Formulation and Evaluation of Sintered Floating Tablets of Cefpodoxime Proxetil

[摘要] Objectives: To develop sintered floating tablets of CP using locust bean gum as a release-controlling material. CP is an orally- administered, extended-spectrum, semi-synthetic antibiotic of the cephalosporin class. Materials and Methods: CP has a short elimination half-life, possesses high solubility, chemical, enzymatic stability and absorption profiles in acidic pH, which makes it a suitable candidate for formulation in a gastro-retentive dose form for improved bioavailability. Camphor was used to get the desired floating properties. The prepared CP floating tablets were subjected to sintering, where the cross linkage within the polymeric structure was increased by exposing the tablets to acetone vapors. The advantage with sintering is that prolonged drug release can be attained at low hardness and low concentrations of polymers. Results: The prepared tablets were evaluated and found to have acceptable physicochemical properties. Formulation S2 containing locust bean gum: drug (0.3:1.0) and camphor (10% w/w), which was exposed to acetone vapors for a period of 6 hrs showed optimum floating properties and a better dissolution profile i.e. 97.3% in 12 hrs. Hence, formulation S2 was considered as the optimized formulation. The in vitro release data of the optimized formulation was treated with mathematical equations and the drug release followed zero-order kinetics (0.9599) with an anomalous transport mechanism (0.5331). Conclusion: Based on the results, it can be concluded that sintered floating matrix tablets of CP containing locust bean provides a better choice for controlled release.

[关键词] Cefpodoxime proxetil;controlled material;gastro-retentive floating tablets;sintering technique