ABSTRACT:
The purpose of the present investigation was to design the multiparticulate floating system to prolong the gastric residence time after oral administration, at a particular site and controlling the release of drug especially useful for achieving controlled plasma level as well as improving bioavailability. Clarithromycin (CTM) is an advanced generation macrolide antibiotic used in treatment of H. pylori and respiratory infection which has a short half-life (3-6 h), low bioavailability (56%) and completely absorbed from GI tract. With this objective, floating particulate dosage form containing clarithromycin as model drug was designed for the treatment of Helicobacter pylori infection. A controlled release floating microspheres system was designed to achieve increase its residence time in the stomach without contact with the mucosa by emulsion solvent diffusion system (ESDS) containing calcium silicate as porous carrier and Eudragit RS100 as release retardant polymer. Floatable microspheres were developed as a dosage form capable of floating in the stomach. The effects of various formulation and process variables on the particle morphology, in vitro floating behavior, micromeritic properties, drug loading and in vitro drug release were studied. The release rate was determined in 0.1N HCl at 370C.The microspheres were found to be regular in shape and highly porous. The formulation confirmed positive in vitro floating and release characteristics. The drug encapsulation efficiency was also on higher side. Incorporation of Calcium silicate in the microspheres proved to be an effective method to achieve the preferred release behavior through diffusion and buoyancy. The designed particulate system, shows excellent buoyant capability and suitable drug release pattern, could possibly be advantageous in terms of increased clarithromycin effectively against H. pylori.