Novel preparation method for aprepitant capsule

A technology of aprepitant and capsules, applied in the field of drug preparation, can solve the problems of long reaction route, unfavorable industrial production, high cost, etc., achieve low cost of process raw materials and equipment, facilitate large-scale production, and improve product quality Effect

Inactive Publication Date: 2017-08-04
SICHUAN PHARMA
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  • Abstract
  • Description
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  • Application Information

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Problems solved by technology

The final oily product obtained by this route is extremely difficult to purify, the reaction route is long, and the yield is low, which is very unfavorable for environmental protection
[0006] JOrg Chem, 2002,67 (19): 6743-6747 reports a kind of method utilizing chiral induction method to synthesize aprepitant, but this method needs to use the chiral alcohol that is difficult to obtain as raw material, chiral alcohol ee value It is required to be more than 99%, which causes high cost and is unfavorable for industrialized production.
Since there are three chiral centers in the aprepitant molecule, namely 1R, 2R, and 3S, it brings considerable difficulty to the synthesis of high optically pure raw materials

Method used

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  • Novel preparation method for aprepitant capsule

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Embodiment

[0024] The novel preparation method of aprepitant capsules of the present invention includes the following process steps:

[0025] (1) Preparation of hydroxypropyl cellulose solution: Weigh warm water and pour it into a stainless steel bucket, add hydroxypropyl cellulose in multiple times, and stir until it is completely dissolved while adding;

[0026] (2) Weigh the main drug aprepitant and slowly add it to the prepared hydroxypropyl cellulose solution, and stir evenly;

[0027] (3) Pour the sodium lauryl sulfate solution into the hydroxypropyl cellulose solution containing the main drug, stir evenly, add the above mixture to the media grinder, wash the container with purified water, and combine the lotion Grind in the feed liquid, and discharge when the particle size is qualified;

[0028] (4) Pour the colloidal dispersion into the coating solution preparation container containing the sucrose aqueous solution, turn on the stirring paddle, mix for 10 minutes, stop sampling at 5, 8 an...

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Abstract

The invention discloses a novel preparation method for an aprepitant capsule. The novel preparation method comprises the following steps: preparation of a hydroxy propyl cellulose solution, addition of the main drug aprepitant, grinding of a medium, preparation of a coating dispersion, bottom spraying of a coating, overall mixing and filling of a capsule. With the preparation method, the capsule is filled with aprepitant; the prepared aprepitant capsule has good stability, high purity and improved quality; and the preparation method is low in cost for raw materials and equipment and beneficial for large-scale production.

Description

Technical field [0001] The invention relates to the field of medicine preparation, in particular to a novel preparation method of aprepitant capsules. Background technique [0002] Aprepitant (trade name: Emend), chemical name: 5-[[2-(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxy ]-3(S)-(4-Fluorophenyl)-4-morpholino]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one, the structural formula is as follows: [0003] [0004] Aprepitant is the first NK1 receptor antagonist approved by the U.S. FDA. Its new mechanism of action makes it different from previous serotonin receptor blockers. It has better antiemetic efficacy and can be used for chemotherapy patients. Come to the gospel. [0005] The synthesis method of aprepitant was first seen in the patent application with publication number WO9516679A1. The method uses the rare unnatural amino acid L-p-fluorobenglycine as the raw material and is cyclized with the highly toxic 1,2-dibromoethane at high temperature. After the end, the excess di...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/5377A61K47/38A61K47/20A61P1/08
CPCA61K9/5063A61K9/5015A61K31/5377A61K47/20A61K47/38
Inventor 朱玮杨敏侯述成
Owner SICHUAN PHARMA
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