Abstract

PHARMACEUTICAL COCRYSTALS: A NOVEL APPROACH FOR SOLUBILITY MODIFICATION

Princy Baby*, A. R. Shabaraya and Bhavyashree T.

Abstract

During the development of new pharmaceutical product, poor aqueous solubility and less oral bioavailability of active drug molecule are the most significant limiting factor. Distinct advances have emerged to solve the solubility related issues of active drug, but the successful outcome of these approaches rely on the physical and chemical nature of molecules being developed. Cocrystallization is the process which involves a change in molecular assemblies and composition of pharmaceutical substance resulting in optimization of drug’s physical characteristics. Cocrystals are molecular complex, constituting Active Pharmaceutical Ingredient (API) and a coformer in a stoichiometric ratio and are combined together with a non-covalent bond in the crystal lattice resulting in the development of pharmaceutical compounds with superior properties to those of free drug. Cocrystals can be obtained by various methods such as grinding, solvent evaporation, slurry conversion, hot melt extrusion, supercritical fluid cocrystallization, spray drying, sonocrystallization, antisolvent addition to produce high purity cocrystals. This review outlines the methodology involved in preparation of cocrystal, altering physiochemical properties, and instrumental analytical techniques for screening this developed cocrystals along with remarkable applications in the pharmaceutical industry with the ultimate aim to generate pharmaceutical compounds superior than the free drug and focussing on current trends and emerging technologies in these areas.

Keywords: Cocrystallization, Cocrystals, API, Solubility, Bioavailability, Coformer.