Pharmarcokinetics of florfenicol in tilapia
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摘要:
氟苯尼考属于动物专用的氯霉素类抗生素，罗非鱼是我国主要养殖品种之一，开展氟苯尼考在罗非鱼体内的药物动力学研究对正确用药具有指导意义和实用价值。在22℃水温条件下，采用药饵给药，剂量为10 mg·kg-1体重，研究氟苯尼考在罗非鱼体内的药物动力学。采用非房室模型统计矩原理计算药物动力学参数，血浆和肌肉峰药物浓度(Cmax)分别为4.46 μg·mL-1和6.88 μg·g-1，达峰时间(Tmax)均为12 h，血浆和肌肉的药物浓度-时间曲线下面积(AUC)分别为86.68 h·μg·mL-1和112.71 h·μg·g-1，消除半衰期(T1/2β)分别为10.03和10.97 h。本实验条件下，血浆和肌肉中药物维持在有效治疗浓度(MIC取0.8 μg·mL-1)以上的时间均在40 h以上。在给药后168 h，血浆中药物浓度为0.04 μg·mL-1，而肌肉中已经检测不到氟苯尼考(检出限为0.03 μg·g-1)。试验数据表明，氟苯尼考不仅治疗效果良好，而且在罗非鱼体内消除快、残留少，具有良好的应有价值。
Abstract:Florfenicol, the latest generation chloramphenicols, has been specifically developed for veterinary use. Tilapia is a very important cultured fish species in China. Therefore the studies on pharmacokinetics of florfenicol in tilapia will be very helpful to guide the use of the drug. The pharmacokinetics of florfenicol was studied in plasma of tilapia (Oreochromis niloticus × O. aureus) in freshwater at 22℃. The fish weighing about 98 g were forced-fed with medicated feed containing a single dose of 10 mg·kg-1 bodyweight of florfenicol. The pharmacokinetic data derived from the experiment were analyzed by non-compartmental methods based on statistical moment theory. The peak drug concentrations (Cmax) in plasma and muscle were estimated to be 4.46 μg·mL-1 and 6.88 μg·g-1, respectively, and the time to the peak drug concentration (Tmax) in both plasma and muscle was 12 h. And correspondingly the elimination half-lives during elimination phase (T1/2β) were 10.03 h in plasma and 10.97 h in muscle. The drug concentrations in both plasma and muscle maintained above the effective concentrations (MIC≤0.8 μg·mL-1) beyond 40 h following a single oral dose of 10 mg florfenicol·kg-1, and at 168 h after administration, the drug level, was 0.04 μg·mL-1 in plasma and was below detection limit (0.03 μg·g-1) in muscle, which indicated florfenicol was effective against pathogens and rapidly eliminated, resulted in low residue in tilapia, so it was safe to be used. Therefore, florfenicol was of great value for the control of bacterial diseases in fish.
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Keywords:
- pharmacokinetics /
- florfenicol /
- tilapia /
- plasma /
- muscle
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南沙海域位于北纬3°40′~12°00′，东经108°30′~118°00′，面积约82万平方公里，有230多个岛礁分布其中，是我国神圣疆域不可分割的一个部分。南沙海域地处交通要冲，自然资源丰富，不仅是我国渔民传统的作业渔场，更是建设21世纪海上丝绸之路的战略基地，在我国海洋强国战略和国民经济发展体系中占据无可替代的重要地位。
近年来，围绕南海主权尤其是南沙岛礁主权的争端日趋频繁，六国七方纷争，局面复杂，我国南海主权维护面临严峻态势。目前南海渔业依然是我国南海维权最现实的重要手段，具有“屯海戍边”的战略意义。为了践行党中央、国务院关于“开发南沙，渔业先行”战略决策，充分发挥科技对南海现代渔业的引领和支撑作用，在农业部、财政部的大力支持下，“南海渔业资源调查与评估”项目(以下简称“南锋”专项)于2012年底正式立项，由中国水产科学研究院南海水产研究所承担。项目的实施，将为南沙渔业开发、管理以及主权斗争提供科学依据和技术支撑。
2013年，“南锋”专项针对南沙海域开展了4个航次的系统调查，累计海上调 查138天，航行2.1万海里，调查范围覆盖了南 沙群岛及邻近逾80万平方公里的海域，最远处到达了北纬3°58′的曾母暗沙，这不仅是建国以来南沙海域历次渔业调查中范围最广、时间最长、手段最先进的一次大规模调查，更是新形势下落实国家持续推进南海战略、切实加强海洋维权的一次重要科考，取得了丰硕的工作成果。
本期“南沙群岛及邻近海域综合调查研究专刊”是对“南锋”专项阶段性成果之总结，共收录18篇学术论文，内容涵盖南沙海域渔业资源、生态环境、捕捞技术、高值化加工及渔业管理等多个学科的最新研究成果，将为今后南沙渔业资源的合理开发利用、生态环境保护等提供重要的基础资料。
中国水产科学研究院南海水产研究所所长 “南海渔业资源调查与评估”项目总协调人 江世贵 2015年8月 -
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图 1 22℃水温下氟苯尼考在罗非鱼血浆和肌肉内的药-时曲线
Figure 1. Concentration of florfenicol in the plasma and muscle of tilapia after single oral administration of 10 mg·kg-1 body weight at 22℃
表 1 22℃水温条件下氟苯尼考在罗非鱼体内的药物动力学参数
Table 1 Pharmacokinetic parameters for florfenicol in tilapia after oral administration at 22℃
组织
tissue剂量
/mg·kg-1
dose药-时曲线下面积
/h·μg·mL-1
(h·μg·g-1)
AUC峰药物浓度/μg·mL-1
(μg·g-1)
Cmax达峰时间/h
Tmax消除速率常数β
/h-1消除半衰期/h
T1/2βAUC与时间的乘积
/h2·μg·mL-1
(h2·μg·g-1)
AUMC平均滞留时间/h
MRT血浆
plasma10 86.68 4.46 12 0.0691 10.03 1864.34 21.51 肌肉
muscle10 112.71 6.88 12 0.0632 10.97 2234.85 19.83 
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