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恩诺沙星在火鸡体内的药代动力学。

Pharmacokinetics of enrofloxacin in turkeys.

作者信息

Dimitrova D J, Lashev L D, Yanev S G, Pandova B

机构信息

Department of Veterinary Pharmacology and Toxicology, Trakia University, Srara Zagora, 6000 Trakia, Bulgaria.

出版信息

Res Vet Sci. 2007 Jun;82(3):392-7. doi: 10.1016/j.rvsc.2006.09.004. Epub 2006 Nov 14.

Abstract

The pharmacokinetics of enrofloxacin (EFL) and its active metabolite ciprofloxacin (CIP) was investigated in 7-8 month old turkeys (6 birds per sex). EFL was administered intravenously (i.v.) and orally (p.o.) at a dose 10 mg kg(-1) body weight. Blood was taken prior to and at 0.17, 0.33, 0.5, 1, 2, 3, 4, 6, 8, 10 and 24 h following drug administration. The concentrations of EFL and CIP in blood serum were determined by high-performance liquid chromatography (HPLC). Serum concentrations versus time were analysed by a noncompartmental analysis. The elimination half-live and the mean residence time of EFL after i.v. injection for the serum were after oral administration 6.64+/-0.90 h, 8.96+/-1.18 h and 6.92+/-0.97 h, 11.91+/-1.87 h, respectively. After single p.o. administration, EFL was absorbed slowly (MAT=2.76+/-0.48 h) with time to reach maximum serum concentrations of 6.33+/-2.54 h. Maximum serum concentrations was 1.23+/-0.30 microg mL(-1). Oral bioavailability for for EFL after oral administration was found to be 69.20+/-1.49%. The ratios C(max)/MIC and AUC(0 --> 24)/MIC were respectively from 161.23+/-5.9 h to 12.90+/-0.5 h for the pharmacodynamic predictor C(max)/MIC, and from 2153.44+/-66.6 h to 137.82+/-4.27 h for AUC(0 --> 24)/MIC, for the different clinically significant microorganisms, whose values for MIC varies from 0.008 microg L(-1) to 0.125 microg mL(-1).

摘要

研究了恩诺沙星(EFL)及其活性代谢产物环丙沙星(CIP)在7 - 8月龄火鸡(每种性别6只)体内的药代动力学。以10 mg kg⁻¹体重的剂量静脉注射(i.v.)和口服(p.o.)给予EFL。在给药前以及给药后0.17、0.33、0.5、1、2、3、4、6、8、10和24小时采集血液。通过高效液相色谱法(HPLC)测定血清中EFL和CIP的浓度。采用非房室分析法分析血清浓度与时间的关系。静脉注射后EFL在血清中的消除半衰期和平均驻留时间,口服给药后分别为6.64±0.90小时、8.96±1.18小时和6.92±0.97小时、11.91±1.87小时。单次口服给药后,EFL吸收缓慢(MAT = 2.76±0.48小时),达到最大血清浓度的时间为6.33±2.54小时。最大血清浓度为1.23±0.30 μg mL⁻¹。口服给药后EFL的口服生物利用度为69.20±1.49%。对于不同临床意义的微生物,其MIC值在0.008 μg L⁻¹至0.125 μg mL⁻¹之间,药效学预测指标C(max)/MIC的比值分别为161.23±5.9小时至12.90±0.5小时,AUC(0→24)/MIC的比值分别为2153.44±66.6小时至137.82±4.27小时。

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