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Gastroretentive Sustained Release Floating and Swellable Cefadroxil Formulation: In vitro and in vivo Evaluation

Chaudhari SV and Vavia PR

A new Gastroretentive Sustained Release (GRSR) tablet of cefadroxil was developed with floating and swellable properties. Various release retarding polymers, swelling agent, gas generating agent and release modifying agents were evaluated. The optimized formulation was studied for various physical parameters, in vitro drug release profile and for in vitro floating properties. The formulation provided sustained drug release for about 14 h with the floating lag time of 30 s and floating duration of about 14 h. Owing to the promising in vitro floating property, the formulation was explored for in vivo floating performance in healthy human volunteers by radio-analytical technique. The developed formulation of Cefadroxil showed prolonged gastric retention in vivo for 7 h. The tablets also showed significant swelling property with excellent tablet integrity till 7 h.

The developed formulation exhibited promising gastroretention in vivo. The radio-analytical technique used to evaluate the in vivo gastroretention was found to be simple, cost-effective and was precisely used for detecting floating time and tablet integrity throughout the study.