JPH0457641B2 - - Google Patents

Description

[Detailed description of the invention]

TECHNICAL FIELD 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 cures cracks and chaps by incorporating a lipid mixture with a water-retaining function obtained from the brain tissue of mammals such as cows and horses into a water-containing external base as an active ingredient. External skin preparations that have a useful effect on diseases that worsen mainly due to skin dryness, and cosmetics that prevent skin aging and provide moisture, smoothness, and a beautiful skin appearance. This is what we intend to provide. Conventionally, when the air is dry in winter, typically due to cracks and chapped skin, the barrier function decreases due to a decrease in skin secretions, especially lipids, and the water retention capacity of the water-retaining components is exceeded, resulting in transepidermal water loss (hereinafter referred to as TWL).
This is a symptom that is induced as a result of the moisture in the epidermis (especially the stratum corneum) being drawn out due to an increase in the size of the epidermis (abbreviation) or due to physical causes (such as washing). On the other hand, a type of keratosis called ichthyosis is a condition in which the skin becomes rough and dry, with a cracked and scaly appearance on the surface, and this condition is said to be especially worse during dry winter months. Furthermore, a condition in which the moisture content of the stratum corneum is about 10% even under normal conditions depending on age and constitution is called dry skin, and senile xeroderma is a suitable example. As mentioned above, the moisture in the stratum corneum of the epidermis normally combines with the constituent components of the stratum corneum to maintain normal skin functions, but due to environmental changes (low temperature, low humidity), aging, etc. A decrease in the moisture content of the layer is closely associated with the appearance of rough skin, where the skin becomes dry, brittle, and cracked. 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, this method is as follows:
There are two methods: using an occlusive agent to suppress TWL and using a humectant to enhance skin hydration. As an example of the former, Vaseline ointment is well known, and as seen in JP-A-54-86630, there is a method in which a sebum-like composition is blended and the skin surface is coated to prevent dryness. In these cases, in order to increase the effect, it is necessary to use a large amount (amount of application), which results in an unpleasant feeling such as oiliness and stickiness during use, and conversely, if the amount used is small, It had the disadvantage of weak occlusion and lack of durability. On the other hand, examples of the latter include polyhydric alcohols such as ethylene glycol, propylene glycol, 1.3-butylene glycol, glycerin, and PCA.
- Moisturizers such as soda are used, but although these have good compatibility with water, their own water retention capacity is not very high, and in low humidity conditions, rather than retaining moisture in the skin, the moisturizer may actually remove moisture from the skin. (especially noticeable with glycerin), and under high humidity conditions, it absorbs moisture from the outside air, causing a sticky and unpleasant feeling.On the other hand, if you reduce the amount used, the effect is weak and does not last long, which is a fatal flaw. It was hot. Therefore, the present inventors conducted intensive research in order to solve the drawbacks of the above-mentioned conventional methods and find a substance and dosage form with a high moisture retention function.
When a lipid mixture obtained from mammalian brain tissue is blended into a topical base or cosmetic base, it forms a water-containing liquid crystal state on the skin and has excellent occlusive properties and water retention properties. It was discovered that the following could be obtained, leading to the completion of the present invention. That is, the present invention uses mammalian brain tissue,
A lipid mixture containing phospholipids, glycolipids, and cholesterol as main components obtained by extracting this with a low polar organic solvent that is immiscible with water in any proportion, or with a mixture of the organic solvent and lower alkyl alcohol. The present invention relates to a skin preparation for external use, which is characterized in that it is blended into an external use base containing water as an active ingredient. The lipid mixture applied to the present invention is obtained from the brain tissue of mammals such as cows, horses, pigs, monkeys, and dogs. Further, in order to obtain the lipid mixture according to the present invention using these animal brain tissues, the following method is adopted. That is, first, fresh brain tissue is used, and as a pretreatment, it is ground with a grinder and freeze-dried, or it is homogenized with an organic solvent that is miscible with water in any proportion, such as methanol, ethanol, acetone, THF, etc. This dehydrates the water in the brain tissue. This dehydration treatment is carried out in order to reduce the amount of extraction solvent used in subsequent extraction operations and to also increase extraction efficiency. Next, an organic solvent is added to the dehydrated brain tissue to thoroughly extract it. The organic solvent used here is preferably one with low polarity, in other words, it is immiscible with water in any proportion; specifically, n-hexane, n-heptane, petroleum ether,
Examples include single or mixed solvents such as ethyl ether and chloroform, or mixtures of the above organic solvents and lower alkyl alcohols, specifically n
- Mixed solvents such as hexane/ethanol, ethyl ether/ethanol, and chloroform/methanol are exemplified. The extract is further washed with water or an aqueous salt solution such as Kcl, Cacl _2, etc., and then the solvent is distilled off to obtain the desired lipid mixture. The above-mentioned lipid mixture obtained in this manner is generally a pale yellow to yellow waxy or solid substance, and crudely contains phosphatidylcholine, phosphatidylethanolamine, etc. Glycerophospholipids (30-45% of the lipid mixture, hereinafter the same), sphingophospholipids such as sphingomyelin (5-15%), sphingoglycolipids such as cerebroside (10-30%), cholesterol (20-30%) 35%)
It is a complex mixture containing trace amounts of ceramides, polysaccharides, proteins, salts, etc. as its main components. Hereinafter, in order to further explain the lipid mixture according to the present invention in detail, a production example thereof will be shown. Production Example 1 After 100 g of fresh bovine brain was homogenized with 15 g of 95% ethanol, 250 ml of 95% ethanol was added and mixed and stirred. After this was filtered to separate the extract and the residue, 300 ml of n-hexane was added to the residue and mixed and stirred for thorough extraction. The extract obtained by filtration was washed with 60 ml of 0.75% KCl aqueous solution.
After repeating this operation twice, the extract was extracted under reduced pressure.
The organic solvent was distilled off at below 40°C to obtain 9.6 g of bovine brain lipid as a pale yellow solid. Production Example 2 After grinding 100 g of fresh pig brain using a grinder, it was freeze-dried. Next, 500 ml of a mixed solvent of chloroform-methanol (2:1 V/V) was added to this, and the mixture was mixed and stirred for thorough extraction. The extract obtained by filtration was washed with 80 ml of 0.04% CaCl ₂ aqueous solution. Then, the organic solvent was distilled off from the extract under reduced pressure at 40° C. or lower to obtain 8.9 g of pale yellow waxy pig brain lipid. Next, the amount of the lipid mixture in the present invention can vary widely depending on the dosage form of the applied skin preparation or cosmetic, but is approximately 0.05 to 90% by weight, preferably 0.05 to 20% by weight. is within the range of In other words, lipid mixtures have a high ability to form liquid crystals when mixed with water, and therefore have a high ability to retain water on the skin after application, but when mixed in large amounts, they tend to become oily. , it may give a sticky feeling and may be undesirable as a cosmetic. On the other hand, raw materials other than water used in the present invention include oils and fats, surfactants, humectants containing polyhydric alcohols, various medicinal ingredients, and preservatives that are usually applied to external skin preparations and cosmetics. Most of the ingredients are listed, 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.For this reason, for example, regarding oils and fats, myristic acid, palmitic acid, stearic acid, cetanol, When comparing solid fats represented by stearyl alcohol, beeswax, microcrystalline wax, etc. and liquid fats represented by liquid paraffin, squalane, soybean oil, olive oil, octyldodecyl myristate, etc., liquid fats are particularly preferred. Furthermore, when blending a combination of liquid fat and solid fat, it is more effective to make the mixture rich in liquid fat. On the other hand, examples of polyhydric alcohols include ethylene glycol, propylene glycol, 1.3-butylene glycol, glycerin, diglycerin, polyethylene glycol, and polyglycerin. More preferred is a mixture with a polyhydric alcohol. As mentioned above, in the case of external skin preparations and cosmetics composed of lipid mixtures, oils and fats, polyhydric alcohols, water, etc., volatile substances (particularly water, etc.) are ) due to transpiration, the lipid mixture content ratio is 0.5 to the total weight of the residue.
~20% by weight, preferably in the range of 1 to 5% by weight, forming a liquid crystal that incorporates water,
It has the best water retention and occlusion effect. Here, the results of evaluating how the lipid mixture according to the present invention has a high liquid crystal forming ability in a state in which water is incorporated and how excellent it is in water retention ability are shown. 1 Hygroscopicity Evaluation Γ Sample: The bovine brain extract lipid mixture according to the present invention obtained in Production Example 1 and glycerin and propylene glycol were used as comparison products. Γ Method: Weigh 5g of each of the above samples into a 3cm diameter shear dish, and add it to the relative humidity.
The sample was placed in a desicada adjusted to RH = 98%, and the weight of the sample was measured after 24 and 48 hours to calculate the moisture absorption rate ^*1) . The results are shown in Table-1. *1) Moisture absorption rate = Sample weight after aging (g) / 5 (g) x 100

[Table] 2 Moisture retention ability evaluation Γ Samples: (a) beef tallow extracted lipid mixture according to the present invention obtained in Production Example 1, and as comparison products (b) sphingomyelin (phospholipid), (c) cerebroside ( glycolipids), (d) cholesterol, (f) a mixture of equal amounts of sphingomyelin and cerebroside, (f) a mixture of equal amounts of sphingomyelin and cholesterol,
(g) A mixture of equal amounts of cerebroside and cholesterol was used. Γ Method: Add 4 times the weight of water to each of the samples (a) to (g) to swell them (80% water content), weigh 1 g each into a 3 cm diameter shear dish, This was set in a furan oven at a temperature of 5°C and a RH of 45%, and after 1 hour, 3 hours, and 5%
After 7 hours, the water content was measured, and the water retention rate ^*2) was calculated using the average value of the three measurements. still,
Moisture content can be measured using a trace moisture meter AQ- manufactured by Hiranuma Sangyo.
3 was used. The results are shown in Table-2. *2) Moisture retention rate = Moisture content in the sample after aging / Moisture content in the sample after aging × 100

[Table] As shown by the results in Tables 1 and 2, it was demonstrated that the lipid mixture according to the present invention has moderate hygroscopicity, and on the other hand, has high water retention ability and excellent water retention. In this way, in situations where individual components or a mixture of two components contained in the lipid mixture according to the present invention do not have a particularly high water retention ability, the lipid mixture according to the present invention has an excellent water retention ability. As mentioned above, the fact that the lipid mixture according to the present invention has a high ability to form liquid crystals in a state in which water is incorporated can be said to be evidence that the water retention property is improved. Furthermore, the results of an assay and a use test conducted to evaluate the external skin preparation of the present invention containing the lipid mixture of the present invention are shown below. 3 Moisture retention function evaluation Γ Samples: The ointment of the present invention shown in Example 1 below, and an ointment containing sorbitan monostearate instead of the bovine brain extract lipid mixture in the ointment of Example 1 below as a comparative product ( A), an ointment containing lecithin (B), and an ointment containing a mixture of equal amounts of sphingomyelin and cerebroside (C) were used. Γ Method: Weigh 5g of each of the above samples into a 3cm diameter shear dish, and heat it at 35℃.
Set it in a furan container with RH45%, and after 1 hour,
The weight of the sample was measured after 3 hours, 5 hours, and 7 hours, and the water transpiration rate ^*3) from the ointment system was calculated. The results are shown in Table-3. *3) Moisture evaporation rate = [5 (g) - sample weight after aging (g)] / 0.39 (g) x 100

[Table] 4 Obstruction Evaluation Γ Samples: The same inventive product and comparative products (A), (B), and (C) as used in the water retention capacity evaluation were used. Γ Method: Pour 10 g of water into a deep-shaped petri dish with a diameter of 35 mm, cover it with RO paper (Toyo RO paper No. 5C), and place a certain amount (0.2 g) of each of the above samples on the RO paper.
After it was applied uniformly and left for 15 hours at 35°C, the remaining amount of water (g) was measured and the blockage rate ^*4) was calculated. The results are shown in Table 4. *4) Blockage rate = (1 - water loss when applying sample (g) / water loss when no sample is applied (g)) x 100

[Table] 5 Evaluation of stratum corneum moisture content and use test evaluation Γ Samples: The same inventive product and comparative products (A), (B), and (C) used in the evaluation of water retention ability were used. Γ Method: Have 5 female panelists apply each of the above samples on the inner side of their forearms, and measure the feeling of use (sensory evaluation) and changes in water content in the stratum corneum over time ^*5) using the impedance meter method. The average values (n=5) were plotted. (See Figure 1) The results of the sensory evaluation are shown in Table 5. *5) Impedance meter method: Measures the amount of water in the stratum corneum by measuring the thin conductivity (μ) in the stratum corneum. Measuring equipment: IBS impedance meter model IB-355, measurement conditions;
20℃, RH=50%.

[Table] As shown by the results in Tables 3 to 5 and Figure 1, the skin external preparation of the present invention has low water evaporation and therefore has water retention properties, and has good occlusive properties and has good stratum corneum water content. It has become clear that the product maintains its properties for a long time and has an excellent feeling of use without any stickiness or the like. Examples are shown below. Incidentally, the blending ratio is in weight %. Example 1 Ointment liquid paraffin 65 Vaseline 5 POE(20) sorbitan monostearate 6 Beeswax 3 Bovine brain extract lipid mixture 3 Glycerin 10 Preservative 0.2 Water 7.8 Example 2 Cream stearic acid 2 Stearyl alcohol 1 Reduced lanolin 1.8 Squalane 10 Bovine Brain extract lipid mixture 1.2 Octyldodecanol 6 POE (25) Cetyl ether 3 Glyceryl monostearate 2 Flavor 0.3 Preservative 0.2 Glycerin 5 Water 67.5 Example 3 Emulsion POE addition (50) Hydrogenated castor oil 1 Coconut oil fatty acid monoglyceride 1 Pig brain extract lipid mixture 0.5 Oleic acid triglyceride 7.5 Glycerin 2.5 Flavor 0.2 Preservative 0.2 Water 87.1 Example 4 Lotion POE addition (60) hydrogenated castor oil 0.5 Bovine brain extract lipid mixture 0.2 Glycerin 5 Citric acid 0.1 Sodium citrate 0.2 Ethanol 10 Fragrance 0.1 Preservative 0.1 Water 83.8

[Brief explanation of drawings]

Figure 1 shows the results of conductivity (μ) in the stratum corneum of the skin after a certain period of time (30 minutes, 60 minutes, 90 minutes, 120 minutes, 180 minutes) using the impedance meter method. X is the invention product, Y is the comparative product (A),
Z is a comparative product (B), and W is a comparative product (C).

[Claims]

1 30 to 70 parts by weight of low boiling point solvent and 70 to 70 parts by weight of liquefied gas
30 parts by weight was filled into an aerosol container for a total amount of 100 parts by weight, and the pressure at 25°C was 2.0.
A hair tonic in an aerosol container with a weight of ~5.0 Kg/cm ² G, the aerosol container having a nozzle that stimulates the scalp when applied to the scalp and has a button that activates a valve to spray the hair tonic. 1. A hair growth agent contained in an aerosol container, characterized in that the container is an aerosol container having an injection port that can directly apply the hair to the scalp. 2. The hair nourishing agent in an aerosol container according to claim 1, which contains 0.01 to 15 parts by weight of a hair nourishing base per 100 parts by weight of the total amount of the low boiling point solvent and liquefied gas. 3. The hair growth agent in an aerosol container according to claim 1, wherein the low boiling point solvent is a low boiling point solvent containing trichloromonofluoromethane and/or dichlorotetrafluoroethane as a main component. 4. Claim 1, wherein the liquefied gas is a liquefied gas whose main component is dichlorodifluoromethane.
Hair nourishing agent in an aerosol container as described in Section 1.

Claims (1)

[Claims] 1. A brain tissue obtained by extracting mammalian brain tissue with a low polar organic solvent that is immiscible with water in any proportion, or with a mixture of the organic solvent and lower alkyl alcohol. 1. A skin external preparation, characterized in that a lipid mixture containing phospholipids, glycolipids, and cholesterol as main components is blended into an external base containing water as an active ingredient. 2. The skin external preparation according to claim 1, wherein the skin external preparation is a cosmetic.