Physicochemical and pharmacokinetic characterization of a spray-dried cefpodoxime proxetil nanosuspension

Abstract

Cefpodoxime proxetil (CP) is a prodrug, the third generation cephem-type broad-spectrum antibiotic administered orally. However, CP was found to be a poorly water-soluble drug with low bioavailability when orally administered. In the present investigation, the spray-dried cefpodoxime proxetil nanosuspension (SDN) was prepared. The physicochemical properties were characterized by rheological evaluation, particle size measurement and its distribution, dynamics of reconstitution, in-vitro dissolution testing, surface morphology, surface area and pore size measurements. The pharmacokinetic study of SDN, in comparison to a marketed cefpodoxime proxetil for oral suspension (MS), was also performed in rabbits after a single oral dose. It was found that SDN exhibited a significant decrease in tmax, a 1.60-fold higher area under curve (AUC) and 2.33-fold higher maximum plasma concentration (Cmax) than MS. © 2010 Pharmaceutical Society of Japan.