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Cinepazide maleate crystal form and preparation thereof

A technology of cinepazide maleate and crystals of cinepazide maleate, applied in the fields of cardiovascular system diseases, drug combination, organic chemistry, etc., can solve adverse reactions, research reports, no crystals of cinepazide maleate Type and other issues, to achieve the effect of good product fluidity, high solubility, and convenient industrial production

Inactive Publication Date: 2009-03-04
BEIJING SIHUAN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, cinepazide maleate prepared by the prior art is prone to produce cis-isomers, which can cause adverse reactions. The unexpected discovery of the present invention is that cinepazide maleate is prepared into a certain crystal The form can make it stable, and there is no research report about the crystal form of cinepazide maleate in the prior art

Method used

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  • Cinepazide maleate crystal form and preparation thereof
  • Cinepazide maleate crystal form and preparation thereof
  • Cinepazide maleate crystal form and preparation thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Embodiment 1 Preparation of cinepazide maleate B crystal form one

[0033] In the dark, add 2 g of cinepazide maleate, add 40 ml of anhydrous acetonitrile, heat to dissolve the raw materials, reflux for 5 minutes, cool at room temperature, filter and collect crystals after standing for 24 hours, and dry under reduced pressure at room temperature for 10 hours to obtain cinepazide maleate Special B crystal form 1.1g.

Embodiment 2

[0034] Example 2 Preparation of Cinepazide Maleate B Crystal Form II

[0035] In the dark, add 2 g of cinepazide maleate, add 30 ml of anhydrous acetone, heat to reflux, then slowly add methanol dropwise until the solid just dissolves, then reflux for 5 minutes, cool at room temperature, and collect crystals by filtration after standing for 24 hours, and depressurize at room temperature After drying for 10 hours, 0.8 g of crystal form B of cinepazide maleate was obtained.

Embodiment 3

[0036] Example 3 Preparation of cinepazide maleate B crystal form three

[0037] Referring to the operation in Example 2, the solvent methanol was replaced with ethanol to obtain 1.6 g of cinepazide maleate B crystal form.

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Abstract

The invention belongs to the pharmaceutical technical field, particularly relates to maleate cinepazide crystal form (including maleate cinepazide A crystal form and maleate cinepazide B crystal form) and preparation method thereof. The maleate cinepazide crystal form has characteristic peak at 9.0 plus or minus 0.2, 16.1 plus or minus 0.2, 19.8 plus or minus 0.2 and 21.7 plus or minus 0.2 in X-ray powder diffraction expressed by 2 THETA using Cu-Ka radiation. The maleate cinepazide crystal form has characteristic peak at 7.6 plus or minus 0.2, 19.7 plus or minus 0.2, and 22.9 plus or minus 0.2 in X-ray powder diffraction expressed by 2 THETA using Cu-Ka radiation.

Description

1. Technical field [0001] The invention belongs to the technical field of medicine, in particular to (E)-1-{4-[(3',4',5'-trimethoxycinnamoyl)]-1piperazine}acetylpyrrolidine maleate That is, the crystal form of cinepazide maleate and the preparation method thereof. 2. Background technology [0002] Cinepazide maleate is a known compound with the chemical name: (E)-1-{4-[(3',4',5'-trimethoxycinnamoyl)]-1piperazine}acetylpyrrole Pyridine maleate, the structural formula is as follows: [0003] [0004] Cinepazide maleate is a calcium ion channel blocker, by blocking Ca 2+ Transmembrane into vascular smooth muscle cells, so that vascular smooth muscle relaxation, cerebral blood vessels, coronary blood vessels and peripheral blood vessels to expand, thereby relieving vasospasm, reducing vascular resistance, increasing blood flow; enhancing the role of adenosine and cyclic adenosine monophosphate; improving red blood cell Flexibility and deformation can improve microcirculati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/18A61P9/00
Inventor 车冯升
Owner BEIJING SIHUAN PHARMA
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