Designing and evaluation of ebastine–benzamide cocrystals

Abstract

Background: Ebastine (EB) is a selective nonsedating H1 antihistamine belonging to Class II(BCS);  it has inadequate oral bioavailability due to its poor water solubility. Cocrystal is one of the most recent methods that has been utilized to improve some physicochemical characteristics of a drug, such as solubility and dissolution rate. This research's main objective was to design and evaluate EB cocrystal as a trial to enhance its solubility. Methods: Various techniques were employed to formulate cocrystals, such as solvent evaporation, slurry, and drop asset grinding using benzamide (BENZ) as a co-former in different molar ratios. The prepared formulas were characterized by percentage yield, drug content,  saturation solubility, in vitro dissolution studies, infrared spectroscopy (FTIR), Raman spectroscopy, powder X-ray diffraction (PXRD),  and differential scanning calorimetry (DSC), Results: Solubility enhanced by 347 fold in distilled water with enhanced dissolution profile. Conclusions: Co-crystallization is a potential solid formation method due to its ability to enhance physicochemical and mechanical characteristics. Co-crystals have been successfully formed from a variety of medicines and co-former, using distinct hydrogen bond synthon motifs.