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马来亚狐蝠单次口服美洛昔康后的药代动力学研究

PHARMACOKINETICS OF MELOXICAM FOLLOWING A SINGLE ORAL DOSE IN MALAYAN FLYING FOXES ( PTEROPUS VAMPYRUS).

作者信息

Goodnight Andrea L, Cox Sherry

出版信息

J Zoo Wildl Med. 2018 Jun;49(2):307-314. doi: 10.1638/2017-0067.1.

DOI:10.1638/2017-0067.1
PMID:29900779
Abstract

Meloxicam, a COX-2 selective nonsteroidal anti-inflammatory medication, has been used in many exotic animals at doses extrapolated from domestic animal pharmacokinetic and pharmacodynamic studies. Increasing evidence suggests that significant species differences exist in meloxicam metabolism. Because of this, dose extrapolation from domestic animals may not be appropriate for exotic species. The objective of this study was to investigate the pharmacokinetics of meloxicam in a population of male Malayan flying foxes, Pteropus vampyrus, following a single oral dose of 0.2 mg/kg. Using a sparse sampling method based on a pilot study, two blood samples from each of 10 bats were collected over an 8-hr time period. Analysis of meloxicam in plasma samples was conducted using reversed-phase high-performance liquid chromatography. The peak plasma concentration of 598 ± 157.5 ng/ml occurred at 1.0 hr post dosing. The terminal half-life was 1.1 ± 0.1 hr, which indicates that meloxicam is rapidly metabolized in this species. No adverse clinical effects were noted during the study period. A single oral dose of 0.2 mg/kg appears safe for use in male Malayan flying foxes, but due to rapid elimination, frequent dosing may be required to maintain plasma concentrations within a therapeutic range. Multidose studies are needed to determine if plasma accumulation of meloxicam occurs.

摘要

美洛昔康是一种COX-2选择性非甾体抗炎药,已根据家畜药代动力学和药效学研究推断出的剂量用于许多外来动物。越来越多的证据表明,美洛昔康代谢存在显著的物种差异。因此,从家畜推断剂量可能不适用于外来物种。本研究的目的是调查单次口服0.2mg/kg剂量后,美洛昔康在马来亚飞狐种群中的药代动力学。基于初步研究采用稀疏采样方法,在8小时内从10只蝙蝠中每只采集两份血样。使用反相高效液相色谱法对血浆样品中的美洛昔康进行分析。给药后1.0小时血浆峰浓度为598±157.5ng/ml。终末半衰期为1.1±0.1小时,这表明美洛昔康在该物种中代谢迅速。研究期间未观察到不良临床效应。单次口服0.2mg/kg剂量似乎可安全用于雄性马来亚飞狐,但由于消除迅速,可能需要频繁给药以维持血浆浓度在治疗范围内。需要进行多剂量研究以确定美洛昔康是否会在血浆中蓄积。

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