Cefpodoxime Concentrations in Human Serum and Oral Tissues Following a Single Oral Administration of Cefpodoxime Proxetil

Abstract

　Cefpodoxime proxetil, an ester prodrug of cefpodoxime, is an oral third-generation cephalosporin antibiotic that is used for the treatment of odontogenic infections such as periodontitis, pericoronitis, and osteitis of jaw. However, there are only a few studies on cephalosporin concentrations in human oral tissues. The present study therefore was undertaken to determine cefpodoxime concentrations in human oral tissues following oral administration of cefpodoxime proxetil. Cefpodoxime concentrations in human serum, gingiva, mandibular bone, and dental follicle following a single oral administration of 200- mg cefpodoxime proxetil were measured by a paper disk method. The mean peak concentrations in serum, gingiva, mandibular bone, and dental follicle occurred at the same time point, 3 hours post-dose, and were 3.07 ± 0.96 μg/mL, 1.16 ± 0.35 μg/g, 0.60 ± 0.27 μg/g, and 1.13 ± 0.34 μg/g, respectively. Mean cefpodoxime concentration ratios of gingiva / serum, mandibular bone / serum, and dental follicle / serum at the peak time were 0.40 ± 0.15, 0.20 ± 0.05, and 0.37 ± 0.03, respectively. Mean concentrations in gingiva, mandibular bone, and dental follicle at the peak time exceeded the minimum inhibitory concentration for 80% of clinically isolated strains of oral streptococci. Therefore, cefpodoxime proxetil may be a valuable antimicrobial agent for the treatment of odontogenic infection.