Gemifloxacin mesylate

The aim of the present work was to develop and optimize gastroretentive floating system of Gemifloxacin mesylate using HPMC polymers, Gelucire 50/13 and Polyox WSR 301 to improve oral bioavailability of Gemifloxacin mesylate floating tablets by increasing gastric residence time. The tablets were prepared by direct compression method. The effect of polymers concentration and viscosity grades of HPMC on drug release profile was evaluated. The result of in vitro dissolution study showed that the drug release profile could be sustained by increasing the concentration of HPMC and Polyox WSR 301. The optimized formulation (F12) containing HPMC K100M, Gelucire 50/13 and Polyox WSR301 showed 99.12% drug release at the end of 12h. The optimized formulations (F12) containing showed desired buoyancy (floating lag time of about 35 seconds and total floating time of >12h). Optimized formulation (F12) followed diffusion controlled zero order kinetics and non-fickian transport of the drug. FTIR studies revealed the absence of any chemical interaction between drug and polymers used.

Gemifloxacin mesylate loaded microspheres were prepared by Ionotropic gelation technique with different drug to carrier ratio. All the microspheres were characterized for particle size, scanning electron microscopy, FTIR study, DSC, percentage yield, drug entrapment, stability studies and for in vitro release kinetics and found to be within the limits. Among all the formulations S8, was selected as optimized formulation based on the physic chemical and release studies. In the in vitro release study of formulation S8 showed 95.92%, after 12 h in a controlled manner, which is essential for anti ulcer therapy. The innovator Gemiflox conventional tablet shows the drug release of 95.23% within 1 h. The drug release of optimized formulation S8 followed zero order and Higuchi kinetics indicating diffusion controlled drug release.