Novel polymorph of safinamide and preparation method therefor

A technology of safinamide mesylate and crystal form, applied in the field of medicinal chemistry, can solve the problems of low dissolution rate, poor stability and the like, and achieve the effects of high dissolution rate, high stability and favorable industrial production.

Active Publication Date: 2015-11-04
NANJING CHIA TAI TIANQING PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the safinamide mesylate crude drug solid has the disadvantages of poor stability and low dissolution rate. For the above problems, the inventor has explored

Method used

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  • Novel polymorph of safinamide and preparation method therefor
  • Novel polymorph of safinamide and preparation method therefor
  • Novel polymorph of safinamide and preparation method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The preparation of embodiment 1 safinamide methanesulfonate crystal form B

[0037] At a temperature of 45-50°C, stir and dissolve 10 g of safinamide mesylate in a mixed solvent of ethanol and water, wherein the volume of ethanol is 6 times the weight of safinamide mesylate, that is, 60 mL; The volume is 1 times the weight of safinamide methanesulfonate, that is, 10mL. After dissolving, filter while it is hot, cool the filtrate to 20-25°C, slowly stir and crystallize, filter the precipitated crystals, and dry under vacuum at 35-40°C to obtain 9.6 g, yield 96%.

Embodiment 2

[0038] The preparation of embodiment 2 safinamide methanesulfonate crystal form B

[0039]At a temperature of 45-50°C, stir and dissolve 10 g of safinamide mesylate in a mixed solvent of methanol and water, wherein the volume of methanol is 5 times the weight of safinamide mesylate, that is, 50 mL; The volume is 0.8 times the weight of safinamide methanesulfonate, that is, 8mL. After dissolving, filter while it is hot, cool the filtrate to 20-25°C, slowly stir and crystallize, filter the precipitated crystals, and vacuum-dry at 35-40°C to obtain 9.4 g, yield 94%.

Embodiment 3

[0040] The preparation of embodiment 3 safinamide methanesulfonate crystal form B

[0041] At a temperature of 45-50°C, 10 g of safinamide mesylate was stirred and dissolved in a mixed solvent of isopropanol and water, wherein the volume of isopropanol was 7 times the weight of safinamide mesylate, i.e. 70mL; the volume of water is 1.2 times the weight of safinamide methanesulfonate, that is, 12mL. After dissolving, filter while hot, cool the filtrate to 20-25°C, stir slowly to crystallize, filter the precipitated crystals, and vacuum dry at 35-40°C. That is, 9.5 g was obtained, and the yield was 95%.

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Abstract

The present invention relates to the field of medicinal chemistry, and particularly relates to a novel polymorph of safinamide mesylate salt, that is a novel polymorph B, and a preparation method therefor, and also relates to a pharmaceutical composition containing the novel polymorph and applications thereof in treating Parkinson's disease. When the polymorph B of safinamide mesylate salt is under radiation of Cu-K alpha, diffraction of X-ray powder represented by 2 theta has diffraction peaks at 7.82, 8.51, 13.01, 17.82, 18.71, 20.37, 21.98, and 22.90.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry, in particular to a new crystal form of safinamide methanesulfonate, i.e. crystal form B and a preparation method thereof, and also to a pharmaceutical composition containing the new crystal form and its use in the treatment of Parkinson's disease Applications. Background technique [0002] Parkinson's disease (PD) is a common degenerative disease of the central nervous system. The main pathological change is the selective degeneration of dopaminergic (DA) neurons in the substantia nigra of the midbrain. also plays an important role. Epidemiological surveys show that there are about 1.7 million PD patients in China, and the incidence of PD among people over 65 years old is 1.7% for men and 1.6% for women. [0003] At present, the first-line drugs for PD treatment include levodopa + carbidopa, DA receptor agonists, MAO-B inhibitors (such as selegiline, etc.), and the second-line drugs i...

Claims

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Application Information

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IPC IPC(8): C07C237/06C07C231/24C07C309/04C07C303/44A61K31/255A61K31/165A61K9/20A61P25/16
Inventor 郭璇柴雨柱徐丹朱春霞田舟山王雪萌葛元丽
Owner NANJING CHIA TAI TIANQING PHARMA
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