DESIGN DEVELOPMENT AND FABRICATION OF PHARMACEUTICAL CO-CRYSTAL: ENHANCE AQUEOUS SOLUBILITY AND IN-VITRO DISSOLUTION RATE OF BCS CLASS 2 OR 4 ACTIVE PHARMACEUTICAL INGREDIENT

Priyanka S. Gala*, Mohammad Wais and Indira Parab

ABSTRACT

In last couple of years many API discoveries found to be poorly soluble in aqueous medium. These poorly soluble APIs have low bioavailability & low absorption. So, to deal with this challenge co-crystal technique found to be boon to pharmaceutical industry. Co-crystals optimize the In-vitro powder dissolution rate of Biopharmaceutical classification system (BCS) class 2 or 4 drugs. Crystalline structure of co-crystals comprises of API and one or more Co-former must be either amino acid or carboxylic acid such as (oxalic acid, succinic acid, serine, proline, glycine, etc.) In stoichiometric ratio hydrogen bonded interactions done between drug and Co-former which improves the aqueous solubility of co-crystal. Co-crystals are prepared by following methods such as Liquid assisted grinding, Hot melt extrusion method, Solvent evaporation method, Anti solvent method, Spray drying method, etc. And further characterized by High performance liquid chromatography, Fourier transform infrared spectroscopy, Differential scanning calorimetry, Powder x-ray diffraction and In-vitro dissolution studies of the formulation.

Keywords: Co-crystal, Co-former, Solubility Enhancement, Co-crystal screening, Synthon approach, Theoretical screening.