Aprepitant microemulsion for injection and preparation method thereof

A technology of tan microemulsion and aprepitant, applied in the field of pharmaceutical preparations, can solve the problems of low bioavailability, inconvenient clinical application of oral aprepitant, poor absorption, etc., and achieve good economic and social benefits , Realize the effect of large-scale industrial production and cost reduction

Inactive Publication Date: 2012-03-21
NANJING YOKO PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Purpose of the invention: In view of the deficiencies in the prior art, the purpose of the present invention is to provide a kind of aprepitant microemulsion for injection to effectively solve the inconvenience of clinical application, poor absorption and bioavailability of aprepitant oral formulations. Not advanced question

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The aprepitant microemulsion for injection is composed of various components: 0.5g aprepitant, 30g soybean oil, 3g egg yolk phospholipid, 1.5g ethanol, 5g glycerin, and 60g water for injection.

[0023] Preparation: mix aprepitant and egg yolk phospholipid, dissolve in ethanol, heat and stir at 60°C until the ethanol is evaporated to a viscous shape, continue to heat and dissolve, stir until uniform, and control the temperature at 60°C to prepare crude milk; Add soybean oil to the crude milk, add an appropriate amount of ethanol to dissolve; continue heating and stirring at 60°C until a clear oil phase is obtained; dissolve glycerin with water for injection heated to 60°C to obtain a water phase; mix the clear oil phase and water phase at high speed Stir, mash, and add an appropriate amount of water for injection at the same time, adjust the pH to 7.2 to obtain colostrum; add the colostrum into a high-pressure homogenizer using the homogenization method, control the pres...

Embodiment 2

[0025] Aprepitant microemulsion for injection is composed of various components: 2g aprepitant, 5g ethyl oleate, 10g poloxamer, 3g glycerol, 20g sucrose, 60g water for injection.

[0026] Mix aprepitant and poloxamer, dissolve with an appropriate amount of ethanol, heat and stir at 60°C until the ethanol is evaporated to a viscous shape, continue to heat and dissolve, stir until uniform, and control the temperature at 60°C to obtain coarse milk; Add ethyl oleate to the crude milk, add an appropriate amount of ethanol to dissolve; continue heating and stirring at 60°C until a clear oil phase is obtained; dissolve sucrose with water for injection heated to 60°C to obtain a water phase, and mix the clear oil phase and water phase, Stir at high speed, mash, and add an appropriate amount of water for injection at the same time, adjust the pH to 6.8 to obtain colostrum; add colostrum into a high-pressure homogenizer using the homogenization method, control the pressure at about 1000M...

Embodiment 3

[0028] Aprepitant microemulsion for injection is composed of various components: 0.05g of aprepitant, 6g of peanut oil, 6g of polysorbate 80, 2g of polyethylene glycol 400, 5.95g of glucose, and 80g of water for injection.

[0029] The preparation method is the same as in Example 2, wherein the pH of the colostrum is 8.0.

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Abstract

The invention discloses an aprepitant microemulsion for injection. The aprepitant microemulsion consists of the following components in percentage by mass: 0.05 to 2 percent of aprepitant, 5 to 30 percent of oil for injection, 0.5 to 10 percent of emulsifier, 1 to 10 percent of co-emulsifier, 5 to 20 percent of protective agent and 60 to 80 percent of water for injection. Compared with the conventional oral aprepitant, the aprepitant microemulsion for the injection has the outstanding advantage that: the aprepitant is insoluble in the water and an organic solvent, in order to realize the aprepitant injection, the aprepitant microemulsion and aprepitant micro emulsion freeze-drying powder are prepared successfully and can be subjected to large-scale industrial production; and compared with a fosaprepitant dimethyl-meglumine injection, the aprepitant microemulsion has the advantages that: the cost is reduced greatly, the practicality is extremely high, and economic and social benefits are relatively good.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to an aprepitant microemulsion for injection and a preparation method thereof. Background technique [0002] Aprepitant (aprepitanl) is an NK-1 receptor antagonist currently on the market for antiemetic. The NK-1 receptor is the binding site for tachykinin (NKA) substance P (SP), located in the brainstem vomiting center and the gastrointestinal tract. Animal experiments have shown that SP can induce vomiting. Drugs that specifically block this receptor prevent vomiting from all emetogenic stimuli, including cisplatin. Aprepitant is an NK-1 receptor blocker, which blocks the action of substance P by binding to NK-1 receptors (mainly present in the central nervous system and its periphery). Aprepitant can pass through the blood-brain barrier and occupy the NK-1 receptors in the brain with selectivity and high affinity, but has low affinity for NK-2 and NK-3 rece...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/5377A61K47/24A61K47/34A61K47/44A61P1/08
Inventor 周卫张峰高建兴陆军曹燕锋姜东成陆修涛刘宇
Owner NANJING YOKO PHARMA GRP CO LTD
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