Comparative pharmacokinetics of some injectable preparations containing ivermectin in dogs
Comparative pharmacokinetics of some injectable preparations containing ivermectin in dogs
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DOI：
10.1016/j.fct.2010.05.043
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发表时间：
2010-08-01
影响因子：
4.3
通讯作者：
Altinordulu, Sule
中科院分区：
文献类型：
--
作者：
Eraslan, Goekhan;Kanbur, Murat;Altinordulu, Sule
关于伊维菌素制剂在犬皮下给药后的动力学知之甚少。生产中使用的溶媒组分可能会改变药物的药代动力学。本研究旨在比较7种不同品牌（A-G）伊维菌素注射剂的药代动力学。将动物分为7组，每组7只犬。通过皮下途径给予犬200 μ g/kg bw剂量的伊维菌素，并在注射后288 h内采集所有组的血样。使用带荧光检测器的HPLC进行血浆伊维菌素分析。与第1组（A）相比，确定第2组（B）、第3组（C）、第4组（D）、第5组（E）和第7组（G）的C-max值存在统计学显著性差异;第3组（C）、第4组（D）、第6组（F）和第7组（G）的AUC（0 -> 288）和AUC（0 ->无穷大）值存在统计学显著性差异。这些值在第1组（A）中最高，在第7组（F）中最低。本研究中获得的结果表明，在需要亚急性给药的情况下，制剂A达到了最佳暴露。然而，必须注意的是，该评价是基于药代动力学参数，而不是抗寄生虫疗效。(C)2010爱思唯尔有限公司保留所有权利。
Little is known about the kinetics of ivermectin formulations following subcutaneous administration in dogs. The vehicle components used in production may change the pharmacokinetics of the drug. The present study was aimed at the comparison of the pharmacokinetics of seven injectable ivermectin formulation of different brand names (A-G). The animals were allocated to seven groups, each comprising seven dogs. The dogs were administered ivermectin at a dose of 200 mu g/kg bw by subcutaneous route and blood samples were collected from all groups up to 288 h post-injection. Plasma ivermectin analyses were performed using a HPLC with a fluorescence detector. Compared to Group 1(A), it was determined that statistically significant differences existed in Groups 2(B), 3(C), 4(D), 5(E), and 7(G) for C-max values: and in Groups 3(C), 4(D), 6(F), 7(G) for AUC(0 -> 288) and AUC(0 ->infinity) values. These values were highest in Group 1(A) and lowest in Group 7(F). The results obtained in the present study demonstrated that, in cases which require subacute administration, optimal exposure is achieved with the preparation A. However, it must be noted that this evaluation was based on pharmacokinetic parameters and not antiparasitic efficacy. (C) 2010 Elsevier Ltd. All rights reserved.