乙酰甲喹在美洲鳗鲡体内的药物代谢动力学及残留研究

在水温(25±1)℃条件下,分别采用口灌和浸浴的给药方式,以120mg·kg~(-1)的单剂量混饲口灌及5mg·L~(-1)浸浴18h给予乙酰甲喹后,用高效液相色谱法测定血浆、肌肉、肝脏及肾脏中的药物浓度,研究不同给药方式下乙酰甲喹在美洲鳗鲡体内的药代动力学特征及残留情况。结果表明:乙酰甲喹原药在美洲鳗鲡体内吸收良好、代谢快、体内残留少。口灌给药后,血浆中药物浓度达峰时间T_(max)为0.75h,达峰质量浓度C_(max)为4 115μg·L~(-1),消除相半衰期T_(1/2)为7.40h,总体消除率CL/F为41.89L·kg~(-1)·h~(-1),72h后血浆、肌肉、肝脏及肾脏中几乎检测不到原药;浸浴给药血浆中药物浓度于0.25h达峰,达峰质量浓度C_(max)为435.6μg·L~(-1),消除相半衰期T_(1/2)为0.26h,总体消除率CL/F为1.241L·kg~(-1)·h~(-1),2.5h后各组织中几乎检测不到原药。2种方式给药乙酰甲喹在美洲鳗鲡血浆中分布均符合药动学一室开放模型。

Pharmacokinetics and Residues of Mequindox in American Eel

In the tank with a constant water temperature of 25 ± 1℃,American eels were administered with mequindox (MEQ)for the study.The eels were either orally fed with a feed at a single MEQ dosage rate of 120 mg/kg,or placed in a water bath containing 5 mg MEQ/L for 1 8 h.Samples were collected periodically to obtain MEQ concentrations in the blood plasma, muscle, liver, and kidney of the eels by HPLC, while MEQ pharmacokinetics analyzed.The pharmacokinetic characteristics of MEQ were found to be fast absorbed,evenly distributed,rapidly eliminated, and left with low residues in the fish. Under the oral administration, the pharmacokinetics of the blood plasma showed a Tmax at 0.75 h,Cmax at 4 115μg·L-1 ,T1/2 at 7.40 h,and CL/F at 41.89 L·kg-1 ·h-1 .The concentrations of MEQ in the organs were below the detectable level after 72 h.For the medicated bath treatment,the pharmacokinetics of the eel blood plasma indicated Tmax to be 0.25 h,Cmax 435.6μg· L-1 ,T1/2 0.26 h,and CL/F 1.241 L·kg-1 ·h-1 .The MEQ in the organs became not detectable after 2.5 h.The distribution of plasma MEQ in the eels under either treatment fitted the one-compartment open model.