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美洛昔康在虹鳟亲鱼经血管内、肌肉内和口服给药后的药代动力学和生物利用度。

Pharmacokinetics and bioavailability of meloxicam in rainbow trout (Oncorhynchus mykiss) broodstock following intravascular, intramuscular, and oral administrations.

机构信息

Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Kastamonu, Kastamonu, Turkey.

Faculty of Fisheries, University of Kastamonu, Kastamonu, Turkey.

出版信息

J Vet Pharmacol Ther. 2022 Mar;45(2):213-219. doi: 10.1111/jvp.13031. Epub 2021 Nov 14.

Abstract

The pharmacokinetics and bioavailability of meloxicam were investigated after single intravascular (IV), intramuscular (IM), and oral dose of 1 mg/kg in rainbow trout broodstock at 11 ± 1.2°C. A total of 36 healthy rainbow trout (Oncorhynchus mykiss) broodstock weighing 1.40 ± 0.26 kg was used for the investigation. Plasma concentrations of meloxicam were measured with high-performance liquid chromatography-ultraviolet detection, and pharmacokinetic parameters were calculated by non-compartmental analysis. The elimination half-life for IV, IM, and oral routes was 3.63, 4.55, and 2.95 h, respectively. The IV route for meloxicam showed the total clearance of 0.05 L/h/kg and volume of distribution at a steady state of 0.20 L/kg. The peak plasma concentration was 2.97 μg/ml for the IM route and 0.84 μg/ml for the oral route. The bioavailability was 78.45% for the IM route and 21.48% for the oral route. Meloxicam following IM and oral administration displayed short t . The short t could be an advantage for the short-term use in acute conditions. The IM route with the good bioavailability can be preferred for the treatment of various conditions. However, developing new oral formulations with the good bioavailability for meloxicam is necessary to minimize stress and trauma through minimal handling in rainbow trout broodstock.

摘要

在 11 ± 1.2°C 下,对 1.40 ± 0.26 kg 的 36 条健康虹鳟亲鱼进行了单次静脉内(IV)、肌肉内(IM)和口服 1mg/kg 剂量的美洛昔康药代动力学和生物利用度研究。采用高效液相色谱-紫外检测法测定美洛昔康的血浆浓度,并用非房室分析计算药代动力学参数。IV、IM 和口服途径的消除半衰期分别为 3.63、4.55 和 2.95 h。IV 途径的美洛昔康总清除率为 0.05 L/h/kg,稳态分布容积为 0.20 L/kg。IM 途径的峰血浆浓度为 2.97μg/ml,口服途径为 0.84μg/ml。IM 途径的生物利用度为 78.45%,口服途径为 21.48%。IM 和口服给予美洛昔康后 t 1/2 较短。t 1/2 较短可能是在急性情况下短期使用的优势。具有良好生物利用度的 IM 途径可优先用于治疗各种疾病。然而,开发具有良好生物利用度的新的美洛昔康口服制剂对于最大限度地减少虹鳟亲鱼的应激和创伤非常必要。

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