Phase I study of multiple-dose cefprozil and comparison with cefaclor.

摘要: The objectives of this study were to assess the safety and tolerance cefprozil, characterize pharmacokinetics cefprozil after administration multiple doses drug, compare these pharmacokinetic parameters with those obtained cefaclor. volunteers received 28 250, 500, or 1,000 mg 500 cefaclor every 8 h for 10 days. Serial blood samples total volume urine voided by each individual collected evaluation on days 1, 5, 10. Both cephalosporins well tolerated oral dosing. peak levels in plasma (Cmax) ranged from 5.7 18.3 micrograms/ml 250- 1,000-mg doses. regression analysis Cmax dose showed a dose-linear response. mean 15.2 16.7 did not change significantly overall terminal half-life was 1.2 invariant respect duration area under plasma-concentration-versus-time curve 0 infinity (AUC0-infinity) increased dose-proportional manner an increase dose. urinary recovery (61% dose) renal clearance values generally While apparently absorbed less rapidly achieved lower than cefaclor, AUC0-infinity nearly twofold greater that also longer observed Although (75% higher dose), concentrations remained 2 postdosing. If therapeutic concept is maintained beta-lactam antibiotics should exceed MIC offending organisms over period approximates dosing interval, then would appear be suitable twice-daily administration, whereas probably administered three even four times day.