, crusts are clear and regular ──── ───────────────────────────────

In each group, the skin roughening improving effect was determined as follows. Judgment ○: The proportion of panelists who were evaluated as 4 or 5 is 75
% Or more △: The proportion of panelists evaluated as 4 or 5 is 25
% Or more and less than 75% x: The proportion of panelists evaluated as 4 or 5 is 25
The results of less than% are shown in Table 6.

[0027]

[Table 6] ─────────────────────────────────── Component Composition example 1 Composition example 2 Comparative example 1 ─ ────────────────────────────────── Erythritol 1.5 1.0-tranexamic acid 1.5 1.0-epsilon aminocaproic acid-1.0-glycerin − − 3.0 Xanthan gum 0.1 0.1 0.1 Propylene glycol 1.0 1.0 1.0 Citric acid 0.2 0.2 0.2 95% Ethanol 10.0 10.0 10.0 POE (20) lauryl ether 0.5 0.5 0.5 Perfume Adequate amount Adequate amount Purified water Residual residue Residual residue ───────── ────────────────────────── Evaluation ○ ○ △ ──────────────────── ─────────────── As can be seen from Table 6, the external preparation for skin according to the present invention is excellent in improving rough skin. It is a skin external preparation.

When the external preparations for skin of the following formulation examples 3 to 11 were prepared by a conventional method, they all had the effects of preventing and improving skin roughness, and had a good feeling in use, and also had papules, pimples, vesicles and erythema. It was a highly safe external preparation for the skin that did not cause the above.

Formulation 3 Pack Kaolin 67.8 wt% Talc 23.0 Propylene glycol 5.0 Calcium acetate 0.01 Urea 0.5 Erythritol 0.3 Tranexamic acid 0.1 Olive oil 3.0 Fragrance Suitable amount

Formulation Example 4 Nourishing Cream Stearic Acid 2.0 wt% Stearyl Alcohol 7.0 Reduced Lanolin 2.0 Squalane 5.0 Octyldodecanol 6.0 Maltitol Hydroxylauryl Ether 3.0 Glyceryl Monostearate 2.0 Preservative Agent Appropriate amount Perfume Appropriate amount Propylene glycol 5.0 Erythritol 10.0 Tranexamic acid 0.5 Purified water Residual

Formulation Example 5 Lip Treatment Candelilla Wax 9.0 wt% Solid Paraffin 8.0 Beeswax 5.0 Carnauba Wax 5.0 Lanolin 11.0 Castor Oil Residual Erythritol 18.0 Tranexamic Acid 10.0 Isopropyl myristate 10. 0 Fragrance Suitable amount Antioxidant Residual

Formulation 6 Emulsion stearic acid 2.0 wt% Cetanol 1.0 Vaseline 3.0 Lanolin alcohol 2.0 Liquid paraffin 8.0 Squalane 2.0 2-Ethylhexyl paradimethylaminobenzoate 2.0 Erythritol 10.0 Tranexamic acid 0.5 Polyoxyethylene (10) monooleate 2.5 Triethanolamine 1.0 Propylene glycol 5.0 Hyaluronic acid 0.1 Preservatives appropriate amount Perfume appropriate amount Purified water residue

Formulation Example 7 Emulsion stearic acid 2.0 wt% Cetanol 1.0 Vaseline 3.0 Lanolin alcohol 2.0 Liquid paraffin 8.0 Squalane 2.0 Octyl methoxycinnamate 2.0 Erythritol 5.0 Tranexamic acid 2. 0 Epsilon aminocaproic acid 3.0 Polyoxyethylene (10) monooleate 2.5 Triethanolamine 1.0 Propylene glycol 5.0 Sodium chondroitin sulfate 0.05 Preservatives proper amount Perfume proper amount Purified water Residue

Formulation Example 8 Nourishing Cream Stearic Acid 2.0 wt% Stearyl Alcohol 7.0 Reduced Lanolin 2.0 Squalane 5.0 Octyldodecanol 6.0 Maltitol Hydroxylauryl Ether 3.0 Glyceryl Monostearate 2.0 Preservative Agent Amount Perfume Amount Propylene glycol 5.0 Erythritol 1.0 Tranexamic acid 0.5 Epsilon aminocaproic acid 0.3 Purified water Residual

Formulation Example 9 Pack Kaolin 65.0 wt% Talc 19.0 Propylene glycol 5.0 Calcium acetate 0.01 Urea 0.5 Erythritol 0.2 Tranexamic acid 0.3 Epsilon aminocaproic acid 0.3 Perfume Suitable amount

Blending Example 10 Lip Treatment Candelilla Wax 9.0 wt% Solid Paraffin 8.0 Beeswax 5.0 Carnauba Wax 5.0 Lanolin 11.0 Castor Oil Residual Erythritol 20.0 Tranexamic Acid 15.0 Epsilon Aminocaproic Acid 10. 0 Isopropyl myristate 10.0 Fragrance Suitable amount Antioxidant Residual

[0037]

The external preparation for skin of the present invention is an external preparation for skin which is excellent in improving and preventing skin roughness, does not cause papules, blisters, vesicles, erythema, etc. is there.

Claims (3)

[Claims] 1. An external preparation for skin, which comprises erythritol and tranexamic acid and a skin-covering component. 2. The external preparation for skin according to claim 1, further comprising epsilon aminocaproic acid. 3. The external skin preparation according to claim 1 or 2, wherein the skin-covering ingredient is oil, wax, hydrocarbon-based or silicone-based oil, fatty acid, higher alcohol, ester oil, gum, molecular weight of 3000 or more. An external preparation for skin, characterized in that any one kind or two or more kinds of the polymers or the clay minerals mentioned above is blended.