Physicochemical and pharmacokinetic characterization of a spray-dried cefpodoxime proxetil nanosuspension.
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.
Gao
Yuan
Y
School of Traditional Chinese Medicine, China Pharmaceutical University, Nanjing, P. R. China.
Qian
Shuai
S
Zhang
Jianjun
J
D000284:Administration, Oral; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D015296:Ceftizoxime / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D011817:Rabbits; D013678:Technology, Pharmaceutical / Q000379:methods*; D000097627:Cefpodoxime Proxetil
D000900:Anti-Bacterial Agents; D015296:Ceftizoxime; D000097627:Cefpodoxime Proxetil