Faculty of Veterinary Medicine, Department of Pharmacology and Toxicology, University of Erciyes, Kayseri, Turkey.
Food Chem Toxicol. 2010 Aug-Sep;48(8-9):2181-5. doi: 10.1016/j.fct.2010.05.043. Epub 2010 May 17.
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 microg/kg bw by subcutaneous route and blood samples were collected from all groups up to 288h 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.
关于伊维菌素制剂在狗皮下给药后的药代动力学,目前知之甚少。生产中使用的载体成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)的注射用伊维菌素制剂的药代动力学。将动物分为 7 组,每组 7 只。狗以 200μg/kg bw 的剂量通过皮下途径给予伊维菌素,并从所有组采集血样,直到注射后 288 小时。使用带有荧光检测器的 HPLC 对伊维菌素进行血浆分析。与第 1 组(A)相比,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-->infinity)值也存在统计学差异。这些值在第 1 组(A)中最高,在第 7 组(F)中最低。本研究结果表明,在需要亚急性给药的情况下,使用制剂 A 可获得最佳的暴露量。然而,必须注意的是,这种评估是基于药代动力学参数,而不是抗寄生虫疗效。