Preparation and Characterization of Co crystals of An Antifungal Drug

Abstract

Pharmaceutical co-crystals are evolving as a promising strategy to alter physicochemical properties of Active Pharmaceutical Ingredient. Fluconazole is a broad-spectrum anti-fungal drug presenting poor flowability, mechanical properties, and limited aqueous solubility. These issues pose challenges for the handling and manufacturing of dosage forms of FLZ. The current research aimed to develop fluconazole co-crystals for improving its aqueous solubility, flowability, and mechanical properties. Benzoic acid and Parahydroxy Benzoic acid were selected as suitable coformers for developing Fluconazole co-crystals. The fluconazole-benzoic acid (FLZ-BA) and fluconazole-parahydroxybenzoic acid (PLZ-PHBA) co-crystals were prepared using the solvent evaporation technique. The prepared co-crystals were characterized for drug content, solubility, anti-fungal activity, dissolution, and stability. Differential Scanning Calorimetry, Powder X-Ray Diffraction, Scanning Electron Microscopy, and Fourier Transmission Infrared spectroscopy were carried out to confirm the co-crystal formation. The co-crystals were further evaluated for their flow characteristics and mechanical properties via compressibility, tabletability, compactibility, Heckel, and Kawakita analysis. newline