Method for preparing novel crystal form of bilastine

Abstract

The invention relates to a method for preparing a novel crystal form of bilastine. The method comprises the following steps: dissolving bilastine in a mixed solvent of an organic solvent and water, heating until all bilastine is dissolved, and cooling and crystallizing to obtain the novel crystal form of bilastine.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry and relates to 2-[4-(2-{4-[1-(2-ethoxy-ethyl)-1H-benzimidazol-2-yl]-piperidin-1-yl }Ethyl)-phenyl]-2-methyl-propionic acid (bilastine) new crystal preparation. Background technique [0002] Bilastine, the 2nd generation histamine H developed for Spanish FAES pharmaceutical company 1 Receptor antagonist, approved by the European Union for the treatment of allergic rhinitis and chronic idiopathic urticaria in 2010, and launched in Ireland in 2011. This product is safe, without the sedative effect and cardiotoxicity of commonly used antihistamines. [0003] [0004] In the Chinese patent CN1628112A, the crystal form of bilastine was first proposed. Crystal forms I, II, III, crystal form II and crystal form III are unstable and can be converted into crystal form I. The patent only gives the unit cell data and infrared data. In the patent CN201310107513.8, a new crystal form of bilastine is men...

AI Technical Summary

Problems solved by technology

[0004] In the Chinese patent CN1628112A, the crystal form of bilastine was first proposed. Crystal forms I, II, III, crystal form II and crystal form III are unstable and can be converted into crystal form I. The patent only gives the unit cell data and infrared data

Images