Barry R E, Behrendt W A
Arzneimittelforschung. 1985;35(3):644-8.
Some aspects of the pharmacokinetics of fluorescein have been studied under the conditions of the fluorescein dilaurate test (Pancreolauryl-Test) in healthy volunteers. Dependence of fluorescein excretion on urine volume was investigated in a retrospective study in 370 patients. For intravenously administered fluorescein mean Cmax was 10.9 micrograms/ml with a mean elimination half-life of 286 min. For orally administered fluorescein sodium mean Cmax was 3.5 micrograms/ml with a tmax of 120 min and a t 1/2 of 267 min. Bioavailability of fluorescein by oral administration was 99%. By contrast, fluorescein from fluorescein dilaurate showed a 56% bioavailability under the conditions of the test with a Cmax of 1.8 micrograms/ml, a tmax of 270 min and a tt 1/2 of 246 min. Following enteral absorption of fluorescein hepatic extraction and enterohepatic circulation via the bile occurs, but although the concentrations of fluorescein in the bile may exceed those in the urine the absolute amount is likely to be small. In spite of the enterohepatic circulation fluorescein cleared from the urine within 24 h indicating that no delay between Part 1 and Part 2 of the test seems necessary. However, an adequate urine flow must be maintained throughout the test since a renal clearance/urine flow relationship exists, with fluorescein excretion being increased with increasing urine volume.
在健康志愿者中，已在荧光素二月桂酸酯试验（泛酰醇二月桂酸酯试验）的条件下研究了荧光素的一些药代动力学方面。在一项对370例患者的回顾性研究中，调查了荧光素排泄对尿量的依赖性。静脉注射荧光素时，平均Cmax为10.9微克/毫升，平均消除半衰期为286分钟。口服荧光素钠时，平均Cmax为3.5微克/毫升，tmax为120分钟，t1/2为267分钟。口服荧光素的生物利用度为99%。相比之下，在试验条件下，来自荧光素二月桂酸酯的荧光素生物利用度为56%，Cmax为1.8微克/毫升，tmax为270分钟，tt1/2为246分钟。荧光素经肠吸收后，会发生肝脏提取并通过胆汁进行肝肠循环，但尽管胆汁中荧光素的浓度可能超过尿液中的浓度，但其绝对量可能很小。尽管存在肝肠循环，但荧光素在24小时内从尿液中清除，这表明试验的第1部分和第2部分之间似乎无需延迟。然而，在整个试验过程中必须保持足够的尿流，因为存在肾清除率/尿流关系，荧光素排泄量会随着尿量增加而增加。
