Salt Selection and Simultaneous Polymorphism Assessment via High-Throughput Crystallization: The Case of Sertraline

摘要: High-throughput (HT) crystallization experiments were conducted with sertraline free base in the presence of mono-, di- and triacidic salt formers. Over 3600 trials conducted, leading to identification characterization 18 crystalline forms. Due large number conditions for a given type, it was possible gauge propensity form exhibit polymorphism. Four forms found exist (in this limited screen) as monomorphic materials. Unlike HCl marketed drug product, HBr appears resistant polymorphism, crystallizing single from over 140 discrete trials. This observation underscores lack predictability polymorphic behavior pharmaceuticals even when seemingly minor changes composition are made. The highlight importance coupling selection studies simultaneous polymorph screening gain more comprehensive understanding solid form...