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Preparation method of fosaprepitant freeze-dried powder injection

A technology of fosaprepitant and freeze-drying protective agent, which is applied in the field of medicine and can solve problems such as the development of fosaprepitant slow-control reagent

Inactive Publication Date: 2019-04-02
SICHUAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current technology has not developed fosaprepitant slow-control reagents

Method used

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  • Preparation method of fosaprepitant freeze-dried powder injection
  • Preparation method of fosaprepitant freeze-dried powder injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A preparation method of fosaprepitant freeze-dried powder injection, is characterized in that, the step comprises:

[0039] (1) Preparation of oil phase: First, 1 part of fosaprepitant and 3 parts of PLGA are added to 30 parts of acetone for dissolution, and the acetone is removed by rotary evaporation, then 10 parts of soybean oil for injection and 0.2 part of soybean phosphatidylcholine are added and stirred Mix to obtain material 1;

[0040] (2) Water phase preparation: add 1 part of isotonic regulator glycerin and 5 parts of xylitol to 500 parts of water for injection and mix evenly to obtain material 2;

[0041] (3) Mix the material 1 obtained in step (1) and the material 2 obtained in step (2) at 45° C., and mechanically stir at 2000 rpm for 30 minutes to obtain colostrum;

[0042] (4) Distill the colostrum obtained in step (3) with water for injection, adjust the pH to 6 with a pH regulator hydrochloric acid or sodium hydroxide, and circulate and homogeneously e...

Embodiment 2

[0046] A preparation method of fosaprepitant freeze-dried powder injection, is characterized in that, the step comprises:

[0047] (1) Preparation of the oil phase: First, 2 parts of fosaprepitant and 5 parts of PLGA were added to 50 parts of acetone for dissolution, and the acetone was removed by rotary evaporation, and then 20 parts of soybean oil for injection and 1 part of emulsifier egg yolk phosphatidylcholine were added. Alkali is stirred and mixed to obtain material 1;

[0048] (2) Water phase preparation: add 2 parts of glycerin, an isotonic regulator, and 8 parts of xylitol, a freeze-drying protective agent, into 800 parts of water for injection and mix evenly to obtain material 2;

[0049] (3) Mix the material 1 obtained in step (1) and the material 2 obtained in step (2) at 60° C., and mechanically stir at 2500 rpm for 40 minutes to obtain colostrum;

[0050] (4) The colostrum obtained in step (3) is fixed to volume with water for injection, the pH is adjusted to ...

Embodiment 3

[0054] A preparation method of fosaprepitant freeze-dried powder injection, is characterized in that, the step comprises:

[0055] (1) Preparation of the oil phase: First, 3 parts of fosaprepitant and 10 parts of PLGA were added to 60 parts of acetone for dissolution, and the acetone was removed by rotary evaporation, then 30 parts of soybean oil for injection and 2 parts of emulsifier egg yolk phosphatidylcholine were added. Alkali is stirred and mixed to obtain material 1;

[0056] (2) Water phase preparation: add 2 parts of isotonicity regulator sodium chloride and 10 parts of freeze-drying protective agent trehalose into 1000 parts of water for injection and mix evenly to obtain material 2;

[0057] (3) Mix the material 1 obtained in step (1) and the material 2 obtained in step (2) at 85° C., and mechanically stir at 3000 rpm for 30-40 minutes to obtain colostrum;

[0058] (4) Distill the colostrum obtained in step (3) with water for injection, adjust the pH to 9 with a p...

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Abstract

The invention discloses a preparation method of a fosaprepitant freeze-dried powder injection. Firstly, fosaprepitant is loaded by PLGA, and then an S / O / W emulsified microsphere preparation is formedafter emulsification and freeze-drying. Emulsification can increase the solubility property and stability of microspheres, and also can improve the syringeability of the microspheres. After 6 weeks ofinjection with the preparation, the preparation with effective blood drug concentration can still be detected in rats, and the preparation prolongs the action time of the drug, reduces the frequencyof drug administration, improves the medication compliance of patients, and is of great significance.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of fosaprepitant freeze-dried powder injection. Background technique [0002] Fosaprepitant (Fosaprepitant) was approved by the US FDA in January 2008, and it is also on the market in Sweden, the Czech Republic, Portugal and the United Kingdom. Fosaprepitant dimeglumine is a human substance P / neurokinin 1 (NK-1) selective high-affinity receptor blocker, which mainly works by blocking the brain's nausea and vomiting signals and a novel mechanism of action . [0003] The chemical name of fosaprepitant is: N-methyl-D-glucosamine [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl) )phenyl]ethoxy]-3-(4-fluorophenyl-4-morpholinyl]methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazole -1-base] phosphoric acid (2:1) salt, the molecular formula is: C 23 h 22 f 7 N 4 o 6 P*2C 7 h 17 NO 5 , the molecular weight is: 1004.83, and the chemical structural formula is as follow...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K47/34A61K31/675A61P1/08
CPCA61K9/0019A61K9/19A61K31/675A61K47/34A61P1/08
Inventor 王静曾涛刘焘
Owner SICHUAN PHARMA
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