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.

Pharmacokinetics of Antibacterial Agents in the Elderly: The Body of Evidence

“…Achievement of free concentration targets associated with efficacy was in most circumstances equivalent, suggesting no negative association with the fed state [113] Cefaclor Cmax decreased, Tmax delayed, but no AUC changes were reported for cefaclor granule and cefaclor suspension under fed state supposing effective use regardless of meal [114] Cefuroxime axetil Positive food effect on absorption with AUC in fed state greater than in the fasted state, suggesting postprandial administration be more effective [109] Cefpodoxime proxetil Achievement of proper Cmax and MIC values was reported in non-fasting patients. In the elderly patients, the absorption is approximately 30% lower compared to younger patients [115][116][117] Azithromycin Capsules have delayed disintegration under fed state, resulting in the extended gastric residence and gastric degradation of azithromycin, thus capsules should be taken only in the fasted state. Tablets can be used regardless of meal [118] Clindamycin The extent to systemic exposure was affected by the delay in absorption in the fed state, suggesting optimal dosing is in the fasted state [119] Linezolid A slight decrease in Cmax, and delay in Tmax were observed in fed state, with no effect on AUC, suggesting effective use regardless of meal [120] Ofloxacin Cmax and AUC were greater in the fasted state, significant decrease of absorption was observed with aluminum co-administration [121] Ciprofloxacin Cmax and AUC were greater in the fasted state, significant decrease of absorption was observed with aluminum co-administration.…”