A simple and effective method to improve bioavailability of glimepiride by utilizing hydrotropy technique.

Abstract The purpose of this study was to improve the solubility and bioavailability of glimepiride (GLMP) by utilizing hydrotropy technique. Meglumine (MU) as a hydrotrope could form the stable complex with glimepiride. The optimal glimepiride and meglumine (GLMP–MU) complex powder was obtained by using lyophilization. GLMP–MU powder was characterized by Fourier transform infrared spectroscopy (FT IR), X-ray powder diffraction (XRD) and differential scanning calorimetry (DSC). The formation of hydrogen bond between glimepiride and meglumine was confirmed by FT IR. The XRD studies indicated the amorphous state of glimepiride was appeared in the GLMP–MU. The DSC results were further confirmed GLMP–MU complex was prepared successfully. Moreover, the in vitro drug release rate of GLMP–MU powder was dramatically faster than that of glimepiride. Meanwhile, the AUC of GLMP–MU solution at an i.g. /or i.v. dose of 5 mg/kg in rat was significantly higher than that of the glimepiride suspensions. Together our results showed that hydrotropy technique was a simple and effective method to increase the solubility of glimepiride.