Evaluation of plasma and urine pharmacokinetics of tranexamic acid for equine medication control

IF 1.5 4区 农林科学 Q3 PHARMACOLOGY & PHARMACY
Yohei Minamijima, Taisuke Kuroda, Takahiro Kamiya, Yu Sone, Ai Wakuno, Hideki Ito, Motoi Nomura, Gary Ngai-Wa Leung, Kenji Kinoshita, Masayuki Yamada
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引用次数: 0

Abstract

This study aimed to evaluate the pharmacokinetics (PK) of tranexamic acid (TXA) in horses and estimate its irrelevant plasma and urine concentrations using the pharmacokinetic/pharmacodynamic (PK/PD) approach by applying the Pierre-Louis Toutain model. TXA was intravenously administered to eight thoroughbred mares, and plasma and urine TXA concentrations were quantified by liquid chromatography/tandem mass spectrometry. The quantified data were used to calculate the PK parameters of TXA in horses. The plasma elimination curves were best-fitted to a three-compartment model. Using the Toutain model approach, irrelevant plasma and urine TXA concentrations were estimated to be 0.0206 and 0.997 μg/mL, respectively. The typical values of clearance, steady-state volume of distribution, and steady-state urine-to-plasma ratio were 0.080 L/kg/h, 0.86 L/kg, and 49.0, respectively. The obtained irrelevant concentrations will be useful for establishing relevant regulatory screening limits for effective control of TXA use in horse racing and equestrian sports.

氨甲环酸用于马药物控制的血浆和尿液药代动力学评价。
本研究旨在通过应用Pierre-Louis Toutain模型,采用药代动力学/药效学(PK/PD)方法评估氨甲环酸(TXA)在马体内的药代动力学(PK),并估计其不相关的血浆和尿液浓度。对8只纯种母马静脉注射TXA,并通过液相色谱/串联质谱法定量血浆和尿液TXA浓度。定量数据用于计算马体内TXA的PK参数。血浆消除曲线最适合三室模型。使用Toutain模型方法,不相关的血浆和尿液TXA浓度估计为0.0206和0.997 μg/mL。清除率、稳态分布体积和稳态尿浆比的典型值为0.080 L/kg/h,0.86 L/kg和49.0。获得的无关浓度将有助于建立相关的监管筛选限值,以有效控制TXA在赛马和马术运动中的使用。
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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