JPWO2014171507A1 - Emulsified composition - Google Patents

Abstract

The emulsion composition characterized by containing (a) polyglyceryl monooleate, (b) glycerin, (c) ceresin, and (d) water is excellent in property stability because separation with time is suppressed. The emulsified composition is useful as an emulsified composition for pharmaceuticals, quasi drugs, cosmetics, and the like. The emulsified composition may further contain an oily component such as liquid paraffin, squalane and white petrolatum, and is preferably W / O type. Typically, it contains 0.1 to 20% by weight of ceresin, 0.5 to 40% by weight of polyglyceryl monooleate with respect to the total weight of the emulsion composition, and the weight ratio of ceresin to polyglyceryl monooleate is preferably 0.1-5: 1.

Description

  The present invention relates to an emulsified composition that suppresses separation with time and improves property stability.

The emulsified compositions are roughly classified into O / W type and W / O type. The W / O type emulsified composition is composed of an oil as an outer phase and water as an inner phase, so that it easily repels water and protects an affected area, but does not have stickiness like an ointment. As described above, since the W / O emulsion composition has a good usability, it is expected to be widely used in the pharmaceutical and cosmetic fields. On the other hand, regarding the stability of the W / O emulsion composition, there is a problem that water is likely to be separated from the inner aqueous phase with time (leaching of water from the preparation). In particular, when the content of water in the inner aqueous phase is increased in order to give a refreshing feeling of use, separation is more likely to occur.
Conventionally, as a method for improving the stability of a W / O type emulsion composition, a liquid oily base is added with a gelling agent of a liquid oily component to cause gelation, and then gelled with a specific water-in-oil surfactant. A method of emulsifying by mixing with water is known (Patent Document 1). However, since the W / O emulsion composition uses an oily gelling agent such as a dextrin fatty acid ester as a gelling agent, stickiness occurs, and there is a problem in terms of usability.

  So far, a high water content W / O emulsion composition has been reported by using a glyceryl monooleate and a surfactant having a branched chain in the alkyl group (Patent Document 2). Regarding W / O type emulsified composition containing liquid paraffin, squalane and white petrolatum selectively and emulsifying polyglyceryl monooleate as an emulsifier, there has been reported an example where ceresin was blended to prevent separation over time. Absent.

Patent 3509108 JP 2007-153824 A

  This invention is providing the emulsion composition which suppressed separation with time and was excellent in property stability in the emulsion composition containing monoglyceryl monooleate and glycerin.

  As a result of intensive studies to solve the above-mentioned problems, the present inventor did not cause separation by blending ceresin into an emulsified composition containing polyglyceryl monooleate and glycerin, and stable in properties even after long-term storage. The present invention has been completed by finding that it can be made into an emulsified composition.

That is, the present invention
(1) An emulsified composition containing (a) polyglyceryl monooleate, (b) glycerin, (c) ceresin, and (d) water,
(2) The emulsion composition according to (1), which is a W / O type,
(3) The emulsion composition according to (1) or (2), further comprising at least one oily component selected from the group consisting of liquid paraffin, squalane and white petrolatum,
(4) The emulsified composition according to (1), wherein the content of ceresin is 0.1 to 20% by mass relative to the total mass of the emulsified composition,
(5) The emulsion composition according to (1), wherein the content of polyglyceryl monooleate is 0.5 to 40% by mass relative to the total mass of the emulsion composition,
(6) The emulsified composition according to (1), wherein the content of ceresin is 0.1 to 5 parts by mass with respect to 1 part by mass of polyglyceryl monooleate,
It is.

  According to the present invention, it is possible to provide an emulsified composition that suppresses separation, is excellent in property stability, and has a good usability.

  Examples of the polyglyceryl monooleate of the present invention include diglyceryl monooleate, tetraglyceryl monooleate, and the like. Among these, diglyceryl monooleate is preferable. As polyglyceryl monooleate, commercially available products such as NIKKOL DGMO-CV (trade name: manufactured by Nikko Chemicals Co., Ltd.) and EMALEX MOG-2 (trade name: manufactured by Nippon Emulsion Co., Ltd.) can be used. The content of polyglyceryl monooleate is preferably 0.5 to 40% by mass, more preferably 1 to 20% by mass, and most preferably 1.5 to 10% by mass with respect to the whole emulsion composition of the present invention. %.

  As glycerin of the present invention, glycerin and / or concentrated glycerin can be used, and there is no particular limitation, but concentrated glycerin is more preferable. As this glycerin, commercially available products such as glycerin (trade name: manufactured by Sakamoto Yakuhin Kogyo Co., Ltd.) and Japanese Pharmacopoeia Concentrated Glycerin (trade name: manufactured by Kao Corporation) can also be used. As for content of glycerol, 5-25 mass% is preferable with respect to the whole emulsion composition of this invention.

  Examples of ceresin of the present invention include mineral-derived solid hydrocarbons obtained by purifying ozokerite. The properties are similar to paraffin, but are characterized by higher molecular weight, specific gravity, viscosity, hardness, melting point, etc. than paraffin. Normally, ceresin has a melting point of about 60 to 80 ° C., but ceresin having a melting point of 65 ° C. or more is preferred in the present invention. The ceresin referred to in the present invention includes synthetic paraffin, which is a mixture of microcrystalline wax and liquid paraffin, which is usually used as a substitute for ceresin, in addition to the above naturally produced one. Even when synthetic paraffin is used, it is recommended that its melting point is about 60 to 80 ° C., preferably 65 ° C. or higher. In the present invention, commercially available products such as ceresin # 810 (trade name: Nikko Rika Co., Ltd.) can also be used. 0.1-20 mass% is preferable with respect to the whole emulsion composition of this invention, and, as for content of the ceresin of this invention, More preferably, it is 1-15 mass%. Moreover, the content of ceresin is preferably 0.1 to 5 parts by mass with respect to 1 part by mass of polyglyceryl monooleate.

The emulsified composition of the present invention preferably contains oily components such as liquid paraffin, squalane, or white petrolatum.
As the liquid paraffin, commercially available products such as HICOAL M-352 (trade name: manufactured by Kaneda Corporation) can be used. 1-30 mass% is preferable with respect to the whole emulsion composition of this invention, and, as for content of a liquid paraffin, 5-30 mass% is especially preferable.

  As the squalane according to the present invention, a commercially available product such as squalane-SK (trade name: manufactured by Kuraray Co., Ltd.) can be used. The content of squalane is preferably 0.1 to 20% by mass, more preferably 0.5 to 10% by mass, and further preferably 1 to 10% by mass with respect to the entire emulsion composition of the present invention.

  As white petrolatum of the present invention, commercial products such as white petrolatum (trade name: manufactured by PENRECO) can be used. 0.1-20 mass% is preferable with respect to the whole emulsion composition of this invention, and, as for content of white petrolatum, More preferably, it is 0.5-10 mass%.

  The emulsified composition of the present invention is preferably a W / O type emulsified composition, and examples of the dosage form include creams and emulsions. The emulsified composition of the present invention is applicable to pharmaceuticals, quasi drugs, cosmetics and the like.

  1-70 mass% is preferable with respect to the whole emulsion composition of this invention, and, as for content of the water in the emulsion composition of this invention, More preferably, it is 20-70 mass%. Moreover, in this invention, even if it contains 50 mass% or more of water in the composition of this invention, preparation of the W / O type | mold emulsion composition which does not produce a separation is possible.

In the emulsified composition of the present invention, components that can be blended in drugs or cosmetics according to the purpose of use can be blended according to the purpose of use within the range not impairing the effects of the present invention. When a drug is blended, it can be widely applied to wound healing, anti-inflammatory antiseptic, stomatitis, hemorrhoid disease, etc., depending on the type of drug.
The drug that can be blended in the emulsified composition of the present invention is not particularly limited, for example, bactericides such as isopropylmethylphenol, chlorhexidine hydrochloride, benzethonium chloride, benzalkonium chloride, decalinium chloride, hinokitiol, wound healing agents such as allantoin, Antihistamines such as diphenhydramine hydrochloride, diphenhydramine, chlorpheniramine maleate, hydrocortisone acetate, prednisolone acetate, hydrocortisone, prednisolone, dexamethasone propionate, betamethasone propionate, dexamethasone valerate, betamethasone valerate, fluocinolone acetonide acetonide Steroids. Other ingredients include antioxidants such as dibutylhydroxytoluene, isopropyl gallate and edetate, refreshing agents such as menthol and camphor, parabens, benzoates, preservatives such as dehydroacetic acid, erythorbic acid and sorbic acid, PH adjusting agents such as acids and citrates, pigments, and fragrances can be blended. In addition, it is not limited about the component described until now.

  The manufacturing method of the emulsion composition of this invention is not specifically limited. Usually, it can manufacture by mixing each component so that it may become a uniform emulsion or paste-form emulsion composition with a suitable manufacturing machine.

  Hereinafter, the present invention will be described in more detail with reference to examples and comparative examples, but the present invention is not limited to these examples. In addition, the ceresin used by the Example and the comparative example is ceresin # 810 (brand name: Nikko Rika Co., Ltd. melting point 72-76 degreeC), and a paraffin is paraffin wax 135 (brand name: Nippon Seiwa wax melting point 55-62 degreeC). .

Examples 1-6, Comparative Examples 1-2
(Preparation method of each emulsified composition)
According to the formulation shown in Table 1 below, each component was weighed, and an oil phase consisting of diglyceryl monooleate, liquid paraffin, squalane, solid fat (ceresin, paraffin or glyceryl monostearate), white petrolatum was brought to about 80 ° C. Warmed and melted. Concentrated glycerin and appropriately purified water were added to form an aqueous phase, heated to about 80 ° C., and then added to the oil phase while applying a homomixer. After stirring, the mixture was cooled to obtain W / O type emulsion compositions of Examples 1 to 6 and Comparative Examples 1 and 2.

(Test Example 1)
After the emulsion compositions of Example 1 and Comparative Examples 1 and 2 were stored at 50 ° C. for 2 months, the properties of each preparation were evaluated based on the following evaluation criteria.

Evaluation criteria ○: No separation ×: With separation The results are shown in Table 1.

  As is clear from Table 1, Example 1 containing ceresin showed no change in properties such as separation of the preparation even after storage at 50 ° C. for 2 months. In contrast, Comparative Examples 1 and 2 containing other solid fats such as paraffin or glyceryl monostearate caused separation of the preparations.

(Test Example 2)
The emulsion compositions of Examples 1 to 6 and Comparative Examples 1 and 2 were centrifuged at 2700 rpm, and the stability was evaluated. The time until the emulsified composition began to separate was evaluated according to the following evaluation criteria.

Evaluation Criteria A: Not separated within 6 hours.
○: Separation began within 0.5 to less than 6 hours.
X: Separation started in less than 0.5 hours.
The results are shown in Table 3.

Comparative Example 3
According to the formulation shown in Table 4 below, each component was weighed, and an oil phase consisting of diglyceryl monoisostearate, liquid paraffin, squalane, solid fat (ceresin, paraffin or glyceryl monostearate), white petrolatum was brought to about 80 ° C. Warmed and melted. Concentrated glycerin and appropriately purified water were added to form an aqueous phase, heated to about 80 ° C., and then added to the oil phase while applying a homomixer. After stirring, the mixture was cooled to obtain a W / O type emulsion composition of Comparative Example 3.

(Test Example 3: Usability test)
About the emulsified composition of Example 1 and Comparative Example 3, the spreadability was evaluated. The spreadability after 3 minutes at 25 ° C. was measured with a spread meter (manufactured by Kogaisha). As a result, the emulsion composition of Example 1 was 35.5 mm, while Comparative Example 3 was 26.5 mm. Therefore, it was found that the emulsified composition of the present invention has a longer elongation and a better feeling when used than other surfactants.

Example 7, Comparative Examples 4-5
(Preparation method of emulsified composition)
According to the formulation shown in Table 5 below, each component is weighed, and an oil phase composed of diglyceryl monooleate, liquid paraffin, squalane, ceresin and white petrolatum is heated to about 80 ° C. and melted. Concentrated glycerin and appropriately purified water were added to form an aqueous phase, and after adding benzethonium chloride, chlorpheniramine maleate, and allantoin, the mixture was heated to about 80 ° C. and dissolved. The water phase was added to the oil phase while applying the homomixer. After stirring, the mixture was cooled to obtain emulsified compositions of Example 7 and Comparative Examples 4 and 5.

(Test Example 4)
After the emulsion compositions of Example 7 and Comparative Examples 4 and 5 were stored for 6 months under 40 ° C. and 75% RH conditions, the properties of each preparation were evaluated based on the following evaluation criteria.

Evaluation criteria ○: No separation ×: With separation The results are shown in Table 6.

  Example 7 containing ceresin did not cause separation until 6 months at 40 ° C. and 75% RH, and maintained stable properties. In Comparative Examples 4 and 5 in which other solid fats such as paraffin or glyceryl monostearate were blended, separation was observed.

(Examples 8 to 10, Comparative Example 6)
(Preparation method of each emulsified composition)
Each component was weighed according to the formulation shown in Table 7 below, and an oil phase consisting of diglyceryl monooleate, liquid paraffin, squalane, solid fat (ceresin or glyceryl monostearate), and white petrolatum was added to about 80 ° C. Warm and melt. Concentrated glycerin and appropriately purified water were added to form an aqueous phase, heated to about 80 ° C., and then added to the oil phase while applying a homomixer. After stirring, the mixture was cooled to obtain W / O type emulsion compositions of Examples 8 to 10 and Comparative Example 6.
The emulsified compositions of Examples 8 to 10 and Comparative Example 6 were centrifuged at 2700 rpm, and the time until the emulsified composition started to be separated was evaluated according to the same evaluation criteria as in Test Example 2. The results are shown in Table 7.

  According to the present invention, it is possible to provide an emulsified composition that suppresses separation with time and is excellent in property stability. The emulsified composition is useful as an emulsified composition for pharmaceuticals, quasi drugs, cosmetics and the like.

Claims (6)

  An emulsified composition comprising (a) polyglyceryl monooleate, (b) glycerin, (c) ceresin, and (d) water.   The emulsified composition according to claim 1, which is W / O type.   Furthermore, the emulsion composition of Claim 1 or 2 containing the at least 1 sort (s) of oily component chosen from the group which consists of a liquid paraffin, squalane, and white petrolatum.   The emulsified composition according to claim 1, wherein the content of ceresin is 0.1 to 20% by mass relative to the total mass of the emulsified composition.   The emulsified composition according to claim 1, wherein the content of polyglyceryl monooleate is 0.5 to 40% by mass with respect to the total mass of the emulsified composition.   The emulsified composition according to claim 1, wherein the content of ceresin is 0.1 to 5 parts by mass with respect to 1 part by mass of polyglyceryl monooleate.