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Aprepitant emulsion formulationpreparation and preparation method thereof

A technology for aprepitant and emulsion preparation, which is applied in the field of preparation of aprepitant injection emulsion, can solve the problems of poor preparation effect, poor preparation efficiency, poor stability, etc. Efficient effect

Inactive Publication Date: 2018-12-18
北京睿悦生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the embodiments of the present invention is to provide an aprepitant milk preparation and its preparation method to solve the defects of poor stability, poor preparation efficiency and poor preparation effect of the existing milk preparations

Method used

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  • Aprepitant emulsion formulationpreparation and preparation method thereof
  • Aprepitant emulsion formulationpreparation and preparation method thereof
  • Aprepitant emulsion formulationpreparation and preparation method thereof

Examples

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Embodiment 1

[0026] The preparation method of the aprepitant milk preparation of the embodiment of the present invention comprises the following steps:

[0027] Firstly, after mixing 1 g of aprepitant, 17 g of egg yolk lecithin, 4 g of ethanol, 1 g of sodium oleate and 18 g of soybean oil, they were stirred together. During the stirring process, the heating temperature of the mixture was controlled between 70°C and 80°C.

[0028] Then, dissolve 8 g of sucrose in 51 g of water for injection, keep the injection temperature between 40°C and 60° C., stir and dissolve continuously to form a water phase.

[0029]

[0030]

[0031] The oil phase formed above is added to the water phase. During the process of adding the oil phase to the water phase, the mixture needs to be stirred at a high speed of 12000r / min to 18000r / min to prepare the colostrum mixture. Then, use a high-pressure microjet 10000psi ~30000psi high-pressure homogenization of the colostrum mixture, repeated 11 times, to form ...

Embodiment 2

[0033] The preparation method of the aprepitant milk preparation of the embodiment of the present invention comprises the following steps:

[0034] First, mix 0.5g of aprepitant, 5g of egg yolk lecithin, 0.5g of ethanol, 1g of sodium oleate and 18g of soybean oil, and stir together. During the stirring process, the heating temperature of the mixture is controlled between 70°C and 80°C .

[0035] Then, dissolve 8 g of sucrose in 51 g of water for injection, keep the injection temperature between 40°C and 60° C., stir and dissolve continuously to form a water phase.

[0036] The oil phase formed above is added to the water phase. During the process of adding the oil phase to the water phase, the mixture needs to be stirred at a high speed of 15000r / min to prepare the colostrum mixture. Then, the colostrum mixture is treated with a high-pressure micro jet of 15000psi Carry out high-pressure homogenization and repeat 10 times to form aprepitant milk preparation, which is sterile ...

Embodiment 3

[0038] The preparation method of the aprepitant milk preparation of the embodiment of the present invention comprises the following steps:

[0039] Firstly, after mixing 1.5 g of aprepitant, 20 g of egg yolk lecithin, 5 g of ethanol, 2 g of sodium oleate and 20 g of soybean oil, they are stirred together. During the stirring process, the heating temperature of the mixture is controlled between 70° C. and 80° C.

[0040] Then, dissolve 10 g of sucrose in 41.5 g of water for injection, keep the injection temperature between 40°C and 60° C., and stir continuously to dissolve to form an aqueous phase.

[0041] The oil phase formed above is added to the water phase. During the process of adding the oil phase to the water phase, the mixture needs to be stirred at a high speed of 15000r / min to prepare the colostrum mixture. Then, the colostrum mixture is treated with a high-pressure micro jet of 30000psi Carry out high-pressure homogenization and repeat 9 times to form aprepitant mil...

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Abstract

The invention discloses an aprepitant emulsion formulationpreparation. The emulsion formulationpreparation is prepared from the following components in percentage by mass: 0.05-1.5% of aprepitant, 2-20% of soybean oil, 5-20% of egg yolk lecithin, 0.5-5% of ethanol, 0.05-2% of sodium oleate, 2-10% of sucrose, and 40-80% of injection water.According to the embodiment of the invention, sodium oleateis added into oil phase, sticky materials are not easily produced during mixing, the time of forming a colostrum formulationpreparation is shorter, and the preparation efficiency is high, and meanwhile, the emulsion formulation prepared during the preparation process provided by the invention is more stable and has a better treatment effect.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a preparation method of aprepitant injection emulsion. Background technique [0002] Aprepitant (Aprepitant), also known as aprepitant, aceminidazole, is an off-white to pale yellow crystal-like solid chemical. Chemical formula such as figure 1 As shown, the chemical name is 5~[2(R)~[1(R)~[3,5~di(trifluoromethyl)phenyl]ethoxy]~3(S)~(4~fluorophenyl ) morpholine ~ 4 ~ base methyl] ~ 3,4 ~ dihydro ~ 2H ~ 1,2,4 ~ triazole ~ 3 ~ ketone, the molecular formula is C 23 h 21 f 7 N 4 o 3 , Molecular weight is 534.42700, insoluble in water, slightly soluble in acetonitrile, slightly soluble in ethanol, melting point 244~246℃. Aprepitant is clinically mainly used to prevent acute and delayed nausea and vomiting during the initial and repeated treatment of highly emetogenic anticancer chemotherapy. Aprepitant emulsion formulations were the earliest capsules prepare...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/12A61K47/44A61K47/24A61K47/10A61K47/26A61K31/5377A61P1/08
CPCA61K9/0019A61K9/1075A61K31/5377A61K47/10A61K47/12A61K47/24A61K47/26A61K47/44A61P1/08
Inventor 付冀峰王文娟郭稼张连成
Owner 北京睿悦生物医药科技有限公司
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