JP4425554B2 - Topical skin preparation - Google Patents

Description

【００２３】
実験例２ 使用試験
実施例１のクリーム及び比較例１の従来のクリームを用いて、肌あれに悩む女性各３０人（２０〜５０才）を対象に１ヶ月間の使用試験を行った。使用後、肌あれ改善についてのアンケート調査を行って、肌あれ改善効果を判定した。アンケートの評価基準は、有効なものを「優」、やや有効なものを「良」、わずかに有効なものを「可」、無効なものを「不可」として評価した。
【００２４】
これらの結果を表２に示した。実施例１のクリームは優れた肌あれ改善効果を示した。なお、試験期間中皮膚トラブルは一人もなく、安全性においても問題なかった。
【００２５】
【表２】

【００２６】
実施例２の化粧水、実施例３の乳液、実施例４の軟膏、実施例５のファンデーション及び実施例６の浴用剤の使用試験を実験例と同様に行ったところ、いずれも安全で優れた肌あれ改善効果を示した。
【００２７】
以上のことから、本発明の塩化カルシウム及び塩化マグネシウムにカリウムミョウバンを加えることにより、ケラチンのＳＳ結合強化効果を示し、角質層バリア機能改善効果を認めた。塩化カルシウム、塩化マグネシウム及びカリウムミョウバンを含有することを特徴とする肌あれ改善皮膚外用剤は安全で優れた皮膚の肌あれ改善作用を示した。[0001]
[Field of Invention]
The present invention relates to a skin external preparation having an excellent skin roughness improving action.
[0002]
[Prior art]
As a cause of skin roughness, deterioration of the barrier function in the stratum corneum is considered, and restoration of the barrier function in the stratum corneum has been one of the themes of the development of an external preparation for improving skin roughness.
The barrier function in the stratum corneum is retained by keratin SS bonds. Therefore, it is generally said that this bond is disturbed and free SH groups are increased as an indicator of deterioration of the barrier function in the stratum corneum (see Non-Patent Document 1). Accordingly, various components that enhance SS bonding have been developed as an external preparation for skin that improves skin roughness.
As components having an effect of improving skin roughness, calcium salts, magnesium salts and potassium salts shown in Patent Document 1 and Non-Patent Document 2 are known. On the other hand, as shown in Non-Patent Document 3, alum is also known to have a rough skin improving effect.
[0003]
[Patent Document 1]
Japanese Patent Laid-Open No. 2001-226248 [Non-Patent Document 1]
Akira Kiyoji, “Skin Biochemistry”, Kanehara Publishing Co., 1966, 68-71
[Non-Patent Document 2]
Mitshiro Hiro Denda. , Arch Dermatol Res. 1999, 89, 560-563.
[Non-Patent Document 3]
Ueda, Norihiko, “Why hot springs are good for the body”, Kodansha Co., Ltd., 1991, 39
[0004]
[Problems to be solved by the invention]
There are various indicators concerning the deterioration of the barrier function in the stratum corneum, and it is not efficient to develop a component that acts or suppresses each of them. Since the barrier in the stratum corneum is retained by the SS bond of keratin, it is considered that strengthening the SS bond of keratin restores the barrier function in the stratum corneum and leads to an excellent skin roughness improving effect.
[0005]
[Means for Solving the Problems]
Under these circumstances, the present inventors have conducted intensive research. As a result, the addition of potassium alum to calcium chloride and magnesium chloride further strengthens the SS bond of keratin and restores the barrier function in the stratum corneum. As a result, the present invention has been completed.
[0006]
That is, the present invention is a skin external preparation for improving skin roughness characterized by containing potassium alum, calcium chloride, and magnesium chloride .
[0007]
The above-mentioned compounds and / or plant extracts may be used as they are in the skin external preparation for improving skin roughness of the present invention, and the fats and waxes that are components used in ordinary external preparations within the range not impairing the effects. Ingredients, hydrocarbons, fatty acids, alcohols, esters, surfactants, metal soaps, pH adjusters, chelating agents, and the like can also be blended.
[0008]
The total amount of calcium chloride, magnesium chloride and potassium alum used in the present invention is preferably 0.0001 to 10% by weight. If it is less than 0.0001%, a sufficient effect is hardly exhibited. When the blending amount exceeds 10% by weight, the effect is hardly increased and it is uneconomical. In addition, the addition method may be added in advance or during the production, and may be appropriately selected in consideration of workability.
[0009]
The blending weight ratio of potassium alum, calcium chloride and magnesium chloride is preferably 0.1 to 1000 times that of potassium alum relative to the total of calcium chloride and magnesium chloride . Among these, 1 to 10 times is more preferable. Adding more potassium alum is less economical and less expensive. The blending ratio of calcium chloride and magnesium chloride is preferably 10: 1 to 1:10.
[0010]
Next, in order to explain the present invention in detail, formulation examples and experimental examples of calcium chloride, magnesium chloride, and potassium alum used in the present invention are given as examples, but the present invention is not limited thereto. The compounding amount shown in the examples indicates% by weight.
[0011]
Example 1 Cream formulation Formulation amount (% by weight)
1. Calcium chloride 0.005
2. Magnesium chloride 0.005
3. Potassium alum 0.05
4). Squalane 5.5
5). Olive oil 3.0
6). Stearic acid 2.0
7). Beeswax 2.0
8). Octyldodecyl myristate 3.5
9. Polyoxyethylene cetyl ether (20E.O.) 3.0
10. Behenyl alcohol 1.5
11. Glycerol monostearate2.5
12 Fragrance 0.1
13.1,3-Butylene glycol 8.5
14 Ethyl paraoxybenzoate 0.05
15. Methyl paraoxybenzoate 0.2
16. Purified water 68.09
“Manufacturing method” Components 4 to 11 are heated and mixed, and kept at 70 ° C. to obtain an oil phase. Ingredients 1 to 3 and 13 to 16 are dissolved by heating and mixed, and kept at 75 ° C. to obtain an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring.
[0012]
Comparative Example 1 Conventional Cream In Example 1, a conventional cream was obtained by replacing potassium alum with purified water.
[0013]
Example 2 skin lotion formulation amount (% by weight)
1. Calcium chloride 0.001
2. Magnesium chloride 0.002
3. Potassium alum 0.02
4.1,3-Butylene glycol 8.0
5). Glycerin 2.0
6). Xanthan gum 0.02
7). Citric acid 0.01
8). Sodium citrate 0.1
9. Ethanol 5.0
10. Methyl paraoxybenzoate 0.1
11. Polyoxyethylene hydrogenated castor oil (40E.O.) 0.1
12 Fragrance 0.1
13. Purified water 84.547
[Manufacturing method] Components 1 to 8 and 13 and components 9 to 12 are uniformly dissolved, and both are mixed and filtered to obtain a product.
[0014]
Example 3 Emulsion Formulation Formulation Amount (% by weight)
1. Calcium chloride 0.001
2. Magnesium chloride 0.005
3. Potassium alum 0.001
4). Squalane 5.0
5). Olive oil 5.0
6). Jojoba oil 5.0
7). Cetanol 1.5
8). Glycerol monostearate 2.0
9. Polyoxyethylene cetyl ether (20E.O.) 3.0
10. Polyoxyethylene sorbitan monooleate 2.0
11. Fragrance 0.1
12 Propylene glycol 1.0
13. Glycerin 2.0
14 Methyl paraoxybenzoate 0.2
15. Purified water 73.193
[Manufacturing method] Components 4 to 10 are heated and dissolved, mixed, and kept at 70 ° C to obtain an oil phase. Ingredients 1 to 3 and 12 to 15 are dissolved by heating and mixed, and kept at 75 ° C. to obtain an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring. The component 11 is added at 45 ° C., and further cooled to 30 ° C. to obtain a product.
[0015]
Example 4 Ointment Formulation Amount (% by weight)
1. Calcium chloride 0.002
2. Magnesium chloride 0.002
3. Potassium alum 0.002
4). Polyoxyethylene cetyl ether (30E.O.) 2.0
5). Glycerol monostearate 10.0
6). Liquid paraffin 5.0
7). Cetanol 6.0
8). Methyl paraoxybenzoate 0.1
9. Propylene glycol 10.0
10. Purified water 66.894
[Manufacturing method] Ingredients 4 to 7 are dissolved by heating and mixed, and kept at 70 ° C to obtain an oil phase. Ingredients 1 to 3 and 8 to 10 are dissolved by heating and mixed, and kept at 75 ° C. to obtain an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled to 30 ° C. with stirring to obtain a product.
[0016]
Example 5 Foundation Formulation Amount (% by weight)
1. Calcium chloride 0.005
2. Magnesium chloride 0.001
3. Potassium alum 0.01
4). Stearic acid 2.4
5). Polyoxyethylene sorbitan monostearate 1.0
(20 EO)
6). Polyoxyethylene cetyl ether (20E.O.) 2.0
7). Cetanol 1.0
8). Liquid lanolin 2.0
9. Liquid paraffin 3.0
10. Isopropyl myristate 6.5
11. Butyl paraoxybenzoate 0.1
12 Sodium carboxymethylcellulose 0.1
13. Bentonite 0.5
14 Propylene glycol 4.0
15. Triethanolamine 1.1
16. Methyl paraoxybenzoate 0.2
17. Titanium dioxide 8.0
18. Talc 4.0
19. Bengala 1.0
20. Yellow iron oxide 2.0
21. Fragrance 0.1
22. Purified water 60.984
[Production Method] Ingredients 4 to 11 are dissolved by heating and kept at 80 ° C. to obtain an oil phase. Ingredient 12 is well swelled into ingredient 22, then ingredients 1-3 and 13-15 are added and mixed uniformly. To this, components 17 to 19 pulverized and mixed with a pulverizer are added, and the mixture is stirred with a homomixer and kept at 75 ° C. to obtain an aqueous phase. Add the oil phase to this aqueous phase while stirring, cool, add component 21 at 45 ° C and cool to 30 ° C with stirring to give the product.
[0017]
Example 6 Bath preparation formulation Formulation amount (% by weight)
1. Calcium chloride 0.001
2. Magnesium chloride 0.002
3. Potassium alum 0.01
4). Sodium bicarbonate 50.0
5). Yellow No. 202 (1) 0.05
6). Fragrance 0.25
7). Anhydrous sodium sulfate 49.687
[Production Method] Components 1 to 7 are uniformly mixed to obtain a product.
[0018]
Next, experimental examples will be given to explain the effects of the present invention in detail.
[0019]
Experimental Example 1 SS Bond Strengthening Test of Keratin Using a three-dimensional cultured skin, the SS bond strengthening effect of keratin was measured under the following conditions. These tests were based on literature (Tatsuo Kojima et al., Tis CultRes Commun, 2001, 20 (2) 110, Hideki Ogawa, Journal of the Japanese Society of Skin, 1978, 88 (8), 525-527).
[0020]
After applying the test substance to the three-dimensional cultured skin (Gunze Co., Ltd.), it was cultured for about one week. After the treatment, kit culture containing 0.5 mg / mL of MTT (3- [4,5-dimethylthiazol-2-yl] -2,5-diphenyl-tetrazolium bromide: Sigma) to evaluate the cytotoxicity of the sample After treatment with the solution for 2 hours, the culture piece was punched using a punch with a diameter of 6 mm, and the MTT dye reduced with isopropanol (Sigma) was extracted. The OD _{540 of} this extract was measured with a microplate reader (Molecular Device), and the absorbance when the absorbance of the solvent was 100% was calculated as the cell viability. Tissue pieces that did not show more than 70% toxicity were subjected to the test. A non-applied three-dimensional cultured skin was used as a control.
The treated three-dimensional cultured skin was fixed with 10% formalin, embedded in paraffin, and a specimen of each test substance was prepared. After deparaffinization, the SH group was specifically stained with DACM (N- [7-dimethylamino-4-methyl-3-coumarinyl] maleimid) staining solution. By image processing under a microscope, the stratum corneum fluorescence color development area ratio was calculated and compared with an unapplied control.
[0021]
The test results are shown in Table 1. As a result, the SS bond strengthening effect was recognized in calcium chloride, magnesium chloride and potassium alum treatment. Calcium chloride and magnesium chloride are said to have an effect of improving the stratum corneum barrier function, but the effect was due to 10 mM. In contrast, potassium alum showed an effect at a lower concentration of 0.1 mM, and therefore, it was considered that the effect of improving the stratum corneum barrier function was the highest among the minerals used in the test.
Furthermore, the combined effect of minerals was examined. As a result, the SS bond strengthening effect was recognized by treatment with 10 mM each of calcium chloride and magnesium chloride. However, this action was weaker than that of calcium chloride alone, equivalent to magnesium chloride, and not considered additive. This action was synergistically enhanced when additional potassium alum was added to the calcium chloride and magnesium chloride mixture. The concentration of the calcium chloride and magnesium chloride mixture was 0.01 mM, and this concentration showed no effect at all. However, by adding the calcium chloride and magnesium chloride mixture to potassium alum, We thought it was effective in improving the function.
[0022]
[Table 1]

[0023]
Experimental Example 2 Use Test Using the cream of Example 1 and the conventional cream of Comparative Example 1, a use test was conducted for one month for 30 women (20 to 50 years old) who suffer from rough skin. After use, a questionnaire survey on skin roughness improvement was conducted to determine the effect of skin roughness improvement. The evaluation criteria of the questionnaire were evaluated as “excellent” for valid, “good” for slightly effective, “good” for slightly effective, and “impossible” for invalid.
[0024]
These results are shown in Table 2. The cream of Example 1 showed an excellent improvement effect on skin roughness. During the test period, there was no skin problem and there was no problem with safety.
[0025]
[Table 2]

[0026]
A test for the use of the lotion of Example 2, the emulsion of Example 3, the ointment of Example 4, the foundation of Example 5 and the bath preparation of Example 6 was carried out in the same manner as in the experimental examples, all of which were safe and excellent. It showed an improvement effect on the skin.
[0027]
From the above, by adding potassium alum to the calcium chloride and magnesium chloride of the present invention, the effect of enhancing the keratin SS bond was shown, and the effect of improving the stratum corneum barrier function was recognized. The skin external preparation for improving skin roughness, characterized by containing calcium chloride, magnesium chloride and potassium alum , showed a safe and excellent skin roughness improving action.

Claims (3)

Skin external preparation for improving skin roughness characterized by containing potassium alum, calcium chloride and magnesium chloride . A skin external preparation for improving the stratum corneum barrier function , comprising potassium alum, calcium chloride and magnesium chloride . The skin external preparation for improving skin roughness according to claim 1, wherein the weight ratio of calcium chloride and magnesium chloride is in the range of 10: 1 to 1:10 with respect to potassium alum .