Multicomponent crystal compromising dasatinib and selected co-crystals formers: a patent evaluation of EP2861589B1

Abstract

Cocrystallization has gained significant prominence in pharmaceutical product development because of the enhancement of physical, chemical and pharmacological properties of active pharmaceutical ingredients, such as stability, solubility, dissolution rate, taste, hygroscopicity, mechanical property, bioavailability, permeability and therapeutic activity. Traditionally, co-crystals can be prepared by a grinding, solvent evaporation and slurry method. However, sophisticated methods such as spa drying, hot-melt extrusion, supercritical fluid and laser irradiation are also reported to be used for producing co-crystals. The selected patent describes the development of multicomponent crystals of dasatinib, with an aim to enhance the aqueous solubility of a selected drug. However issues surrounding the toxicity, stability, large scale manufacture, in vivo performance in human beings and regulations require adequate addressal prior to exploring the commercial viability of pharmaceutical co-crystals.