Meyer B H, Muller F O, Luus H G, Drees B, Röthig H J, Badian M, Eckert H G
Department of Pharmacology, University of the Orange Free State, Bloemfontein, Republic of South Africa.
J Antimicrob Chemother. 1992 Apr;29 Suppl A:63-70. doi: 10.1093/jac/29.suppl_a.63.
The pharmacokinetics of cefpirome were studied in healthy male subjects following single (0.5, 1.0 and 2.0 g) and multiple (1.0 g every 12 h for 3.5 days) intramuscular injections. High pressure liquid chromatography was used to determine cefpirome concentrations in plasma and urine. Cefpirome was absorbed rapidly, mean peak times were 1.6-2.3 h. Pharmacokinetics were linear over the 0.5 to 2.0 g range with mean total body clearance ranging from 148 to 154 mL/min. The peak plasma concentration and area under the curve increased in a dose proportional manner. The terminal half-life (2 h) was not influenced by dose or duration of dosing. There was no drug accumulation after multiple in administrations. About 70-80% of an administered dose was excreted in the urine as unchanged cefpirome. Cefpirome was well tolerated, slight to moderate pain being reported in less than 30% of the injections.
在健康男性受试者中,对头孢匹罗单次(0.5、1.0和2.0克)及多次(每12小时1.0克,共3.5天)肌内注射后的药代动力学进行了研究。采用高压液相色谱法测定血浆和尿液中的头孢匹罗浓度。头孢匹罗吸收迅速,平均达峰时间为1.6 - 2.3小时。在0.5至2.0克范围内药代动力学呈线性,平均全身清除率为148至154毫升/分钟。血浆峰浓度和曲线下面积呈剂量比例增加。终末半衰期(2小时)不受剂量或给药疗程的影响。多次给药后无药物蓄积。约70 - 80%的给药剂量以原形头孢匹罗经尿液排泄。头孢匹罗耐受性良好,不到30%的注射报告有轻微至中度疼痛。