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恩诺沙星及其代谢产物环丙沙星在水牛犊牛体内的药代动力学-药效学整合

Pharmacokinetic-pharmacodynamic integration of enrofloxacin and its metabolite ciprofloxacin in buffalo calves.

作者信息

Daundkar Prashant S, Vemu Bhaskar, Dumka Vinod K, Sharma Suresh K

机构信息

Department of Veterinary Pharmacology and ToxicologyCollege of Veterinary ScienceGADVASULudhianaIndia.

出版信息

Vet Med Sci. 2015 Nov 26;1(2):63-71. doi: 10.1002/vms3.10. eCollection 2015 Oct.

Abstract

The present study was planned with an objective to test the pharmacokinetics of a new formulation of enrofloxacin (Flobac SA) in buffalo calves. The drug was administered at the dose rate of 7.5 mg kg body weight through the intravenous (i.v.) and intramuscular (i.m.) route followed by plasma collection and analysis at different time intervals. After analysis, using High Performance Liquid Chromatography - Ultraviolet, various pharmacokinetic parameters were calculated using visual fit for compartmental analysis, followed by integration with pharmacodynamic parameters against and . Although total area under plasma drug concentration time curve was higher through the i.v. route, mean residence time and metabolic conversion ratio was higher following administration by the i.m. route indicating longer persistence of the drug in body. Overall i.m. bioavailability of the parent compound with its metabolite was found to be 91%. Upon, Pharmacokinetic-Pharmacodynamic integration, all the parameters indicated significant antibacterial activity. It can be concluded that the dose of enrofloxacin used in the present study can be administered to contain infections caused by and in buffalo calves.

摘要

本研究旨在测试恩诺沙星新制剂(氟苯尼考SA)在水牛犊牛体内的药代动力学。通过静脉注射(i.v.)和肌肉注射(i.m.)途径,以7.5毫克/千克体重的剂量率给药,随后在不同时间间隔采集血浆并进行分析。分析后,使用高效液相色谱 - 紫外法,通过直观拟合进行房室分析计算各种药代动力学参数,然后将其与针对[具体药物]和[具体药物]的药效学参数进行整合。尽管静脉注射途径的血浆药物浓度 - 时间曲线下总面积较高,但肌肉注射给药后的平均驻留时间和代谢转化率较高,表明药物在体内的持续时间更长。总体而言,母体化合物及其代谢物的肌肉注射生物利用度为91%。通过药代动力学 - 药效学整合,所有参数均表明具有显著的抗菌活性。可以得出结论,本研究中使用的恩诺沙星剂量可用于控制水牛犊牛由[具体病菌]和[具体病菌]引起的感染。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e762/5645818/bd2648fe8cfb/VMS3-1-63-g001.jpg

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