Hall T L, Tell L A, Wetzlich S E, McCormick J D, Fowler L W, Pusterla N
William R. Pritchard Veterinary Medical Teaching Hospital Department of Medicine and Epidemiology, School of Veterinary Medicine, University of California, Davis, CA 95616, USA.
J Vet Pharmacol Ther. 2011 Aug;34(4):403-9. doi: 10.1111/j.1365-2885.2010.01252.x. Epub 2010 Nov 18.
Ceftiofur, a third generation cephalosporin, demonstrates in vitro efficacy against microorganisms isolated from septicemic neonatal foals. This pharmacokinetic study evaluated the intravenous and subcutaneous administration of ceftiofur sodium (5 mg/kg body weight; n = 6 per group) and subcutaneous administration of ceftiofur crystalline free acid (6.6 mg/kg body weight; n = 6) in healthy foals. Plasma ceftiofur- and desfuroylceftiofur-related metabolite concentrations were measured using high performance liquid chromatography following drug administration. Mean (±SD) noncompartmental pharmacokinetic parameters for i.v. and s.c. ceftiofur sodium were: AUC(0→∝) (86.4 ± 8.5 and 91 ± 22 h·μg/mL for i.v. and s.c., respectively), terminal elimination half-life (5.82 ± 1.00 and 5.55 ± 0.81 h for i.v. and s.c., respectively), C(max(obs)) (13 ± 1.9 μg/mL s.c.), T(max(obs)) (0.75 ± 0.4 h for s.c.). Mean (± SD) noncompartmental pharmacokinetic parameters for s.c. ceftiofur crystalline free acid were: AUC(0→∝) (139.53 ± 22.63 h·μg/mL), terminal elimination half-life (39.7 ± 14.7), C(max(obs)) (2.52 ± 0.35 μg/mL) and t(max(obs)) (11.33 ± 1.63 h). No adverse effects attributed to drug administration were observed in any foal. Ceftiofur- and desfuroylceftiofur-related metabolites reached sufficient plasma concentrations to effectively treat common bacterial pathogens isolated from septicemic foals.
头孢噻呋是一种第三代头孢菌素，对从患败血病的新生马驹中分离出的微生物具有体外抗菌活性。本药代动力学研究评估了健康马驹静脉注射和皮下注射头孢噻呋钠（5mg/kg体重；每组n = 6）以及皮下注射头孢噻呋晶体游离酸（6.6mg/kg体重；n = 6）的情况。给药后，采用高效液相色谱法测定血浆中头孢噻呋及去呋喃甲酰头孢噻呋相关代谢物的浓度。静脉注射和皮下注射头孢噻呋钠的平均（±标准差）非房室药代动力学参数为：AUC(0→∝)（静脉注射和皮下注射分别为86.4±8.5和91±22h·μg/mL）、末端消除半衰期（静脉注射和皮下注射分别为5.82±1.00和5.55±0.81h）、C(max(obs))（皮下注射为13±1.9μg/mL）、T(max(obs))（皮下注射为0.75±0.4h）。皮下注射头孢噻呋晶体游离酸的平均（±标准差）非房室药代动力学参数为：AUC(0→∝)（139.53±22.63h·μg/mL）、末端消除半衰期（39.7±14.7）、C(max(obs))（2.52±0.35μg/mL）和t(max(obs))（11.33±1.63h）。未在任何马驹中观察到与给药相关的不良反应。头孢噻呋及去呋喃甲酰头孢噻呋相关代谢物在血浆中达到了足以有效治疗从患败血病马驹中分离出的常见细菌病原体的浓度。
