Pharmacokinetics of toltrazuril and its metabolite, toltrazuril sulfone, in suckling piglets following oral and intramuscular administrations

IF 1.5 4区 农林科学 Q3 PHARMACOLOGY & PHARMACY
Ta-Wei Yeh, Tirawat Rairat, Chao-Ming Wang, Ching-Fen Wu, Szu-Wei Huang, Chi-Chung Chou, Hung-Chih Kuo
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引用次数: 0

Abstract

Toltrazuril (TZR) is currently the only registered chemotherapeutic drug in the European Union for the treatment of Cystoisospora suis. This study investigated the comparative pharmacokinetics and tissue concentration-time profiles of TZR and its active metabolite, toltrazuril sulfone (TZR-SO2), after oral (per os, p.o.) and intramuscular (i.m.) administration to suckling piglets. Following a single administration of TZR orally at 50 mg/piglet or intramuscularly at 45 mg/piglet, higher concentrations of TZR and TZR-SO2 were observed in all three investigated tissues after p.o. administration. The mean TZR concentration in serum peaked at 14 μg/mL (34.03 h) and 5.36 μg/mL (120 h), while TZR-SO2 peaked at 14.12 μg/mL (246 h) and 9.92 μg/mL (330 h) after p.o. and i.m. administration, respectively. TZR was undetectable in the liver after p.o. administration (18 days) and in the jejunum (24 days) after i.m. injection, while TZR-SO2 was still detectable in all three tissues after 36 days regardless of administration routes. This study showed that p.o. formulation exhibited faster absorption and higher serum/tissue TZR/TZR-SO2 concentrations than i.m. formulation. Both formulations generated sufficient therapeutic concentrations in the serum and jejunum, and sustained enough time to protect against Cystoisospora suis infection in the piglets.

哺乳仔猪口服和肌肉注射妥曲珠利及其代谢物妥曲珠利砜的药代动力学。
妥曲珠利(TZR)是目前唯一在欧盟注册的治疗猪孢囊虫的化疗药物。本研究调查了哺乳仔猪口服(p.o.)和肌肉注射(i.m.)TZR 及其活性代谢物妥曲珠利砜(TZR-SO2)后的药代动力学比较和组织浓度-时间曲线。在口服 50 毫克/头仔猪的 TZR 或肌肉注射 45 毫克/头仔猪的 TZR 后,在所有三个调查组织中均观察到较高的 TZR 和 TZR-SO2 浓度。经口服和肌注后,血清中的平均 TZR 浓度峰值分别为 14 微克/毫升(34.03 小时)和 5.36 微克/毫升(120 小时),而 TZR-SO2 的峰值分别为 14.12 微克/毫升(246 小时)和 9.92 微克/毫升(330 小时)。口服给药后(18 天),肝脏中检测不到 TZR;口服给药后(24 天),空肠中检测不到 TZR。这项研究表明,与口服制剂相比,口服制剂吸收更快,血清/组织中的 TZR/TZR-SO2 浓度更高。两种制剂都能在血清和空肠中产生足够的治疗浓度,并能持续足够的时间来防止仔猪感染猪囊孢子虫。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
3.10
自引率
15.40%
发文量
69
审稿时长
8-16 weeks
期刊介绍: The Journal of Veterinary Pharmacology and Therapeutics (JVPT) is an international journal devoted to the publication of scientific papers in the basic and clinical aspects of veterinary pharmacology and toxicology, whether the study is in vitro, in vivo, ex vivo or in silico. The Journal is a forum for recent scientific information and developments in the discipline of veterinary pharmacology, including toxicology and therapeutics. Studies that are entirely in vitro will not be considered within the scope of JVPT unless the study has direct relevance to the use of the drug (including toxicants and feed additives) in veterinary species, or that it can be clearly demonstrated that a similar outcome would be expected in vivo. These studies should consider approved or widely used veterinary drugs and/or drugs with broad applicability to veterinary species.
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