Emulsion composition

A technology for emulsifying compositions and compounds, which can be used in drug combinations, cosmetics, emulsion delivery, etc., can solve problems such as strong skin irritation, and achieve good emulsifying stability.

Inactive Publication Date: 2015-09-30
FUJIFILM CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, propylene glycol is known to be highly irritating to the skin as disclosed in Contact Dermatitis 2005, 53, 247-259.

Method used

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  • Emulsion composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0114]

[0115] Add 2.5 g of isostearic acid (mixture) (manufactured by Advanced Alcohol Industry Co., Ltd., "Isostearic Acid EX" (trade name, the same below), and 1,3-butanediol ( 5.0 g of Wako Pure Chemical Industries, Ltd.), stirred at room temperature for 10 minutes. After 0.6 g of minoxidil (manufactured by SOLMAG) was added, the sodium hydroxide solution (manufactured by Wako Pure Chemical Industries, Ltd.) was added. , 1mol / L) 2.0g, 39.9g of Milli-Q water, stirred at room temperature for 3.5 hours. After the resulting mixture was allowed to stand at room temperature for 12 hours, a high-pressure homogenizer was used for high-pressure emulsification Thus, a target emulsion ((C-1), minoxidil concentration 1.2% by mass, pH 8.0) containing emulsified particles with a particle diameter of 223 nm was obtained.

Embodiment 2

[0117]

[0118] Add 2.5 g of isostearic acid (mixture) (manufactured by Advanced Alcohol Industry Co., Ltd., "isostearic acid EX") and 1,3-butanediol (Wako Pure Chemical Industries, Ltd.) to a 110 mL vial equipped with a stir bar Preparation) 5.0g, stirred at room temperature for 10 minutes. After adding 0.6 g of minoxidil (manufactured by SOLMAG), 5.0 g of sodium hydroxide solution (Wako Pure Chemical Industries, Ltd., 1 mol / L) prepared in advance, 35.2 g of Milli-Q water, and sucrose were added Fatty acid ester (manufactured by Daiichi Kogyo Pharmaceutical Co., Ltd., "DK ESTER F-90" (trade name, the same below), sucrose stearate (mono-substituted 45%, di- and tri-substituted 55%), HLB value 9.5) 1.7 g, stirred at room temperature for 3.5 hours. After the obtained mixed solution was allowed to stand at room temperature for 12 hours, it was subjected to a high-pressure emulsification treatment under the same conditions as in Example 1 by a high-pressure homogenizer, thereby ob...

Embodiment 3

[0120]

[0121] Except that 1.7 g of sucrose fatty acid ester (DK ESTER F-90) described in Example 2 was changed to sucrose fatty acid ester (manufactured by Daiichi Kogyo Co., Ltd., "DK ESTER SS" (trade name, the same below), sucrose Stearate (monosubstituted 100%), HLB value 19) 0.5g, the same operation as Example 2 to obtain the target emulsion containing 54nm particle diameter emulsified particles ((C-3), minoxidil Concentration 1.2% by mass, pH 8.3).

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Abstract

An emulsion composition which contains a compound having a diaminopyrimidine skeleton, at least one fatty acid component that is selected from the group consisting of fatty acids having 14 or more carbon atoms in total and salts of the fatty acids, and an aqueous medium in an amount of 50% by mass or more relative to the mass of the emulsion composition. In this emulsion composition, the total content of a monohydric alcohol that has 3 or less carbon atoms in total and a dihydric alcohol that has 3 or less carbon atoms in total is less than 10% by mass relative to the mass of the emulsion composition. This emulsion composition has a pH of 6.5 or more.

Description

Technical field [0001] The present invention relates to emulsified compositions. Background technique [0002] Among the compounds having a diaminopyrimidine skeleton (hereinafter referred to as "diaminopyrimidine derivatives"), for example, minoxidil (2,4-diamino-6-piperidinylpyrimidine-3-oxide), etc. , It is known as a compound with the treatment and prevention effects of androgen alopecia. Japanese Patent Application Laid-Open No. 2004-155689 and Japanese Patent Application Publication No. 2004-155690 disclose that diaminopyrimidine derivatives have low solubility in water and therefore use 50% or more of ethanol to dissolve them in a water solvent. [0003] However, regarding the composition containing more than 50% ethanol, as disclosed in Contact Dermatitis 1994, 30, 1-6. and The Journal of Investigative Dermatology 1977, 69, 219-222., there is concern about scalp irritation caused by ethanol. Sex and so on. Therefore, in order to make minoxidil soluble, a liquid compositi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61K8/34A61K8/36A61K8/37A61K8/49A61K8/86A61K9/10A61K47/10A61K47/12A61K47/14A61K47/34A61P17/14A61Q7/00
CPCA61K31/506A61K2800/21A61K8/4953A61K9/107A61K8/062A61Q7/00A61K8/361A61P17/14A61K8/06A61K8/34A61K8/345A61K8/60A61K8/922A61K2800/412
Inventor 桥本真一辻畑茂朝
Owner FUJIFILM CORP
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