JP3135294B2 - External preparation for skin - Google Patents

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,
More specifically, it relates to a skin external preparation having a high skin cell proliferation effect. The external preparation for skin is suitably applied to cosmetics such as lotions, creams, emulsions, packs, cosmetics for scalp, and pharmaceuticals such as wound treatments and anti-inflammatory ointments.

[0002]

2. Description of the Related Art Psychosaponins extracted from plants such as Saiko have the effects of healing wounds on the skin, preventing and improving skin roughness, and preventing aging that prevents sagging and disappearance of the skin. It is blended.

Further, the extracted saikosaponin is separated into saikosaponin a, saikosaponin b ₁ , saikosaponin b ₂ , saikosaponin c, and saikosaponin d,
A technique that enhances the above effects by using each component alone has been proposed (Japanese Patent Application Laid-Open No. 61-7216).

[0004] However, external preparations for the skin that further enhance the above effects are desired.

[0005]

DISCLOSURE OF THE INVENTION The present invention relates to an external preparation for skin which has further improved effects such as wound healing of the skin, prevention and improvement of rough skin, and prevention of aging which prevents sagging and loss of skin. The purpose is to provide.

[0006]

A first gist of the present invention is to provide at least one of saikosaponin b ₁ and saikosaponin b ₂ .
An external preparation for skin characterized by containing a seed and urea.

[0007] The second aspect, in the first aspect, there at least one saikosaponins b ₁ and saikosaponins b ₂ to the skin external agent characterized in that it comprises from 0.0001 wt%.

[0008] A third aspect of the present invention is the skin preparation for external use according to the first or second aspect, characterized in that the urea contains 0.1 to 20% by weight.

[0009]

The operation of the present invention will be described below in detail.

[0010] In the skin external preparation of the present invention, at least one of saikosaponins b ₁ and saikosaponins b ₂ is blended. The compounding amount is 0.0001 in the total amount of the external preparation for skin.
-20% by weight is preferable, and 0.001-10% by weight is more preferable. When the content is 0.001% by weight or more, the effect of improving skin roughness is further improved. On the other hand, when the content is 10% by weight or less, effects such as loss of stickiness and irritation are produced.

In the present invention, the amount of the urea is as follows:
The content is preferably 0.1 to 20% by weight based on the total amount of the external preparation for skin.
5 to 15% by weight is more preferred. At 0.5% by weight or more, the skin cell proliferation effect is further improved, and the feeling of use such as moisture and moist feeling is further improved. When the content is 15% by weight or less, the feeling of use is further improved such that the sticky feeling is eliminated.

As described above, urea has the effect of synergistically improving the skin cell proliferation effect of saikosaponin b ₁ or saikosaponin b ₂ . That is, by combining them together, the skin cell proliferation effect of saikosaponins b ₁ and b ₂ , that is, the wound healing effect, the skin roughness improving effect, and the like are significantly improved.

The external preparation for skin of the present invention may contain, in addition to the above-mentioned essential components, components used in cosmetics and pharmaceuticals, such as aqueous components, powder components, oil components, surfactants, as long as the effects of the present invention are not impaired. An agent, a humectant, a thickener, a preservative, an antioxidant, a fragrance, a coloring agent, a drug and the like can be compounded.

The dosage form of the external preparation for skin is arbitrary, and for example, dosage forms such as a solubilizing system such as a lotion, an emulsion system such as a milky lotion and a cream, an ointment and a dispersion.

[0015]

EXAMPLES Next, the present invention will be described in detail with reference to examples, but it goes without saying that the technical scope of the present invention is not limited to these examples.

First, the effects of psychosaponins b ₁ and b ₂ such as wound healing of the skin, prevention and improvement of skin roughness, anti-aging to prevent sagging and loss of skin, and feeling of use are synergistically achieved by adding urea. The following tests were conducted on the skin cell proliferation promoting effect, wound healing effect, and irritation (hemolytic action) suppressing effect.

(Skin Cell Proliferation Promoting Action) A human skin tissue is sliced and adhered to the bottom of a cell culture dish.
When cultured in o's MEM culture medium (containing 10% fetal calf serum) for 2 weeks, the bottom of the Petri dish is almost completely filled with fibroblasts. The fibroblasts were treated with a 0.1% trypsin solution to form single cells, and a culture solution of 1000 cells / ml was prepared. The solution was petri dish per 1ml taken, to which a Dulbecco's MEM culture and saikosaponins b ₁ of various concentrations was added, or in addition to urea, CO ₂ - and cultured for 2 weeks in an incubator. Thereafter, the cells were fixed and stained, and the number of cell colonies was counted.

FIG. 1 shows the results. The solid line in Figure 1 is the result when only saikosaponins b ₁ was added to the culture,
The broken line (Example) shows the result when urea was further added at 100 ppm. Cell proliferation rate figure, with respect to the number of cells without the addition of saikosaponins b _1, expressed by the ratio thereto.

As is clear from the figure, the cell proliferation rate was significantly improved by adding urea. For even saikosaponins b _2, similar results were obtained.

(Wound healing effect) Five Wistar rats, 6 weeks old, were grouped into a group and subjected to a test after shaving. The rat was anesthetized with nemptal, and the back skin was incised about 2 cm along the midline. Immediately, the incision was sutured with a Mitsuheru, and 200 mg of saikosaponin b ₁ was added to 0.1 ml of physiological saline 0.1.
those that have been dissolved ml, and or saikosaponin b ₁ 20
An aqueous solution prepared by dissolving 0 mg and 0.05 g of urea in 0.1 ml of physiological saline was diluted to 1000 times with physiological saline and applied once a day for 2 weeks. Two weeks later, the suture needle was removed, and a skin section was prepared so as to have a cross section of 1 cm. The cutting tension of this section was measured by Tensilon UTM manufactured by Toyo Sokki Co., Ltd.
-4.

The average tension in the case of only saikosaponin b ₁ was 470 g / cm, whereas the average tension of the case where urea was added was 525 g / cm, and the wound healing of psychosaponin b ₁ by adding urea. It was found that the effect was improved. Regarding the saikosaponin b _2, the average tension 535 g / cm was obtained.

(Irritant Suppressive Effect) Erythrocytes are collected from human blood and saikosaponin b ₁ or saikosaponin b ₁
And 100 μg of urea were added and left for 1 hour, and the amount of hemolysis was measured. The results obtained for the relationship saikosaponins b ₁ concentration hemolysis shown in FIG.

As is apparent from the figure, the hemolytic effect of saikosaponins b ₁ by the addition of urea was found to be suppressed to a high concentration.

(Example 1 and Comparative Example) An aqueous phase and an alcohol phase having the compositions shown in Table 1 were respectively prepared, mixed and solubilized, and then filtered to prepare a lotion.

[0025]

[Table 1] Samples 1 to 6 are examples of the present invention, and sample 7 is a comparative example. Of these, samples 1 and 2 are examples satisfying claims 2 and 3, samples 3 and 4 are examples satisfying claim 3, and samples 5 and 6 are examples satisfying claim 2.

Skin roughness improvement effect Using the lotions of Samples 1 to 7, a skin roughness improvement effect test was conducted on a human body panel. The test method is as follows.

The replica of the skin of a healthy female subject is morphologically observed by a replica method using a millisin resin and observed with a microscope. Samples 1 to 6 of the example and sample 7 of the comparative example were placed on the left and right half of the face of 25 panels evaluated as rough skin condition 1 or 2 based on the criteria of Table 2 based on the state of the skin pattern and the peeling state of the stratum corneum. The lotion was applied once a day for 2 weeks.

After two weeks, the condition of the skin was observed again by the replica method described above, and the condition of the skin was evaluated according to the criteria shown in Table 2. Table 3 summarizes the results.

[0029]

[Table 2]

[0030]

[Table 3] Stickiness and Irritation For each of the lotions of Samples 1 to 6, 25 testers actually applied the lotion and organoleptically evaluated the feeling of use (stickiness and irritation). Table 4 shows the number of persons who felt sticky and irritated for each sample.

[0031]

[Table 4] As shown in Tables 3 and 4, all of the lotion of this example has an improved skin roughening effect as compared with Sample 7 of Comparative Example, and Samples 1 and 3 satisfying Claims 2 and 3 are extremely small. It showed good skin roughness improvement effect and high feeling of use.

When the saikosaponin b ₁ content is 0.0
Sample 3 less than 001% by weight had no irritation, but the skin roughness improving effect was inferior to Samples 1 and 3.
Sample 4 having a saikosaponin b ₁ content of more than 20%
Although a good skin roughness improving effect was exhibited, it was found that a sticky feeling appeared. Sample 5 having a urea content of less than 0.1% is inferior in skin roughness improvement effect as compared to Samples 1 and 2, and Sample 6 having a urea content of more than 20% has good skin roughness as in Samples 1 and 2. It was found that although it exhibited an improving effect and no irritation, a sticky feeling appeared.

(Examples 2 to 6) All of the external preparations for skin prepared based on the compositions and production methods shown in the following examples have improved skin roughening effects or wound healing effects as compared with the conventional examples, and have irritation. Was also suppressed, indicating that urea synergistically improves the above effects of saikosaponin.

(Example 2) Cream wt% (oil phase) Saikosaponin b ₂ 1.0 Cetostearyl alcohol 3.5 Squalane 38.0 Beeswax 3.0 Reduced lanolin 5.0 Ethyl stearate 4.0 Ethyl paraben 0 0.3 Perfume 0.03 (aqueous phase) Urea 1.0 1,3-butylene glycol 2.0 glycerin 2.0 Deionized water 40.17 (Preparation method) Heat and melt the oil phase and keep it at 75 ° C. 7
It was added to the aqueous phase heated to 5 ° C. with stirring. Next, the mixture was uniformly emulsified with a homomixer and then rapidly cooled with stirring to obtain a cream.

(Example 3) Emulsion weight% (alcohol phase) Saikosaponin b ₂ 0.001 Fragrance 0.03 Ethanol 3.0 (oil phase) Stearic acid 1.5 Cetyl alcohol 0.5 Beeswax 2.0 Polyoxy Ethylene (10) oleyl 2.0 alcohol Ethyl paraben 0.3 (aqueous phase) Urea 2.0 propylene glycol 3.0 ion-exchanged water 65.669 Quince seed extract (5% aqueous solution) 20.0 (production method) 70 ° C The oil phase heated and melted at 70 ° C. was added to the aqueous phase of the above (1), preliminarily emulsified, and further homogenized with a homomixer. While stirring, the alcohol phase and the quince seed extract were added, and the mixture was cooled to 30 ° C. to obtain an emulsion.

(Example 4) Pack weight% Saikosaponin b ₁ 0.1 Urea 5.0 Polyvinyl alcohol 10.0 Polyethylene glycol 3.0 Propylene glycol 7.0 Ethanol 10.0 Methyl paraben 0.05 Fragrance 0.05 ions Exchanged water 64.8 (Production method) Urea, polyethylene glycol, propylene glycol, and methyl paraben were added to ion-exchanged water and dissolved by stirring. Next, polyvinyl alcohol was added, and the mixture was heated and stirred. Psychosaponin b ₁ and ethanol in which a flavor was dissolved were added, and the mixture was stirred and dissolved to obtain a pack.

[0037] (Example 5) Scalp cosmetic wt% (A phase) saikosaponins b ₁ 0.5 urea 0.5 1,3-butylene glycol 6.5 polyethylene glycol 1500 5.0 Ethanol 5.5 hydroxide Potassium 0.05 Deionized water 40.95 (B phase) 2-Hexyldecyl palmitate 10.0 Squalane 5.0 Butylparaben 0.3 Vitamin E acetate 0.15 Fragrance 0.05 (C phase) Deionized water 25 0.4 Carboxyvinyl polymer 0.2 (Production method) A solution obtained by dissolving phase B at 75 ° C was added to phase A heated to 75 ° C while stirring, and phase C dissolved by stirring at room temperature was further added. After cooling, a scalp cosmetic was obtained.

(Example 6) Ointment wt% Saikosaponin b ₂ 5.0 Urea 20.0 Vaseline 40.0 Stearyl alcohol 4.5 Mocrow 20.0 Polyoxyethylene (10) oleyl 0.5 Alcohol Ion exchange water 10 5.5 (Preparation method) Other components mixed and dissolved at 70 ° C. in ion-exchanged water at 70 ° C. were added, and the mixture was uniformly emulsified by a homomixer, emulsified and cooled to obtain an ointment.

[0039]

According to the present invention, namely by incorporating a urea saikosaponins b ₁ or saikosaponins b _2, cell proliferation activity of saikosaponins is synergistically improved. As a result, it is possible to provide a skin external preparation having a high skin roughness preventing and improving effect, a skin aging preventing effect or a wound healing effect and a good feeling upon use.

[Brief description of the drawings]

[1] Cell proliferative effects of saikosaponins b ₁ is a graph showing that enhanced by urea.

FIG. 2 is a graph showing that hemolysis of red blood cells is suppressed by the addition of urea.

Continuation of front page (56) References JP-A-61-7216 (JP, A) JP-A-61-207306 (JP, A) JP-A-4-29917 (JP, A)

Claims (2)

(57) [Claims] An external preparation for skin containing at least one of saikosaponin b ₁ and saikosaponin b ₂ and urea.
There, small of the saikosaponins b ₁ and the saikosaponins b ₂
An external preparation for skin, comprising at least one of 0.0001 to 20% by weight . 2. A 1 Symbol placement skin external preparation according to claim, characterized in that it comprises 0.1 to 20 wt% of the urea.