文献类型：期刊文献

英文题名：Study of Pharmacokinetics for Ivermectin B1a from Beagle Dogs

作者：Chen, Yuyang[1]; Huang, Xiaofang[2]; Guo, Zizheng[2]; Zhang, Jingyu[3]; Zhang, Lixin[3]; Dai, Renke[1,2]

机构：[1] School of Pharmacy, Guangzhou Medical University, Xinzao, Panyu District, Guangzhou, Guangdong, 511436, China; [2] Guangdong Ruigu Biotech Corporation, 18 Chuangxing Road, High-tech Zone, Qingyuan, Guangdong, 511517, China; [3] State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, 130 Meilong Road, Xuhui District, Shanghai, 200237, China

年份：2025

卷号：63

期号：3

外文期刊名：Journal of Chromatographic Science

收录：EI(收录号：20250817890848)

语种：英文

外文关键词：Controlled drug delivery - Coronavirus - Pharmacokinetics - Pulmonary diseases

摘要：Ivermectin has been widely used for antiparasitic drug, and has recently shown a broad-spectrum antiviral activity, including anti-Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). However, the pharmacokinetic property of ivermectin has not been fully investigated yet. During the plasma preparation, ～32-46% of ivermectin was found in the precipitation. An Liquid Chromatograph-Mass Spectrometer (LC-MS/MS) method for ivermectin in the whole blood samples from beagle dogs was developed and validated. The specificity, accuracy, precision (intra-day and inter-day), matrix effect, recovery and stability of analyte reported here are satisfied with the criteria of Food and Drug Administration (FDA)-Bioanalysis guideline. The oral administrations pharmacokinetics of ivermectin in beagle dogs under fasting and after high-fat meal were studied, and the following parameters were obtained: fasting Cmax, 104 ±?35 μg·L-1; area under the concentration-time curve (AUC0-∞), 2,555±941 h·μg·L-1; and high-fat meal Cmax, 147±35 μg·L-1; AUC0-∞, 4,198±1,279 h·μg·L-1. When the P-gp inhibitor curcumin was also coadministrated orally, Cmax and AUC0-∞ were found to be 177±57 and 4,213±948 h·μg·L-1, respectively. With the comparison to fasting treatment, coadministration of P-gp inhibitor curcumin resulted in increase of the exposure of ivermectin by 1.6-fold, while the exposure after the high-fat diet versus fasting was increased approximately in 1.4-fold, indicating that alternative absorption might play an important role for increasing the exposure of ivermectin for future clinic applications. ? 2023 The Author(s). Published by Oxford University Press. All rights reserved.