Shan Q, Yang F, Wang J, Ding H, He L, Zeng Z
National Reference Laboratory of Veterinary Drug Residues (SCAU), College of Veterinary Medicine, South China Agricultural University, Guangzhou, China; Pearl River Fisheries Research Institute, Chinese Academy of Fishery Sciences, Guangzhou, China.
J Vet Pharmacol Ther. 2014 Apr;37(2):178-85. doi: 10.1111/jvp.12076. Epub 2013 Aug 26.
The cephalosporin antimicrobial drug cefquinome was administered to yellow cattle intravenously (i.v.) and intramuscularly (i.m.) at a dose of 1 mg/kg of body weight in a two-period crossover study. The pharmacokinetic (PK) properties of cefquinome in serum, inflamed tissue-cage fluid (exudate), and noninflamed tissue-cage fluid (transudate) were studied using a tissue-cage model. The in vitro and ex vivo activities of cefquinome in serum, exudate, and transudate against a pathogenic strain of Pasteurella multocida (P. multocida) were determined. A concentration-independent antimicrobial activity of cefquinome was confirmed for levels lower than 4 × MIC. Integration of in vivo pharmacokinetic data with the in vitro MIC provided mean values for the time that drug levels remain above the MIC (T > MIC) in serum was 14.10 h after intravenous and 14.46 h after intramuscular dosing, indicating a likely high level of effectiveness in clinical infections caused by P. multocida of MIC 0.04 μg/mL or less. These data may be used as a rational basis for setting dosing schedules, which optimize clinical efficacy and minimize the opportunities for emergence of resistant organisms.
在一项两阶段交叉研究中，以1毫克/千克体重的剂量对黄牛静脉注射（i.v.）和肌肉注射（i.m.）头孢喹肟这种头孢菌素类抗菌药物。使用组织笼模型研究了头孢喹肟在血清、炎症组织笼液（渗出液）和非炎症组织笼液（漏出液）中的药代动力学（PK）特性。测定了头孢喹肟在血清、渗出液和漏出液中对多杀巴斯德氏菌（P. multocida）致病菌株的体外和离体活性。对于低于4×MIC的水平，证实了头孢喹肟具有浓度依赖性抗菌活性。将体内药代动力学数据与体外MIC相结合，得出静脉给药后血清中药物水平保持高于MIC（T＞MIC）的时间平均值为14.10小时，肌肉注射给药后为14.46小时，这表明对MIC为0.04μg/mL或更低的多杀巴斯德氏菌引起的临床感染可能具有较高的有效性。这些数据可作为制定给药方案的合理依据，以优化临床疗效并尽量减少耐药菌出现的机会。
