JP3135295B2 - 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 in which the above effects are enhanced by using each component alone has been proposed (JP-A-61-7216).

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

On the other hand, an external preparation containing saikosaponin b ₁ and saikosaponin b ₂ becomes unstable when left standing for a long period of time, and the above-mentioned effects are reduced. It is rare.

[0006]

SUMMARY OF THE INVENTION Under the above circumstances, the present invention has improved the effects of healing the skin, preventing and improving the rough skin, and preventing the aging of the skin from sagging and disappearing. In addition, an object of the present invention is to provide a skin external preparation that stabilizes the system and can maintain the above-mentioned effects for a long period of time.

[0007]

The first aspect of the present invention resides in an external preparation for skin characterized by containing at least one of saikosaponins b ₁ and b ₂ and batyl alcohol.

A second aspect is the first aspect, wherein at least one of saikosaponins b ₁ and b ₂ is 0.0001
About 20% by weight. A third aspect of the present invention resides in the external preparation for skin according to the first or the second aspect, characterized in that the composition comprises 0.01 to 20% by weight of the batyl alcohol.

[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. Wound healing of the skin at 0.001% by weight or more,
The effects of preventing and improving skin roughness and preventing aging, which prevents sagging and loss of skin, are further improved. When the weight is 10% or less, effects such as a further decrease in sticky feeling and irritation are produced.

In the present invention, the compounding amount of batyl alcohol is preferably 0.01 to 20% by weight, more preferably 0.5 to 8% by weight, based on the total amount of the external preparation for skin. At 0.5% or more, the effects of wound healing of the skin, prevention and improvement of skin roughness, anti-aging to prevent sagging and loss of skin, and the like, are further improved, and the stability of the system is further improved, and the above effects are obtained over a long period of time. Is maintained. When the content is 8% by weight or less, the sticky feeling is further reduced, and the refreshing feeling of use is further improved.

The external preparation for skin of the present invention may contain, in addition to the above essential components, components used in cosmetics and pharmaceuticals, such as aqueous components, powder components, oil components, and surface active agents, 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.

[0013]

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 saikosaponins b ₁ and b ₂ , such as wound healing of the skin, prevention and improvement of skin roughness, anti-aging that prevents sagging and loss of skin, and the feeling of use, are synergistically achieved by blending batyl alcohol. In order to show that these effects have been improved over time and that these effects last for a long time,
(A) to prepare an aqueous solution containing saikosaponins b ₁ or an aqueous solution and (b) saikosaponins b ₁ or b ₂ and batyl alcohol b _2, skin cell growth-promoting effects, wound healing effect and irritation (hemolysis) inhibiting effect The following tests were carried out on the samples, and their effects and changes over time were examined.

(Skin cell proliferation promoting action) 1) Cell proliferation effect A human skin tissue is sliced, adhered to the bottom of a cell culture dish, and cultured in Dulbecco's MEM culture medium (containing 10% fetal bovine serum) for 2 weeks. Then, the bottom surface of the Petri dish is almost entirely filled with fibroblasts. 0.1% of these fibroblasts
The cells are treated with a trypsin solution to form single cells, and a culture solution of 1000 cells / ml is prepared. This solution is added 1 per petri dish
and ml collected, which in the Dulbecco'sMEM culture and saikosaponins b ₁ In addition, or even a batyl alcohol 100
ppm addition, 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. The results are shown in FIG.

The solid line in FIG. 1 indicates that saikosaponin b
The cell growth rate when ₁ is added, and the broken line (Example) is the cell growth rate when further adding batyl alcohol. Cell proliferation rate figure, with respect to the number of cells without the addition of saikosaponins b _1, expressed by the ratio thereto.

[0017] 2) to prepare an aqueous solution containing a persistent (a) Psycho 0.01% aqueous solution and the saponin b ₁ (b) saikosaponins b ₁ 0.01% and batyl 0.01% alcohol of cell proliferation effect, Leave at room temperature.

[0018] 1) and in the same manner to prepare a culture solution, this way saikosaponins b ₁ concentration of 20ppm an aqueous solution of (a) or (b) was added, the number of colonies was counted cells in the same manner . The results are shown in the figure.

The solid line in FIG. 1 shows the result when the aqueous solution of (a) was added to the culture solution, and the broken line (Example) shows the result when the aqueous solution of (b) was added.

The cell growth rates in the figures are (a) and (b)
The aqueous solution of was used as a reference, and the ratio was expressed relative to the number of colonies of cells in a test performed immediately after the preparation.

As is clear from FIGS. 1 and 2, the addition of batyl alcohol greatly increased the cell growth rate. Furthermore, even after lapse of 2,000 hours, the cell proliferation effect hardly decreased, indicating that the effect was maintained.
On the other hand, in the sample containing no batyl alcohol, the cell growth effect decreased over time.

[0022] The results, also saikosaponin b _2, was obtained in the same manner.

[0023] (wound healing effect) (a) a psycho saponin b ₁ 200mg or (b)
200 mg of saikosaponin b ₁ and batyl alcohol 10
A sample in which 0 mg was dissolved in 1 ml of physiological saline was prepared and allowed to stand at room temperature.

Five Wistar rats, 6 weeks old, were
Groups were cut and subjected to a test after shearing. The rat was anesthetized with Nemptal and then the back skin was incised about 2 cm along the midline. Immediately the incision was sutured with a Mitsuheru, and the aqueous solutions of (a) and (b) were diluted to 1 / 1,000 with physiological saline. Was 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 U manufactured by Toyo Sokki Co., Ltd.
It measured using TM-4. The results are summarized in Table 1.

[0025]

[Table 1] As Table 1 shows, by adding batyl alcohol, wound healing effect of saikosaponins b ₁ is remarkably improved, also was found that even very high stability over time. Similarly good results for saikosaponins b ₂ was obtained.

(Irritation Suppression Test) Erythrocytes are collected from human blood and saikosaponin b ₁ or saikosaponin b ₁
And batyl alcohol were added and left for 1 hour, and the amount of hemolysis was measured. The results are shown in FIG. As shown in the figure, it was found that the addition of batyl alcohol suppressed the hemolytic action to a high concentration. It was also confirmed that the hemolytic action did not change over time.

(Example 1 and Comparative Example 1)
Psychosaponin b ₂ , batyl alcohol and a flavor were added and dissolved to prepare an alcohol phase. Mix other components except ion-exchanged water and quince seed extract,
By heating and dissolving in, an oil phase was prepared.

Next, the oil phase was added to ion-exchanged water heated to 70 ° C. to carry out preliminary emulsification, and then homogenized uniformly with a homomixer. The alcohol phase and the quince seed extract were added to the emulsion while stirring, and the emulsion was cooled to 30 ° C. to prepare an emulsion having the composition shown in Table 2. As Comparative Example 1, an emulsion without the addition of batyl alcohol was also prepared.

[0029]

[Table 2] Samples 1 to 4 are Examples of the present invention, and Sample 5 is Comparative Example 1. Of these, samples 1 and 2 are embodiments satisfying claims 2 and 3, and samples 3 and 4 are embodiments satisfying claim 3.

Using the emulsions of Samples 1 to 5, a skin roughness improvement effect test was conducted on a human body panel. In addition, use feeling tests such as stickiness and irritation were also performed. Table 4 shows the results. The test method is as follows.

Skin roughness improvement effect test 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.
The emulsions of Example and Comparative Example 1 were applied to the left and right half of the face of 25 panels evaluated as having rough skin condition “1” or “2” based on the criteria in Table 3 based on the condition of the skin pattern and the peeling condition of the stratum corneum. It 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 3.

Usability (stickiness, irritation) test 25 testers applied the above emulsions, and evaluated the stickiness and irritation organoleptically. For each sample, the number of people who felt stickiness or irritation was shown.

[0034]

[Table 3]

[0035]

[Table 4] As shown in Table 4, all of the emulsions of the present example have improved skin roughness improvement effects compared to Sample 5 of Comparative Example, and Samples 1 and 2 satisfying Claims 2 and 3 have particularly excellent skin roughness improvement effects. And showed a high usability.

When the saikosaponin b ₁ content is 0.0
Sample 3 having less than 001% by weight had no irritation or stickiness, but was inferior to samples 1 and 2 in improving skin roughness. Sample 4 having a saikosaponin b ₁ content of more than 20% exhibited a good effect of improving rough skin, but it was found that a sticky feeling appeared.

Example 2 In the same manner as in Sample 1 of Example 1, emulsions containing various concentrations of batyl alcohol were prepared. The change in the content of batyl alcohol was offset by ion-exchanged water, and the content of the other components was the same as in Sample 1 of Example 1. Here, the batyl alcohol content of the sample 6 of this example is 15%, the sample 7 is 0.005%, and the sample 8 is 22%.
It is.

With respect to the obtained samples, (1) immediately after preparation and (2) after standing in a constant temperature room at 50 ° C. for 6 months, a skin roughness improvement effect test was performed on a human body panel to examine the stability over time of the skin roughness improvement effect. Table 5 shows the results.

[0039]

[Table 5] As shown in Table 5, the emulsion of Sample 5 (Comparative Example) left in a thermostat at 50 ° C. for 6 months had a significantly reduced skin roughness effect, whereas the emulsion of the present Example had a time-dependent improvement in skin roughness improvement effect. It turns out that it is stable. In particular, Samples 1 and 6 of Examples satisfying claim 3 exhibited a high persistence of the rough skin improvement effect. Sample 7 having a batyl alcohol concentration of less than 0.01% is inferior in the effect of improving skin roughness as compared with Samples 1 and 6 satisfying claim 3, but is more stable over time than the comparative example containing no batyl alcohol. Met. In addition, it was found that Sample 8 containing more than 20% of batyl alcohol exhibited a high skin roughness improvement effect and its stability over time, but showed a sticky feeling and a poor feeling of use.

(Examples 3 to 7) In each case, the external preparation for skin prepared based on the composition and the production method shown in each of the following examples improved the effect of improving the rough skin or the effect of healing the wound as compared with the conventional example. In addition, the stability over time of these effects was improved.

(Example 3) Lotion by weight (alcohol phase) Saikosaponin b ₁ 0.05 Bacyl alcohol 4.0 Ethanol 7.0 Polyoxyethylene oleyl alcohol 0.6 Methyl paraben 0.05 Perfume 0.05 (Water Phase) Glycerin 4.0 Citric acid 0.01 Sodium citrate 0.1 Ion-exchanged water 84.14 (Preparation method) Prepare an aqueous phase and an alcohol phase, mix and solubilize them, and then filter to obtain lotion. Produced.

(Example 4) Cream weight% (oil phase) Saikosaponin b ₂ 1.0 Bacyl alcohol 2.0 Cetostearyl alcohol 3.5 Squalane 38.0 Beeswax 3.0 Reduced lanolin 5.0 Ethyl stearate 2 0.0 Ethylparaben 0.3 Fragrance 0.03 (Aqueous phase) 1,3-butylene glycol 7.0 Glycerin 5.0 Ion-exchanged water 33.17 (Production 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 5) Pack weight% saikosaponin b ₁ 0.01 Bacyl alcohol 9.0 Polyvinyl alcohol 7.0 Polyethylene glycol 3.0 Propylene glycol 6.0 Ethanol 10.0 Methyl paraben 0.05 Fragrance 0.05 Ion-exchanged water 64.89 (Production method) Polyethylene glycol, propylene glycol, and methylparaben were added to ion-exchanged water and dissolved by stirring. Next, add polyvinyl alcohol and heat and stir,
Psychosaponin b ₁ , batyl alcohol, and ethanol in which a fragrance was dissolved were added, and the mixture was stirred and dissolved to obtain a pack.

[0044] (Example 6) scalp cosmetics wt% (A phase) saikosaponins b ₁ 0.5 1,3-butylene glycol 6.5 polyethylene glycol 1500 5.0 Ethanol 5.5 Potassium hydroxide 0.05 Ion-exchanged water 46.95 (B phase) Bacyl alcohol 8.0 2-Hexyldecyl palmitate 2.0 Squalane 5.0 Butylparaben 0.2 Vitamin E acetate 0.15 Fragrance 0.05 (C phase) Ion-exchanged water 19.9 Carboxyvinyl polymer 0.2 (Preparation method) A solution prepared 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 stirred. While cooling, a cosmetic for the scalp was obtained.

(Example 7) Ointment% by weight Saikosaponin b ₂ 4.0 Batyl alcohol 20.0 Vaseline 35.0 Stearyl alcohol 15.0 Mokurou 15.0 Polyoxyethylene (10) oleyl 0.5 alcohol Ion-exchanged water 10.5 (Preparation method) Other components mixed and dissolved at 70 ° C. in ion-exchanged water at 70 ° C. were added, uniformly emulsified by a homomixer, and emulsified and then cooled to obtain an ointment.

[0046]

According to the present invention, namely by blending batyl alcohol saikosaponins b ₁ or saikosaponins b _2, increased cell proliferation effect possessed by saikosaponins b ₁ or b _2, moreover temporal stability of effect Is improved. As a result, it is possible to provide a skin external preparation that exhibits a high effect of preventing and improving rough skin, an effect of preventing skin aging or an effect of healing wounds stably over a long period of time.

[Brief description of the drawings]

FIG. 1 is a graph showing that the cell growth effect of saikosaponin b ₁ is improved by batyl alcohol.

2 is a graph showing the time course of cellular proliferative effects of saikosaponins b _1.

FIG. 3 is a graph showing that hemolysis of red blood cells is suppressed by the addition of batyl alcohol.

──────────────────────────────────────────────────続 き Continuation of the front page (56) References JP-A-61-7216 (JP, A) JP-A-49-55821 (JP, A) JP-A-57-197236 (JP, A) (58) Field (Int.Cl. ⁷ , DB name) A61K ^7/ 00-7/50 CA (STN) REGISTRY (STN)

Claims (2)

(57) [Claims] 1. Saikosaponin b ₁ and saikosaponin b ₂
Skin containing at least one and batyl alcohol
An external preparation, less the saikosaponins b ₁ and saikosaponins b ₂
An external preparation for skin characterized by containing 0.0001 to 20% by weight of at least one of them . 2. The method according to claim 1, wherein said batyl alcohol is contained in an amount of 0.01 to 20.
1 Symbol placement skin external preparation according to claim, characterized in that it comprises by weight%.