Optimizing Solubility Through Co-crystal Technology: A Rigorous Investigation into Tablets Loaded with Azelnidipine Co-crystals

In the pursuit of enhancing the therapeutic efficacy of azelnidipine, a widely prescribed antihypertensive agent with limited aqueous solubility, this research delves into the innovative realm of co-crystal technology. The formulation phase incorporates co-crystal strategies designed to optimize the azelnidipine solubility profile. Three co-formers were employed for co-crystal formulation by wet grinding and solvent evaporation methods. Best co-crystals were found with co-former saccharin by solvent evaporation methods with the help of different analytical characterization. Azelnidipine-loaded co-crystals using saccharin as a co-former were compressed in tablet dosage form using the wet granulation method. The evaluation process encompasses a spectrum of pharmaceutical attributes, including dissolution behavior and stability, ensuring a holistic understanding of the developed dosage form. In vitro bioequivalent studies form a pivotal component of this investigation, elucidating the comparative pharmacokinetics and bioavailability of the optimized azelnidipine co-crystal tablet formulation against the conventional dosage form. The findings of this research promise to contribute significantly to the field of drug delivery, offering a comprehensive exploration of co-crystal technology’s role in optimizing solubility and bioavailability.