CHARACTERIZATION AND DISSOLUTION RATE STUDIES OF INCLUSION COMPLEX OF GLIBENCLAMIDE AND HYDROXYPROPYL-Β-CYCLODEXTRIN USING CO-GRINDING METHOD

Abstract

Objective: Glibenclamide belongs to the 2nd generation sulfonylurea group as an oral antidiabetic with low solubility in water and high bioavailability in systemic circulation (Biopharmaceutical Classification System class II). This study aimed to increase the solubility and dissolution rate of glibenclamide by preparing an inclusion complex of Glibenclamide and Hydroxypropyl-β-cyclodextrin. Methods: Inclusion complexes were prepared by the co-grinding method in two ratios 1:1 and 1:2 mol. Characterizations of inclusion complex were carried out by Scanning Electron Microscopy (SEM), Fourier Transform Infrared (FT-IR) spectroscopy, Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) analysis. Solubility test was carried out in CO2-free distilled water and dissolution rate was carried out in phosphate buffer pH 7.4. Results: The results of the SEM analysis showed changes in particle morphology. FT-IR spectroscopy shows a shift in wavenumber. DSC analysis showed a decrease in the melting point of the inclusion complex. XRD characterization results showed a decrease in the intensity of the inclusion complex. Solubility of inclusion complex of glibenclamide increased nine times 1:1 mol inclusion complex, twelve times 1:2 mol inclusion complex compared to intact glibenclamide. The dissolution of glibenclamide, inclusion complex 1:1, and inclusion complex 1:2 in phosphate buffer pH 7.4 medium at 60 min was 17.19%, 34.15% and 52.83% respectively. Conclusion: Based on the results of the study, it can be said that the glibenclamide inclusion complex with Hydroxypropyl-β-cyclodextrin successfully increases the solubility and dissolution rate of glibenclamide significantly.