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拜有利(恩诺沙星)在犬体内的药代动力学

[Pharmacokinetics of baytril (enrofloxacin) in dogs].

作者信息

Küng K, Wanner M

机构信息

Abteilung für Tierernährung, Universität Zürich.

出版信息

Schweiz Arch Tierheilkd. 1994;136(10):329-34.

PMID:7801085
Abstract

Baytril with the active ingredient enrofloxacin was given to four dogs in a single intravenous and oral dose of 5 mg/kg body weight. Measured plasma concentrations were different depending on the method of analysis used. Using high performance liquid chromatography quantitative determination of both enrofloxacin and its main metabolite ciprofloxacin is possible whereas antimicrobially active substance is measured by bioassay. Ciprofloxacin occurred early in the concentration-time curves after intravenous and oral administration of the parent drug enrofloxacin with cmax 0.2 and 0.3 microgram/ml, respectively, at tmax 2 and 4 h, respectively. Areas under the curve (AUC) calculated from concentration-time-curves with bioassay data are overestimated, because ciprofloxacin may be more active than enrofloxacin against E. coli 14 (ICB 4004) used in this test. Thus, pharmacokinetic parameters which are derived from AUC-values are overestimated, too. Oral bioavailability calculated with bioassay results was more than 100% whereas availability of enrofloxacin was only 53%. Clearance was 10.3 ml/min.kg (antimicrobially active substance) and 27.1 ml/min.kg (enrofloxacin). Elimination half life was 3.7 and 2.4 h, respectively.

摘要

将有效成分恩诺沙星的拜有利以5毫克/千克体重的单次静脉内和口服剂量给予4只犬。根据所使用的分析方法,测得的血浆浓度有所不同。使用高效液相色谱法可以对恩诺沙星及其主要代谢物环丙沙星进行定量测定,而抗菌活性物质则通过生物测定法进行测量。在静脉内和口服给予母体药物恩诺沙星后,环丙沙星在浓度-时间曲线中出现较早,静脉给药时tmax为2小时,cmax为0.2微克/毫升,口服给药时tmax为4小时,cmax为0.3微克/毫升。根据生物测定数据从浓度-时间曲线计算出的曲线下面积(AUC)被高估了,因为在该试验中使用的大肠杆菌14(ICB 4004)中,环丙沙星可能比恩诺沙星更具活性。因此,从AUC值得出的药代动力学参数也被高估了。根据生物测定结果计算的口服生物利用度超过100%,而恩诺沙星的生物利用度仅为53%。清除率分别为10.3毫升/分钟·千克(抗菌活性物质)和27.1毫升/分钟·千克(恩诺沙星)。消除半衰期分别为3.7小时和2.4小时。

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