Preparation and Evaluation of Pharmaceutical Cocrystals for Solubility Enhancement of Ketoconazole

Abstract

Drug - drug co-crystallization is proposed as a new method to improve the solubility and hence the bioavailability of drugs. Cocrystal consists of two or more neutral molecular components in a crystal lattice with well- defined stoichiometric ratio. Formation of cocrystal mainly depends on functional group of APIs and co-formers to allow for the formation of hydrogen bonds or other weak type of interactions, mainly hydrogen bonding. The basis for co-formers selection is its ability to form non - covalent interactions especially hydrogen bonds with an APIs. The drug-drug cocrystals batches of ketoconazole and hydroquinone coformer were successfully prepared by various methods Co grinding, Solvent evaporation and Liquid assisted grinding. The physicochemical properties were characterized by various characterizations. Improved permeability of the drug is attributed to drug conformer interaction. This study showed the utility of the co-crystallization approach to improve bioavailability of drug after formulating tablet dosage form and various characterization and in vitro dissolution study was performed.