ABSTRACT:
Glibenclamide is a hydrophobic compound belonging to class II of the biopharmaceutics Classification System (BCS). The aim of this study is to investigate cocrystallization of glibenclamide using ascorbic acid as a coformer to enhance the solubility and dissolution rate of glibenclamide. Interaction between Glibenclamide (GCM) and coformer was investigated by virtual screening. Ascorbic acid (AA), the selected coformer, was cocrystallized with GCM at equimolar ratios of 1:1 and 1:2 using the solvent evaporation method. The cocrystal of GCM-AA was evaluated by saturated solubility test and dissolution rate test (USP type 2 apparatus). Then characterization was performed using fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD). The result show that cocrystal 1:2 was more highly 26-fold more soluble compared to pure GCM. The dissolution rate of GCM also increased from 46.83% to 63.24 % in 60 minutes. Based on the IR spectrum, a chemical reaction did not occur during the cocrystallization. Characterization of the GCM-AA cocrystal (1:2) including FT-IR, DSC, and PXRD showed the formation of a new solid crystal phase that is different from GCM and AA.