Solvent drop grinding approach assisted development of glimepiride co-crystals: Solubility enhancement journey of bcs class-ii product

Abstract

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 co-crystals 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.