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氟苯尼考在羊静脉注射和肌肉注射后的药代动力学。

Pharmacokinetics of florfenicol after intravenous and intramuscular dosing in llamas.

机构信息

Department of Veterinary Clinical Sciences, College of Veterinary Medicine, Ohio State University, Columbus, OH 43210, USA.

出版信息

Res Vet Sci. 2013 Oct;95(2):594-9. doi: 10.1016/j.rvsc.2013.05.009. Epub 2013 Jun 12.

Abstract

Florfenicol, is a broad spectrum antimicrobial agent with wide tissue distribution commonly used to treat camelids. To address the lack of drug disposition data for florfenicol in llamas, we evaluated the pharmacokinetics after 20mg/kg intravenous (i.v.) and intramuscular (i.m.) dosing. Serum concentrations were determined using a HPLC-UV assay and pharmacokinetic analysis was conducted using non-compartmental analysis. Following i.v. injection, systemic clearance and Vdss in llamas were 4.6 mL/min/kg and 737 mL/kg, respectively. Mean residence time after i.v. dosing was 3h. After i.m. injection, florfenicol was rapidly absorbed, with Cmax concentrations being 3.2 μg/mL at 0.5h, mean residence time was 15 h, mean absorption time was 12h and absolute bioavailability of florfenicol after i.m. injection was 63%. The prolonged absorption of florfenicol after i.m. administration suggests the apparent HL_λz reflects the absorption process rather than elimination of the drug. Florfenicol administration was not associated with adverse reactions after dosing by either route. Serum florfenicol concentrations remained >1.0 μg/mL for 12h after i.m. administration. For susceptible pathogens, once daily dosing of 20mg/kg body weight appears appropriate.

摘要

氟苯尼考是一种广谱抗菌药物,具有广泛的组织分布,常用于治疗骆驼科动物。为了研究氟苯尼考在羊驼体内的药物代谢动力学数据,我们评估了 20mg/kg 静脉(i.v.)和肌肉(i.m.)给药后的药代动力学。使用 HPLC-UV 检测法测定血清浓度,并采用非房室分析进行药代动力学分析。静脉注射后,羊驼的全身清除率和 Vdss 分别为 4.6mL/min/kg 和 737mL/kg。静脉注射后的平均驻留时间为 3 小时。肌肉注射后,氟苯尼考迅速吸收,Cmax 浓度在 0.5 小时时达到 3.2μg/mL,平均驻留时间为 15 小时,平均吸收时间为 12 小时,肌肉注射后的氟苯尼考绝对生物利用度为 63%。肌肉注射后氟苯尼考的吸收延长表明,表观 HL_λz 反映了药物的吸收过程,而不是消除过程。两种途径给药后,均未观察到氟苯尼考引起的不良反应。肌肉注射后 12 小时内,羊驼的血清氟苯尼考浓度仍保持在 1.0μg/mL 以上。对于敏感病原体,每日一次 20mg/kg 体重的剂量似乎是合适的。

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