Formulation, development and optimization of ofloxacin FDDS sustained release for UTI and H. pylori

Abstract

Objective: Development & Optimization of Ofloxacin Floating tablets to enhance gastric retention time. Sustained release effect of formulation will reduce the dosing frequency for UTIs and prolonged local effect will benefit against H-pylori infection. Materials: Pre formulation tests were performed which include bulk characteristics and flow properties. Post formulation studies include weight variation, thickness, content uniformity, hardness, friability, dissolution studies, release kinetics and compatibility & stability analysis. Kinetic studies were done and models were applied to understand the drug release mechanism. Accelerated stability analysis was also done for time period of 6 months. Results: All pre formulation tests were within range of USP standards, all the formulations showed good buoyancy. The in-vitro dissolution testing showed that F2 released drug at much slower rate, 64.97% within 24 hrs. F3 & F4 released ofloxacin at faster rate, 98.6% & 99.90% respectively, however, F1 released 91.66% drug within 24 hrs. F1 followed Higuchi model, F2 & F3 followed 1^st order kinetics and F4 followed 1^st order & Higuchi model. For F1, FTIR & DSC analysis curves showed no interaction or change of state of ofloxacin. Conclusion: Formulation F1 was proved to be the optimized formulation and followed non-Fickian release independent of concentration of drug also confirmed from Korsmeyer-Peppas equation. The Stability analysis also proved that F1 is the best fit formulation to be used as Floating Drug Delivery System of Ofloxacin. Stability analysis proved that polymers used in F1 formulation were effective effervescent agents and made the formulation optimized and efficacious.