JPS61204109A - Emulsion-type composition for external use - Google Patents

Abstract

PURPOSE:An emulsion-type composition for external use, containing lecithin having an iodine value within a specific range and a specified polyhydric alcohol ester of a fatty acid, having high affinity for the skin and stable emulsion state, and usable for medicines and cosmetics, etc. CONSTITUTION:An emulsion-type composition for external use containing (A) lectithin having 10-50 iodine value, e.g. phospholipid-containing substance derived from egg yolk or soybean or a hydrogenated substance thereof and (B) 0.07-20pts.wt., preferably 0.2-10pts.wt., based on one pts.wt. component (A), monoglycerol ester or monopropylene glycol ester of a 12-22C fatty acid, preferably stearic acid, palmitic acid or myristic acid. The above-mentioned composition can be prepared by mixing a fat or oil or oil-soluble component with both the components (A) and (B), dissolving the resultant mixture under heating to 60-70 deg.C, adding water or a water-soluble component heated at almost the same temperature thereto while stirring, emulsifying the components and cooling the resultant emulsion to 30-40 deg.C.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an emulsified external composition that has high affinity for the skin and is stable in an emulsified state.

Traditionally, in emulsified external compositions, synthetic surfactants, typified by polyoxyethylene additives, have been used for the purpose of emulsifying fats and oils or oil-soluble components and water or water-soluble components in the composition. I've been However, although this polyoxyethylene adduct type surfactant has excellent emulsifying power, it is not necessarily satisfactory in imparting mild affinity to the skin to the composition.

Therefore, in recent years, attempts have been made to use basic amino acid salts of fatty acids as emulsifiers to replace such synthetic surfactants, especially in the field of cosmetics (Japanese Patent Application No. 127131.55-127132゜55-1
27133.56-97208). However, in this case, the pH of the composition tends to be alkaline, and the hydrophilicity of the surfactant is so strong that the affinity of the composition for the skin is poor.

Similarly, instead of the synthetic surfactant, natural gums such as gum arabic, xanthan gum, algae colloid, or synthetic water-soluble polymers such as lfcMc-Na,
HPC, sodium polyacrylate, etc. are used, but in this case) they have poor emulsifying power. In view of these circumstances, the present inventor conducted various studies with the aim of providing an emulsified external composition with excellent skin affinity and emulsion stability, and here are the results.

It was discovered that a desired composition could be obtained by containing lecithin and polyhydric alcohol fatty acid ester, and patent application No. 57-1736 (Japanese Unexamined Patent Publication No. 58-121209)
It was completed as an invention related to.

Now, the inventor has conducted further research.

In the above invention, the lecithin has an iodine value of 50 or less, and the polyhydric alcohol fatty acid ester is a glycerin monofatty acid ester or a propylene glycol monofatty acid ester, and the fatty acid has 12 carbon atoms.
It has been found that particularly excellent effects can be obtained when the number is between 22 and 22. In other words, it has been found that the above invention provides particularly excellent skin affinity and emulsion stability when specific technical limitations included in the invention are selected. The present invention is a selection invention completed based on such knowledge. That is, the object of the present invention is to provide an emulsified external composition with particularly excellent skin affinity and emulsion stability.
This disclosure discloses specially selected technical limitations of the constituent features of the invention according to No. 1736.

The present invention will be explained below.

The lecithin according to the present invention is a phospholipid-containing substance extracted from egg yolk or vegetable oil, further purified in some cases, a hydrogenated product thereof, a synthetic glycerophosphate ester represented by the following general formula, and a mixture thereof, Refers to those with an iodine value of 50 or less.

H [In the formula, Rb Rt is hydrogen or a saturated or unsaturated hydrocarbon having 8 to 20 carbon atoms, and R3 is hydrogen or choline.

It represents ethanolamine, serine, inositol, glycerol, etc.] The iodine value is the amount of absorbed halogen converted into iodine and expressed as a percentage of the sample. In the present invention, the precise definition of the iodine value can be found in the ``Iodine Value'' section of the Oil and Fat Testing Methods of the Japanese Pharmacopoeia, 10th edition, and the measurement of the iodine value in the present invention can be found in the ``Operation Method'' in the same section. This is done based on the method described. According to the results of experiments, it has been found that the emulsion stability is particularly good when the iodine value is 50 or less. One feature of the present invention is found in the selection of this technical limitation.

Since lecithin is one of the components of sebum composition, it is already known that it has a high affinity for the skin and is excellent as a cosmetic component. However, since lecithin has a weak emulsifying power, it is difficult to provide a stable emulsified external composition using lecithin alone. Therefore, a special combination with lecithin must be found in order to improve the emulsion stability without impairing lecithin's skin affinity.

According to the results of experiments, the above object can be achieved by specifically selecting a glycerin monofatty acid ester or a propylene glycol monofatty acid ester whose fatty acid has 12 to 22 carbon atoms in combination with lecithin according to the present invention. It was found that this is another feature of the present invention. Preferred fatty acids include, for example, stearic acid, palmitic acid, and myristic acid. Furthermore, the two fatty acid esters selected in the present invention may be used alone, or may be used in combination.
The invention is not limited thereby.

Next, the preferable weight ratio of lecithin and fatty acid ester in the composition of the present invention is within a range of 0.07 to 20 parts by weight, more preferably 0.2 to 10 parts by weight, per 1 part by weight of lecithin/thin. The range is within the range.

This preferred range is the same as the range in the invention related to Japanese Patent Application No. 57-1736, and the reasons and experiments described in the same publication can be directly referred to. That is, fatty acid ester is 0.0
If the amount is less than 5 parts by weight, the emulsion stability will deteriorate. Therefore, this part by weight is the minimum necessary amount to achieve the object of the present invention, and on the other hand, if the amount is increased beyond the above part by weight, the emulsion stability will improve.

It is preferable that the amount does not exceed 20 parts by weight, since the consistency of the composition itself increases significantly and if it exceeds 20 parts by weight, the commercialability will be impaired.

Since the composition of the present invention is an emulsion-type composition, the composition contains 1 fat or oil-soluble component, such as an animal or vegetable oil.

Synthetic esters, waxes, fat-soluble vitamins, etc. and water or water-soluble ingredients are essential components, and preservatives are added as necessary.

Contains humectants, thickeners, UV absorbers, antioxidants, and fragrances. Also, beauty ingredients such as vitamins.

Polypeptides, acyl polypeptides, etc. can also be blended in the same manner. Further as needed.

Surfactants other than the surfactant according to the present invention 9 may be used within a range that does not impair the purpose of the present invention, such as polyoxyethylene fatty acid esters, polyoxyethylene higher alcohol ethers, polyoxyethylene sorbitan fatty acid esters, etc. It is optional to add anionic surfactants such as nonionic surfactants, higher alcohol sulfates, fatty acid alkali metal salts, and fatty acid basic amino acid salts (Japanese Patent Publication No. 55-127318).

Next, the type of emulsification in the composition of the present invention can be either an oil-in-water type or a water-in-oil type. In other words, lecithin,
Polyhydric alcohol fatty acid ester.

A desired emulsion type can be obtained by appropriately selecting the raw materials and ratios of the oils and fats or oil-soluble components and water or the water-soluble components. The composition of the present invention can be in a semi-solid form such as a cream or ointment, or in a liquid form such as an emulsion. That is, by appropriately selecting the raw materials and ratios of each component, the desired form can be prepared in the same manner as in the case of emulsion type.

The composition of the present invention may be manufactured according to a general conventional method for manufacturing emulsion-type preparations. Therefore.

For example, fats and oils, oil-soluble components, lecithin, and polyhydric alcohol fatty acid esters are mixed and dissolved by heating to 60 to 70°C, and water or water-soluble components heated to the same temperature is added to this while stirring to emulsify. A method such as cooling to 30 to 40°C may be used. of course.

Minor modifications to the method may be made at will.

As shown in the experimental examples below, the effects of the composition of the present invention are its skin affinity and emulsion stability, and in particular, it has good skin affinity (and exhibits an excellent feeling of use). Therefore, it is possible to prepare external medicinal preparations containing medicinal raw materials such as vitamins and steroid hormones as crude drugs, and also for use in moisturizing cream, night cream, pine surge cream, etc. , use in cosmetics such as cleansing creams, lotions, and packs will bring even more favorable results.

The present invention will be explained in more detail with reference to Examples described below.

Example 1 (Oil-in-water moisture cream) Formula (2) Methyl haloxybenzoate 0.1
(3) Propylene glycol 8.
0(4) Flavorings
0.1 total amount 100
．． 0 (1) group components were uniformly heated and dissolved, maintained at 700C, and while stirring, (2), +31
．． Heat the ingredients in +51 at the same temperature as above to make a homogeneous solution, emulsify it, and cool it while stirring to 40°C.
Then, component (4) was added and cooled while stirring to obtain a moisture cream. This moisture cream had sufficient stability and mild effect on the skin, and gave a good feeling of use. The phospholipid content of partially hydrogenated egg yolk lecithin is 25%, and the iodine value is 41.

Example 2 (oil-in-water emulsion) Prescription ingredients Parts by weight (2)
Glycerin 10.0 (3) Methylparaben 0.2 (4) Algecolloid 0.2 (5) Fragrance 0.0
5 (6) Purified water 74.05 total
Quantity 100.0 The ingredients of group (1) were uniformly heated and dissolved, kept at 706C, and while stirring, (2), (3), (4),
The ingredients in (6) were heated at the same temperature as above to make a homogeneous solution, then emulsified, cooled with stirring, and heated to 408C (
Component 5) was added, and the mixture was further cooled while stirring to obtain a cosmetic emulsion. This cosmetic emulsion had sufficient stability and a mild effect on the skin, and gave a good feeling of use. Note that the phospholipid content of the doubly hydrogenated egg yolk lecithin is 65%, and the iodine value is 15.

Example 3 (water-in-oil pine surge cream) Prescription ingredients Parts by weight (2)
1.3 Butylene glycol 5.0 (3
) Methyl paraoxybenzoate 0.15 (
4) Paraoxypropyl benzoate 0.05
(5) Fragrance 0.2 (6) Purified water
52.55 total
ff1100.0 The components of group (1) and (4) were uniformly heated and dissolved at 70%
°C and stirred in advance (21,
(31° (6) ingredients were heated at the same temperature as above to make a homogeneous solution, emulsified, cooled with stirring,
Component (5) was added at 8C, and the mixture was cooled while stirring to obtain pine surge cream. This pine surge cream has sufficient stability and gentle action on the skin.

It gave a good usability. In addition, the phospholipid content of purified soybean lecithin is 95%, and the iodine value is 25.

Example 4 (oil-in-water night cream) Prescription ingredients Parts by weight (2)
Glycerin 10.0 (3) Methyl paraoxybenzoate 0.1 (4) Propyl paraoxybenzoate 0.1 (5) Flavor 0.1
(6) Purified water 5C168 total
fik 100.0 The same operation as described in Example 3 was performed to prepare a night cream. This night cream had sufficient stability and mild action on the skin, and gave a good feeling of use. In addition, the phospholipid content of purified partially hydrogenated egg yolk lecithin is 99%,
The iodine value is 27.

Example 5 (water-in-oil moisture cream) formulation (2) Glycerin 10.0 (3
) Methyl paraoxybenzoate 0.2(4)
Fragrance 0.2
The components of group (1) were uniformly dissolved by heating and kept at 70°C, and while stirring, the components (21, (3), (5)
Component 1 was heated at the same temperature as above to make a homogeneous solution, then emulsified, cooled while stirring, and heated to 406C (4)
The ingredients were added and cooled while stirring to obtain a moisture cream. This moisture cream had sufficient stability and mild effect on the skin, and gave a good feeling of use. In addition, the phospholipid content of purified soybean lecithin is 95
%, and the iodine value is 47.

Example 6 (emulsion lotion) Prescription ingredients Parts by weight (2)
Glycerin 8.0 (3) Refined soybean 1/cytin 0.2 (4) Methylparaben 0.1 (5) Fragrance
Fee 0.05
(6) Purified water Total amount 100.0 The ingredients of group (1) and (5) were uniformly heated and dissolved in an airtight container, and the total amount was 60.0.
Keep this solution at 9C (21, (31, (41, (6
) were uniformly mixed and dissolved, added to the solution heated to the same temperature with stirring, emulsified, and cooled to obtain an emulsion lotion. This emulsion lotion had sufficient stability and a mild effect on the skin, and gave a good feeling of use. In addition, the phospholipid content of purified partially hydrogenated egg yolk lecithin is 9996,
The iodine value is 27.

Example 7 (Hydrophilic ointment base) Formulation [13 parts by weight (II) parts by weight (2) Propylene glycol 10.0
12.0(3) Methyl paraoxybenzoate 0.1
5 0.05(4) Paraoxybenzoic acid methyl 0.05 0.05(5) Purified water
59.8 38L9 Components of group (1) are uniformly heated and dissolved, kept at 70°C, and while stirring, components (2), (3), (4), +5) are brought to the same temperature in advance. The mixture was heated to form a homogeneous solution and emulsified, and cooled while stirring to obtain hydrophilic ointment bases CI) and [II). This hydrophilic ointment base [technique] and (
II] all had sufficient stability and mild effects on the skin, and gave a good feeling of use. In addition.

The phospholipid content of partially hydrogenated egg yolk lecithin is 25%,
The iodine value is 41.

Example 8 (Pack agent) Prescription (1) The components of the liquid were uniformly heated and dissolved in an airtight container to 60%
While maintaining the temperature at °C, this solution was added to liquid (2) heated to the same temperature as above, and cooled while stirring to obtain liquid A. On the other hand, the components of liquid (3) were dissolved by heating at 85°C in advance, cooled to 35°C while stirring, and liquid A and liquid (4) were added thereto.
The mixture was mixed uniformly to form a pack agent. This pack has sufficient stability and mild effects on the skin.

It gave a good usability. The purified partially hydrogenated egg yolk lecithin has a phospholipid content of 9796 and an iodine value of 27.

The present invention will be explained in detail using the experimental examples described below.

Experimental Example 1 A specimen sample (composition of the present invention), a control sample I, and a control sample ■ were prepared. The composition of each sample is as shown in the column ζ in the table below.The phospholipid content of the 9-partially hydrogenated egg yolk lecithin in the table is 2596, and the iodine value is 20. The salt is composed of 2.5 parts by weight of stearic acid and 0.5 parts by weight of l-arginine.

In addition, each sample was prepared using the following methods.

That is, components (1) to (7) are uniformly heated and dissolved,
The mixture was kept at 75° C., and a solution consisting of the components (81. (91, 10) previously heated and dissolved at 756 C was added with stirring to emulsify, and the mixture was cooled to 356 C while stirring.

Method: 40 women were divided into two groups, 20 each in Group A and Group B, and each sample was used continuously as a moisturizing cream for one month.The effectiveness of use was investigated for the evaluation items listed in Table 1, and the effectiveness rate was determined. Note that the effectiveness rate was calculated using the following formula.

Results The results are shown in Table 1. Table 1 shows that the composition of the present invention is excellent in improving skin roughness and moisturizing the skin.

Experimental Example 2 Samples and Method Samples A to E were prepared. The composition of each sample is as shown in the respective columns of Table 2. In the table, the phospholipid content of the 9-partially hydrogenated egg yolk lecithin is 2596.

The iodine value is 20. In addition, each sample was prepared as follows. That is, 5.5 g of each of (2) and (3) alone or a combination of (2) and (3) was added to 15 g of squalane, dissolved by heating, and heated to 75"C.
Purified water heated to 75°C was added to this while stirring to emulsify it, and the mixture was cooled to 35°C while stirring to form an emulsion.

Each sample was stored at room temperature and 40°C, and changes over time in the emulsified state were observed.

Results: In samples A to C, significant separation of the aqueous phase was already observed after 3 days at room temperature. On the other hand, the emulsions in sample No. 1 and E were both stable, and no change in appearance was observed even after one month at 406C. Therefore, it has been found that lecithin and fatty acid ester according to the present invention have poor emulsification stabilizing power when used alone, but exhibit excellent emulsifying power when used in combination.

Experimental Example 3 Samples A to G were prepared. The composition of each sample is as shown in each column of Table 3. In the table, the phospholipid content of the partially hydrogenated egg yolk lecithin is 2596, and the iodine content is 20.

The table also shows the parts by weight of glycerin monostearate relative to 1 part by weight of partially hydrogenated egg yolk lecithin for each sample. In addition, each sample was prepared using the following methods.

In other words, the same (1) and q are added to the components of group (3) listed in Table 9.
Add the same ingredients (2).

Dissolve by heating and keep at 70°C, add a solution consisting of the components of the same group (4) that has been uniformly dissolved by heating to 70°C with stirring, emulsify, and dissolve at 35°C while stirring.
It was cooled to °C to form an emulsion. Each sample was stored at room temperature and 40°C, and changes over time in the emulsified state were observed.

Results: In samples A and B, significant separation of the aqueous phase was already observed after 3 days at room temperature. Sample C is 10 at room temperature.
Although slight separation of the aqueous layer in the lower layer was observed after a day had passed, the stability was better than that of Samples A and B. Samples E, F
and G were stable in appearance, with no emulsion separation observed not only at room temperature but also after one month at 40°C.

Experimental Example 4 Emulsions A to A were prepared as samples. Each emulsion is shown in the following formulation (, common ingredients (3), (4), (
5).

(6), and components (1) and (2) that differ depending on the emulsion, and components +11. (2) is as shown in Table 4 for each emulsion.

Prescription ingredients Parts by weight (1) Listed in Table 4 25.0 (2)
Listed in Table 4 6.0 (3) Partially hydrogenated egg yolk lecithin 6.0 (4) Stearic acid 1.0 (5) Glycerin
10.0 (6) Purified water 65.0 Table 4 The phospholipid content of the 9 partially hydrogenated egg yolk lecithin in the table is 25% and the iodine value is 20. Each emulsion was prepared as follows. That is, (11, (23, +31 °
51. (The mixed solution of 61 was added and emulsified, and the mixture was cooled to 35° C. while stirring to form an emulsion.

Method and results Each sample was examined for its affinity to the skin.

All were good and gave a mild feel on the skin. Furthermore, when we examined changes during storage at 40°C, we found that
All were stable with no change in appearance and properties even after one month had passed.

Experimental Example 5 Samples Nineteen types of samples were prepared using various lecithins as listed in the lecithin column and iodine value column of Table 5 in the following formulations and containing only the parts by weight listed in the table. However, purified egg yolk lecithin.

In purified soybean lecithin and fractionated soybean lecithin.

To each was further added 3.5 parts by weight of hydrogenated soybean oil, which was then incorporated into the sample.

Prescription weight parts Squalane 16.0 Octyldodecyl myristate 3.0 Lecithin
Cholesterol listed in Table 5
0.5 glycerin monostearic acid
1.0 Ester stearic acid 1.5 Methylparaben 0.2 Glycerin
10.0 Purified water total amount 100
．． 0 Table 5 Methods and Results The samples were stored at 40°C for 3 months, and aqueous phase separation due to the collapse of emulsification was observed. The results are shown in Table 5. In the table, - indicates no separation at all, while 9 cases appear to have separation.

It is small and can be ignored. +: Separation is clearly recognized. +
+ represents significant separation, respectively. Table 5 shows that when the iodine value of lecithin is 50 or less, the stability against aqueous phase separation increases.

Procedural amendment (spontaneous) dated 19th February 1985 Manabu Shiga, Commissioner of the Patent Office1, Indication of the case, 1985 Patent Application No. 437972, Title of the invention: Emulsified external composition 4, Subject of amendment (1) Scope of claims in the specification (2) Column 5 of detailed explanation of the invention in the specification, content of amendments (1) Scope of claims as shown in Attachment 1 (2)
fH specification, page 3, line 3 from the bottom, page 4, line 2 from the bottom
In the first line, the fifth line from the bottom of page 5, and the seventh line from the top of page 37, the words “50 or less” were replaced with “10 to 50.”
” is corrected.

(11) Add the following partial waxing column to the right of the aqueous phase separation column in Table 5 on page 36 of the specification. Attachment 2 shows Table 5, which has been reprinted with two partial waxing columns added.

On page 37 of the Hill specification, the following items a and 2 are added.

B. Addition of "and 00C" after "40℃" in the first line 0. Addition of "warming" before "collapse" in the first line C. Addition of "warming" in the first line "
Addition of “and partial smoking by cooling” after “aqueous phase separation” Addition of “and partial smoking” after “aqueous phase separation” in lines 2 and 7 to 8 2, Claims (1) Iodine value Emulsified composition for external use containing lecithin having a carbon number of 10 to 50 and glycerin monofatty acid ester or propylene glycol monofatty acid ester having a fatty acid carbon number of 12 to 22 (2) A phospholipid in which the lecithin is derived from egg yolk or soybean Emulsified external composition (3) Lecithin 1 according to claim 1, which is a compound or a hydrogenated product thereof
Glycerin monofatty acid ester Mataha flopylene glycol monofatty acid ester is 0.07 to 20% by weight
Emulsified external composition according to claim 1 or 2, which is in parts by weight (4) Claims 1 to 2, wherein the emulsified external composition is a pharmaceutical external preparation or a cosmetic. Amendment form for procedures for emulsified external compositions described in Paragraph 3 (voluntary) June 1q, 1985

Claims (4)

[Claims] (1) An emulsified composition for external use containing lecithin with an iodine value of 50 or less and a glycerin monofatty acid ester or propylene glycol monofatty acid ester with a fatty acid having 12 to 22 carbon atoms. (2) Claim 1, wherein the lecithin is a phospholipid-containing substance derived from egg yolk or soybean, or a hydrogenated product thereof.
Emulsified external composition described in Section 1. (3) The emulsified external composition according to claim 1 or 2, wherein the glycerin monofatty acid ester or propylene glycol monofatty acid ester is 0.07 to 20 parts by weight per 1 part by weight of lecithin. (4) The emulsified external composition according to claims 1 to 3, wherein the emulsified external composition is a pharmaceutical external preparation or a cosmetic.