TW201509441A - Emulsification composition - Google Patents

Abstract

This emulsified composition is characterized by containing (a) polyglyceryl monooleate, (b) glycerin, (c) ceresin, and (d) water. The emulsified composition has reduced separation over time, and exceptionaly stable properties, making it useful as an emulsified composition for pharmaceuticals, quasi-drugs, cosmetics, and the like. The emulsified composition may additionally contain oil components such as liquid paraffin, squalane, white petrolatum, and the like, and is preferably of W/O type. A typical formulation contains 0.1 to 20 mass% of ceresin and 0.5 to 40 mass% of polyglyceryl monooleate with respect to the total amount of the emulsified composition, and the ceresin to polyglyceryl monooleate mass ratio is preferably 0.1 to 5:1.

Description

Emulsified composition

The present invention relates to an emulsified composition which can suppress the separation over time and can improve the stability of properties.

The emulsified composition can be roughly classified into an O/W type and a W/O type. The W/O type emulsified composition is composed of oil and internal phase water, and is easy to be water-repellent. Although it has the function of protecting the affected part, it is a preparation which is not sticky like an ointment. As described above, the W/O type emulsified composition has a good feeling of use and is expected to be widely used in the field of pharmaceuticals or cosmetics. On the other hand, in terms of the stability of the W/O type emulsified composition, there is a problem that water separation (water oozing out from the preparation) is likely to occur from the internal water phase over time. In particular, in order to impart a refreshing feeling of use and increase the content of water in the internal water phase, separation is more likely to occur.

Conventionally, as a method for improving the stability of a W/O type emulsified composition, a gelling agent for adding a liquid oily component to a liquid oily base is known to be gelled, and a specific type of oil is used. A method in which a surfactant is emulsified by mixing gelatinized water (Patent Document 1). However, the above W/O Since the emulsified composition uses an oil gelling agent such as a dextrin fatty acid ester as a gelling agent, it has a sticky feeling and has a problem in use.

Heretofore, there has been reported a high water content W/O type emulsified composition obtained by using a glycerol monooleate and a surfactant having a branched chain on an alkyl group (Patent Document 2), but for blending glycerin and An example of a W/O type emulsified composition in which a paraffin wax, a squalane, a white petrolatum, and a polyglycerol monooleate are used as an emulsifier, and an example in which a ground wax is blended to suppress the separation over time is not present. Its report.

[Previous Technical Literature]

[Patent Literature]

[Patent Document 1] Japanese Patent No. 3509108

[Patent Document 2] Japanese Patent Laid-Open Publication No. 2007-153824

The present invention provides an emulsified composition which is excellent in property stability in suppressing chronological separation in an emulsified composition containing polyglycerol monooleate and glycerin.

As a result of intensive studies to solve the above problems, the present inventors have found that an emulsified composition containing polyglycerol monooleate and glycerin is obtained. The present invention can be prepared by blending a ground wax with an emulsified composition which does not undergo separation and which is stable even after long-term storage.

That is, the present invention is: (1) an emulsified composition characterized by containing (a) polyglycerol monooleate, (b) glycerin, (c) ceresin, and (d) water; (2) as ( 1) an emulsified composition, which is a W/O type; (3) an emulsified composition according to (1) or (2), further comprising at least one selected from the group consisting of mobile paraffin, squalane and white petrolatum. (1) The emulsified composition of (1), wherein the content of the ground wax is 0.1 to 20% by mass based on the total mass of the emulsified composition; (5) the emulsified composition of (1), wherein The content of the polyglycerol monooleate is from 0.5 to 40% by mass based on the total mass of the emulsified composition; (6) The emulsified composition of (1), wherein, relative to 1 part by mass of the polyglycerol monooleate, The wax content is 0.1 to 5 parts by mass.

According to the present invention, it is possible to provide an emulsified composition which can suppress separation, has excellent property stability, and is excellent in handling feeling.

Examples of the polyglycerol monooleate of the present invention include diglycerin monooleate and tetraglycerol monooleate, and among these, diglycerin monooleate is preferred. As a polyglycerol monooleate, for example, NIKKOL can also be utilized. Commercial products such as DGMO-CV (trade name: manufactured by Nikko Chemicals Co., Ltd.) and EMALEX MOG-2 (trade name: manufactured by NIHON EMULSION Co., Ltd.). The content of the polyglycerol monooleate is preferably from 0.5 to 40% by mass, more preferably from 1 to 20% by mass, most preferably from 1.5 to 10% by mass, based on the entire emulsified composition of the present invention.

As the glycerin of the present invention, glycerin and/or concentrated glycerin can be used without particular limitation, and more preferably concentrated glycerin. Commercially available products such as glycerin (trade name: manufactured by Sakamoto Pharmaceutical Co., Ltd.) and concentrated glycerin (trade name: manufactured by Kao Co., Ltd.) contained in the Japanese Pharmacopoeia can be used as the glycerin. The content of glycerin is preferably from 5 to 25% by mass based on the entire emulsified composition of the present invention.

As the ceresin of the present invention, first, a solid hydrocarbon derived from minerals obtained by refining natural ozocerite may be mentioned. Although its properties are similar to paraffin, it has the characteristics of higher molecular weight, specific gravity, viscosity, hardness and melting point than paraffin. In general, the ceresin has a melting point of about 60 to 80 ° C, but in the present invention, a ceresin having a melting point of 65 ° C or more is preferred. Further, the "ground wax" referred to in the present invention includes, in addition to the above-mentioned natural producers, a synthetic paraffin which is generally used as a wax and which is a mixture of microcrystalline wax and flowing paraffin. When synthetic paraffin is used, it is recommended to use a melting point of about 60 to 80 ° C, preferably 65 ° C or more. In the present invention, a commercially available product such as ozoke #810 (trade name: NIKKO RICA Co., Ltd.) can also be used. The content of the ceres of the present invention is preferably from 0.1 to 20% by mass, more preferably from 1 to 15% by mass, based on the entire emulsified composition of the present invention. Further, the content of the ground wax is preferably 0.1 to 5 parts by mass based on 1 part by mass of the polyglycerol monooleate.

Preferably, the emulsified composition of the present invention is blended with an oily component. Mobile paraffin, squalane, or white petrolatum.

Commercially available products such as HIGHCALL M-352 (trade name: manufactured by KANEDA Co., Ltd.) can also be used as the liquid paraffin. The content of the liquid paraffin is preferably from 1 to 30% by mass, particularly preferably from 5 to 30% by mass, based on the entire emulsified composition of the present invention.

Commercial products such as squalane-SK (trade name: manufactured by KURARAY Co., Ltd.) can also be used as the squalane of the present invention. The content of squalane is preferably from 0.1 to 20% by mass, more preferably from 0.5 to 10% by mass, even more preferably from 1 to 10% by mass, based on the entire emulsified composition of the present invention.

As the white petrolatum of the present invention, a commercially available product such as white petrolatum (trade name: manufactured by PENRECO Co., Ltd.) can be used. The content of white petrolatum is preferably from 0.1 to 20% by mass, more preferably from 0.5 to 10% by mass, based on the entire emulsified composition of the present invention.

Further, the emulsified composition of the present invention is preferably a W/O type emulsified composition, and examples of the dosage form thereof include an emulsifiable concentrate, an emulsion, and the like. The emulsified composition of the present invention can be applied to pharmaceuticals, quasi-drugs, cosmetics, and the like.

The content of water in the emulsified composition of the present invention is preferably from 1 to 70% by mass, more preferably from 20 to 70% by mass, based on the entire emulsified composition of the present invention. Further, in the present invention, even if 50% by mass or more of water is contained in the composition of the present invention, a W/O type emulsified composition which does not cause separation can be prepared.

The emulsified composition of the present invention may be blended with a component which can be blended with a drug or a cosmetic according to the purpose of use, within the range in which the effects of the present invention are not impaired. When blending drugs, depending on the type of drug Class, widely used in wound healing or anti-inflammatory and itching, endophthalmitis, hemorrhoids and so on.

The drug which can be blended in the emulsified composition of the present invention is not particularly limited, and examples thereof include isopropylmethylphenol, chlorhexidine hydrochloride, benzyloxyethylamine chloride, benzalkonium chloride, and quinoxaline. Ammonium, Japanese tar tar and other fungicides; wound healing agents such as allantoin; anti-histamines such as diphenylamine, diphenylamine, and chlorpheniramine maleate; hydrocortisone acetate, prednisolone acetate , hydrocortisone, prednisolone, dexamethasone propionate, betamethasone propionate, dexamethasone valerate, betamethasone valerate, acetone fluoxetol, triamcinolone steroids and the like. As other components, an antioxidant such as dibutylhydroxytoluene, isopropyl gallate or ethylenediaminetetraacetate; a coolant such as menthol or camphor; a paraben or a benzoate may be blended; , dehydroacetic acid, isoascorbic acid, sorbic acid and other preservatives; citric acid, citrate and other pH adjusters; pigments, spices and so on. Further, it is not limited to the components described so far.

The method for producing the emulsified composition of the present invention is not particularly limited. In general, each component can be produced by mixing into a uniform emulsion or paste-like emulsified composition in an appropriate manufacturing machine.

[Examples]

Hereinafter, the present invention will be further described in detail by way of examples and comparative examples, but is not limited to the examples and the like. Further, the ceres used in the examples and comparative examples were ceresin # 810 (trade name: NIKKO RICA Co., Ltd.; melting point 72 to 76 ° C), and paraffin wax was Paraffin Wax 135 (trade name: NIPPON SEIRO; melting point 55 to 62 °C).

Examples 1 to 6 and Comparative Examples 1 to 2

(modulation method of each emulsified composition)

According to the formula shown in Table 1 below, weigh the ingredients and make the oil phase of diglycerin monooleate, mobile paraffin, squalane, solid fat (ground wax, paraffin or glyceryl monostearate) and white petrolatum. It is heated to about 80 ° C to be melted. The concentrated glycerin and an appropriate amount of pure water were added to prepare an aqueous phase, and after heating to about 80 ° C, the mixture was added to the oil phase while using a homogenizer. After stirring, the W/O type emulsified compositions of Examples 1 to 6 and Comparative Examples 1 and 2 were obtained by cooling.

(Test Example 1)

After the emulsified compositions of Example 1 and Comparative Examples 1 and 2 were stored at 50 ° C for 2 months, the properties of the respective formulations were evaluated based on the following criteria.

Evaluation basis

○: no separation

×: There is separation

The results are shown in Table 1.

As is clear from Table 1, Example 1 in which ceresin was blended did not show changes in properties such as separation of the preparation after storage at 50 ° C for 2 months. On the other hand, in Comparative Examples 1 and 2 in which paraffin wax or glyceryl monostearate belonging to other solid fats was blended, the preparation was separated.

(Test Example 2)

The emulsified compositions of Examples 1 to 6 and Comparative Examples 1 and 2 were centrifuged at 2,700 rpm, and the stability thereof was evaluated. The time before the emulsified composition began to separate was evaluated according to the following criteria.

Evaluation basis

◎: not separated within 6 hours; ○: separation was started after 0.5 to 6 hours; ×: separation was started within 0.5 hours.

The results are shown in Table 3.

Comparative example 3

According to the formula shown in Table 4 below, weigh each component and make it into diglycerin monoisostearate, mobile paraffin, squalane, solid fat (ground wax, paraffin or glyceryl monostearate) and white petrolatum. The oil phase is heated to about 80 ° C for melting. The concentrated glycerin and an appropriate amount of pure water were added to prepare an aqueous phase, and after heating to about 80 ° C, the mixture was added to the oil phase while using a homogenizer. After stirring, the W/O type emulsified composition of Comparative Example 3 was obtained by cooling.

(Test Example 3: feeling test)

The emulsified compositions of Example 1 and Comparative Example 3 were evaluated for their ductility. The stretchability after being placed at 25 ° C for 3 minutes was measured using a spread meter (produced by RIGO). As a result, it was 35.5 mm with respect to the emulsified composition of Example 1, and 26.5 mm of Comparative Example 3. From this, it is understood that the emulsified composition of the present invention has better ductility and a good feeling of use than those using other surfactants.

Example 7, Comparative Example 4~5

(modulation method of emulsified composition)

According to the formula shown in the following Table 5, each component was weighed, and the oil phase formed by diglycerin monooleate, flowing paraffin, squalane, ozokerite, and white petrolatum was heated to about 80 ° C to be melted. Add concentrated glycerin and an appropriate amount of pure water to prepare an aqueous phase, and add benzyl chloroacetamide, chlorpheniramine maleate and allantoin, and then heat to about 80 ° C to dissolve. Add to the oil phase while using a homogenizer. After stirring, the emulsified compositions of Example 7 and Comparative Examples 4 and 5 were obtained by cooling.

(Test Example 4)

After the emulsified compositions of Example 7 and Comparative Examples 4 and 5 were stored at 40 ° C and 75% RH for 6 months, the properties of the respective formulations were evaluated based on the following criteria.

Evaluation basis

○: no separation

×: There is separation

The results are shown in Table 6.

Example 7 blended with ceresin did not separate at 40 ° C from 75% RH to 6 months, maintaining stable properties. Comparative Examples 4 and 5 incorporating other solid fat paraffin or glyceryl monostearate showed separation.

(Examples 8 to 10, Comparative Example 6)

(modulation method of each emulsified composition)

According to the formula shown in Table 7 below, weigh the ingredients and heat the oil phase of diglycerin monooleate, flowing paraffin, squalane, solid fat (homoxyl or glyceryl monostearate) and white petrolatum to It is melted at about 80 °C. The concentrated glycerin and an appropriate amount of pure water were added to prepare an aqueous phase, and after heating to about 80 ° C, the mixture was added to the oil phase while using a homogenizer. After stirring, the W/O type emulsified compositions of Examples 8 to 10 and Comparative Example 6 were obtained by cooling.

The emulsified compositions of Examples 8 to 10 and Comparative Example 6 were centrifuged at 2,700 rpm, and the time before the emulsified composition was started to be separated was evaluated on the same basis as in Test Example 2. The results are shown in Table 7.

[Industrial availability]

According to the present invention, it is possible to provide an emulsified composition which can suppress temporal separation and is excellent in property stability. This emulsified composition is used as a pharmaceutical. Quasi-pharmaceuticals. An emulsified composition such as cosmetics.

Claims (6)

An emulsified composition characterized by comprising (a) polyglycerol monooleate, (b) glycerin, (c) ceresin, and (d) water. The emulsified composition of claim 1, which is of the W/O type. The emulsified composition according to claim 1 or 2, further comprising at least one oil component selected from the group consisting of mobile paraffin, squalane and white petrolatum. The emulsified composition of claim 1, wherein the content of the ceresin is 0.1 to 20% by mass based on the total mass of the emulsified composition. The emulsified composition of claim 1, wherein the content of the polyglycerol monooleate is from 0.5 to 40% by mass based on the total mass of the emulsified composition. The emulsified composition of claim 1, wherein the content of the ceresin is 0.1 to 5 parts by mass based on 1 part by mass of the polyglycerol monooleate.