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替米考星在肉用火鸡单次静脉注射和口服给药后的药代动力学()

Pharmacokinetics of Tylvalosin in Broiler Turkeys () After Single Intravenous and Oral Administration.

作者信息

Elbadawy Mohamed, Aboubakr Mohamed, Abugomaa Amira

机构信息

Department of Pharmacology, Faculty of Veterinary Medicine, Benha University, Moshtohor, Egypt.

Faculty of Veterinary Medicine, Mansoura University, Mansoura, Egypt.

出版信息

Front Vet Sci. 2019 Oct 17;6:355. doi: 10.3389/fvets.2019.00355. eCollection 2019.

Abstract

Pharmacokinetics of tylvalosin (TVN) were determined in eight broiler turkeys following a single intravenous (IV) and peroral (PO) administration of 25 mg/kg b.w using a crossover design with a 3 weeks washout period. Blood samples were taken between 0.083 and 24 h following TVN administration, plasma was separated and assayed for TVN concentrations by HPLC. The non-compartmental analysis was used to analyze plasma concentration-time curves. After IV administration, the pharmacokinetic profile was best described by a two-compartment model. The mean distribution and elimination half-lives were 0.382 and 5.71 h, respectively. The distribution volume at steady state, total body clearance and mean residence time were 8.30 L/kg, 1.17 L/h, and 7.16 h, respectively. After administering orally, the mean absorption half-life and absorption time of TVN was 0.955 and 2.31 h, respectively. The peak plasma concentration was 1.08 μg/mL and achieved at 2.0 h post-administration and the bioavailability was 53.3%. The plasma protein binding percent was 13%. For a successful clinical efficacy of TVN in broiler turkeys, a dosage regimen of 25 mg/kg b.w, given orally each day is recommended to keep efficient plasma levels above the MIC for most susceptible microorganisms.

摘要

采用交叉设计,在8只肉用火鸡中测定替瓦洛星(TVN)的药代动力学,给药剂量为25mg/kg体重,静脉注射(IV)和口服(PO)各一次,洗脱期为3周。在TVN给药后0.083至24小时内采集血样,分离血浆,采用高效液相色谱法测定TVN浓度。采用非房室分析法分析血浆浓度-时间曲线。静脉注射后,药代动力学特征最好用二室模型描述。平均分布半衰期和消除半衰期分别为0.382小时和5.71小时。稳态分布容积、总体清除率和平均驻留时间分别为8.30L/kg、1.17L/h和7.16小时。口服给药后,TVN的平均吸收半衰期和吸收时间分别为0.955小时和2.31小时。给药后2.0小时达到血浆峰浓度1.08μg/mL,生物利用度为53.3%。血浆蛋白结合率为13%。为使TVN在肉用火鸡中取得成功的临床疗效,建议采用每天口服25mg/kg体重的给药方案,以使有效血浆水平维持在大多数敏感微生物的最低抑菌浓度(MIC)以上。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbc/6812644/9f4d58383f23/fvets-06-00355-g0001.jpg

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