JPH0369882B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to an oil-in-water type (O/W type) emulsion composition for external use on the skin, which is stable, does not irritate the skin, and has excellent gloss. Conventional emulsifiers for preparing O/W type creams, milky lotions, etc. are generally selected from triethanolamine-stearic acid, caustic alkali-stearic acid, borax-beeswax, and polyoxyethylene activators. Emulsions have been prepared by using a selected species or a combination of three or more species as an emulsifier. However, in the case of triethanolamine-stearic acid, it is known that it may cause allergic reactions depending on one's constitution. In addition, in the case of caustic alkali-stearic acid type
It has problems in use, such as difficulty in pH adjustment, and drawbacks, such as poor emulsification at high temperatures. Furthermore, in the case of a borax-beeswax system, if a large amount of borax is used, there is a risk of causing an allergic reaction. In addition, polyoxyethylene-based products have problems such as irritation, and while sucrose fatty acid ester-based products contain phenolic substances found in polyoxyethylene-based active agents and have little effect on reducing the potency of antibiotics, they have poor emulsifying power. It is said that it is difficult to obtain a stable emulsion when used alone. The present inventors have conducted various studies and studies in consideration of the above circumstances, and have found that a system consisting of an aqueous solution containing specific amounts of polysaccharides, sucrose fatty acid esters, caseinates, and polyhydroxy compounds has been developed. The present invention was completed by discovering that oily substances can be emulsified easily, uniformly and stably. The emulsification mechanism of these is not clear, but they are very similar in chemical structure and form a stable sol or weak gel due to hydrogen bonds, etc., and a type of interfacial complex compound is generated, so a stable emulsion can be obtained. It is thought that it will be possible. or,
When preparing ordinary creams and emulsions, higher alcohols such as cetanol, cetostearyl alcohol, and stearyl alcohol are used, and these are essential components as gel stabilizing components of emulsions. In some cases, it is also possible to prepare creams and emulsions without using these higher alcohols. As is well known, these higher alcohols are substances that may cause allergic reactions, so it is surprising that a stable emulsion composition can be formed without using them, and it is also significant from a safety perspective. It is. The present invention will be explained in detail below. The oil-in-water emulsion composition for external use on the skin of the present invention comprises 0.01 to 1.5% by weight based on the total weight of the composition.
Polysaccharides, 0.1-6.0% by weight, HLB ranges approximately
It is made by blending an oily substance into an aqueous solution of a sucrose fatty acid ester of 2.0 to 16.0%, a caseinate of 0.1 to 8.0% by weight, and a polyhydroxy compound of 1.0 to 30.0% by weight as an anhydride, or a mixture of an oily substance and water. be. The polysaccharides used in the present invention include, for example, polysaccharides produced by microorganisms such as Xancort, Xanfuro, xanthan gum, curdlan, succinoglucan, No. 271 gum, and schizophyllan, guar gum, locust bean gum, quinseed gum, and tara gum. A type selected from the group consisting of seed polysaccharides, resin polysaccharides such as arabinogalactan gum, gum arabic, gum tragacanth, and gum karaya, water-soluble polysaccharides such as carrageenan, seaweed polysaccharides such as alginic acid, and fruit polysaccharides such as pectin. Or it consists of a mixture of two or more types. These are just examples, and the material is not limited to these as long as it is water-soluble.
Further, the blending amount of the polysaccharide is 0.01 to 1.5% by weight, preferably 0.05 to 1.5% by weight based on the total weight of the composition.
It is 1.0% by weight. In general, sucrose fatty acid esters include sucrose fatty acid monoester, which is made by adding one molecule of fatty acid to one molecule of sucrose, sucrose fatty acid diester, which is made by adding two molecules of fatty acid to one molecule of sucrose, and sucrose fatty acid diester, which is made by adding two molecules of fatty acid to one molecule of sucrose. Examples include sucrose fatty acid triester, which is made by adding three molecules of fatty acid to one molecule of sugar. Since one sucrose molecule has eight hydroxyl groups, theoretically up to sucrose fatty acid octaesters exist, but commercially available products are mixed esters of these mono-, di-, and tri-esters. However, depending on the reaction conditions and purification methods during production, there are various products ranging from products containing a large amount of monoester to wax-like products containing a large amount of di- and triester. In addition, by changing the type of fatty acid,
It is also possible to make a variety of different HLB products. The sucrose fatty acid ester used in the present invention has an HLB range of about 2.0 to 16.0, and is one or a mixture of two or more selected from the above mono-, di-, and tri-ester groups. The amount of the sucrose fatty acid ester blended is 0.1 to 6.0% by weight, preferably 0.3 to 4.0% by weight, based on the total weight of the composition. Caseinates used in the present invention include, for example, inorganic salts such as sodium caseinate, potassium caseinate, and calcium caseinate, organic amine salts such as casein monoethanolamine, casein diethanolamine, and casein triethanolamine, and bases such as casein arginine and casein lysine. It is one kind or a mixture of two or more kinds selected from the group consisting of amino acid salts. These are examples, and the invention is not limited to these. Further, the amount of the caseinate is 0.1 to 8.0% by weight, preferably 0.5 to 5.0% by weight, based on the total weight of the composition. If the weight is less than 0.1%, emulsification is generally poor;
It is difficult to give a good feeling,
If the amount is too large, the consistency of the emulsion may decrease and emulsion stability may deteriorate. Examples of the polyhydroxy compound used in the present invention include ethylene glycol, diethylene glycol, dipropylene glycol, higher polypropylene glycols, glycerin, diglycerin, higher polyglycerols, sorbitol, mannitol, xylitol, maltitol, etc. Sugar alcohols, monosaccharides, disaccharides, trisaccharides such as glucose, fructose, various invert sugars obtained by hydrolysis of starch, starch syrup, dextrin, high fructose sugar, syrup, jams, honey, glycerin and sugar alcohols , EO, PO adducts of sugars, etc., or a mixture of two or more thereof. The above-mentioned polyhydroxy compound is just an example, and any substantially water-soluble compound can be used, and the compound is not limited to the above-mentioned one. In addition, the amount of the polyhydroxy compound blended is 1.0 in terms of anhydride based on the total weight of the composition.
-30.0% by weight, preferably 3.0-20.0% by weight. Examples of oily substances used in the present invention include liquid or pasty hydrocarbons such as liquid paraffin, squatene, and petrolatum, ester oils such as octyldodecyl myristate, isopropyl palmitate, butyl stearate, and cetyl isooctanoate; Waxes such as solid paraffin, microcrystalline wax, ceresin wax, beeswax, spermaceti, vegetable oils such as olive oil, soybean oil, safflower oil, almond oil, avocado oil, animal oils such as mink oil and turtle oil, cetanol. , higher alcohols such as stearyl alcohol, oleyl alcohol, and octyldodecanol, and higher fatty acids such as stearic acid and palmitic acid. If necessary, polar waxes such as glycerin monostearate, ethylene glycol monostearate, and propylene glycol monostearate may be blended as semi-oily substances (surfactants with relatively low HLB).
These are examples, and are not limited to these. In addition, the amount of the above oily substance is usually 0.5~
It is 80% by weight. In the present invention, the amount of water added to the aqueous solution containing polysaccharide, sucrose fatty acid ester, caseinate, and polyhydroxy compound as essential components is usually determined based on the total weight of the composition.
3.0 to 40.0% by weight, preferably 7.0 to 30.0% by weight. This water plays an important role in emulsification,
This water is a necessary and sufficient condition for solubilizing or good emulsification of the oily substance to be blended in the next step, and the amount of water may be small or too large, resulting in poor results. As described above, the composition of the present invention is obtained by blending an oily substance into an aqueous solution containing polysaccharide, sucrose fatty acid ester, caseinate, and polyhydroxy compound as essential components to solubilize or emulsify it. It can also be formed by adding water afterwards to emulsify it. By doing the above, efficient emulsification is performed under sol or weak gel conditions, so the emulsion particle size becomes uniform and constant.
It is possible to prepare an oil-in-water emulsion that is extremely glossy, has a good firm feel, and is highly safe and stable. In the present invention, preservatives, humectants, bactericidal agents,
We prepare cosmetics (including quasi-drugs) such as skin creams, milky lotions, cleansing creams, and make-up creams, as well as external medicines such as hydrophilic ointments, by appropriately blending UV absorbers, pigments, medicinal agents, fragrances, and other ingredients. can do. Furthermore, these emulsified compositions do not substantially irritate the skin and have a mild effect on the skin. Examples of the oil-in-water emulsion composition of the present invention are shown below. These Examples are provided to explain the present invention in more detail, and do not limit the scope of the present invention, and various changes are possible. It should be noted that in the examples, [%] indicates weight %. Example 1 Skin cream ● Ingredients and proportion [%] (1) Zancort 0.2 (2) Maltitol 3.0 (3) Sodium caseinate 1.0 (4) Sucrose fatty acid ester (HLB approx. 6) 2.0 (5) Glycerin 3.0 ( 6) Methyl paraoxybenzoate 0.1 (7) Purified water 15.0 (8) Stearic acid 4.0 (9) spermaceti 4.0 (10) Ethylene glycol monostearate 5.0 (11) Glycerin monostearate 3.0 (12) Squalane 6.0 (13) Octyldodecyl myristate 7.0 (14) Propyl paraoxybenzoate 0.1 (15) Purified water 46.6 total 100.0 ●Preparation method [] Dissolve the components (1) to (7) above by heating to prepare a mixture at 80°C. [] Components (8) to (14) above are heated and dissolved at 80°C. [] Heat the ingredients in (15) above to 80°C. [] Next, add [] while stirring [] with a homomixer to emulsify, and then add []. Cool to 30℃ while stirring,
An oil-in-water emulsion (skin cream) was obtained. A portion of the obtained emulsion was taken out and heated to 40°C.
When the emulsion was left in a constant temperature bath to examine its heat resistance and stability, the emulsion did not break down even after 30 days, indicating that a stable emulsion had been obtained. Examples 2 to 5 Emulsions were obtained according to Example 1 using locust bean gum, guar gum, Karaya gum, and pectin instead of Zancort. The emulsions obtained in these Examples 2 to 5 were sufficiently emulsified and had similar stability as the emulsion obtained in Example 1. Examples 6 to 9 Emulsions were obtained according to Example 1 using sorbitol, mannitol, glucose, and xylitol instead of maltitol. The emulsions obtained in Examples 6 to 9 were sufficiently emulsified and had similar stability as the emulsion obtained in Example 1. Example 10 Cleansing cream Ingredients and ratio [%] (1) Zancort 0.1 (2) Sodium caseinate 1.0 (3) Sucrose fatty acid ester (HLB approx. 6) 2.0 (4) Maltitol 2.0 (5) Glycerin 5.0 ( 6) Methyl paraoxybenzoate 0.1 (7) Purified water 19.2 (8) Liquid paraffin 50.0 (9) Vaseline 10.0 (10) Cetyl isooctanoate 10.0 (11) Methyl polysiloxane 0.5 (12) Propyl paraoxybenzoate 0.1 Total 100.0 ●Preparation method [] Components (1) to (7) above are heated and dissolved to prepare a mixture at 80°C. [] Components (8) to (12) above are heated and dissolved at 80°C. [] Then, while stirring [] with a homomixer, [] is added to emulsify. Thereafter, the mixture was cooled to 30° C. with stirring to obtain a stable oil-in-water emulsion (cleansing cream). The resulting emulsion had a mild effect on the skin. Example 11 Milky lotion ●Ingredients and proportions (1) Zancort 0.1 (2) Sodium caseinate 1.0 (3) Sucrose fatty acid ester (HLB approx. 6) 1.5 (4) Maltitol 3.0 (5) Glycerin 5.0 (6) 1,3-Butylene glycol 2.0 (7) Methyl paraoxybenzoate 0.1 (8) Purified water 15.0 (9) Ethylene glycol monostearate 2.0 (10) Glycerin monostearate 1.5 (11) Squalane 5.0 (12) Octyldodecyl myristate 5.0 (13) Propyl paraoxybenzoate 0.1 (14) Purified water 58.7 total 100.0 ●Preparation method [] Heat and dissolve the components (1) to (8) above to prepare a mixture at 80°C. [] Components (9) to (13) above are heated and dissolved at 80°C. [] Heat the ingredients in (14) above to 80°C. [] Next, add [] while stirring [] with a homomixer to emulsify, and then []
Add. The mixture was cooled to 30° C. with stirring to obtain a stable oil-in-water emulsion (milky lotion). The resulting emulsion had a mild effect on the skin. Example 12 Hydrophilic ointment Ingredients and proportions [g] (1) Zancort 1 (2) Sodium caseinate 5 (3) Sucrose fatty acid ester (HLB approx. 12) 5 (4) Maltitol 20 (5) Purified water 150 (6) Propylene glycol 120 (7) Ethyl paraoxybenzoate 0.25 (8) Propyl paraoxybenzoate 0.15 (9) Stearyl alcohol 220 (10) White petrolatum 250 (11) Purified water Appropriate amount total 1000 ●Preparation method [] No. 10 According to the revised Japanese Pharmacopoeia (Part 2) hydrophilic ointment manufacturing method, the components (1) to (7) above are heated and dissolved to prepare a mixture at 75°C. [] Components (8) to (10) above are heated and dissolved at 75°C. [] Heat the ingredients in (11) above to 75°C. [] Next, emulsify by adding [] while stirring [] with a homomixer. After that, add [] and stir and cool until solidified.
A stable oil-in-water emulsion (hydrophilic ointment) was obtained. The resulting emulsion had a mild effect on the skin. Comparative Examples 1 to 12 Skin creams were prepared in the same manner as in Example 10 using the formulations shown in the table below, and the emulsion particle size, emulsion uniformity, emulsion stability, and texture were compared with those in Example 10. The results are shown in the table below.

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Claims (1)

[Scope of Claims] 1 Polysaccharide, sucrose fatty acid ester, caseinate and polyhydroxy compound are essential components, and 0.01 to 1.5% by weight of polysaccharide and 0.1 to 6.0% by weight based on the total weight of the composition. sucrose fatty acid ester,
0.1-8.0% by weight of caseinate, and as anhydrous
An oil-in-water emulsion composition for external use on the skin, which is prepared by blending an oily substance into an aqueous solution containing 1.0 to 30.0% by weight of a polyhydroxy compound, or blending an oily substance and water. 2. A patent claim in which the polysaccharide is one or a mixture of two or more selected from the group consisting of water-soluble polysaccharides such as microorganism-produced polysaccharides, seed polysaccharides, resin polysaccharides, seaweed polysaccharides, and fruit polysaccharides. The oil-in-water emulsion composition for external use on the skin according to Item 1. 3. The oil-in-water emulsion composition for external use on the skin according to claim 1, wherein the sucrose fatty acid ester is composed of one type or a mixture of two or more types, and has an HLB range of about 2.0 to 16.0. 4. The oil in water for external use on the skin according to claim 1, wherein the caseinate is one or a mixture of two or more selected from the group consisting of sodium caseinate, potassium caseinate, calcium caseinate, caseinate triethanolamine, and casein arginine. type emulsion. 5. The oil in water for external use on the skin according to claim 1, wherein the polyhydroxy compound is one or a mixture of two or more selected from the group consisting of alkylene glycol, glycerin polyalkylene oxide, sugar alcohol, sugar, and sugar derivatives. Type emulsion composition. 6. The oil-in-water emulsion composition for external use on the skin according to claim 1, wherein the amount of water contained in the aqueous solution is 3.0 to 40.0% by weight based on the total weight of the composition.