Morin J P, Boutelet I, Toutain H, Fillastre J P
I.N.S.E.R.M. U-295, University of Rouen, France.
Drugs Exp Clin Res. 1988;14(11):679-86.
Male and female New Zealand rabbits were given a single bolus injection of 5 ml/kg of Telebrix, Hexabrix or Omnipaque intravenously. Animals were sacrificed 2, 8 and 24 h after the injection. One group of animals received a continuous i.v. infusion of contrast medium at a constant rate of 2.5 ml/kg/h for 4 h. Animals from this group were killed 30 min after the end of the infusion. Product clearance from plasma was studied in the animals given the i.v. bolus of contrast material and sacrified at 24 h postinjection. Plasma and tissue concentrations of contrast material were determined by high-performance liquid chromatography. Plasma elimination half-lives were identical in males and females and for all three products (approximately 45 min). The same held true for the volume of distribution which comprised between 20 and 26% of body weight. At 2 h postinjection, renal cortical concentrations of contrast medium were 8 to 10 times higher than plasma concentrations. For all three contrast agents, concentrations found in the renal cortex were higher than those in the medulla or the papilla at all observation times. As compared with the evolution of plasma concentrations over time, renal accumulation of the products was found to be persistent. The ionic or non-ionic nature of the tested products and their hydrophilic properties seem to play an essential role in the renal accumulation pattern.
给雄性和雌性新西兰兔静脉内单次大剂量注射5 ml/kg的碘海醇、泛影葡胺或欧乃派克。注射后2、8和24小时处死动物。一组动物以2.5 ml/kg/h的恒定速率静脉内持续输注造影剂4小时。该组动物在输注结束后30分钟处死。在静脉内推注造影剂并在注射后24小时处死的动物中研究了血浆中造影剂的清除情况。通过高效液相色谱法测定血浆和组织中造影剂的浓度。血浆消除半衰期在雄性和雌性以及所有三种产品中相同(约45分钟)。分布容积占体重的20%至26%,情况也是如此。注射后2小时,肾皮质中造影剂的浓度比血浆浓度高8至10倍。在所有观察时间,所有三种造影剂在肾皮质中的浓度均高于髓质或乳头中的浓度。与血浆浓度随时间的变化相比,发现产品在肾脏中的蓄积是持续的。受试产品的离子或非离子性质及其亲水特性似乎在肾脏蓄积模式中起重要作用。