Preparation and evaluation of glibenclamide binary solid dispersions prepared by fusion and solvent-fusion method

Abstract

Solid dispersions (SDs) of the poorly water soluble antidiabetic drug, glibenclamide(GLB), were prepared using polyethylene glycol 4000(PEG) through the fusion and solvent-fusion method. Solid-state analysis and the in vitro drug release profiles of the prepared formulations were assessed. Compressibility and flowability of the prepared solid dispersions were also evaluated. The dissolution rate of the prepared SDs was greatly superior to GLB. The release profile was more dependent on drug to hydrophilic polymer ratio than the preparation technique. The FTIR studies showed no interaction between drug and polymer. DSC thermograms of the prepared SDs showed no endothermic peak of GLB, which could be attributed to the gradual dissolving of the GLB in the melted PEG and/or drug amorphization. Moreover, prepared SDs were showed superior compressibility and flowability. According to the obtained results, GLB/PEG SDs both prepared successfully by fusion and solvent-fusion technique and showed improved flowability and dissolution. This will likely lead to an increase in drug bioavailability and glucose control performance in diabetic patients. There was no significant difference between the obtained result from fusion and solvent-fusion method. However, due to the lack of organic solvent as well as simple and economical manufacturing process fusion method is more reasonable.