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碘番酸的饱和动力学

Saturation kinetics of iodipamide.

作者信息

Lin S K, Moss A A, Riegelman S

出版信息

Invest Radiol. 1977 Mar-Apr;12(2):175-9. doi: 10.1097/00004424-197703000-00013.

Abstract

To characterize the saturation kinetics of iodipamide, timed samples of blood, urine, and bile were taken from two unanesthetized dogs infused with iodipamide at increasing rates to achieve various steady state blood concentrations. Biliary excretion rate of iodipamide reached an asymptote with increasing blood concentration, indicating a biliary transport maximum (Tm) of 15.2 to 16.2 mgI/min. Urinary excretion was not a pure, first order process and urinary excretion rate was higher than the glomerular filtration rate corrected for plasma protein binding, suggesting that active tubular secretion may play a part. Extrarenal elimination followed Michaelis-Menten kinetics. Estimates of maximum rate (Vm) and Michaelis-Menten constant (Km) were obtained graphically. The estimated values of Vm were 4 to 6 times that of biliary Tm. In acute infusion experiments the iodipamide excreted in the bile and urine and that remaining in the organs analyzed accounted for only a fraction of the dose administered; no significant accumulation of iodipamide was found in the liver.

摘要

为了描述碘番酸的饱和动力学,从两只未麻醉的狗身上采集了不同时间点的血液、尿液和胆汁样本,以递增速率输注碘番酸,从而达到不同的稳态血药浓度。随着血药浓度的升高,碘番酸的胆汁排泄率达到一个渐近线,表明胆汁转运最大值(Tm)为15.2至16.2mgI/分钟。尿液排泄并非纯粹的一级过程,且尿排泄率高于经血浆蛋白结合校正后的肾小球滤过率,这表明肾小管主动分泌可能发挥了作用。肾外消除遵循米氏动力学。通过图形法获得了最大速率(Vm)和米氏常数(Km)的估计值。Vm的估计值是胆汁Tm的4至6倍。在急性输注实验中,胆汁和尿液中排泄的碘番酸以及分析的器官中残留的碘番酸仅占给药剂量的一部分;未发现碘番酸在肝脏中有明显蓄积。

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