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左氧氟沙星在绵羊静脉注射和肌肉注射后的处置动力学

Disposition kinetics of levofloxacin in sheep after intravenous and intramuscular administration.

作者信息

Goudah Ayman, Hasabelnaby Sherifa

机构信息

Pharmacology Department, Faculty of Veterinary Medicine, Cairo University, Giza, P.O. Box 12211, Egypt.

出版信息

Vet Med Int. 2010 Nov 2;2010:727231. doi: 10.4061/2010/727231.

Abstract

The present study was planned to investigate the disposition kinetics of levofloxacin in plasma of female native Barky breed sheep after single intravenous (IV) and intramuscular (IM) administration of 4 mg/kg body weight. The concentrations of levofloxacin in the plasma were measured using high-performance liquid chromatography (HPLC) with a UV detector on samples collected at 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 4, 6, 8, 10, 12, 18, 24, 32, and 48 h after treatment. Following intravenous injection, the decline in plasma drug concentration was biexponential with half-lives of (t(1/2α)) 0.33 ± 0.12 h and (t(1/2β)) 3.29 ± 0.23 h for distribution and elimination phases, respectively. The volume of distribution at steady state V((d(ss))) was 0.86 ± 0.23 l/kg. After intramuscular administration of levofloxacin at the same dose, the peak plasma concentration (C(max)) was 3.1 ± 0.35 μg/mL and was obtained at 1.64 ± 0.29 h (T(max)), the elimination half-life (T(1/2el)) was 3.58 ± 0.30 h, and AUC was 20.24 ± 1.31 μg.h/mL. The systemic bioavailability was 91.35 ± 6.81 %. In vitro plasma protein binding was 23.74%. When approved therapy fails, levofloxacin may be used in some countries for therapy of food animals, however, that is not true in the US.

摘要

本研究旨在探讨在雌性本地巴基品种绵羊单次静脉注射(IV)和肌肉注射(IM)4mg/kg体重的左氧氟沙星后,其在血浆中的处置动力学。使用配备紫外检测器的高效液相色谱(HPLC)测定治疗后0、0.08、0.16、0.33、0.5、1、2、4、6、8、10、12、18、24、32和48小时采集的样本中血浆左氧氟沙星的浓度。静脉注射后,血浆药物浓度下降呈双指数形式,分布相和消除相的半衰期(t(1/2α))分别为0.33±0.12小时和(t(1/2β))3.29±0.23小时。稳态分布容积V((d(ss)))为0.86±0.23L/kg。以相同剂量肌肉注射左氧氟沙星后,血浆峰浓度(C(max))为3.1±0.35μg/mL,在1.64±0.29小时(T(max))达到,消除半衰期(T(1/2el))为3.58±0.30小时,AUC为20.24±1.31μg·h/mL。全身生物利用度为91.35±6.81%。体外血浆蛋白结合率为23.74%。当批准的治疗失败时,左氧氟沙星在一些国家可用于食用动物的治疗,但在美国并非如此。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2ea/2971565/a9ec036c2860/VMI2010-727231.001.jpg

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