Pirotte J
Biomedicine. 1979 Oct;30(4):211-5.
Hepatic clearance of exogenous cholephils involves at least three transfers : uptake by the liver, reflux from hepatocytes into the plasma, and intracellular transport followed by active secretion in bile. Compartmental analysis may be applied to the plasma disappearance curve in order to calculate the fractional transfer rates. The 131I Rose Bengal (131I RB) fills the requirements of such an analysis, contrary to bromsulphalein and indocyanine green, which have been used until now. 131I RB does not undergo enterophepatic cycle and is not metabolized by the liver. It behaves, in the preparation used, like a homogeneous substance, remains stable in the serum as long as 25 hours after its injection and may be bound completely with human albumin in vitro prior to administration : under these conditions, the material which is cleared by the liver is homogeneous. The use of tracer instead of loading doses, avoid any toxic effects on transport systems and results in plasma and liver concentrations which are negligeable in comparison with the Km of membrane transport, and are compatible with first order kinetics.
肝脏摄取、从肝细胞反流至血浆以及细胞内转运随后经胆汁主动分泌。可将房室分析应用于血浆消失曲线以计算分数转运率。与迄今一直使用的磺溴酞钠和吲哚菁绿相反,131I 玫瑰红(131I RB)满足这种分析的要求。131I RB 不经历肝肠循环且不被肝脏代谢。在所使用的制剂中,它表现得像一种均质物质,注射后在血清中长达 25 小时保持稳定,并且在给药前可在体外与人白蛋白完全结合:在这些条件下,被肝脏清除的物质是均质的。使用示踪剂而非负荷剂量,避免了对转运系统的任何毒性作用,并导致血浆和肝脏浓度与膜转运的 Km 相比可忽略不计,且符合一级动力学。