JP3360341B2 - Transparent solubilizing composition of oily component - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a sucrose fatty acid ester and a specific nonionic surfactant other than the sucrose fatty acid ester, an oily component and water as essential components. The present invention relates to a transparent solubilized composition of an oil component having excellent temperature stability. The composition of the present invention is a solubilized composition that is stable around room temperature,
Used for pharmaceuticals.

[0002]

2. Description of the Related Art Conventionally, there are roughly two methods for producing a transparent solubilized composition of an oil component, a so-called microemulsion. That is, the first is a method using an ordinary nonionic surfactant and oil, and the second is a method using an oil.
Is a method in which an anionic (anionic) surfactant is used in combination with a lipophilic nonionic surfactant and, if necessary, an electrolyte.

[0003] The first method is to add a hydrocarbon (oil) such as cyclohexane or tetradecane to an aqueous solution of a nonionic surfactant such as polyethylene glycol alkyl ether, and increase the temperature. Just before the cloud point of the activator, there appears a region where the amount of solubilized hydrocarbons sharply increases. In the region from the solubility limit temperature to the cloud point shown in the phase diagram, it is known that the solubility of the oil in the aqueous phase increases dramatically, forming a so-called microemulsion. However, microemulsions with increased oil solubilization obtained with nonionic surfactant-hydrocarbon systems that have been studied previously have a very high hydrophilic-hydrophobic balance (HLB) of the system. It exists only in a narrow temperature range (generally, about 10 ° C.). Outside this temperature range, the system becomes cloudy immediately or over time, and has a drawback that it is separated into an aqueous phase and an oil phase. For this reason, application to cosmetics and pharmaceuticals is very limited.

A second method is to add an electrolyte to a lipophilic nonionic surfactant and a specific anionic surfactant or a combination of a lipophilic nonionic surfactant and an ionic surfactant. In a very narrow ratio range in which the HLB of the system is balanced from the composition, a region in which the solubilization amount of hydrocarbon (oil) is rapidly increased is used (JP-A-58-128311). And JP-A-58-131127). However, although the stability with respect to temperature has been solved, the composition in which the microemulsion can exist stably is very limited, and the composition is limited in an actual product system.

[0005] Further, a hydrophilic nonionic surfactant,
A method for preparing a microemulsion from oil (in the organic conceptual diagram) and a carbon number limited to a specific range, and water (JP-A-63-126543, JP-A-63-12)
6544) is disclosed, but the type of oil to be used, the amount of surfactant added, and the mixing ratio of oil and water are in specific ranges, which limits the range of use.

[0006]

For this reason, the use of conventionally known microemulsions for cosmetics and pharmaceuticals intended for use at ordinary temperatures requires a narrow temperature range in which the first method can stably exist. It is difficult from the viewpoint of temperature stability as described above, and the second method is problematic from the viewpoint of compounding. However, with a small amount of nonionic surfactant,
The properties of microemulsions that can uniformly solubilize a large amount of oil are very useful, have high temperature stability, and have been desired to complete microemulsions with a wide range of formulations.

[0007]

Means for Solving the Problems Accordingly, the present inventors have:
As a result of various studies to provide a transparent solubilized composition of an oily component which is stable at around room temperature and has excellent temperature stability in a wide range of composition ratio of an aqueous phase and an oil phase, sucrose fatty acid ester and sucrose fatty acid ester The present invention has been found to be possible by using a specific nonionic surfactant other than the above in combination.

That is, the gist of the present invention is that (a) a sucrose fatty acid ester, (b) an alkyl glycoside or a polyethylene glycol type surfactant, (c) an oily component, (d) water as an essential component, and (a) And (b) in a transparent solubilized composition of an oily component, wherein the composition is used in a combination in which one of them is lipophilic and the other is hydrophilic.

Hereinafter, the present invention will be described in detail. Examples of the sucrose fatty acid ester used in the present invention include sucrose caprylate, sucrose caprate, sucrose laurate, sucrose myristate, sucrose palmitate, sucrose stearate, and sucrose. Oleic acid esters and the like can be mentioned, and if they are replaced with HLB values indicating the degree of hydrophilicity / lipophilicity, about 3 to
Sucrose caprylate, sucrose caprate, sucrose laurate, sucrose myristate, sucrose palmitate in the range of 7, and in the range of about 12-16 are preferred. Here, the hydrophilicity means an HLB value of 11 or more, and the lipophilicity means an HLB value of 10 or less.

The alkyl glycoside used in the present invention includes 1-O-hexyl-β-D-glucopyranoside, 1-O-octyl-β-D-glucopyranoside,
-O-decyl-β-D-glucopyranoside, 1-O-dodecyl-β-D-glucopyranoside, 1-S-heptyl-β-D-thioglucopyranoside, 1-S-octyl-
β-D-thioglucopyranoside, 1-O-octyl-β
-D-galactoside, 1-O-octyl-β-D-fucose, 1-O-octyl-β-D-xylose, 1-O
-Octyl-β-D-cellobiose, 1-S-octyl-β-D-thiocellobiose, 1-O-decyl-β-D
-Maltoside, 1-O-dodecyl-β-D-maltoside, and the like, and ether-type alkyl glycosides such as 1-O-octyl-β-D-glucopyranoside are preferable.

The polyethylene glycol type surfactants used in the present invention include higher alcohols, thioalcohols, alkylphenols, higher fatty acids, alkyl ethers, alkylamines, alkylamides and polypropylene glycols. . Among them, a polyethylene glycol alkyl ether having a polyoxyethylene chain length of about 5 to 9.5 when converted to an HLB value and a carbon chain length of an alkyl group of 6 to 16, or HLB
If the value is replaced with about 10-14, the polyoxyethylene chain length is about 5-10, and the carbon chain length of the alkyl group is about 6-14.
Is preferred.

In the present invention, it is essential to use (a) a sucrose fatty acid ester and (b) an alkyl glycoside or a polyethylene glycol type surfactant in a combination in which one is hydrophilic and the other is lipophilic. The oily component used in the present invention is not limited, but hydrocarbons such as n-heptane, n-octane, n-decane, cyclohexane, squalene, squalane, ethers such as diheptyl ether, diethers such as ethylene glycol dibutyl ether , Long-chain alcohols, long-chain amino alcohols such as sphingosine, long-chain aldehydes, long-chain ketones, terpenoids, steroids, carotenoids, waxes, acylglycerols, ether glycerides, ceramides, phospholipids, glycolipids, phosphoglycolipids, sulfates Examples thereof include lipids, amino acid lipids, and the like, and mixtures of liquid paraffin, vaseline, animal oils such as fish oil, vegetable oils such as soybean oil, and mineral oil may be used.

The composition of the transparent solubilizing composition of the oily component in the present invention can be selected from a wide range. For example, in order to obtain a transparent composition at 5 to 45 ° C., (a)
And the total amount of (b) is 0.05 to 30% by weight, preferably 2 to 20% by weight in the transparent solubilizing composition of the oily component. When the combination of both surfactants is the hydrophilic sucrose fatty acid ester (a) and the lipophilic nonionic surfactant (b), the weight fraction of the hydrophilic sucrose fatty acid ester ( Ratio to the total amount of surfactants) is 0.05 to
0.45, preferably 0.1 to 0.4. When the lipophilic sucrose fatty acid ester (a) and the hydrophilic nonionic surfactant (b) are used, the weight fraction of the lipophilic sucrose fatty acid ester is 0.05 to 0.6. Yes, 0.1
~ 0.5 is preferred. In the case of a lipophilic sucrose fatty acid ester and a hydrophilic alkyl glycoside, the weight fraction of the lipophilic sucrose fatty acid ester is 0.80 to 0.99, preferably 0.82 to 0.95.

In the transparent solubilized composition of the oily component of the present invention, the mixing ratio of the oily component and water is arbitrary, and expressed as a weight fraction of the oily component with respect to the total weight of the oily component and water.
5 to 0.95. The feature of the transparent solubilized composition of the oily component according to the present invention is that it is stable near room temperature and temperature stability in a wide mixing ratio of the aqueous phase and the oil phase. No turbidity or phase separation occurs in the sex test. In addition, since a large amount of oil can be stably compounded with a much smaller amount of surfactant than the conventional solubilization system, it can be said that the safety is extremely high.

[0015] The transparent solubilized composition of the oil component is as follows:
It can be produced by any known method. For example, it can be prepared by using an emulsifier that gives a strong shearing force, for example, a high-pressure homogenizer. However, in this method, a transparent solubilizing composition of a good oily component is generally required unless the amount of the surfactant to the oil is increased. You can't get anything. On the other hand, when producing a transparent solubilized composition of the present oily component, according to the production method in which the temperature of the system is once increased to the solubilization limit temperature of the system and then cooled, a special emulsifying machine is used. The use of a simple stirrer or shaker and a thermostat for temperature control makes it possible to easily prepare a transparent solubilized composition of an oily component. As described above, the feature of the present method is that a more stable system can be easily obtained irrespective of the mechanical shearing force, and at the same time, the production process can be labor-saving.

The transparent solubilized composition of the oily component of the present invention further comprises an ionic surfactant in addition to sucrose fatty acid ester and nonionic surfactant other than sucrose fatty acid ester depending on the use. You may. In addition, a liquid crystal region may be generated in a microemulsion region (also referred to as a surfactant region) in the vicinity where the hydrophilic lipophilicity of the system is balanced, but by adding an amphiphilic substance such as a salt alcohol, etc. It is known that this liquid crystal region can be reduced to expand the target microemulsion region (Yamaguchi Shigehiro et al .: Yuki Kagaku, 38 , p.
p. 157-160 (1989)), and salts and amphiphilic substances may be added as necessary. In the aqueous phase, sugars such as glucose and oligosaccharides, linear polyols such as glycerol, sorbitol and ethylene glycol, sugar alcohols such as maltitol and reduced oligosaccharides, lower alcohols such as methyl alcohol and propyl alcohol,
Proteins, peptides, amino acids, mucopolysaccharides such as chondroitin sulfate and hyaluronic acid, and glycosides such as saponin may be added as necessary.

Further, if necessary, a fragrance, a pigment, a preservative, a drug, a thickener, a chelating agent, etc. may be added to a product to which the transparent solubilizing composition of the oily component according to the present invention is applied. Is done.

[0018]

As described in detail above, the present invention relates to transparent sucrose fatty acid esters and specific nonionic surfactants other than sucrose fatty acid esters, oily components, and oily components containing water as an essential component. Pertains to a solubilizing composition,
5 which was considered difficult with conventional microemulsions
The stability near the room temperature of 45 ° C. and the temperature stability are remarkably improved, and the oil component can be stably compounded with a small amount of a surfactant with respect to the conventional solubilization system. It can be said that it is highly practical in terms of functionality. In the industrial field, the utility value is extremely high in that the preparation is easy and the efficiency is high. In particular, the present invention, due to its advantages, has cleaning agents, shampoos,
Rinse, hair tonic, hair oil, hair lotion, after shave lotion, body lotion, emollient oil, makeup lotion, cleansing oil, aerosol products, deodorant, fragrance, deodorant,
It can be used for products such as pharmaceutical solutions and bath preparations.

[0019]

EXAMPLES Next, the present invention will be described more specifically with reference to examples, but the present invention is not limited to the following examples unless it exceeds the gist of the present invention.

Examples 1-5 Sucrose monolaurate (L-1695, HLB value 16, Mitsubishi Chemical Foods Co., Ltd.) as a sucrose fatty acid ester, and tetraethylene glycol dodecyl ether (NIKK) as a polyethylene glycol type surfactant
OL BL-4SY, HLB value of 9.5, Nikko Chemicals Co., Ltd., heptane (special grade, Tokyo Chemical Industry Co., Ltd.), and distilled water were charged into a container with the composition shown in Table 1 and heated to 95 ° C. After shaking, the mixture was cooled to room temperature. The evaluation was performed by measuring a temperature range in which the composition was transparent. The results are as shown in Table 1. The transparent solubilized composition of the oily component prepared by the method of the present invention was stable near room temperature over a wide temperature range.

Examples 6 to 9 Sucrose dilaurate (L-595, HLB value 5, Mitsubishi Kasei Food Co., Ltd.) as a sucrose fatty acid ester, and octaethylene glycol dodecyl ether (NIKKOL BL-) as a polyethylene glycol type surfactant.
8SY, HLB value 13, Nikko Chemicals Co., Ltd., heptane (special grade, Tokyo Kasei Kogyo Co., Ltd.), and distilled water in a container in the same manner as described in Examples 1 to 5 with the composition shown in Table 2. The mixture was shaken while heating to 95 ° C., and then cooled to room temperature. The evaluation was performed by measuring a temperature range in which the composition was transparent. The results are as shown in Table 2. The transparent solubilized composition of the oil component prepared by the method of the present invention,
It was stable in a wide temperature range near room temperature.

Examples 10 to 14 Sucrose dilaurate (L-595, HLB value 5, Mitsubishi Kasei Food Co., Ltd.) as a sucrose fatty acid ester, and 1-O-octyl-β-D-glucopyranoside (HLB value) as an alkyl glycoside. 19, Dojin Chemical Research Laboratories), heptane (special grade, Tokyo Chemical Industry Co., Ltd.), and distilled water in the same manner as described in Examples 1 to 5 in the formulation shown in Table 3 in a container, The mixture was shaken while being heated to 95 ° C., and then cooled to room temperature. The evaluation was performed by measuring a temperature range in which the composition was transparent. The results are as shown in Table 3. The transparent solubilized composition of the oily component prepared by the method of the present invention was stable near room temperature over a wide temperature range.

Comparative Examples 1-2 Tetraethylene glycol dodecyl ether (NIKKOL BL) was used as a polyethylene glycol type surfactant.
-4SY, HLB value 9.5, Nikko Chemicals Co., Ltd.) and octaethylene glycol dodecyl ether (NI
KKOL BL-8SY, HLB value 13, Nikko Chemicals Co., Ltd., heptane (special grade, Tokyo Chemical Industry Co., Ltd.),
Compositions were prepared and evaluated in the same manner as in Examples 1 to 5 using distilled water in the composition shown in Table 4. As shown in Table 4, in Comparative Examples 1 and 2, a transparent solubilized composition of an oily component stable at around room temperature could not be obtained.

Comparative Examples 3 and 4 Sucrose monolaurate (L-1695, HLB value 16, Mitsubishi Kasei Food Co., Ltd.) and sucrose dilaurate (L-59) were used as sucrose fatty acid esters.
5, an HLB value of 5, Mitsubishi Kasei Foods Co., Ltd., decane (special grade, Tokyo Chemical Industry Co., Ltd.), and distilled water were prepared in the same manner as in Examples 1 to 5 with the composition shown in Table 5. evaluated.
As shown in Table 5, in Comparative Examples 3 and 4, a transparent solubilized composition of an oily component stable at around room temperature could not be obtained.

[0025]

[Table 1]

[0026]

[Table 2]

[0027]

[Table 3]

[0028]

[Table 4]

[0029]

[Table 5]

Claims (2)

(57) [Claims] 1. A sucrose fatty acid ester, (b) an alkyl glycoside or a polyethylene glycol type surfactant, (c) an oily component, (d) water as an essential component, and any of (a) and (b) A transparent solubilized composition of an oil component, wherein the composition is used in a combination in which one is lipophilic and the other is hydrophilic. 2. The solubilizing composition according to claim 1, which has a uniform and transparent appearance in a temperature range of 5 to 45 ° C.