JPH0517334A - Skin medicine for external use - Google Patents

Abstract

PURPOSE:To obtain a skin medicine for external use capable of achieving further improvement is effects by saikosaponins b1 and b2 such as curing of wounds in the skin, prevention and improvement of skin roughening and prevention of skin slackness and loss of its luster by blending the saikosaponins b1 and b2 having the aforementioned effects with urea. CONSTITUTION:A skin medicine for external use is obtained by blending at least one of (especially 0.0001-20wt.%) saikosaponin b1 and saikosaponin b2 prepared by extraction and separation from a plant such as Bupleuri Radix with urea (preferably 0.1-20wt.%, especially 0.5-15wt.%). Skin cell proliferating effects and feeling in use such as moderating moistness or wetness is further improved by blending the urea. The aforementioned skin medicine for the external use can be applied to cosmetics such as toilet water, a cream, a milky lotion, a pack or a cosmetic for the scalp or medicines, e.g. a therapeutic agent for wounds or an antiinflammatory ointment.

Description

Detailed Description of the Invention

[0001]

The present invention relates to a skin external preparation,
More specifically, it relates to a skin external preparation having a high skin cell growth effect. The external preparation for skin is preferably applied to cosmetics such as lotions, creams, emulsions, packs, cosmetics for scalp, and pharmaceuticals such as ointment for treating wounds and anti-inflammatory.

[0002]

2. Description of the Related Art Psychosaponin extracted from plants such as Saiko has effects such as wound healing on skin, prevention and improvement of skin roughness, and aging prevention to prevent sagging and loss of skin. It is compounded.

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 also been proposed (Japanese Patent Laid-Open No. 61-7216).

[0004] However, there is a demand for an external preparation for the skin which further enhances the above effects.

[0005]

DISCLOSURE OF THE INVENTION The present invention provides a skin preparation for external use, which has improved effects such as wound healing on the skin, prevention and improvement of skin roughness, and aging prevention to prevent sagging and loss of skin. The purpose is to provide.

[0006]

The first gist of the present invention is to provide at least one of saikosaponin b ₁ and saikosaponin b ₂ .
It is present in an external preparation for skin characterized by containing seeds and urea.

A second aspect resides in the external preparation for skin according to the first aspect, which comprises 0.0001 to 20% by weight of at least one of saikosaponin b ₁ and saikosaponin b ₂ .

A third aspect of the present invention resides in the external preparation for skin according to the first or second aspect, characterized in that the urea is contained in an amount of 0.1 to 20% by weight.

[0009]

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

In the external preparation for skin of the present invention, at least _{one of} saikosaponin b ₁ and saikosaponin 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. If it is 0.001% by weight or more, the skin roughening improving effect is further enhanced. On the other hand, if it is 10% by weight or less, the sticky feeling is lost and the stimulative effect is lost.

In the present invention, the blending amount of the above urea is
The total amount of the external preparation for skin is preferably 0.1 to 20% by weight, and
5 to 15% by weight is more preferable. When it is 0.5% by weight or more, the skin cell proliferation effect is further improved, and the feeling of use such as moisture and moistness is further improved. When the content is 15% by weight or less, the feeling of use is further improved such that the stickiness is lost.

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, when both are blended together, the skin cell proliferation effect of Psychosaponins b ₁ and b ₂ , that is, the wound healing effect and the rough skin improving effect are remarkably improved.

The external preparation for skin of the present invention contains, in addition to the above-mentioned essential components, components used in cosmetics, pharmaceuticals, etc., such as an aqueous component, a powder component, an oil component, and a surface active agent as long as the effects of the present invention are not impaired. Agents, moisturizers, thickeners, preservatives, antioxidants, fragrances, coloring agents, agents and the like can be added.

The external preparation for skin may be in any dosage form, for example, a solubilization system such as lotion, an emulsion system such as emulsion or cream, an ointment or a dispersion liquid.

[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.

[0016] First, the effect of saikosaponins b ₁ and b ₂ on skin wound healing, prevention and improvement of skin roughness, prevention of aging to prevent sagging and loss of skin, and the feeling of use are synergistic by blending urea. In order to show that the effect is improved, the following tests were carried out for skin cell proliferation promoting effect, wound healing effect and stimulating (hemolytic effect) suppressing effect.

(Skin cell proliferation promoting action) Human skin tissue is cut into small pieces and attached to the bottom surface of a cell culture dish, and Dulbecc
After culturing in o's MEM culture solution (containing 10% fetal bovine serum) for 2 weeks, the bottom surface of the petri dish is almost entirely filled with fibroblasts. The fibroblasts were treated with a 0.1% trypsin solution to give single cells, and a culture medium containing 1000 cells / ml was prepared. This solution was sampled in an amount of 1 ml per dish, to which Dulbecco's MEM culture medium and various concentrations of saikosaponin b ₁ were added, or urea was further added, and the cells were cultured in a CO ₂ -incubator for 2 weeks. Then, 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 is the result when only saikosaponin b ₁ was added to the culture solution,
The broken line (Example) is the result when 100 ppm of urea was further added. The cell growth rate in the figure was expressed as a ratio based on the number of cells without the addition of saikosaponin b ₁ .

As is clear from the figure, the cell growth rate was significantly improved by adding urea. Similar results were obtained with saikosaponin b ₂ .

(Wound healing effect) A group of 5 Wistar rats 6 weeks old was used as a group and subjected to a test after hair cutting. After anesthetizing the rat with Nemptal, an incision of the back skin was made about 2 cm along the midline. Immediately, the incision was sutured with Mitsuhel, and 200 mg of saikosaponin b ₁ was added to 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 1/1000 with physiological saline and applied once a day for 2 weeks. Two weeks later, the suture needle was removed to prepare a skin section having a cross section of 1 cm. Tensileon UTM manufactured by Toyo Sokki Co., Ltd.
It was measured using -4.

[0021] The average tension when only saikosaponins b ₁ whereas was 470 g / cm, an average tension despite the addition of urea 525 g / cm, and the wound healing saikosaponins b ₁ by blending urea It turned out that the effect improves. Further, regarding saikosaponin b ₂ , an average tension of 535 g / cm was obtained.

(Irritation-suppressing effect) Erythrocytes are collected from human blood to obtain saikosaponin b ₁ or saikosaponin b _1.
And 100 μg of urea were added and left for 1 hour to measure the amount of hemolysis. The results obtained for the relationship between the saikosaponin b ₁ concentration and the hemolysis rate are shown in FIG.

As is clear from the figure, it was found that the hemolytic action of saikosaponin b ₁ was suppressed to a high concentration by adding urea.

(Example 1 and Comparative Example) A water phase and an alcohol phase having the compositions shown in Table 1 were 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. Among them, 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 facial surface morphology of a healthy female is taken as a replica of the skin using the replica method using myricin resin and observed under a microscope. Based on the condition of the skin print and the peeling condition of the stratum corneum, the skin was evaluated as rough skin condition 1 or 2 based on the criteria in Table 2. The lotion was applied once a day for 2 weeks.

After 2 weeks, the skin condition was observed again by the above replica method, and the skin condition was evaluated according to the criteria shown in Table 2. The results are summarized in Table 3.

[0029]

[Table 2]

[0030]

[Table 3] Stickiness and Irritation Twenty-five testers actually applied each of the lotions of Samples 1 to 6 and sensory-evaluated the feeling of use (stickiness, irritation) of each. Table 4 shows the number of people who felt stickiness and irritation for each sample.

[0031]

[Table 4] As shown in Tables 3 and 4, the lotion of the present example has an improved skin roughening effect as compared with the sample 7 of the comparative example, and particularly, the samples 1 and 3 satisfying claims 2 and 3 are extremely rare. It showed a good effect of improving rough skin and a high feeling of use.

Further, the saikosaponin b ₁ content is 0.0
Sample 3 with less than 001% by weight was not irritating, but the rough skin improving effect was inferior to Samples 1 and 3.
Sample 4 having a saikosaponin b ₁ content of more than 20%,
Although it showed a good effect of improving rough skin, it was found that a sticky feeling appeared. Sample 5 having a urea content of less than 0.1% is inferior in the rough skin improving effect to Samples 1 and 2, and Sample 6 having a urea content of more than 20% has good rough skin as in Samples 1 and 2. It was found that a sticky feeling appears although the effect is improved and the irritation is lost.

(Examples 2 to 6) The external preparations for the skin prepared based on the compositions and the production methods shown in the following Examples all have improved rough skin improving effect or wound healing effect and are more irritating than conventional examples. Was also suppressed, indicating that urea synergistically enhances the above effects of saikosaponin.

(Example 2) Cream wt% (oil phase) Psychosaponin b ₂ 1.0 Cetostearyl alcohol 3.5 Squalane 38.0 Beeswax 3.0 Reduced lanolin 5.0 Ethyl stearate 4.0 Ethylparaben 0 .3 fragrance 0.03 (aqueous phase) urea 1.0 1,3-butylene glycol 2.0 glycerin 2.0 ion-exchanged water 40.17 (production method) The oil phase was melted by heating and kept at 75 ° C. 7
It was added with stirring to the aqueous phase heated to 5 ° C. 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) Psychosaponin 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 ethylparaben 0.3 (aqueous phase) Urea 2.0 Propylene glycol 3.0 Ion-exchanged water 65.669 Quinceseed extract (5% aqueous solution) 20.0 (Production method) 70 ° C The oil phase heated and melted at 70 ° C. was added to the water phase of 1 above, preliminarily emulsified, and further homogenized with a homomixer. While stirring this, an alcohol phase and a quince seed extract were added, and the mixture was cooled to 30 ° C. to obtain an emulsion.

Example 4 Pack Weight% Psychosaponin b ₁ 0.1 Urea 5.0 Polyvinyl alcohol 10.0 Polyethylene glycol 3.0 Propylene glycol 7.0 Ethanol 10.0 Methylparaben 0.05 Perfume 0.05 Ion Exchanged water 64.8 (Production method) Urea, polyethylene glycol, propylene glycol and methylparaben were added to ion exchanged water and dissolved with stirring. Next, polyvinyl alcohol was added and heated and stirred, and psychosaponin b ₁ and ethanol in which a fragrance was dissolved were added and dissolved by stirring to obtain a pack.

Example 5 Scalp Cosmetic Weight% (Phase A) Psychosaponin b ₁ 0.5 Urea 0.5 1,3-Butylene Glycol 6.5 Polyethylene Glycol 1500 5.0 Ethanol 5.5 Hydroxylation Potassium 0.05 Ion-exchanged water 40.95 (Phase B) 2-hexyldecyl palmitate 10.0 Squalane 5.0 Butylparaben 0.3 Vitamin E acetate 0.15 Perfume 0.05 (Phase C) Ion-exchanged water 25 0.4 Carboxyvinyl Polymer 0.2 (Production Method) Phase B dissolved at 75 ° C. was added to Phase A heated to 75 ° C. with stirring, and further dissolved at room temperature with stirring to prepare Phase C and stirred. 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 Mokurou 20.0 Polyoxyethylene (10) oleyl 0.5 Alcohol ion-exchanged water 10 .5 (Production method) Other components mixed and dissolved in 70 ° C. ion-exchanged water at 70 ° C. were added, homogenized with a homomixer, cooled after emulsification to obtain an ointment.

[0039]

According to the present invention, that is, by adding urea to Psychosaponin b ₁ or Psychosaponin b ₂ , the cell growth action of Psychosaponin is synergistically improved. As a result, it is possible to provide an external preparation for the skin which has a high effect of preventing and improving rough skin, a high effect of preventing skin aging or a effect of wound healing, and has a good feeling in use.

[Brief description of drawings]

FIG. 1 is a graph showing that the cell growth effect of saikosaponin b ₁ is improved 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 (51) Int.Cl. ⁵ Identification code Office reference number FI Technical display location A61K 31/70 ADA 8314-4C ADS 8314-4C 47/16 J 7329-4C

Claims (3)

[Claims] 1. A skin external preparation comprising at least one of saikosaponin b ₁ and saikosaponin b ₂ and urea. _2. The external preparation for skin according to claim 1, comprising 0.0001 to 20% by weight of at least one of the saikosaponin b ₁ and the saikosaponin b ₂ . 3. The external preparation for skin according to claim 1, which contains 0.1 to 20% by weight of the urea.