Pharmacokinetics of ceftiofur and metabolites after single intravenous and intramuscular administration and multiple intramuscular administrations of ceftiofur sodium to sheep

被引:27
作者
Craigmill, AL [1 ]
Brown, SA [1 ]
Wetzlich, SE [1 ]
Gustafson, CR [1 ]
Arndt, TS [1 ]
机构
[1] PHARMACIA & UPJOHN INC,DIV ANIM HLTH,KALAMAZOO,MI 49001
关键词
D O I
10.1046/j.1365-2885.1997.00820.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Twenty-four sheep (38.0-54.1 kg body wt) were allocated into four treatment groups and dosed with ceftiofur sodium at 1.1 mg ceftiofur free acid equivalents (CFAE)/kg or 2.2 CFAE/kg using a complete two-route (intravenous, i.v.; intramuscular, i.m.), two-period crossover design, with a two-week washout between injections. After another two-week washout period, 12 sheep were selected and dosed with ceftiofur sodium i.m. for five consecutive days at either 1.1 or 2.2 mg CFAE/kg. After all injections, blood samples were obtained serially for determination of serum concentrations of ceftiofur and metabolites. The terminal phase half-lives derived from the last 3-5 concentration-time points were 350 and 292 min (harmonic means) after i.v. doses of 1.1 and 2.2 mg/kg, respectively, and 389 and 459 min after i.m. doses of 1.1 and 2.2 mg/kg, respectively. The i.m. bioavailability of ceftiofur sodium in sheep was 100%, and the area under the curve from time 0 to the limit of quantitation (AUC(O-LOQ)) was dose-proportional from 1.1-2.2 mg CFAE/kg body wt in sheep. After 5 daily i.m, doses of ceftiofur sodium at either 1.1 or 2.2 mg CFAE/kg there was minimal accumulation of drug in serum as assessed by the observed maximum serum concentration (C-max), and serum concentrations were dose-proportional after the multiple dosing regimen.
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页码:139 / 144
页数:6
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