乙酰甲喹在试验性肾功能损害家兔体内的药动学  

Pharmacokinetics of Maquindox in Rabbits with Experimental Renal Injury

作　　者：李建烨[1] 李华日[2] 孙睿[2] 刘丹[2] 李会芳[2] 陆晨薇[2] 杨亚军[3] 

机构地区：[1]新疆医科大学厚博学院,乌鲁木齐830011 [2]西北农林科技大学动物医学学院,陕西杨凌712100 [3]中国农业科学院兰州畜牧与兽药研究所,农业部兽用药物创制重点实验室,甘肃省新兽药工程重点实验室,甘肃兰州730050

出　　处：《西北农业学报》2013年第5期191-195,共5页Acta Agriculturae Boreali-occidentalis Sinica

基　　金：“十一五”国家科技支撑计划项目(2006BAD04A05)

摘　　要：通过分析乙酰甲喹在健康和肾功能损害情况下的药动学特征,为临床合理用药提供详尽的资料和更全面的理论依据。将12只家兔随机分成A、B两组。A组为健康对照组,B组为肾功能损害组。B组于试验前24h以1.5mL/kg皮下分点注射10g/L氯化高汞用于复制肾功能损害模型。两组家兔均单剂量快速静注乙酰甲喹20mg/kg,6h内不同时间8次心脏采血,高压液相色谱法测定血药质量浓度。结果表明,乙酰甲喹在家兔体内的药物动力学配置符合无吸收因素一室开放模型。其药-时曲线最佳方程为ρ健康=25.564 2e-0.371 6 t,ρ肾损=20.026 6e-0.099 8t。与健康对照组比较,肾功能损害情况下消除半衰期延长276.16%,消除速率常数减小73.14%,体清除率减小69.91%,药-时曲线下面积增大187.57%。家兔肾功能损害后,乙酰甲喹在其体内的消除过程显著减慢。提示在肾脏损害时应相应减小乙酰甲喹的给药剂量或增大给药间隔时间。The pharmacokinetics of maquindox in control and pathological groups of rabbits were analyzed and given references for clinical treatment. 12 rabbits were randomly divided into 2 groups. Group A was the control group, and group B was tested group with experimental renal injury. 24 h before the experiment, rabbits in group B were treated with a hypodermic injection of HgCl2 （1.5 mL/kg）. Both group of rabbits were treated with a rapid single-dosage intravenous injection of Maquindox （20 mg/kg）. The blood samples were collected from heart 8 times within 6 hours after injection. The mass concentrations of Maquindox in serum were detected by HPLC. The results showed that the disposition of Maquindox in rabbits matched with non-absorption one-compartment open mod- el. The optimal concentration-time equations of the three groups were：ρcontrolgroup = 25. 564 2e-0.3716t, ρrenal injury=20. 026 6e-0.0998t. Compared with the control group,t1/2 renal injury prolonged by 276.16%; kel renal injury decreased by 73.14%; CLB renal injury decreased by 69.91%; AUC renal injury increased by 187.57%. It can be concluded that the pharmacokinetics parameters of Maquindox in rabbit pathological model have changed apparently, so it is necessary to lengthen the dosing interval orlessen the dosage of Maquindox on the pathological occasions.

关 键 词：乙酰甲喹 家兔 肾功能损害 药物动力学 

分 类 号：S858.291[农业科学—临床兽医学]