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泰乐菌素酒石酸盐和泰乐菌素磷酸盐在鸡单次口服和静脉注射给药后的比较药代动力学和生物利用度

Comparative pharmacokinetics and bioavailability of tylosin tartrate and tylosin phosphate after a single oral and i.v. administration in chickens.

作者信息

Ji L-W, Dong L-L, Ji H, Feng X-W, Li D, Ding R-L, Jiang S-X

机构信息

Laboratory of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Nanjing Agricultural University, Nanjing, Jiangsu Province, China.

出版信息

J Vet Pharmacol Ther. 2014 Jun;37(3):312-5. doi: 10.1111/jvp.12092. Epub 2013 Dec 11.

DOI:10.1111/jvp.12092
PMID:24325541
Abstract

The pharmacokinetics and oral bioavailability of tylosin tartrate and tylosin phosphate were carried out in broiler chickens according to a principle of single dose, random, parallel design. The two formulations of tylosin were given orally and intravenously at a dose level of 10 mg/kg b.w to chicken after an overnight fasting (n = 10 chickens/group). Serial blood samples were collected at different time points up to 24 h postdrug administration. A high performance liquid chromatography method was used for the determination of tylosin concentrations in chicken plasma. The tylosin plasma concentration's time plot of each chicken was analyzed by the 3P97 software. The pharmacokinetics of tylosin was best described by a one-compartmental open model 1st absorption after oral administration. After intravenous administration the pharmacokinetics of tylosin was best described by a two-compartmental open model, and there were no significant differences between tylosin tartrate and tylosin phosphate. After oral administration, there were significant differences in the Cmax (0.18 ± 0.01, 0.44 ± 0.09) and AUC (0.82 ± 0.05, 1.57 ± 0.25)between tylosin phosphate and tylosin tartrate. The calculated oral bioavailability (F) of tylosin tartrate and tylosin phosphate were 25.78% and 13.73%, respectively. Above all, we can reasonably conclude that, the absorption of tylosin tartrate is better than tylosin phosphate after oral administration.

摘要

根据单剂量、随机、平行设计的原则,对肉鸡进行了酒石酸泰乐菌素和磷酸泰乐菌素的药代动力学及口服生物利用度研究。在禁食过夜后,以10mg/kg体重的剂量水平对鸡口服和静脉注射两种泰乐菌素制剂(每组10只鸡)。在给药后24小时内的不同时间点采集系列血样。采用高效液相色谱法测定鸡血浆中泰乐菌素的浓度。用3P97软件分析每只鸡的泰乐菌素血浆浓度-时间曲线。口服给药后,泰乐菌素的药代动力学最好用单室开放模型一级吸收来描述。静脉给药后,泰乐菌素的药代动力学最好用二室开放模型来描述,酒石酸泰乐菌素和磷酸泰乐菌素之间无显著差异。口服给药后,磷酸泰乐菌素和酒石酸泰乐菌素在Cmax(0.18±0.01,0.44±0.09)和AUC(0.82±0.05,1.57±0.25)方面存在显著差异。酒石酸泰乐菌素和磷酸泰乐菌素计算得到的口服生物利用度(F)分别为25.78%和13.73%。综上所述,我们可以合理地得出结论,口服给药后酒石酸泰乐菌素的吸收优于磷酸泰乐菌素。

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