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恩诺沙星在山羊体内肌肉注射后恩诺沙星及其代谢产物环丙沙星的药代动力学

Pharmacokinetics of enrofloxacin and its metabolite ciprofloxacin after intramuscular administration of enrofloxacin in goats.

作者信息

Rao G S, Ramesh S, Ahmad A H, Tripathi H C, Sharma L D, Malik J K

机构信息

Division of Pharmacology and Toxicology, Indian Veterinary Research Institute, Izatnagar.

出版信息

Vet Res Commun. 2001 Apr;25(3):197-204. doi: 10.1023/a:1006481625615.

Abstract

The pharmacokinetics of enrofloxacin and its active metabolite ciprofloxacin were investigated in goats after a single intramuscular administration of enrofloxacin at 2.5 mg/kg body weight. The plasma concentrations of enrofloxacin and ciprofloxacin were determined simultaneously by a HPLC method. The peak concentrations (Cmax) of enrofloxacin (1.13 microg/ml) and ciprofloxacin (0.24 microg/ml) were observed at 0.8 and 1.2 h, respectively. The elimination half-life (t1/2beta), volume of distribution (Vd(area)), total body clearance (Cl(B)) and mean residence time (MRT) of enrofloxacin were 0.74 h, 1.42 L/kg, 1329 ml/h per kg and 1.54 h, respectively. The t1/2beta, area under the plasma concentration-time curve (AUC) and the MRT of ciprofloxacin were 1.38 h, 0.74 microg h/ml and 2.73 h, respectively. The metabolic conversion of enrofloxacin to ciprofloxacin was appreciable (36%) and the sum of the plasma concentrations of enrofloxacin and ciprofloxacin was maintained at or above 0.1 microg/ml for up to 4 h. Enrofloxacin appears to be useful for the treatment of goat diseases associated with pathogens sensitive to this drug.

摘要

在山羊以2.5毫克/千克体重单次肌内注射恩诺沙星后,对其药代动力学及其活性代谢产物环丙沙星进行了研究。采用高效液相色谱法同时测定恩诺沙星和环丙沙星的血浆浓度。恩诺沙星(1.13微克/毫升)和环丙沙星(0.24微克/毫升)的峰浓度(Cmax)分别在0.8小时和1.2小时观察到。恩诺沙星的消除半衰期(t1/2β)、分布容积(Vd(area))、全身清除率(Cl(B))和平均驻留时间(MRT)分别为0.74小时、1.42升/千克、1329毫升/小时每千克和1.54小时。环丙沙星的t1/2β、血浆浓度-时间曲线下面积(AUC)和MRT分别为1.38小时、0.74微克·小时/毫升和2.73小时。恩诺沙星向环丙沙星的代谢转化相当可观(36%),恩诺沙星和环丙沙星的血浆浓度总和在长达4小时内维持在0.1微克/毫升或以上。恩诺沙星似乎可用于治疗与对该药物敏感的病原体相关的山羊疾病。

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