JPH01275511A - External drug for skin - Google Patents

Abstract

PURPOSE:To obtain an external drug for skin, exhibiting excellent preventive and amelioration effect against any kind of chapped skin and having high safety and stability, by compounding uric acids or betaines as active component. CONSTITUTION:The objective external drug for skin, useful as a facial cosmetic, foundation, etc., and effective not only in preventing and ameliorating chapped skin but also in increasing the turn-over rate of cuticle and preventing the aging of the skin can be produced by using one or more kinds of compounds selected from (A) uric acid or its derivative (a uric acid salt such as sodium urate, N-alkyl-modified uric acid such as 3-N-methyluric acid, 3-N-lauryluric acid or 9-N-butyluric acid, uric acid glycoside such as 3-N-ribosyluric acid, etc.) and (B) betaines (e.g. homaline, trigoneline, lysine betaine or taurobetaine) or their salts as essential components and compounding the components in an amount of 0.001-0.5wt.% each.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to a skin preparation for external use, and particularly to a skin preparation for use in preventing and improving rough skin.

[Prior Art] In general, external skin preparations include cosmetics, pharmaceuticals, quasi-drugs, etc. In particular, external skin preparations aimed at preventing and improving rough skin have conventionally been made using raw materials extracted from natural products. It is used in combination with various raw materials.

That is, for example, extracted extracts such as loofah extract and placenta extract, natural polymers such as quince, proteins such as collagen, polysaccharides such as chitin, single amino acids such as arginine, skin activators such as vitamin E, or glycerin, etc. Moisturizers and the like are actively used in external skin preparations for the purpose of preventing and improving rough skin, and have continued to this day.

[Problem to be solved by the invention] Ai Atsushi Technique Example Dish Cup However, these conventional substances that have been used to prevent and improve skin roughness are not suitable for skin roughness caused by a low amount of sebum and moisture in the facial skin. It has been used for the prevention and improvement of
f a 5 scientific method for
C1assification of Facial
5kin Types, Hiroko Kumag
ai et al: VIIICongreso
International de 1a 1. F,
S, C, C, vol. 1-19. 1984), the prevention of another type of skin roughness, that is, the type of skin roughness with a large amount of sebum, indistinct skin mounds and skin folds, and exfoliation. There was a problem in that no improvement effect was observed at all, and therefore a sufficient effect could not be expected for the normalization of a wide range of skin types.

The present invention has been made in consideration of the problems of the prior art described above, and its purpose is to provide an excellent prevention and improvement effect on all kinds of skin roughness, as well as excellent safety and stability. The purpose of the present invention is to provide external preparations for the skin.

In order to achieve the above object, the present inventors have conducted extensive research in order to obtain a substance that is effective in preventing and improving all types of skin roughness and is also satisfactory in terms of safety and stability. As a result, external skin preparations obtained by blending one or more compounds selected from the group consisting of uric acid and its derivatives, or betaines and their salts have been shown to be effective in preventing and improving all types of skin roughness. The present inventors have discovered that the present invention is extremely useful for patients with disabilities, and have completed the present invention.

[Means for Solving the Problems] That is, the invention according to claim 1 is an external skin preparation characterized by containing one or more compounds selected from the group consisting of uric acid and its derivatives.

Moreover, the invention according to claim 2 is an external skin preparation characterized by containing one or more compounds selected from the group consisting of betaines and their salts.

The present inventors also recognized that blending uric acid and its derivatives, or betaines and their salts not only prevents and improves rough skin, but also accelerates the turnover rate of the stratum corneum, and has developed the present invention. It is being developed.

In other words, it has been observed that in aging skin, the turnover rate of the stratum corneum slows down due to a decline in cell metabolism, and from this fact, substances that increase the turnover rate without stimulation may regenerate cell metabolic function. It is believed that the skin external preparation of the present invention is also useful for preventing aging, as it is believed that it can rejuvenate aging skin.

Hereinafter, the configuration of the present invention will be explained in detail.

Examples of uric acid and its derivatives used in the present invention include uric acid, uric acid or its salts such as sodium urate, potassium urate, ammonium urate, 3-N-methyluric acid, 3-N-lauryluric acid, 7-N- N-alkyl uric acid modified products such as butyluric acid, 1-N-ethyluric acid, 9-N-lauryluric acid, 3.7-N-dimethyluric acid, 3-N-ribosyluric acid,
Examples include uric acid glycosides such as 9-N-glycodyluric acid.

These uric acid, its salts, and uric acid glycosides are also found in serum, and recently the relationship between the average survival age of mammals and serum uric acid concentration, and the relationship between cancer incidence and serum uric acid level have been studied. Although this substance is attracting attention, there are currently no examples of its application for external use.

The amount of uric acid and its derivatives incorporated into the skin external preparation is not particularly limited, but the amount is usually 0.001 to 0.5% by weight based on the total amount of the external preparation.

If it is less than 0.001% by weight, the effect of preventing and improving skin roughness and increasing the turnover rate of the skin's stratum corneum tends to be poor; There is no hope for an increase.

The betaines used in the present invention include lysine betaine, ornithine betaine, homarin, trigonelline, alanine betaine, taurobetaine, carnitine, stachydrine,
Glutamate betaine, phenylalanine betaine, γ
-Butyrobetaine, betaine and the like.

These betaines or their salts are found in seaweed, fish, and crustaceans, but their physiological significance is not necessarily clear, and there are currently no examples of their use as external preparations. I can't find it.

The amount of such betaines and their salts added to the skin FM external preparation is not particularly limited to the total amount of the external preparation, but the amount usually is about 0.001 to 5% by weight.

If it is less than 0.001% by weight, the effect of preventing and improving skin roughness and increasing the turnover rate of the skin's stratum corneum tends to be poor.On the other hand, if it is added more than 5% by weight, the effect will not increase significantly. I can't hope.

The uric acid and its derivatives, or betaines and their salts of the present invention are easily soluble in water and insoluble or poorly soluble in oils and fats and organic solvents, but they can be incorporated into external skin preparations even in a suspended state. and has no effect on the effect.

The external skin preparation of the present invention is suitable for use as a skin cosmetic, and contains common ingredients that are included in general skin cosmetics, such as oil, water, surfactants, humectants, lower alcohols, and thickeners. , a chelating agent, a pigment, a preservative, a fragrance, etc. can be added as appropriate.

The external skin preparation according to the present invention broadly refers to those used on the skin, and is typified by facial cosmetics such as lotions, milky lotions, creams, and packs, and skin cosmetics such as foundations.

It is also possible to combine uric acid and its derivatives, betaines and their salts.

[Example] Next, the present invention will be explained in more detail with reference to Examples.

Note that the present invention is not limited to this.

Moreover, the blending amount is shown in weight%.

and its - [ First, a comparative test was conducted on the skin external preparation according to the present invention using uric acid and its derivatives.

Table 1 shows the composition of the cream used in the comparative test.

Table 1 First, phase B listed in Table 1 was heated to 70
It was kept at ℃. Phase A was added to this, and after preliminary emulsification, it was uniformly emulsified with a homomixer, and then slowly cooled to create a cream (Examples 1 to 3).
4. Comparative Example) was prepared.

Panels with each cream in Table 1 (women between 22 and 32 years old)
It was applied to the right half of five people's faces twice a day for two consecutive months.

After the test was completed, the skin at the applied areas on both the left and right sides of the face was measured using the skin impedance and replica method, and the moist feeling and fineness of the skin were observed.

Skin impedance was measured using a high-frequency resistance-capacitance measurement device devised such as pressure intensification. This device consists of a main body that includes a 3.5 MHz high-frequency current generator and a resistance and capacitance detector, a 1 cm long cord, and a cylindrical electrode attached to the tip. The electrodes are concentric and consist of a center electrode with a diameter of 1 mm and an outer electrode with an inner diameter of 4 mm placed at a distance of 1.5 mm. When the electrodes are applied to the skin, high frequency waves flow through them, but they are in the order of a few μA. The panel doesn't feel any discomfort. When this electrode is lightly touched to the detected part, the resistance rises rapidly to a certain value within one second.

The reciprocal of this resistance is the conductance
ce), and its unit is μΦ. This conductance is almost proportional to the amount of moisture on the skin surface, and the higher the moisture content of the skin, the better the moist feeling of the skin. Therefore, the moist feeling of the skin can be quantitatively evaluated by increasing conductance. It was to be.

Table 2 compares the conductance in the skin impedance on the face of the panel using the cream according to the second example with the facial application site of the panel using the cream according to the comparative example.

The conductance of the application site (right face) of the panel using the cream containing 10-4% by weight of 3-N-ribosyluric acid is significantly higher than that of the application site on the face of the panel using the cream of the comparative example above. Help students understand that it can be obtained as a numerical value. This shows that the cream that gave a more moist feeling to the skin was the cream according to the second example.

Table 2 (blank below) The conductance of all panels was measured in the same manner. 3-
The conductance of the right face of the panel using the cream containing N-ribosyluric acid was compared with the conductance of the left face of the panel using the cream of the comparative example, and if it increased by 70% or more, it was considered to be significantly effective, and 50% or more 70%. An increase of less than 50% is considered somewhat effective, and an increase of 50% or less is considered no effect. The results are shown in Table 3.

Table 3 On the other hand, the fineness of skin texture was observed using the replica method.

A surface image of the skin was taken by bringing silicone rubber into close contact with the skin, and then an inverted image was obtained by pouring epoxy resin into the silicone rubber. The skin condition was examined by scanning the surface of this inverted image with a surface roughness tester. It was determined that the greater the undulations of the skin surface, the finer the skin texture.

In the same way, replica images of the faces of all panels were taken and the left and right sides of the face were compared. If the right side of the face had clearly larger undulations, it was determined that there was an effect, and if there was no obvious difference, it was determined that there was no effect. The results are summarized in Table 3 above.

It was found that 3-N-ribosyluric acid added to the cream exerts an excellent effect on improving the moist feeling and fineness of the skin almost in proportion to the concentration added.

In addition, the turnover of the stratum corneum was measured using the Danzyl chloride method. That is, an ointment containing 5% by weight of danzyl chloride in white petrolatum is prepared and applied to the skin of the forearm of the panel for 24 hours to allow danzyl chloride to penetrate and bind to the stratum corneum. Thereafter, the cream was applied to the same area at least twice a day (at least in the morning and evening), the fluorescence of danzyl chloride was measured every day, and the number of days until the fluorescence disappeared was defined as the turnover of the stratum corneum of the skin.

The measurement results are shown as the average value of the number of days for each panel.

The normal turnover of the stratum corneum of the skin is 14 to 1
It takes about 6 days, but in aging skin it can last around 18 days. - As is clear from Table 3, it can be seen that when the example cream is used, the turnover is shorter than in aged skin, and the cell metabolic function is activated.

Other examples are shown below. As a result of use tests similar to those described above, both showed excellent effects in preventing and improving rough skin, and it was observed that the turnover time was shortened.

Uratane■5 8g of 95% ethyl alcohol and 0 polyvinylpyrrolidone
, 05 g, 0.1 g of L'yl alcohol, 1.2 g of polyoxyethylene monooleate), 0.2 g of perfume, 0.1 g of paraoxybenzoic acid methyl ester, a small amount of antioxidant, and a small amount of pigment were mixed and dissolved. Add this to 0.02g of sodium urate, 5g of glycerin, 85'g of purified water, and 33'g.
A lotion with the effect of improving rough skin was obtained by stirring and adding it to the solution.

Back week 1 Cetyl alcohol 1.2g, Squalane 10g1 Vaseline 2g1 Paraoxybenzoic acid ethyl ester 0.2g,
1 g of glycerin monostearate, 1 g of polyoxyethylene (20 mole addition) monostearate, 1 g of polyoxyethylene (20 mole addition) monooleate, and 0.1 g of fragrance were heated and mixed and dissolved at 70°C, and 3-N-
0.1 g of methyluric acid, 5 g of dipropylene glycol, 2 g of polyethylene glycol, 0.2 g of reethanolamine, and 76.2 g of purified water were heated and dissolved at 75°C. Both were mixed and emulsified, and the emulsified particles were prepared using a homogenizer and cooled to obtain a W2O type emulsion having an effect of improving rough skin.

0. Olg, dipropylene glycol 5g 1 triethanolamine 0.5g, powder coloring 10g 1 fragrance 0.
Ig, 0.2 g of paraoxybenzoic acid ethyl ester, a small amount of antioxidant, and 60.69 g of purified water were mixed, uniformly dispersed, and heated to 75°C. A mixture of 1.2 g of stearic acid, 0.3 g of cetyl alcohol, 20 g of liquid paraffin, and 2 g of polyoxyethylene oleate was mixed and dissolved into this mixture, and the mixture was kept at 75°C. The mixture was gradually added to react and emulsify, and the mixture was stirred while cooling. I obtained a foundation that has the effect of preventing rough skin.

Inurimasu 1: 8 g of 95% ethyl alcohol, 5 g of 1,3-butylene glycol, 1.5 g of polyoxyethylene (addition of 20 moles) monooleate, 0.05 g of 7-N-butyluric acid, 0.2 g of paraoxybenzoic acid ethyl ester, Fragrance 0. I
g, mix and dissolve a small amount of dye, add polyvinyl alcohol 1
0 g 1 polyethylene glycol 2000 1 g and 74.15 g of purified water were heated and dissolved at 80° C., and the mixture was stirred and added, and the mixture was cooled to room temperature to obtain a dry film-type pack having an effect on improving rough skin.

Yuko Kyo 1 5g of 95% ethyl alcohol, 1.2g of polyoxyethylene sorbitan monooleate, O sodium alginate
, Ig, sodium chondroitin sulfate 0.2g, hyaluronic acid 0.1g, vitamin E acetate) 0. Ig, glycyrrhizic acid monoammonium salt 0. Mix Ig, paraoxybenzoic acid ethyl ester O,Ig, 0.05 g of 3-N-lauryl uric acid, and an appropriate amount of pigment, and stir and add this to a mixture of 5 g of glycerin and 88.05 g of purified water. I obtained a beauty serum that has an improving effect.

Betaines and Their Salts Next, a comparative test was conducted on the skin external preparations of the present invention using betaines and their salts.

Table 4 shows the composition of the creams used in the comparative test.

The cream manufacturing method and testing method shall be the same as when using urea and its derivatives.

(Margin below) 1ha 110 11 12 13 Table 4 Table 5 shows the conductance in the skin impedance on the face of the panel using the cream of the 11th example, and the facial area of the panel using the cream of the comparative example. This is a comparison.

The conductance of the application site (right face) of the panel using the cream containing 10-4% by weight of Homarin was significantly higher than that of the application site of the panel using the cream of the comparative example above. be understood.

This shows that the cream that gave a more moist feeling to the skin was the cream according to the eleventh example.

The conductance of all panels was measured in the same manner as in Table 5. The conductance of the right face of the panel using the cream containing Homarin was compared with the conductance of the left face of the panel using the cream of the comparative example, and the results are shown in Table 6.

Table 6 On the other hand, the fineness of skin texture was observed using the same replica method as described above. The results are summarized in Table 6.

Homalin added to the cream was found to have an excellent effect on improving skin moisturization and fineness in proportion to the added concentration.

In addition, the turnover of the stratum corneum was measured using the Danzyl chloride method.

The measurement results are shown as the average value of the number of days for each panel.

As is clear from Table 6, it can be seen that when the Example cream was used, the turnover was shorter than in aged skin, and the cell metabolic function was activated.

Other examples are shown below. As a result of use tests similar to those described above, both showed excellent effects in preventing and improving rough skin, and it was observed that the turnover time was shortened.

Fruit 1” LLA 95% ethyl alcohol 8g and polyvinylpyrrolidone 0
．． 05g, oleyl alcohol 0. Ig.

Polyoxyethylene monooleate 1.2g, fragrance 0.
2g of paraoxybenzoic acid methyl ester, Ig, a small amount of antioxidant, and a small amount of pigment were mixed and dissolved. This is Homarin O, 001g, glycerin 5g and purified water 85.3g.
A lotion having an effect on improving rough skin was obtained by stirring and adding the mixture to 49 g of the solution.

Hidara masu 11 1.2 g of cetyl alcohol, 10 g of squalane.

Vaseline 2g 1 paraoxybenzoic acid ethyl ester 0.
2 g, glycerin monostearate 1 g 1 polyoxyethylene (20 mole addition) monostearate 1 g polyoxyethylene (20 mole addition) monooleate Ig, and fragrance 0. Ig was heated and mixed and dissolved at 70'C, and trigonelline was added in the same manner. Ig.

Dipropylene glycol 5g 1 polyethylene glycol 1500 2g, triethanolamine 0゜2g,
76.2 g of purified water was heated and dissolved at 75°C. Both were mixed and emulsified, and the emulsified particles were prepared using a homogenizer and cooled to obtain a W2O type emulsion having an effect on improving rough skin.

Lined blood plate 11 Lysine betaine 0.05g, dipropylene glycol 5
g1 Triethanolamine 0.5g, powder colorant Lo
g, 0.1 g of perfume, 0.2 g of paraoxybenzoic acid ethyl ester, a small amount of antioxidant, and 60.65 g of purified water were mixed, uniformly dispersed, and heated to 75°C. A mixture of 1.2 g of stearic acid, 0.3 g of cetyl alcohol, 20 g of liquid paraffin, and 2 g of polyoxyethylene oleate was mixed and dissolved into this mixture and kept at 75°C, and the mixture was gradually added to react and emulsify, followed by stirring while cooling. I obtained a foundation that has the effect of preventing rough skin.

1 unit 95% ethyl alcohol 8g 1.3-butylene glycol 5g 1 polyoxyethylene (addition of 20 moles) 1.5g monooleate, taurobetaine 0.2g, paraoxybenzoic acid ethyl ester 0.2g, fragrance 0.1g , mix and dissolve a small amount of pigment, and add 10 g of polyvinyl alcohol.
1g of polyethylene glycol 2000 and 7 parts of purified water
4.18 g of the solution was stirred and added to a solution heated and dissolved at 80° C., and the mixture was cooled to room temperature to obtain a dry film-type pack having an effect on improving rough skin.

Maruyugo 11 95% ethyl alcohol 5g, polyoxyethylene sorbitan monooleate 1.2g, sodium alginate 0
．． 1g, sodium chondroitin sulfate 0.2g, hyaluronic acid 0.1g, vitamin E acetate 0.1g1 glycyrrhizic acid monoammonium salt 0.1g, paraoxybenzoic acid ethyl ester 0.1g, homarin 0.05
g and an appropriate amount of pigment were mixed, and the mixture was stirred and added to a mixed solution of 5 g of glycerin and 88.05 g of purified water to obtain a beauty serum having an effect on improving rough skin.

[Effects of the Invention] Since the present invention is configured as described above, it produces the effects described below.

According to the skin external preparation according to claim 1, since it contains uric acid and its derivatives, it is extremely effective in preventing and improving all kinds of skin roughness.

According to the skin external preparation according to claim 2, since it contains betaines and their salts, it is extremely useful for preventing and improving all kinds of skin roughness.

Claims (2)

[Claims] (1) An external skin preparation characterized by containing one or more compounds selected from the group consisting of uric acid and its derivatives. (2) A skin external preparation characterized by containing one or more compounds selected from the group consisting of betaines and their salts.