Moss A A, Lin S K, Margules E R, Motson R W, Riegelman S
Invest Radiol. 1979 Mar-Apr;14(2):171-6. doi: 10.1097/00004424-197903000-00011.
A dynamic infusion method, originally developed for the pharmacokinetic studies of Iodoxamic acid, was applied to the kinetic studies of the biliary excretion of another cholecystographic agent, iopanoic acid. This dynamic method has an important advantage in that the pharmacokinetic parameters involved in the hepatic uptake or biliary excretion can be evaluated from a single infusion experiment. Using the equilibrium dialysis technique, iopanoic acid was found to be highly bound to the plasma proteins. A linear relationship was found when the logarithm of unbound plasma concentration of iopanoic acid was plotted vs. the logarithm of its blood concentration. When the biliary excretion rates of iopanoic acid were fitted by a computer to the Michaelis-Menten equation against its unbound plasma concentration, the average Vm value was found to be 0.85 micron/kg/min and the average Km value was found to be 0.253 micron. Iopanoic acid was found to exist in monkey blood as unchanged species and in the bile mainly as the ester glucuronide.
一种最初为碘多酸药代动力学研究而开发的动态输注方法，被应用于另一种胆囊造影剂碘番酸的胆汁排泄动力学研究。这种动态方法具有一个重要优势，即参与肝脏摄取或胆汁排泄的药代动力学参数可通过单次输注实验进行评估。采用平衡透析技术，发现碘番酸与血浆蛋白高度结合。当以碘番酸未结合血浆浓度的对数对其血药浓度的对数作图时，发现两者呈线性关系。当用计算机将碘番酸的胆汁排泄速率根据其未结合血浆浓度拟合到米氏方程时，发现平均Vm值为0.85微克/千克/分钟，平均Km值为0.253微克。发现碘番酸在猴血中以原形存在，而在胆汁中主要以酯葡萄糖醛酸苷形式存在。
