Mucoadhesive biphasic minitablets of cefuroxime axetil: Formulation development, characterization and in vivo bioavailability study

Abstract

Mucoadhesive biphasic minitablets of cefuroxime axetil consists of immediate release and sustain release minitablets. Loading dose of cefuroime axetil was formulated into immediate release (IR) minitablets by fusion method using poloxamer 188 and Sylysia 350. Maintenance dose was formulated as sustain release (SR) mucoadhesive minitablets by direct compression method using chitosan, HPMC K100M and sodium carboymethyl cellulose as mucoadhesive polymers. FT-IR and DSC study revealed no interaction between cefuroxime axetil and excipients. In vitro dissolution study of optimized IR minitablets showed more than 70% of drug release within 15 min. Chitosan based SR mucoadhesive minitablets exhibited highest mucoadhesive strength. The drug release from chitosan based SR mucoadhesive minitablets was linear with square root of time with non-Fickian diffusion controlled release mechanism. The optimized batches of minitablets (both IR and SR) were filled in to 0 size hard gelatin capsule. In vitro dissolution study for capsule showed a biphasic release i.e. immediate burst release followed by sustained release up to 12 h. In vivo bioavailability study in albino rabbits showed four times improvement in oral bioavailability.