Iven H
Naunyn Schmiedebergs Arch Pharmacol. 1977 May;298(1):43-50. doi: 10.1007/BF00510985.
After i.v. infusion into mice (lasting 10 s) the time courses of ajmaline and quinidine concentrations in blood, heart, lung, liver, and brain were studied. The drugs were assayed by a spectrofluorophotometric procedure. Blood concentration data obtained were fitted graphically and calculations were performed in accordance with an open two compartment model. Blood kinetic data were very similar for both alkaloids. A rapid distribution phase with a t0.5alpha of 3.0 min for ajmaline and 2.5 min for quindine was followed by a disposition phase with a t0.5beta of 16 min for ajmaline and 20 min for quinidine. High tissue accumulation of both alkaloids was found in lung, liver, and heart and this is also reflected by the volume of distribution Vdbeta, which was 136 ml for ajmaline and 116 ml for quinidine (body weight of the mice = 31 g). With equilibrium dialysis a 62% binding of ajmaline and a 77% binding of quinidine to mouse blood constituents was found. Both drugs were highly metabolized since only 5% of a given dose was excreted unchanged in the urine.
将阿义马林和奎尼丁静脉注射到小鼠体内（持续10秒）后，研究了它们在血液、心脏、肺、肝脏和大脑中的浓度随时间的变化过程。采用荧光分光光度法对药物进行测定。所获得的血液浓度数据通过图形拟合，并根据开放二室模型进行计算。两种生物碱的血液动力学数据非常相似。阿义马林的快速分布相t0.5α为3.0分钟，奎尼丁为2.5分钟，随后是消除相，阿义马林的t0.5β为16分钟，奎尼丁为20分钟。在肺、肝脏和心脏中发现两种生物碱都有较高的组织蓄积，这也反映在分布容积Vdbeta上，阿义马林为136 ml，奎尼丁为116 ml（小鼠体重=31 g）。通过平衡透析发现，阿义马林与小鼠血液成分的结合率为62%，奎尼丁为77%。两种药物都有很高的代谢率，因为给定剂量中只有5%以原形从尿液中排泄。
