JPS61289013A - Skin external agent - Google Patents

Abstract

PURPOSE:A skin external agent, particularly cosmetic, containing phopholipid, sterol and glycolipid in a specific proportion, capable of keeping water on the skin surface and having improved water retaining function for giving moisture always to the skin. CONSTITUTION:A skin external agent containing three components of (A) phospholipid, e.g. phosphatidyl choline, phosphatidyl ethanolamine or sphingophospholipid, (B) a sterol, e.g. cholesterol, sitosterol, stigmasterol, cholestanol, etc. and (C) a glycolipid, e.g. sphingophospholipid or glyceroglycolipid, etc., at 50/50-80/20, preferably 60/40-70/30 weight ratio of the components (A) to (B) and 70/30-95/5, particularly 75/25-85/15 weight ratio of the total of the components (A) and (B) to component (C) in an amount of 0.05-90wt%, particularly 0.05-20wt% in the external agent. When the agent is applied to the skin, the amount of the three component mixture reaches 0.5-20wt%, preferably 1-5wt% based on the total amount of the residue, a liquid crystal in the state of incorporating water is formed to give most improved water retaining and blocking effect.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an external skin preparation, particularly a cosmetic, which retains moisture on the skin surface and has an excellent water-retaining function that constantly moisturizes the skin. More specifically, the present invention contains phospholipids, sterins, and glycolipids as active ingredients, thereby providing useful effects on diseases that are mainly caused by skin dryness, such as cracks and chapped skin. The purpose of the present invention is to provide a skin preparation for external use and a cosmetic that prevents skin aging and imparts moisture, smoothness to the skin, and a beautiful appearance to the skin.

Traditionally, cracks, chapped skin, etc. are generally caused by transepidermal water loss (T ,W.

This is a symptom that is induced when the epidermis (especially the stratum corneum) moisture is drawn out due to an increase in the epidermis (abbreviated as L) or due to physical causes (such as washing).

On the other hand, a type of keratosis called keratosis is a condition in which the skin becomes dry and cracked, giving it a scaly appearance, and this condition is said to be particularly aggravated during the dry winter season. Also,
Even under normal conditions, a condition in which the water content of the stratum corneum is about 10% depending on age and constitution is called dry skin, and senile xeroderma is a suitable example. As mentioned above, the moisture in the epidermis stratum corneum 1 normally combines with the constituent components of the stratum corneum to maintain normal skin function, but due to environmental changes (low temperature, low humidity), aging, etc. A decrease in water content is closely associated with skin irritation, where the skin becomes dry, brittle, and cracked. and, .

In order to deal with these symptoms, it is necessary to prevent a decrease in the water content of the stratum corneum and maintain normal skin function, and various methods have been studied.

Conventionally, such methods include a method of suppressing D, W, and L by using an occlusive agent, and a method of increasing the skin hydration effect by using a humectant.

As an example of the former, Vaseline ointment is well known, and Japanese Patent Application Laid-Open No. 1983-1989. As seen in No. 86630, there was a method of blending a sebum-like composition and covering the skin surface to prevent dryness, but in these cases, in order to increase the effect, the use of m
(Amount of application) has to be increased, which results in an unpleasant feeling such as oiliness and stickiness during use, and conversely, if less is used, the occlusion property is weak and it does not last long. there were.

On the other hand, examples of the latter include polyhydric alcohols such as ethylene glycol, propylene glycol, 1,3-butylene glycol, and glycerin, and humectants such as PCA-soda, which have good compatibility with water, but Its own water retention capacity is not very high, and in low humidity conditions, rather than retaining moisture in the skin, moisturizers actually draw moisture from the skin (especially noticeable with glycerin), and in high humidity conditions, they absorb moisture from the outside air. It has a fatal flaw: it gives a sticky and unpleasant feeling when used, and on the other hand, if the amount used is reduced, the effect is weak and not long-lasting.

Therefore, the present inventors conducted intensive research in order to solve the drawbacks of the conventional methods mentioned above and find a substance and dosage form with high water retention function. It was discovered that when blended into external use bases or cosmetic bases at a certain content ratio, it forms a water-containing liquid crystal state on the skin, resulting in a product with excellent occlusive properties and water retention properties. , which completed the present invention.

In other words, the present invention provides (a>phospholipid as a component, (b)
Contains three components, sterine as a component and glycolipids as component (c), in a total amount of O, OS ~ 90W%, and the above (
The weight ratio of components a)/(b) is in the range of 50,150 to 80/20, and the weight ratio of the above (a>+ (b)/(c) components is in the range of 70/30 to 9,515. The present invention relates to a skin preparation for external use, which is characterized by:

The present invention will be explained in detail below.

Known phospholipids that can be used in the present invention can be used as they are, and examples of such phospholipids include phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylglycerol, phosphatidylinositol, and sphingophospholipids. Of course, analogs of these or compositions containing these, such as soybean lecithin, egg yolk lecithin, corn lecithin, hydrogenated lecithin, and lipids extracted from living organisms, are also included in the phospholipids applicable to the present invention. It goes without saying.

In the present invention, the above-mentioned phospholipids are used alone or in combination of two or more.

Next, known sterins can be used for the present invention, such as cholesterin, sitosterin such as β-sitosterin, stigmasterin, lanosterin, campesterin, ergosterin, cholestanol, Thymosterin, dihydro-γ-
sitosterin, β-sitostanol, cholestanol,
Episterin, celebisterin, fecosterin, 5-
Examples include dihydroergosterin, 24-dehydroergosterin, cholesterin, sargasterin, α-spinasterin, etc., and esters derived from these.Of course, alkyl esters of lanostadienol such as similar norisostearates have liquid crystal forming ability. Because of its weak strength, it cannot be used in the present invention. In the present invention, the above-mentioned sterins may be used alone or in combination of two or more.

Next, known glycolipids can be used as the glycolipids that can be applied to the present invention, and include carbohydrates bound to fatty acids or aliphatic alcohols. For example, such things include:
Examples include sphingoglycolipids (glycosphingolipids) containing sphingosine bases, phytoglycolipids containing phytosphingosine bases, glyceroglycolipids containing glycerol, and other glycolipids. xosylceramide (cerebroside), sphingoplusuroside ester), D-galactosyl (1→4) D-glycodyl (1
→) ceramide, dihexosylceramide such as D-galactosyl (1 → 4) D-galactosyl (1 →) ceramide,
D-galactosyl (1 → 4) D-galactosyl (1 → 4
) Trihexosylceramide such as D-glucosyl (1→)ceramide, galactosyl-ceramide@acid ester (cerebroside Fi7ts or sulfatide), dihexosylceramide sulfate ester, and N-acetylgalactosamine (1→3) D -galactosyl (1→4) galactosyl (1→4) D-glucosyl (1→) ceramide [globoside I], N-7 cetylgalactosamine (1→
4) D-galactosyl (1→4) D-glucosyl (1→
) Ceramide, D-galactosyl (1→3) N-7 cetylgalactosamine (1→4) D-galactosyl (1→4)
gluco, syl(1→)ceramide, D-galactosyl(1
→3) D-galactosyl (1 → 3) N-7 cetylglucosamine (1 → 3) D-galactosyl (1 → 4) D-glucosyl (1 →) Ceramide, etc.→) Ceramide, N-7 cetylneuraminic acid (2 →3) In addition to hematocytes such as D-galactosyl (1→) ceramide, and neutral sugars, there are gangliosides containing both sialic acid and hexosamine. Phytoglycolipids have a basic structure consisting of ceramide-phosphoric acid-inositol-oligosaccharides, and glyceroglycolipids include glucosyl diglyceride, heptgalactosyl diglyceride, digalactosyl diglyceride, and the like. Of course, in addition to the above-mentioned glycolipids, analogs thereof or compositions containing these, such as glycosphingolipids and glycolipids extracted from living organisms, can also be used. In the present invention, the above-mentioned glycolipids are used alone or in combination of two or more.

Next, the amounts of the three components (a), (b), and (c) mentioned above in the present invention, that is, phospholipids as the (a) component, sterins as the (b) component, and glycolipids as the (c) component are as follows. The total amount is generally in the range of 0.05 to 90% by weight, preferably 0.05 to 20% by weight, although it may vary widely depending on the dosage form of the applied skin preparation or cosmetic. That is, the three-component mixture of (a), (b), and (c) above has a high ability to form liquid crystals in a form that incorporates water when mixed with water, and therefore has a high water retention ability on the skin after application. I'll send it out.

In order to form such a preferable liquid crystal, the above (a)
>>(b) The weight ratio of component is approximately 50150 to 80/
The range is preferably 20, 60/40 to 70/
A range of 30 is most preferred. For the same reason, it is desirable that the weight ratio of the components (a) + (b)/(c) is approximately in the range of 70/30 to 9515;
A range of 75/25 to 85/15 is most preferred.

On the other hand, raw materials other than water used in the present invention include oils and fats that are usually applied to external skin preparations and cosmetics, surfactants, moisturizing agents containing polyhydric alcohols, various medicinal ingredients, and preservatives. Most formulations, such as agents, are included, and are appropriately selected and adjusted depending on the purpose, use, dosage form, etc. However, the important point here is that the formulation system does not inhibit liquid crystal formation after application of the product to the skin. , solid fats such as stearyl alcohol, beeswax, microcrystalline wax, liquid paraffin, squalane, soybean oil,
When comparing liquid fats such as olive oil and octyldodecyl myristate, liquid fats are particularly preferred, and when blending a combination of liquid fats and solid fats, it is more effective to use liquid fats rich in liquid fats. be. On the other hand, examples of polyhydric alcohols include ethylene glycol, propylene glycol, 1,3-butylene glycol, glycerin, diglycerin, polyethylene glycol, and polyglycerin, but considering the formation of liquid crystals,
In particular, glycerin or a mixture of glycerin and another polyhydric alcohol is more preferred.

As mentioned above, in the case of external skin preparations and cosmetics composed of the three-component mixture (a>, (b), and (c)), oils and fats, polyhydric alcohol, water, etc., in the prescription system, After application to the skin, as volatile substances (especially water) evaporate, the content ratio of the 3-component mixture (a), (b), and (c) increases by 0.5 to 20% by weight based on the total weight of the remaining material. 4% preferably 1-5
When it reaches the 70% range, it forms a liquid crystal that incorporates water and has the best water retention and occlusion effects.

Here, in order to investigate the relationship between the mixing ratio of the three-component mixture (a>, (b), and (c)) and the moisture retention function, the following test was conducted and the results are shown in Table 2.

Test method: As samples, compositions A to E were prepared as shown in Table 1 below to make them uniform, and each of these was swollen by adding water equal to the amount of mold 4 (80% water content by weight). 1. Weigh out 0 g each into a petri dish with a diameter of 3 cm, and place it at a temperature of 35°C per household vs. temperature PI-(=50
%, the water content was measured over time until 11 hours later, and the water retention rate was calculated using the following formula using the average value of three times. The moisture content was measured using a trace moisture meter AQ-3 manufactured by Hiranuma Sangyo.

Moisture retention rate (%) Moisture content in Keijikan samples Table-1 Table-2 As described above, the above (a) and (b) applied to the present invention
, (c) The three-component mixture forms a water-containing liquid crystal state and therefore has excellent water retention ability. In order to ensure sufficient liquid crystal formation, the above (
As mentioned above, the blending ratio of the three components a), (b), and (c) is regulated by the layer balance problem. Therefore, as in Sample E shown in Tables 1 and 2, the above (a
), (b), (c) even if it contains three components,
If these compounding ratios are outside the range described in claim 1, liquid crystal formation will not be sufficient;
It is not included in the present invention.

Next, in order to evaluate the above-mentioned 3-component mixture (a), (b), and (c) and the skin external preparation of the present invention, we will examine the test results conducted by the following methods 1) to 4) and the test results of 5 people. The results of usage tests conducted by female panelists are shown in Tables 3 to 6 and Figure 1.

1) Hygroscopicity evaluation/sample: Phosphatidylcholine:cholesterol:cerebroside was 50% as a mixture of the three components (a), (b), and (c) above.
:30:20 weight ratio (hereinafter referred to as lipid mixed crab) and glycerin and propylene glycol were used as comparative amounts.

・Method: Weigh 5 g of each of the above samples into a petri dish with a diameter of 3 cm, set this in a desiccator adjusted to relative humidity RH = 98%, and measure the weight of the sample after 24 hours and 48 hours. The moisture absorption rate *1) was calculated.

Moisture absorption rate *1) (%) 5 (g) 2) Moisture retention ability evaluation/sample: In place of the ointment of the present invention shown in Example 1 below, and as a comparative amount, in place of the lipid-mixed crab in the ointment of Example 1 below. , an ointment containing sorbitan monostearate (A>) and an ointment containing lecithin (B) were used.

・Method: Weigh out 5 g of each of the above samples into a petri dish with a diameter of 3 cm, set this in a furan mold containing 5% RNA at 35°C, and after 1 hour, 3 hours, 5 hours, and 7 hours. Measure the weight of the sample after a period of time and determine the water transpiration rate from the soft II system*
2) was calculated.

Moisture transpiration rate *2) (%) 0.39 (g> 3) Obstruction evaluation/sample: The same inventive product as used for water retention evaluation and comparative amounts (A> and (B)) were used. .

・Method: Put 10 g of water in a deep Petri dish with a diameter of 35 mm, cover with a cap paper (Toyo Kuchishi Nα5C), and uniformly apply a certain amount (0, 2 g) of each of the above samples onto the cap paper. , 35°C
After 15 hours of standing, the remaining amount of water (g) was measured and the blockage rate*
3) was calculated.

Occlusion rate*3) (%) 4) Evaluation of stratum corneum water content and use test Evaluation/sample: The same inventive product as used for evaluation of water retention ability and comparative amounts (A) and (B) were used.

・Method: Five female panelists were asked to apply each of the above samples on the inner side of their forearms, and the sensation of use (sensory evaluation) and changes in water content in the stratum corneum over time were measured using an impedance meter method. The average values (n=5) were graphed. (1st
See figure> Impedance meter method*4).

By measuring the conductivity (μΩ) in the stratum corneum of the skin,
Measures the amount of water in the stratum corneum.

Measuring equipment: 1. B, S company impedance meter model IB-355, measurement conditions: 20'C, RH = 50%.

Table-3 Moisture absorption rate (%) (Hereinafter in the margin) Table-5 Occlusion rate (%) (Hereinafter in the margin) As shown by the results in Tables-3 to Table-6 and Figure 1, the lipid mixture according to the present invention absorbs moisture. In addition, the product of the present invention, which contains the same, has low water evaporation, so it has good water retention, has good occlusive properties, maintains the moisture content of the stratum corneum for a long time, and has a good feeling of use, such as stickiness. It is clear that there is nothing better.

Examples are shown below. Incidentally, the blending ratio is expressed in % by weight.

Example 1. Ointment Liquid Paraffin 65 Vaseline
5P, O, E, (20>
6 Sorbitan Monostearate Beeswax 3 Lipid Mixture ■
3 Glycerin 10 Preservatives
0.2 water
7.8 Example 2
．． Cream Stearic Acid 2 Stearyl Alcohol 1 Reduced Lanolin
1,8 squalane
10 octyldodecanol 6P, O
,E, (25) 3 cetyl ether glyceryl monostearate 2 phosph 1 tidyl ethanolamine 0.6 β-sitosterol
0.3 ganglioside
0.3 Fragrance 0
．． 3 Preservative 0.2 Glycerin 5 Water
67.5 Example 3. Emulsion P, O, E, addition (50) 1 Hydrogenated castor oil coconut oil fatty acid monoglyceride 1 Purified soybean lecithin 0.3 Cholesteryl isostearate 0.2 Cerebroside sulfate ester
0.1 Oleic acid triglyceride 7,
5 Glycerin 2.5 Fragrance
0.2 preservative 9 preservative
0.2 water
87.1 Example 4. Lotion' P, O, E, addition (60) 0.5 hydrogenated castor oil phosphatidylserine 0.1 cholesterol 0.06 monogalactosylglycerite 0.04 glycerin
5 citric acid
0.1 Sodium citrate 0.2 Ethanol 10 Fragrance
0.1 preservative
0.1

[Brief explanation of the drawing]

Figure 1 shows the constant time (
The results show the conductivity (μΩ) in the stratum corneum of the skin after 30 minutes, 60 minutes, 90 minutes, 120 minutes, 180 minutes), where X is the product of the present invention and Y is the comparative example (A >, Z is a comparative example (B). Patent applicant Pola Chemical Industries, Ltd. Figure 1 Time (minutes) Procedural amendment (Jiri May 1985 298 1. Indication of case 1985 Patent application no. No. 130784 2. Title of the invention: Skin preparation for external use 3. Relationship with the person making the amendment Patent applicant address: 648-4 Yayoi-cho, Shizuoka City, Shizuoka Prefecture Date of amendment order: Invention 5. Contents of Amendment No. 66 (1) The statement "the present invention" on page 10, line 9 of the specification is corrected to the statement "external skin preparation of the present invention." (2) Specification No. Change the description of “Amount” on page 10, line 12 to “
The description has been corrected to "Content". (3) “Relative temperature PH = 50%” on page 13, line 12 of the specification
" will be corrected to "Relative humidity RH = 50%." □ Above □

Claims (1)

[Scope of Claims] 1) A total of 0.0% of the three components: phospholipids as component (a), sterins as component (b), and glycolipids as component (c).
05 to 90% by weight, and the weight ratio of the above (a)/(b) components is in the range of 50/50 to 80/20, and the above (a) + (b)/(c) components The weight ratio is 70/
An external preparation for skin, characterized in that the ratio is in the range of 30 to 95/5. 2) The above phospholipid is phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylglycerol, phosphatidylinositol,
The skin external preparation according to claim 1, which is one or a mixture of two or more selected from sphingophospholipids and the like. 3) The above-mentioned sterins include cholesterin, sitosterin such as β-sitosterin, stigmasterin, lanosterin, campesterin, ergosterin, coprostanol, thymosterin, dihydro-γ-sitosterin, β-sitostanol, cholestanol, episterin, cerebisterin, and fecosterin. , 5-dihydroergosterine,
The skin external preparation according to claim 1, which is one or a mixture of two or more selected from 24-dehydroergosterin, corbisterin, sargasterin, α-spinasterin, etc., and esters derived therefrom. 4) The skin external preparation according to claim 1, wherein the skin external preparation is a cosmetic.