JPH0517332A - Skin medicine for external use - Google Patents

Abstract

PURPOSE:To obtain a skin medicine for external use capable of further improving the 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 combining the saikosaponin b1 and b2 having the aforementioned effects with a saccharide. CONSTITUTION:A skin medicine for external use is obtained by blending at least one of (especially 0.001-20wt.%) saikosaponin b1 and saikosaponin b2 prepared by separating the saikosaponin extracted from a plant such as Bupleuri Radix with a saccharide (e.g. a monosaccharide such as D-glyceraladehyde, an oligosacharide such as sucrose or a polysaccharide such as cellulose in an amount of 0.01-20wt.%). The aforementioned saccharide is blended in an amount of especially preferably 0.5-15wt.%. The saccharide has a bynergistio promoting action on the skin cell proliferation by the saikosaponin b1 or further together with the saikosaponin b2, and the improving effects, etc., on skin roughening can remarkably be improved by blending both together.

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 exists in an external preparation for skin characterized by containing seeds and sugar.

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 gist resides in the external preparation for skin, which is characterized in that the sugar is contained in an amount of 0.01 to 20% by weight in the first or second gist.

The structure 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 disappears and the stimulative effect disappears.

As the sugar of the present invention, for example, monosaccharide, oligosaccharide or polysaccharide is used.

The monosaccharides include, for example, three-carbon sugars such as D-glyceraldehyde and dihydroxyacetone, D-erythrose, D-erythrulose, four-carbon sugars of a D-threose tower, L-arabinose, D-xylose and L. Pentoses such as lyxose, D-arabinose, D-ribose, D-ribulose, D-xylulose and L-xylulose,
D-glucose, D-talose, D-psicose, D-
Galactose, D-fructose, L-galactose,
L-sorbose, D-mannose, D-tagatose and other hexoses, aldoheptose, heptulose and other heptasaccharides,
Octoculose and other octose sugars, 2-deoxy-D-debose, 6-deoxy-L-galactose, 6-deoxy-
Deoxy sugars such as L-mannose, D-glucosamine, D
-Amino acids such as galactosamine, sialic acid, aminouronic acid, and muramic acid; uronic acids such as D-glucuronic acid, D-mannuronic acid, L-guluronic acid, D-galacturonic acid, and L-iduronic acid.

Examples of oligosaccharides include sucrose, gentianose, umbelliferose, lactose, planteose, isoliknoses, α, α-trehalose,
Raffinose, lychnose, umbilicin, and stachyose bell bass course.

Examples of the polysaccharides include cellulose, quince seed, chondroitin sulfate, starch, galactan, dermatan sulfate, glycogen, gum arabic, heparan sulfate, hyaluronic acid, tragacanth gum, keratan sulfate, chondroitin, xanthan gum, mucoitin sulfate, guar gum and dextran. , Keratosulfate, locust bingham, succinoglucan, caronic acid and salts thereof.

In the present invention, at least one of the above sugars
Seeds are blended. The blending amount of these is preferably 0.01 to 20% by weight, and 0.5 to 15% by weight in the total amount of the skin external preparation.
Is more preferable. When it is 0.5% or more, the skin cell proliferation effect is further improved, and when it is 15% by weight or less, the feeling of use is further improved.

As described above, sugar has an action of synergistically promoting 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 Psychosaponin, that is, the effect of improving skin roughness, etc., is significantly 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 surfactant, 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.

Further, the dosage form of the external preparation for skin is arbitrary, and for example, a solubilization system such as lotion, an emulsion system such as emulsion or cream, an ointment, a dispersion liquid and the like can be adopted.

[0019]

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 on healing skin wounds, preventing and improving skin roughness, preventing aging to prevent sagging and loss of skin, and the feeling of use are synergistic by incorporating sugar. 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 to give 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 sugar was further added, and the mixture was cultured for 2 weeks in a CO ₂ -incubator. Then, the cells were fixed and stained, and the number of cell colonies was counted. The results are shown in Fig. 1. The solid line in FIG. 1 is the result when only saikosaponin b ₁ was added to the culture solution, and the broken line (Example)
Is the result when 100 ppm of L-arabinose was further added as a sugar. 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 sugar. Similar results were obtained with saikosaponin b ₂ .

(Wound healing effect) A group of 5 Wistar rats aged 6 weeks 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
0 mg and L-arabinose 50 mg are added to physiological saline solution 0.1.
An aqueous solution prepared by diluting a solution dissolved in ml with physiological saline to 1/1000 was 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. The cutting tension of this section was measured by using Tensilon UTM-4 manufactured by Toyo Sokki Co., Ltd.

The average tension of the saikosaponin b ₁ alone was 470 g / cm, whereas the average tension of the sugar-added one was 510 g / cm, and the wound healing of the saikosaponin b ₁ was achieved by adding the sugar. It turned out that the effect improves. Also, regarding saikosaponin b ₂ ,
An average tension of 505 g / cm was obtained.

[0025] The red blood cells from (stimulatory inhibitory effect) human blood was collected, Psycho saponin b ₁ or saikosaponins b ₁
And L-arabinose (500 ppm) were added and the mixture was allowed to stand 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 the sugar L-arabinose.

(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.

[0028]

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

Skin Roughness Improvement Effect Using the lotions of Samples 1 to 6, 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 by replicating the skin using a replica method using myricin resin and observed with a microscope. Based on the condition of the skin print and the peeling state of the stratum corneum, based on the criteria of Table 2, the skin condition 1 or 2 was evaluated on the left and right sides of the face of each of the 25 panel members. 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.

[0032]

[Table 2]

[0033]

[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.

[0034]

[Table 4] As shown in Tables 3 and 4, the lotion of the present example has an improved effect of improving skin roughness as compared with the sample 6 of the comparative example. Particularly, the sample 1 satisfying claims 2 and 3 has extremely good skin roughness. The improvement effect and high usability were exhibited.

Further, the saikosaponin b ₁ content is 0.0
Although the sample 2 with less than 001% by weight had no irritation, the rough skin improving effect was inferior to the sample 1. It was found that Sample 3 having a saikosaponin b ₁ content of more than 20% showed a good effect of improving rough skin, but showed a sticky feeling. Sample 4, which has an L-arabinose content of less than 0.01%, is inferior in skin roughening improving effect to Samples 1 and 3, and Sample 5, which has an L-arabinose content of more than 20%, is similar to Samples 1 and 3. It was found that, although it shows a good effect of improving rough skin, a sticky feeling appears.

(Examples 2 to 6) The external preparations for skin prepared based on the compositions and manufacturing methods shown in each of the following Examples have improved rough skin improving effect or wound healing effect and are more irritating than conventional examples. Is also suppressed, and sugar is saikosaponin b ₁
It was shown that the above effects of b and b ₂ are synergistically improved.

(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) D-galactosamine 8.0 1,3-butylene glycol 2.0 glycerin 2.0 ion-exchanged water 33.17 (manufacturing method) The oil phase was melted by heating and kept at 75 ° C. This is 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) D-mannuronic acid 5.0 Propylene glycol 3.0 Ion-exchanged water 62.669 Quinceseed extract (5% aqueous solution) 20.0 (production method) ) The oil phase heated and melted at 70 ° C. was added to the 70 ° C. aqueous phase, preliminarily emulsified, and further homogenized by 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 Umbelliferose 5.0 Polyvinyl alcohol 10.0 Polyethylene glycol 3.0 Propylene glycol 7.0 Ethanol 10.0 Methylparaben 0.05 Perfume 0.1. 05 Ion-exchanged water 64.8 (Production method) Polyethylene glycol, propylene glycol, and methylparaben were added to ion-exchanged water and dissolved with stirring. Next, add polyvinyl alcohol, heat and stir,
Psychosaponin b ₁ , umbelliferose, and ethanol in which a fragrance was dissolved were added and dissolved by stirring to obtain a pack.

Example 5 Cosmetic for scalp wt% (Phase A) Psychosaponin b ₁ 0.5 Sucrose 6.0 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 19 .9 Carboxyvinyl Polymer 0.2 (Production Method) Phase B dissolved at 75 ° C was added to Phase A heated to 75 ° C with stirring, and then 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 Hyaluronic acid 3.0 Vaseline 40.0 Stearyl alcohol 15.0 Mokurou 20.0 Polyoxyethylene (10) oleyl 0.5 Alcohol ion-exchanged water 16.5 (Production method) Other components mixed and dissolved in 70 ° C. ion-exchanged water at 70 ° C. were added, the mixture was uniformly emulsified with a homomixer, and after emulsification, cooled to obtain an ointment.

[0042]

INDUSTRIAL APPLICABILITY According to the present invention, that is, by adding a sugar to saikosaponin b ₁ or saikosaponin b ₂ , the cell-proliferating action of saikosaponin is improved and its stimulative property is suppressed. As a result, rough skin prevention and improvement effect,
It is possible to provide a skin external preparation having a high skin aging prevention effect or a wound healing effect and 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 sugar.

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

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁵ Identification code Office reference number FI Technical indication location A61K 31/70 ADS 8314-4C 47/26 J 7329-4C 47/36 J 7329-4C

Claims (3)

[Claims] 1. An external preparation for skin, comprising at least one of saikosaponin b ₁ and saikosaponin b ₂ and a sugar. _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 0.01 to 20% by weight of the sugar.