JPH0366281B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention is stable and does not cause skin irritation.
This invention relates to an oil-in-water type (O/W type) emulsion composition for external use on the skin that has excellent gloss. Conventional emulsifiers for preparing O/W type creams, emulsions, etc. are generally two types selected from triethanolamine-stearic acid type, caustic alkali-stearic acid type, borax, beeswax type, and polyoxyethylene type activators. Alternatively, emulsions have been prepared using composition emulsifiers selected and combined with three or more. However, in the case of triethanolamine-stearic acid, it is known that it may cause allergic reactions depending on the constitution.
In addition, in the case of caustic alkali-stearic acid type, the PH
It has problems in use, such as difficulty in adjustment, and disadvantages, such as poor emulsifying properties 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. Furthermore, polyoxyethylene-based materials have problems such as irritation. In addition, sucrose fatty acid esters contain phenolic substances found in polyoxyethylene activators and have little effect on reducing the potency of antibiotics, but on the other hand, they have weak emulsifying power, and it is said that it is difficult to obtain stable emulsions when used alone. ing. The present inventors have conducted various studies in consideration of the above circumstances.
As a result of research, it was discovered that a system consisting of an aqueous solution containing specific amounts of polysaccharides, sucrose fatty acid esters, and polyhydroxy compounds emulsified oily substances easily, uniformly, and stably, and the present invention was completed. Although the emulsification mechanism is not clear,
It is composed of sucrose fatty acid ester, polysaccharide, and polyhydroxy compound, and because these chemical structures are similar, they have good compatibility, and a type of interfacial complex compound is formed due to hydrogen bonding, etc., resulting in a stable sol or weak gel. It is believed that a stable emulsion is obtained due to the formation of the emulsion. Furthermore, one advantage of the present invention is that a glossy and stable emulsion can be obtained with approximately 1/2 to 1/3 of the amount of sucrose fatty acid ester used as an emulsifier compared to the amount conventionally used. Can be mentioned. Furthermore, 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. 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
A system consisting of a sucrose fatty acid ester of 5.0 to 16.0%, an anhydride of 1.0 to 30.0% by weight of a polyhydroxy compound, and 3.0 to 40% by weight of water, combined with an oily substance, or 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. The above polysaccharides are just examples, and the polysaccharides are not limited to these as long as they are water-soluble. The amount of the polysaccharide blended is 0.01 to 1.5% by weight, preferably 0.05 to 1.0% by weight, based on the total weight of the composition. If it is less than 0.01% by weight, there is no effect, and if it is more than 1.5% by weight, it is not preferable because of hardening phenomenon. 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 sucrose has eight hydroxyl groups in one molecule, 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 with a high content of monoesters to wax-like products with a high content of di- and triesters. Furthermore, by changing the type of fatty acid, it is also possible to produce a variety of different HLB products. The sucrose fatty acid ester used in the present invention has an HLB range of about 5.0 to 16.0, preferably 8.0 to 16.0.
14.0, and is one or a mixture of two or more selected from the above mono-, di-, and tri-ester groups. If the HLB is less than 5, a W/O type emulsion tends to be formed and emulsification becomes poor, which is not preferable.
Further, 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. If the amount is less than 0.1% by weight, emulsification will generally be poor and it will be difficult to provide a good feeling, and if it is too much, the emulsion stability will be poor and the feeling of use may also be poor. Examples of the polyhydroxy compound used in the present invention include ethylene glycol, diethylene glycol, triethylene glycol, higher polyethylene glycols, propylene glycol, dipropylene glycol, higher polypropylene glycols, glycerin, diglycerin, and higher polyethylene glycols. Polyglycerols, sugar alcohols such as sorbitol, mannitol, xylitol, and maltitol; monosaccharides, disaccharides, and trisaccharides such as glycose, and fructose; various invert sugars obtained by hydrolysis of starch, starch syrup, dextrin, Isomerized sugar, syrup, jams, honey,
It is one or a mixture of two or more selected from the group consisting of glycerin, sugar alcohols, EO and PO adducts of sugars, etc. 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 compounded is
Anhydrous equivalent based on the total weight of the composition
1.0 to 30.0% by weight, preferably 3.0 to 20.0% by weight. Examples of oily substances used in the present invention include liquid or pasty hydrocarbons such as liquid paraffin, squalane, and petrolatum, and 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,
Examples include higher alcohols such as stearyl alcohol, oleyl alcohol, and octyl dodecal, 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).
In addition, the amount of the above oily substance added is usually 0.5 to 80% by weight.
It is. In the present invention, the amount of water added to the aqueous solution containing polysaccharide, sucrose fatty acid ester, and polyhydroxy compound as essential components is usually 3.0 to 40.0% by weight based on the total weight of the composition. %, preferably 7.0 to 30.0% by weight. This water plays an important role in emulsification and is a necessary and sufficient condition for solubilizing or good emulsification of the oily substances that will be blended in the next step. If there is too much, bad results will result. As described above, the composition of the present invention is formed by blending an oily substance into an aqueous solution containing a polysaccharide, a sucrose fatty acid ester, and a polyhydroxy compound as essential components to solubilize or emulsify it. Alternatively, it can also be formed by further adding water and emulsifying it. By doing the above, efficient emulsification is carried out under sol or weak gel conditions, so the amount of sucrose fatty acid ester blended is smaller than usual, the emulsion particle size is uniform and constant, and the emulsion is extremely glossy. It is possible to prepare an oil-in-water emulsion that has a good firm feel and is also 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 proportions (1) Zancort 0.2 [%] (2) Maltitol 2.0 (3) Sucrose fatty acid ester (HLB approx. 12)
0.4 (4) Glycerin 6.0 (5) Methyl paraoxybenzoate 0.1 (6) Purified water 15.0 (7) Stearic acid 4.0 (8) spermaceti 4.0 (9) Ethylene glycol monostearate
8.0 (10) Hydrogenated oil 5.0 (11) Squalane 6.0 (12) Octyldodecyl myristate 7.0 (13) Propyl paraoxybenzoate 0.1 (14) Purified water 42.2 total 100.0 ● Preparation method [] Above (1) to (6) Prepare a mixture at 80°C by heating and dissolving the ingredients. [] Components (7) to (13) above are heated and dissolved at 80°C. [] Heat the ingredients in (14) above to 80°C. [] Next, while stirring [] with a homomixer, add [] to emulsify it, 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 heat resistance stability of the emulsion was examined by leaving it in a constant temperature bath, the emulsion did not break even after 30 days, which indicates that a stable emulsion was obtained. Examples 2 to 7 Xanthan gum, locust bean gum, guar gum,
An emulsion was obtained according to Example 1 using gum tragacanth, gum karaya, or alginic acid. The emulsions obtained in Examples 2 to 7 were sufficiently emulsified and had similar stability as the emulsion obtained in Example 1. Examples 8 to 11 Emulsions were obtained according to Example 1, using sorbitol, mannitol, glycol, and xylitol instead of maltitol, and replacing half of the glycerin with 1,3-butylene glycol. . The emulsions obtained in Examples 8 to 11 were sufficiently emulsified and had similar stability as the emulsion obtained in Example 1. Example 12 ●Cleansing cream● Ingredients and proportions (1) Zancort 0.2 [%] (2) Maltitol 1.0 (3) Glycerin 6.0 (4) Sucrose fatty acid ester (HLB approx. 12)
0.8 (5) Sucrose fatty acid ester (HLB approx. 6)
1.5} HLB approx. 8.1 (6) Methyl paraoxybenzoate 0.1 (7) Purified water 19.8 (8) Liquid paraffin 55.0 (9) Glycerin isooctanoate 10.0 (10) Ethylene glycol monostearate
4.0 (11) Methyl polyhydroxy 0.5 (12) Propyl paraoxybenzoate 0.1 total 100.0 ● Preparation method [] Heat and dissolve the components (1) to (7) above to prepare a mixture at 80°C. [] Components (8) to (12) above are heated and dissolved at 80°C. [] Next, emulsify by adding [] while stirring [] with a homomixer. 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 13 ●Milky lotion● Ingredients and proportions (1) Zancort 0.1 [%] (2) Maltitol 3.0 (3) Sucrose fatty acid ester (HLB approx. 12)
0.5 (4) Glycerin 5.0 (5) 1,3-butylene glycol 5.0 (6) Methyl paraoxybenzoate 0.1 (7) Purified water 15.0 (8) Ethylene glycol monostearate
2.0 (9) Glycerin monostearate 1.0 (10) Squalane 5.0 (11) Octyldodecyl myristate 5.0 (12) Propyl paraoxybenzoate 0.1 (13) Purified water 58.2 total 100.0 ● Preparation method [] (1) to (7) above Prepare a mixture at 80°C by heating and dissolving the ingredients in ). [] Components (8) to (12) above are heated and dissolved at 80°C. [] Heat the ingredients in (13) above to 80°C. [] Next, while stirring [] with a homomixer, add [] to emulsify it, and then add []. Cool to 30℃ while stirring,
A stable oil-in-water emulsion (milky lotion) was obtained. The resulting emulsion had a mild effect on the skin. Example 14 ●Hydrophilic ointment● Ingredients and proportions (1) Zancort 1 [g] (2) Maltitol 20 (3) Sucrose fatty acid ester (HLB approx. 12)
10 (4) Purified water 150 (5) Propylene glycol 120 (6) Ethyl paraoxybenzoate 0.25 (7) Propyl paraoxybenzoate 0.15 (8) Stearyl alcohol 220 (9) White petrolatum 250 (10) Purified water Appropriate amount total 1000 ● Preparation method [] According to the method for producing hydrophilic ointment according to the Japanese Pharmacopoeia, 10th edition (Part 2), components (1) to (6) above are heated and dissolved to prepare a mixture at 75°C. [] Components (7) to (9) above are heated and dissolved at 80°C. [] Heat the ingredients in (10) above to 80°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 9 Skin creams were prepared in the same manner as in Example 1 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 1. The results are shown in the table below.

【table】

【table】

Claims (1)

[Claims] 1. Polysaccharide, sucrose fatty acid ester, and polyhydroxy compound as essential components, 0.01 to 1.5% by weight of polysaccharide, 0.1 to 1.5% by weight based on the total weight of the composition.
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 6.0% by weight of sucrose fatty acid ester and 1.0 to 30.0% by weight of a polyhydroxy compound as anhydride, 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 5.0 to 16.0. 4. 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. 5. 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.