Volume :
6
Issue :
2
Abstract :
The aim of the present work was to develop and optimize gastroretentive floating system of cefixime (CF) for the effective treatment. The present study was carried out with an objective of preparation and in vivo evaluation of floating tablets of using cefixime as a model drug using Eudragit polymers (Eudragit-S100, Eudragit-RLPO & Eudragit-RSPO) to improve oral bioavailability of cefixime floating tablets by increasing gastric residence time. The tablets were prepared by direct compression method. The effect of polymers concentration and viscosity grades of Eudragit on drug release profile was evaluated. The result of in vitro dissolution study showed that the drug release profile could be controlled by increasing the concentration of Eudragit-RLPO. The optimized formulation (F18) containing Eudragit-RLPO showed 99.24% drug release at the end of 24h. Changing the viscosity grade of Eudragit-RLPO had no significant effect on drug release profile. The optimized formulations (F18) containing sodium bicarbonate 40mg per tablet showed desired buoyancy (floating lag time of about 20 min and total floating time of >24hr). Optimized formulation (F18) followed diffusion controlled zero order kinetics and fickian transport of the drug. FTIR and DSC studies revealed the absence of any chemical interaction between drug and polymers used. The best formulation (F18) was selected based on in vitro characteristics and was used in vivo radiographic studies by incorporating BaSO4. These studies revealed that the tablets remained in the stomach for 24hrs in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered desirable for the absorption window drugs. Studies to evaluate the pharmacokinetics in vivo showed better bioavailability, area under the concentration time curve, elimination rate constant and half-life than marketed product.