Perpustakaan Digital ITB

The aim of this study was to improve the aqueous solubility of the oral hypoglycemic agent, glibenclamide, in order to improve its absorption, and hence its bioavailability after oral administration. Several approaches have been done to improve the solubility of glibenclamide. One of them is by the formation of an inclusion complex. In this study, we did the complexation of glibenclamide with cyclodextrin by comparing two different types of cyclodextrin, i.e. ?-cyclodextrin (?CD) and 2-hydroxyropyl-?- cyclodextrin (HP?CD). The complex was prepared by two different methods, i.e. freeze drying (FD) and coevaporation (CO). The phase solubility studies were performed for 2 days in phosphate buffer pH 7.4. The obtained solution was filtered and the glibenclamide concentration was measured by using High- Performance Liquid Chromatography (HPLC) with UV-Vis detector at the wavelength of 300 nm. Furthermore, the FD and CO products were prepared by dissolving ?CD and HP?CD in ammonia-water solution. The reaction was carried out for 1 day, and the solvents were eliminated by either freeze drying for FD product or using rotary evaporator for CO product. The dissolution study was conducted to evaluate the influence of complexation on the dissolution rate of glibenclamide. Furthermore, Differential Scanning Calorimetry (DSC), X-ray Powder Diffraction (X-RD), and Fourier-Transform Infrared Spectroscopy (FTIR) studies were performed to characterize the powder properties. The highest stability constant was obtained from the complex prepared using HP?CD, and the highest percentage of dissolved glibenclamide was obtained from FD product of complexation with HP?CD. In addition, the DSC, XRD, and FTIR results confirmed the chemical interaction between glibenclamide and cyclodextrin.