Solvent Drop Grinding Approach Assisted Development of Glimepiride Co-crystals: Solubility Enhancement Journey of BCS Class-II Product

Background: Glimepiride has limited aqueous solubility and majorly suffers from bioavailability issues that eventually reduce the pharmacotherapeutic potentials of the moiety. Materials and Methods: For the possible augmentation of all the crucial factors, co-crystals were developed using a Generally Recognized As Safe (GRAS) co-former (caffeine) in the presence of few drops of solvent (acetone) by employing a very simple green approach (solvent drop grinding method). The pharmacokinetic study of the cocrystals was performed in Wistar albino rats, the data was compared with free drug form and pharmacokinetic parameters were determined. The fabricated co-crystal product was comprehensively characterized through sophisticated analytical techniques that ascertained the complete product formation. Results: The formation of the glimepiride crystal with the co-former was confirmed through FTIR, DSC, XRD and SEM. From the pharmacokinetic study in rats, the procured data expressed several-folds higher plasma drug concentration which can be correlated with increased bioavailability of glimepiride. Conclusion: This study will positively inspire researchers working in the field of solubility/ bioavailability enhancement due to the simplicity of the method, green approach and positive results which will open several future avenues of drug applications.