JPH06262060A - Solubilized composition with transparent oily component - Google Patents

Abstract

PURPOSE:To obtain the title compsn. with improved temp. stability by incorporating a sucrose fatty ester (a), an alkyl glycoside or polyethylene glycol-type surfactant (b), an oily component (c) and water (d) as essential ingredients and using a combination wherein either one of (a) and (b) is lipophilic and another is hydrophilic. CONSTITUTION:A sucrose fatty ester (a) (e.g. sucrose caprylate), an alkyl glycoside e.g. 1-0-hexyl-beta-D-glycopyranoside) or a polyethylene glycol-type surfactant (e.g. polyethylene glycol alkyl ether) (b), an oily component (c) (e.g. heptane) and water (d) are incorporated as essential ingredients and a combination wherein either one of (a) and (b) is lipophilic and another is hydrophilic is used. As the result, stability in the neighborhood of 5-45 deg.C and stability with temp. which have been difficult to realize with the conventional microemulsion can significantly be improved and practical performance on safety and functional side is high.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION The present invention uses sucrose fatty acid ester and a specific nonionic surfactant other than sucrose fatty acid ester, an oil component, and water as essential components, and has a wide composition ratio of water phase and oil phase. The present invention relates to a transparent solubilizing composition of an oily component having excellent temperature stability. The composition of the present invention is a stable solubilizing composition near room temperature,
It is used for pharmaceutical products.

[0002]

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

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 raise the temperature to bring the nonionic surface A region in which the amount of solubilized hydrocarbons sharply increases appears before the cloud point of the activator. It is known that in the region from the solubilization limit temperature to the cloud point shown in the phase diagram, the solubility of oil in the aqueous phase dramatically increases, forming a so-called microemulsion. However, the microemulsion obtained with the nonionic surfactant-hydrocarbon system, which has been conventionally studied, has an increased oil solubilization amount, and thus the hydrophilic-hydrophobic balance (HLB) of the system is maintained. It exists only in a narrow temperature range (usually about 10 ° C.), and outside this temperature range, the system becomes turbid immediately or with time, and eventually has a drawback of separating into an aqueous phase and an oil phase. Therefore, its application to cosmetics and pharmaceuticals is very limited.

The 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 the composition, a region where the solubilization amount of hydrocarbon (oil) is rapidly increased is utilized within a very narrow ratio range in which the HLB of the system is balanced (JP-A-58-128311). , JP-A-58-131127, etc.). However, although the stability against temperature has been solved, the composition in which the microemulsion can stably exist is very limited, and the formulation is limited in the actual product system.

Further, a hydrophilic nonionic surfactant,
A method for preparing a microemulsion from oil (on an organic conceptual diagram) and carbon number limited to a specific range, and water (JP-A-63-126543, JP-A-63-12).
6544) is disclosed, but since the type of oil used, the amount of surfactant added, and the mixing ratio of oil and water are within specific ranges, the range of use thereof is limited.

[0006]

Therefore, the use of the conventionally known microemulsion in cosmetics and pharmaceuticals intended for use at ordinary temperatures has a narrow temperature range in which stable microparticles can exist in the first method. This is difficult from the viewpoint of temperature stability, and the second method has a problem from the viewpoint of compounding. However, with a small amount of nonionic surfactant,
The characteristics of a microemulsion capable of uniformly solubilizing a large amount of oil are very useful, high temperature stability, and completion of a microemulsion having a wide range of blending are desired.

[0007]

Therefore, the present inventors have
As a result of various studies to provide a transparent solubilized composition of an oily component which is stable at room temperature and has excellent temperature stability in a wide composition ratio of an aqueous phase and an oil phase, sucrose fatty acid ester and sucrose fatty acid ester are obtained. The inventors have found that this is possible by using a specific nonionic surfactant other than the above, and have reached the present invention.

That is, the gist of the present invention is that (a) sucrose fatty acid ester (b) alkylglycoside or polyethylene glycol type surfactant (c) oily component (d) water is contained as an essential component, and (a) And a transparent solubilizing composition for an oily component, characterized in that one of (b) and (b) is used in a lipophilic and the other is hydrophilic.

The present invention will be described in detail below. 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 ester and the like can be mentioned, and if replaced with an HLB value representing the degree of hydrophilicity / lipophilicity, it is about 3 to
7, and sucrose caprylate, sucrose caprate, sucrose laurate, sucrose myristate, sucrose palmitate in the range of 7 and 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.

Alkyl glycosides used in the present invention include 1-O-hexyl-β-D-glucopyranoside, 1-O-octyl-β-D-glucopyranoside and 1
-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 are mentioned, and ether type alkyl glycosides such as 1-O-octyl-β-D-glucopyranoside are preferable.

Polyethylene glycol type surfactants used in the present invention include higher alcohol type, thioalcohol type, alkylphenol type, higher fatty acid type, alkyl ether type, alkylamine type, alkylamide type and polypropylene glycol type surfactants. . Of these, polyethylene glycol alkyl ether having a polyoxyethylene chain length of 2 to 4 and a carbon chain length of an alkyl group of 6 to 16, which is about 5 to 9.5 if replaced by an HLB value, or HLB
If it is replaced with a value, it is about 10-14. The polyoxyethylene chain length is 5-10, and the carbon chain length of the alkyl group is 6-14.
Polyethylene glycol alkyl ethers are preferred.

In the present invention, it is essential to use (a) sucrose fatty acid ester and (b) alkyl glycoside or 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 and 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, sulfur Examples thereof include lipids, amino acid lipids, and the like, and liquid paraffin, vaseline, animal oils and fats such as fish oil, vegetable oils and fats such as soybean oil, and a mixture of mineral oils 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)
The total amount of (b) and (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 ( The ratio of the total amount of surfactant) is 0.05 to
It is 0.45, and 0.1 to 0.4 is preferable. In the case of the lipophilic sucrose fatty acid ester (a) and the hydrophilic nonionic surfactant (b), the lipophilic sucrose fatty acid ester has a weight fraction of 0.05 to 0.6. Yes, 0.1
~ 0.5 is preferred. In the case of the lipophilic sucrose fatty acid ester and the 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 solubilizing composition of the oily component of the present invention, the mixing ratio of the oily component and water is arbitrary, and the weight ratio of the oily component to the total weight of the oily component and water is 0.0.
It is 5 to 0.95. The characteristic feature of the transparent solubilizing composition of the oily component according to the present invention is that it is stable at around room temperature and has temperature stability in a wide mixing ratio of an aqueous phase and an oil phase, and as long as it is used at a temperature below the cloud point, any ordinary stability is obtained. The sex test does not cause white turbidity or phase separation. In addition, since a large amount of oil can be stably compounded with a much smaller amount of surfactant than the conventional solubilized system, it can be said that the safety is extremely high.

The transparent solubilizing composition of such oily component is
It can be produced by any known method. For example, it can be prepared by using an emulsifying machine which gives a strong shearing force, for example, a high-pressure homogenizer, but in this method, generally, a transparent solubilizing composition of an oily component is required unless the amount of the surfactant relative to the oil is increased. You can't get things. On the other hand, in producing a transparent solubilizing composition of the present oily component, the temperature of the system is once raised above the solubilization limit temperature of the system, and then cooled according to the production method. It is not necessary to use, and a transparent solubilized composition of an oily component can be easily prepared with a simple stirrer or shaker and a constant temperature bath for temperature control. As described above, the feature of this method is that a stable system can be obtained easily and irrespective of mechanical shearing force, and at the same time, labor saving of the manufacturing process can be achieved.

The transparent solubilizing composition of the oily component of the present invention comprises a sucrose fatty acid ester and a nonionic surfactant other than the sucrose fatty acid ester, and further contains an ionic surfactant depending on the application. May be. In addition, a liquid crystal region may occur in a microemulsion region (also called a surfactant region) in the vicinity where the hydrophilic and lipophilic properties of the system are balanced, but by adding an amphipathic substance such as salt alcohol, etc. It is known that this liquid crystal region can be reduced to enlarge the desired microemulsion region (Shigehiro Yamaguchi et al .: Oil Chemistry, 38 , p.
p. 157-160 (1989)), salts and amphipathic substances may be added, if 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,
If necessary, proteins, peptides, amino acids, mucopolysaccharides such as chondroitin sulfate and hyaluronic acid, glycosides such as saponin, etc. may be added.

Further, to the product to which the transparent solubilizing composition of the oily component according to the present invention is applied, a fragrance, a dye, a preservative, a drug, a thickener, a chelating agent, etc. are appropriately added. To be done.

[0018]

As described in detail above, the present invention provides a transparent sucrose fatty acid ester and a specific nonionic surfactant other than sucrose fatty acid ester, an oil component, and an oil component containing water as an essential component. A solubilized composition,
5 was difficult with conventional microemulsions
The stability near room temperature of 45 ° C and the temperature stability are remarkably improved, and the oil component can be stably compounded with a slightly smaller amount of surfactant than that of the conventional solubilization system. It can be said that it is highly practical in terms of functionality. Further, in the industrial field, the utility value is extremely high in that it is efficient because of easy preparation. In particular, the present invention, due to its advantages, includes cleaning agents, shampoos,
Rinse, hairnic, hair oil, hair lotion, aftershave lotion, body lotion, emollient oil, makeup lotion, cleansing oil, aerosol product, deodorant, fragrance, deodorant,
It can be used for products such as medicinal liquids and bath salts.

[0019]

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

Examples 1 to 5 Sucrose monolaurate (L-1695, HLB value 16, Mitsubishi Kasei Foods Co., Ltd.) as sucrose fatty acid ester, and tetraethylene glycol dodecyl ether (NIKK) as polyethylene glycol type surfactant.
OL BL-4SY, HLB value 9.5, Nikko Chemicals Co., Ltd., heptane (special grade, Tokyo Chemical Industry Co., Ltd.), distilled water were put in a container with the composition shown in Table 1 and heated to 95 ° C. While shaking, the mixture was cooled to room temperature. The evaluation was performed by measuring the 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 in a wide temperature range near room temperature.

Examples 6 to 9 Sucrose dilaurate (L-595, HLB value 5, Mitsubishi Kasei Foods Co., Ltd.) as sucrose fatty acid ester, 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.), distilled water were added to the container in the same manner as described in Examples 1 to 5 with the formulation shown in Table 2. The mixture was charged, shaken while being heated to 95 ° C., and then cooled to room temperature. The evaluation was performed by measuring the temperature range in which the composition was transparent. The results are as shown in Table 2. A transparent solubilizing composition of an oily 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 Foods Co., Ltd.) as sucrose fatty acid ester, and 1-O-octyl-β-D-glucopyranoside (HLB value as alkyl glycoside). 19, Dojindo Laboratories Co., Ltd., heptane (special grade, Tokyo Kasei Kogyo Co., Ltd.), and distilled water were added to the container in the same manner as described in Examples 1 to 5 with the composition shown in Table 3, The mixture was shaken with heating at 95 ° C. and then cooled to room temperature. The evaluation was performed by measuring the 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 in a wide temperature range near room temperature.

Comparative Examples 1-2 Tetraethylene glycol dodecyl ether (NIKKOL BL as a polyethylene glycol type surfactant was used.
-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 in the same manner as in Examples 1 to 5 with distilled water in the formulations shown in Table 4 and evaluated. As shown in Table 4, in Comparative Examples 1 and 2, a transparent solubilized composition of an oily component stable near room temperature could not be obtained.

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

[0025]

[Table 1]

[0026]

[Table 2]

[0027]

[Table 3]

[0028]

[Table 4]

[0029]

[Table 5]

Claims (2)

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