Carvedilol solubility enhancement by multicomponent crystallization with coformers of benzoic acid, isonicotinamide, and saccharin

Multicomponent crystallization is a method that can modify the physicochemical properties of Carvedilol (CVD), thereby increasing its solubility. Based on in silico screening coformers (Benzoic Acid, Isonicotinamide, and Saccharin) showed non-covalent interactions with CVD, so multicomponent crystal preparation CVD by solvent evaporation used these mole ratios 1:1, 1:2, 2:1. CVD:Isonicotinamide (1:2) exhibits increased saturation solubility up to 140 mg/L dissolution 99.48%. The infra-red (IR) spectrum peak shift, thermogram pattern was different from DSC results, new XRD diffractogram indicating formation solid phase compared pure Carvedilol. Therefore, crystals increase rate all characteristics indicate presence interaction between phase.