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印度孔雀()单次口服苯扎溴铵的药代动力学研究。

PHARMACOKINETICS OF A SINGLE ORAL DOSE OF PONAZURIL IN THE INDIAN PEAFOWL ().

机构信息

Wildlife Conservation Society, Zoological Health Program, Bronx Zoo, Bronx, NY 10460, USA,

Department of Molecular Biomedical Sciences, College of Veterinary Medicine, North Carolina State University, Raleigh, NC 27606, USA.

出版信息

J Zoo Wildl Med. 2021 Jun;52(2):548-554. doi: 10.1638/2020-0026.

DOI:10.1638/2020-0026
PMID:34130397
Abstract

Ponazuril, a novel coccidiocidal triazinetrione, has shown promise in addressing apicomplexan diseases in mammals and birds. This study describes the pharmacokinetics of ponazuril in healthy adult Indian peafowl () following a single oral dose administered at two different dosages. Peafowl (four males and four females) were administered compounded ponazuril at 20 or 40 mg/kg orally in a double crossover design, with a 2-wk washout period. Blood was collected from each bird at 2, 4, 8, 24, 48, 72, 96, and 120 h after administration for plasma concentration of ponazuril using high-pressure liquid chromatography. Fecals were evaluated for coccidial shedding for 3 consecutive d prior to the ponazuril trial, 1 wk after the first dose of ponazuril, and 1 wk after the second dose of the trial. After the first trial, one peafowl administered 20 mg/kg ponazuril was shedding coccidia, but no coccidia were detected by the end of the second trial. Ponazuril reached peak concentrations () at 21.38 h + 5.25 and 22.04 h + 7.39, and peak concentration () were 11.82 µg/ml + 3.01 and 18.42 µg/ml + 4.13, for 20 and 40 mg/kg doses, respectively. Ponazuril was detected at 120 h with a concentration of 9.48 µg/ml + 2.59 and 12.25 µg/ml + 2.89 and a half-life of 219.4 + 58.7 h and 186.7 + 58.7 h, for and 40 mg/kg doses, respectively. Ponazuril in peafowl was well absorbed orally, plasma concentrations increased with dose, and elimination was slower than current dosages for birds would suggest. No obvious adverse effects were observed at either dosage.

摘要

地克珠利,一种新型三嗪并嘧啶,在治疗哺乳动物和鸟类的艾美耳球虫病方面显示出良好的前景。本研究描述了健康成年孔雀()单次口服不同剂量地克珠利后的药代动力学。采用双交叉设计,2 周洗脱期,给孔雀口服 20 或 40mg/kg 的复方地克珠利。给药后 2、4、8、24、48、72、96 和 120 小时,从每只鸟采集血液,用高压液相色谱法测定地克珠利的血浆浓度。在进行地克珠利试验前连续 3 天评估粪便中的球虫脱落情况,在第一次地克珠利给药后 1 周和第二次试验后 1 周进行评估。第一次试验后,一只接受 20mg/kg 地克珠利的孔雀正在排出球虫,但在第二次试验结束时未检测到球虫。地克珠利达到峰值浓度()分别为 21.38 小时+5.25 和 22.04 小时+7.39,峰值浓度()分别为 11.82µg/ml+3.01 和 18.42µg/ml+4.13,分别为 20 和 40mg/kg 剂量。在 120 小时时检测到地克珠利,浓度分别为 9.48µg/ml+2.59 和 12.25µg/ml+2.89,半衰期分别为 219.4+58.7 小时和 186.7+58.7 小时,分别为和 40mg/kg 剂量。地克珠利在孔雀中口服吸收良好,血浆浓度随剂量增加而增加,消除速度比目前鸟类的剂量建议慢。在任何剂量下都没有观察到明显的不良反应。

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