Harding S M, Monro A J, Thornton J E, Ayrton J, Hogg M I
Glaxo Group Research Limited, Greenford, Middlesex, UB6 0HE, England.
J Antimicrob Chemother. 1981 Sep;8 Suppl B:263-72. doi: 10.1093/jac/8.suppl_b.263.
The pharmacokinetic behaviour of two aminothiazolyl cephalosporins, ceftazidime (CAZ) and cefotaxime (CTX), were compared in three studies. Doses of each antibiotic were given intravenously (500 mg, n=4; 1 g, n=4) or intramuscularly (1 g, n=8) in a cross-over manner to healthy male volunteers. Antibiotic assays were performed by HPLC and microbiological assay techniques. Both antibiotics appeared to fit a two-compartment iv kinetic model with terminal half-lives of 1.7 h (CAZ) and 0.8 h (CTX). CAZ was metabolically stable whereas there was 34% conversion of CTX to desacetyl-CTX. The 24 h urinary recovery of CAZ averaged 89% but only 51% for CTX. The protein binding of CAZ was 17% and of CTX was 47%. CTX was more painful than CAZ on im injection in seven of the eight volunteers. CAZ therefore appeared to possess a number of features more favourable than those of CTX, when assessed in healthy volunteers.
在三项研究中比较了两种氨噻唑基头孢菌素（头孢他啶（CAZ）和头孢噻肟（CTX））的药代动力学行为。以交叉方式给健康男性志愿者静脉注射（500mg，n = 4；1g，n = 4）或肌肉注射（1g，n = 8）每种抗生素。通过高效液相色谱法（HPLC）和微生物测定技术进行抗生素测定。两种抗生素似乎都符合二室静脉动力学模型，终末半衰期分别为1.7小时（CAZ）和0.8小时（CTX）。CAZ代谢稳定，而CTX有34%转化为去乙酰头孢噻肟。CAZ 24小时尿回收率平均为89%，而CTX仅为51%。CAZ的蛋白结合率为17%，CTX为47%。在8名志愿者中的7名中，CTX肌肉注射比CAZ更痛。因此，在健康志愿者中评估时，CAZ似乎具有一些比CTX更有利的特性。
