Preparation and in vitro characterization of porous carrier-based floating microspheres of model drug for gastric delivery

摘要

Floating microspheres have been utilized to obtain prolonged and uniform release of drug in the stomach for development of once-daily formulations. A controlled-release system designed to increase residence time in the stomach without contact with the mucosa was achieved through the preparation of floating microspheres by the emulsion solvent diffusion technique, using (?) calcium silicate (CS) as porous carrier; (ii) Atenolol, an oral antihypertensive agent; and (iii) Eudragit® S as polymer. The effects of various formulations and process variables on the internal and external particle morphology, micromeritic properties, in vitro floating behavior, drug loading, and in vitro drug release were studied. The microspheres were found to be regular in shape and highly porous. The prepared microspheres exhibited prolonged drug release and remained buoyant for 10 h. The mean particle size increased and the drug release rate decreased at higher polymer concentrations. No significant effect of the stirring rate during preparation on drug release was observed. In vitro studies demonstrated diffusion-controlled drug release from the microspheres. Microsphere formulation F4, containing 1:4 drug: calcium silicate, showed the best floating ability (85% buoyancy) in simulated gastric fluid. The release pattern of Atenolol in 0.1 N Hcl from all floating microspheres followed the Higuchi matrix model and.