Preparation and evaluation of ketoprofen floating oral delivery system

A sustained release system for ketoprofen designed to increase its residenc e time in the stomach without contact with the mucosa was achieved through the preparation of floating microparticles by the emulsion-solvent diffusio n technique. Four different ratios of Eudragit S100 (ES) with Eudragit RL ( ERL) were used to form the floating microparticles. The drug retained in th e floating microparticles decreased with increase in ERL. content. All floa ting microparticle formulations showed good flow properties and packability . Scanning electron microscopy and particle size analysis revealed differen ces between the formulations as to their appearance and size distribution. X-ray and DSC examination showed the amorphous nature of the drug. Release rates were generally low in 0.1 N HCl especially in presence of high conten t of ES while in phosphate buffer pH 6.8. high, amounts of ES tended to giv e a higher release rate. Floating ability in 0.1 N HCl, 0.1 N HCl containin g 0.02% Tween 20 and simulated gastric fluid without pepsin was also tested . The formulation containing ES:ERL1:1 (FIII) exhibited high percentage of floating particles in all examined media. (C) 2001 Elsevier Science B.V. Al l rights reserved.