European Journal of Biomedical and Pharmaceutical Sciences

SYNTHESIS AND CHARACTARIZATION OF NEBIVOLOL- NICOTINAMIDE COCRYSTALS

*Ms. Pranita V. Tarde, Dr. Pravinkumar N. Sable, Mr. Sarang D. Kulkarni, Mrs. Sharda S. Kulkarni, Ms. Rutuja S. Kulkarni

ABSTRACT

Nebivolol nicotinamide cocrystals are essentially the result of a fundamental study designed to improve nebivolol's low oral bioavailability and low water solubility (0.091 g/100 ml). Nebivolol hydrochloride is a BCS Class II antihypertensive medication whose high permeability and low water solubility may restrict its oral bioavailability and rate of dissolution. In order to enhance the physicochemical properties of nebivolol hydrochloride, nicotinamide is used as a co-former in the creation and characterisation of pharmaceutical cocrystals. Using various drug-to-co-former molar ratios, cocrystals were made by solvent evaporation and liquid-assisted grinding methods. Fourier Transform Infrared Spectroscopy (FTIR), Powder X-ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), and High-Performance Liquid Chromatography (HPLC) were used to characterise the produced cocrystals. Nebivolol hydrochloride and nicotinamide formed intermolecular hydrogen bonds, according to FTIR analysis, and cocrystal formation was confirmed by PXRD patterns that showed the emergence of new diffraction peaks and the elimination of parent compound distinctive peaks. DSC thermograms revealed clear melting endotherms that differed from those of the co-former and pure drug, suggesting the formation of a new crystalline phase. Studies on solubility and dissolution showed that the cocrystals' water solubility and rate of dissolution were significantly higher than those of pure nebivolol hydrochloride. These results imply that co-crystallization with nicotinamide is a successful crystal engineering strategy for enhancing nebivolol hydrochloride's medicinal performance, which may lead to increased oral bioavailability and therapeutic efficacy.[1]

Keywords: Pharmaceutical Cocrystals, Crystal Engineering, Solubility Enhancement, Solvent Evaporation Method, Liquid-Assisted Grinding, Drug–Co-former Interaction, Hydrogen Bonding, Physicochemical Characterization, Bioavailability Enhancement