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对奶牛进行非肠道给药后泰乐菌素和替米考星在乳汁和血液中的药代动力学

Milk and blood pharmacokinetics of tylosin and tilmicosin following parenteral administrations to cows.

作者信息

Avci Tulay, Elmas Muammer

机构信息

Department of Toxicology, Veterinary Control Institute, 42080 Konya, Turkey.

Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Selcuk, 42003 Konya, Turkey.

出版信息

ScientificWorldJournal. 2014;2014:869096. doi: 10.1155/2014/869096. Epub 2014 Aug 6.

Abstract

The aim of this study is to determine the pharmacokinetics of tylosin and tilmicosin in serum and milk in healthy Holstein breed cows (n = 12) and reevaluate the amount of residue in milk. Following the intramuscular administration of tylosin, the maximum concentrations (C max) in serum and milk were found to be 1.30 ± 0.24 and 4.55 ± 0.23 µg/mL, the time required to reach the peak concentration (t max) was found to be 2nd and 4th h, and elimination half-lives (t 1/2β ) were found to be 20.46 ± 2.08 and 26.36 ± 5.55 h, respectively. Following the subcutaneous administration of tilmicosin, the C max in serum and milk were found to be 0.86 ± 0.20 and 20.16 ± 1.13 µg/mL, the t max was found to be 1st and 8th h, and the t 1/2β were found to be 29.94 ± 6.65 and 43.02 ± 5.18 h, respectively. AUCmilk/AUCserum and C max-milk/C max-serum rates, which are indicators for determining the rate of drugs that pass into milk, were, respectively, calculated as 5.01 ± 0.72 and 3.61 ± 0.69 for tylosin and 23.91 ± 6.38 and 20.16 ± 1.13 for tilmicosin. In conclusion, it may be stated that milk concentration of tylosin after parenteral administration is higher than expected like tilmicosin and needs more withdrawal period for milk than reported.

摘要

本研究的目的是确定泰乐菌素和替米考星在健康荷斯坦奶牛(n = 12)血清和乳汁中的药代动力学,并重新评估乳汁中的残留量。肌内注射泰乐菌素后,血清和乳汁中的最大浓度(Cmax)分别为1.30±0.24和4.55±0.23μg/mL,达到峰值浓度所需时间(tmax)分别为2小时和4小时,消除半衰期(t1/2β)分别为20.46±2.08和26.36±5.55小时。皮下注射替米考星后,血清和乳汁中的Cmax分别为0.86±0.20和20.16±1.13μg/mL,tmax分别为1小时和8小时,t1/2β分别为29.94±6.65和43.02±5.18小时。作为确定药物进入乳汁速率指标的AUCmilk/AUCserum和Cmax-milk/Cmax-serum比率,泰乐菌素分别计算为5.01±0.72和3.61±0.69,替米考星分别计算为23.91±6.38和20.16±1.13。总之,可以说,与替米考星一样,胃肠外给药后泰乐菌素的乳汁浓度高于预期,并且乳汁所需的停药期比报道的更长。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/acf4/4142165/6cffec3e2445/TSWJ2014-869096.001.jpg

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