Salts of Crizotinib with Dicarboxylic Acids: Structural Characteristic, Stability Analysis, and Solubility Performance

• DOI: 10.1021/acs.cgd.4c00020
• Publication Date: 2024-04-04T02:40:41Z
• Authors: Xingjun Ou; Chunling Liu; Lixing Song; Fanhong Wu

Crizotinib is a well-known anticancer medicine used for the targeted treatment of nonsmall cell lung cancer. The water solubility crizotinib quite low and restricts its oral bioavailability. In this work, saturated alkyl dicarboxylic acids were selected as salt formers, two salts with malonic acid adipic prepared comprehensively characterized by different analytical techniques. Both exhibited comparable physical chemical stability in contrast to crizotinib. most important point was that demonstrated remarkable improved water, pH 1.2 HCl buffer, 6.8 phosphoric buffer. addition, according computation on ADMETlab Web server, Caco-2 permeability remained same level after formation. Therefore, both are expected promote further investigations toward improvement formulation.