JPH0436137B2 - - Google Patents

Description

[Detailed description of the invention]

[Industrial Application Field] The present invention is a topical skin revitalizing product that is effective in healing wounds, preventing skin roughness, improving skin roughness, and preventing aging by preventing skin sagging and loss of luster, by incorporating saikosaponin. Regarding drugs. [Problems to be solved by the prior art and the invention] Saikosaponin is known to have an antigranulation effect, but its mechanism of action has not yet been fully elucidated. The present inventors discovered that saikosaponin has a skin cell proliferation promoting effect, which is the opposite effect to the conventionally known antigranulation effect, and focused on this fact. As a result of extensive research into the effects that occur when the agent is administered transdermally, it has been found to be effective in healing skin wounds, preventing skin roughness, improving skin roughness, and preventing aging by preventing skin sagging and loss of luster. This discovery led to the completion of the present invention. [Means for Solving the Problems] That is, the present invention provides a skin revitalizing external preparation characterized by containing saikosaponin. Saikosaponin used in the present invention includes saikosaponin a, saikosaponin b ₁ , saikosaponin b ₂ ,
There are Saikosaponin C and Saikosaponin D. All of these compounds have the effect of healing skin wounds, preventing skin roughness, improving skin roughness, and preventing aging by preventing skin sagging and loss of luster, but especially saikosaponin a, saikosaponin b ₁ ,
_2. Psychosaponin d has excellent effects. The amount of saikosaponin in the present invention is preferably 0.001 to 5% by weight based on the total amount of the skin activating external preparation. In addition to the above-mentioned essential ingredients, the skin revitalizing external preparation of the present invention may optionally include various ingredients commonly used in cosmetics, pharmaceuticals, etc., such as aqueous ingredients, powder ingredients, Oil, surfactant, humectant, thickener, preservative, antioxidant,
Flavors, colorants, drugs, etc. can be added. Further, the dosage form of the skin revitalizing topical preparation of the present invention is arbitrary,
For example, it can take the form of a solubilized system such as a lotion, an emulsified system such as a milky lotion or a cream, or a dosage form such as an ointment or a dispersion. [Effects and Examples of the Invention] Preferred examples of the present invention will be described below. First, saikosaponin according to the present invention was produced as follows. After drying 8 kg of purple root (raw root), air-dry it to 90 kg.
Extract with 201% methanol solution. Then, the filtrate is concentrated and separated by HPLC to obtain saikosaponins a, b ₁ , b ₂ , c, and d, respectively. The elution order is saikosaponin c, a, b ₂ , b ₁ , d. For HPLC, ODS column (Waters
Using System500A 57mmi.d. x 300mm) manufactured by
Eluent acetonitrile:water (40:60) at a flow rate of 1ml
The elution of each saikosaponin is confirmed using the wavelength
Preferably, this is carried out at an absorbance of 210 nm. In order to demonstrate the effects of saikosaponin on skin wound healing, prevention of rough skin, improvement of rough skin, and anti-aging effects such as skin sagging and loss of luster, the following skin cell growth promoting effect test was conducted. (Skin cell proliferation effect) When human skin tissue is cut into small pieces and attached to the bottom of a cell culture shear dish and cultured for one week in Eagle's MEM culture solution (containing 10% calf serum), almost the entire bottom of the shear dish is covered. Filled with fibroblasts. These fibroblasts were treated with a 0.25% trypsin solution to make them into single cells, and then a culture solution containing 10,000 cells/ml was prepared, and 0.1 ml of this solution was added per shear, followed by Eagle's MEM culture solution and Saikosaponin (final concentration 5 μg/ml) was further added and cultured in a CO ₂ -incubator for 2 weeks, after which cells were fixed and stained, and cell colonies were counted. Note that the case in which saikosaponin was not added was used as a control. In addition, the saiko extract that was simultaneously tested was used in an amount equal to that of the saiko saponin in terms of dry solid content. The results are shown in Figure 1. Colony formation rate was calculated using the following formula. Colony formation rate = T / C × 100 (%) T = number of colonies of cells treated with saikosaponin / number of implanted cells per shear C = number of colonies of cells not treated with saikosaponin / number of implanted cells per shear 1st As shown in the figure, saikosaponin had a significant effect compared to the control. The effect of saikosaponin on skin cell proliferation is a>d>b ₁
The order is >c>b ₂ >. Furthermore, the following test was conducted to demonstrate the wound healing effect on the skin. (Wound Healing Effect) A group of 5 Wistar rats aged 6 weeks old were subjected to a test after their hair was shaved. After the rats were anesthetized with Nembutal, an approximately 2 cm dorsal skin incision was made along the midline, and the incision was immediately closed with Mitsuhel sutures.
0.05 g of Saikosaponin was dissolved in 0.1 ml of saline solution and applied once a day for 2 weeks. Two weeks later, the rats were sacrificed and the suture needles were removed, and skin sections with a cross section of 1 cm were prepared. For tension measurement, Tensilon UTM-4 (manufactured by Toyo Sokki Co., Ltd.) was used to measure the cutting tension of the skin section. As a control, a skin section coated with physiological saline not containing saikosaponin was used. The results are shown in Table 1.

[Table] From the results in Table 1, the tension was increased in all areas where saikosaponin was applied compared to the non-applied area (control), and a significant healing promoting effect was observed. Next, the present invention will be explained in more detail with reference to Examples. Note that the present invention is not limited to this. The blending amount is in weight%. Example 1 Lotion (wt%) Saikosaponin a 0.05 Glycerin 4.0 1,3-butylene glycol 4.0 Ethanol 7.0 Polyoxyethylene oleyl alcohol 0.5 Methylparaben 0.05 Citric acid 0.01 Sodium citrate 0.1 Fragrance 0.05 Purified water 84.24 Citric acid in purified water , dissolve sodium citrate, glycerin, and 1,3-butylene glycol; separately, dissolve polyoxyethylene oleyl alcohol, saikosaponin A, fragrance, and methylparaben in ethanol, and add this to the purified aqueous solution described above to solubilize; A lotion was obtained by filtration. Example 2 Cream A (wt%) Cetostearyl alcohol 3.5 Squalane 40.0 Beeswax 3.0 Reduced lanolin 5.0 Stearic acid monoglyceride 2.0 Polyoxyethylene (20) Sorbitan monopalmitate ester 2.0 Ethylparaben 0.3 Saikosaponin d 1.0 Fragrance 0.03 B 1,3 Butylene glycol 5.0 Glycerin 5.0 Purified water 33.17 Phase A was dissolved by heating and kept at 75°C, and then added to phase B, which had been heated to 75°C, with stirring. After processing with a homomixer to make emulsified particles fine, the mixture was rapidly cooled while stirring to obtain cream. Example 3 Emulsion (wt%) Saikosaponin c 0.001 Stearic acid 1.5 Cetyl alcohol 0.5 Beeswax 2.0 Polyoxyethylene (10 mol) monooleate 1.0 Glycerin monostearate 1.0 Quince seed extract (5% aqueous solution) 20.0 Propylene Glycol 5.0 Ethanol 3.0 Ethylparaben 0.3 Fragrance 0.03 Purified water 65.669 Add Saikosaponin C and fragrance to ethyl alcohol and dissolve (alcohol phase). Add propene glycol to purified water, heat to dissolve, and keep at 70℃ (aqueous phase). Mix other ingredients except quince seed extract, heat and dissolve and keep at 70℃ (oil phase). Pre-emulsification is performed by adding the oil phase to the water phase.
Uniformly emulsify with a homomixer. While stirring, add the alcohol phase and quince seed extract. Thereafter, the mixture was cooled to 30° C. with stirring to obtain a milky lotion. Example 4 Pack (% by weight) Saikosaponin b ₁ 0.1 Polyvinyl alcohol 15.0 Polyethylene glycol 3.0 Propylene glycol 7.0 Ethanol 10.0 Methylparaben 0.05 Fragrance 0.05 Purified water 64.8 Add polyethylene glycol, propylene glycol, and methylparaben to purified water and dissolve with stirring. Next, polyvinyl alcohol was added and stirred with heating, and ethanol in which saikosaponin b ₁ and fragrance were dissolved was added and dissolved with stirring to obtain a pack. Example 5 Scalp cosmetics (scalp treatment) A (% by weight) Saikosaponin b ₂ 0.5 1,3-butylene glycol 6.5 Polyethylene glycol 1500 5.0 Ethanol 5.5 Caustic potash 0.05 Purified water 46.95 B 2-hexyldecyl palmitate 10.0 Squalane 5.0 Butyl Parapen 0.2 Vitamin E acetate 0.15 Fragrance 0.05 C Purified water 19.9 Carboxyvinyl polymer 0.2 Phase B was dissolved at 75℃ and A was kept at 75℃.
A scalp treatment was obtained by adding phase C with stirring, and then adding phase C which had been stirred and dissolved at room temperature, and cooling with stirring to obtain a scalp treatment. Example 6 Ointment (wt%) Vaseline 40.0 Stearyl alcohol 18.0 Mokuro 20.0 Polyoxyethylene (10 mol) monooleate 0.25 Glycerin monostearate 0.25 Saikosaponin C 5.0 Purified water 16.5 Purified water was kept at 70°C (aqueous phase ), other ingredients at 70℃
Mix and dissolve (oil phase). Add the oil phase to the water phase,
The mixture was uniformly emulsified using a homomixer and cooled to obtain an ointment. Example 7 Lotion (wt%) Saikosaponin b ₁ 0.05 Glycerin 4.0 1,3-butylene glycol 4.0 Ethanol 7.0 Polyoxyethylene oleyl alcohol 0.5 Methylparaben 0.05 Citric acid 0.01 Sodium citrate 0.1 Fragrance 0.05 Purified water 84.24 The manufacturing method is the same as the example According to 1. A rough skin improvement effect test was conducted using Example 1 as a sample. The results are shown below. (Effect on improving rough skin) Lotion obtained in Example 1 and blank lotion [not containing Saikosaponin A (replaced with purified water)]
A skin improvement effect test was conducted using human body panels. That is, a replica of the skin surface of a healthy female person (face) is taken using the replica method using Millisne resin and observed using a microscope (17x magnification). The results of Example 1 were obtained on the left and right half of the face of 25 people (skin roughness panel) who were judged to have a rough skin rating of 1 or 2 based on the condition of skin marks and peeling of the stratum corneum based on the criteria shown in Table 2. 1 lotion and 1 blank lotion
It was applied once a day for 2 weeks. Two weeks later, the skin condition was observed again using the replica method described above and evaluated according to the criteria in Table 2.

【table】 The results are shown in Table-3.

[Table] From the results, it was found that the facial area using the lotion containing Saikosaponin A had a remarkable effect on improving rough skin compared to the facial area using the blank lotion. Next, the skin lotion of Example 7 was also subjected to the same rough skin improvement effect test. The results are shown in Table 4 below.

[Table] From the results, a sufficient effect on improving rough skin was observed even when saikosaponin b ₁ was used. Furthermore, a replica test was also conducted on Saikosaponin b ₂ using a lotion with the same formulation (Example 8). The results are shown in Table 5 below.

[Table] From the results, it was found that the use of saikosaponin _b2 also had a sufficient effect on improving rough skin.

[Brief explanation of drawings]

FIG. 1 is a graph showing the skin cell proliferation effect of the skin revitalizing external preparation according to the present invention.

Claims (1)

[Claims] 1. A skin revitalizing external preparation characterized by containing saikosaponin.