Kees F, Naber K G, Bartoschik-Wich B, Stockmann P, Meyer G P, Grobecker H
Arzneimittelforschung. 1985;35(7):1099-104.
In plasma and urine of 10 healthy volunteers after intravenous administration of 4 g mezlocillin and piperacillin, respectively, the parent compounds as well as degradation products were assayed by high-performance liquid chromatography. Ioxitalamic acid, a renal contrast medium, was administered simultaneously, in order to measure the glomerular filtration rate, and to control the collection of 24-h urine. As metabolite of mezlocillin the corresponding penicilloic acid only was found, whereas in the case of piperacillin a further degradation product was observed. Half of the doses given was recovered in the urine as unchanged drugs, and in addition 5-10% as metabolites. No differences were found in the pharmacokinetic behaviour of both antibiotics.
分别对10名健康志愿者静脉注射4克美洛西林和哌拉西林后,采集其血浆和尿液,采用高效液相色谱法对母体化合物及其降解产物进行测定。同时给予肾造影剂碘他拉酸,以测定肾小球滤过率并控制24小时尿液的收集。仅发现美洛西林的相应青霉噻唑酸作为其代谢物,而哌拉西林则观察到一种进一步的降解产物。给药剂量的一半以原形药物形式在尿液中回收,另外5 - 10%以代谢物形式回收。两种抗生素的药代动力学行为未发现差异。