Dissolution kinetics of Glibenclamide amorphous solid dispersions in biorelevant media

Title

Poster

Description

Vladimir Petkov1, Zahari Vinarov2, Slavka Tcholakova2
1Department of chemical and pharmaceutical engineering , Sofia university "St. Kliment Ohridski"
2Department of chemical and pharmaceutical engineering , Sofia university "St. Kliment Ohridski"

Subject

In this research, we investigated the dissolution kinetics of the drug glibenclamide, in ASD with cellulose polymers: hydroxypropylcellulose (HPC) and hydroxypropylmethylcellulose-acetatesuccinate (HPMCAS), prepared by spray-drying, as well as the potential of different cellulose polymers to act as precipitation inhibitors during supersaturation. The dissolution kinetics were evaluated using in vitro GIT model, developed by Vinarov et al. The spray dried formulations showed significant increase in the dissolved drug concentrations, compared to the crystalline compound. Best results were obtained with the HPC based formulations. More modest increase in drug release was observed for the HPMCAS based systems. The formulation that did not contain any polymer, but only pure amorphous glibenclamide, possessed very slow drug release when the drug is exposed to the stomach phase, due to crystallization. When polymer is present in the solution, crystallization can be inhibited. HPC was the polymer with the best crystallization inhibitory potential and it was inversely proportional to the molecular weight of the polymer. As a conclusion, the glibenclamide amorphous solid dispersion based on HPC and HPMCAS, significantly enhanced the drug release in bio relevant media. The best results were obtained with the HPC based formulations and this polymer was also the best precipitation inhibitor.
Acknowledgments: Part of the research is done using equipment bought for Project BG05M2OP001-1.002-0012 financed by OP NEIG sufinanced by the EU via european structural and investment funds.
Keywords: Amorphous solid dispersion