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山羊静脉、肌肉和皮下注射莫西沙星后的处置动力学

Disposition Kinetic of Moxifloxacin following Intravenous, Intramuscular, and Subcutaneous Administration in Goats.

作者信息

Patel Harshad B, Mody Shailesh K, Patel Hitesh B, Patel Vipul A, Patel Urvesh D

机构信息

Department of Pharmacology and Toxicology, College of Veterinary Science and Animal Husbandry, Junagadh Agricultural University, Junagadh 362 001, Gujarat State, India.

出版信息

ISRN Vet Sci. 2011 Dec 29;2011:584342. doi: 10.5402/2011/584342. Print 2011.

Abstract

The present study was carried out to investigate disposition kinetics of moxifloxacin following single-dose intravenous (i.v.), intramuscular (i.m.), and subcutaneous (s.c.) administration at a dose rate of 5 mg/kg of body weight (b.wt.) in goats. Plasma samples collected after treatments were analyzed for drug concentration using high-performance liquid chromatography (HPLC). After i.v. administration, distribution of the drug was rapid and wide as reflected by high steady-state volume of distribution. Drug elimination was relatively faster with a total body clearance of 0.59 ± 0.03 L/h/kg. Following i.m. injection, the drug has shown the rapid and near-to-complete absorption with bioavailability of 98.20 ± 3.96 per cent. The maximum plasma drug concentration (Cmax) of 1.21 ± 0.04 μg/mL was attained at 1 h (Tmax). The drug was widely distributed as reflected by high apparent volume of distribution. The elimination half-life (t 1/2β ) of the drug was 6.26 ± 0.08  h. Following s.c. administration, the drug was rapidly absorbed (Cmax: 1.16 ± 0.02 μg/mL; tmax: 1 h) and slowly eliminated from the body. The elimination half-life and total body clearance (ClB) were 5.61 ± 0.10 h and 0.60 ± 0.03 L/h/kg, respectively. The bioavailability of moxifloxacin following s.c. administration was 90.44 ± 3.96 per cent.

摘要

本研究旨在探讨山羊单次静脉注射(i.v.)、肌肉注射(i.m.)和皮下注射(s.c.)5mg/kg体重剂量的莫西沙星后的处置动力学。治疗后采集的血浆样本采用高效液相色谱法(HPLC)分析药物浓度。静脉注射后,药物分布迅速且广泛,表现为高稳态分布容积。药物消除相对较快,全身清除率为0.59±0.03L/h/kg。肌肉注射后,药物吸收迅速且接近完全,生物利用度为98.20±3.96%。1小时(Tmax)时达到最大血浆药物浓度(Cmax)为1.21±0.04μg/mL。药物分布广泛,表现为高表观分布容积。药物的消除半衰期(t1/2β)为6.26±0.08小时。皮下注射后,药物吸收迅速(Cmax:1.16±0.02μg/mL;tmax:1小时),并从体内缓慢消除。消除半衰期和全身清除率(ClB)分别为5.61±0.10小时和0.60±0.03L/h/kg。皮下注射后莫西沙星的生物利用度为90.44±3.96%。

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