4.3 Article

Physicochemical and Pharmacokinetic Characterization of a Spray-Dried Cefpodoxime Proxetil Nanosuspension

Journal

CHEMICAL & PHARMACEUTICAL BULLETIN
Volume 58, Issue 7, Pages 912-917

Publisher

PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.58.912

Keywords

cefpodoxime proxetil; nanosuspension; spray dried; theological; pharmacokinetics

Funding

  1. Technology Platform for New Formulation and New DDS, Important National Science and Technology Specific Projects [2009ZX09310-004]

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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 t(max), a 1.60-fold higher area under curve (AUC) and 2.33-fold higher maximum plasma concentration (C-max) than MS.

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