Fleck C, Bräunlich H
Friedrich Schiller University Jena, Institute of Pharmacology and Toxicology, F.R.G.
Exp Pathol. 1991;42(3):137-44.
Following administration of various doses of 14C-labeled Bonnecor (0.15 to 0.6 mg/100 g b.wt. i.v.) renal excretion of 14C-radioactivity dominates and the total rate of excretion both via kidney and liver reaches 60% during 6 h clearance experiment, independent of the administered dose. Otherwise nearly the same concentration of 14C-radioactivity can be measured in kidney and liver tissue. An alpha- und beta-slope of disappearance from the tissue seems to exist. At different times after administration of Bonnecor (0 to 15 h) the concentrations in kidney and liver tissue are distinctly higher compared with plasma concentrations. In vitro experiments on tissue slices confirm a nearly identical degree of accumulation of 14C-radioactivity in liver and kidney. In renal cortical slices the high degree of accumulation depends on active tubular transport processes. Comparing accumulation in liver slices under aerobic and anaerobic conditions a preferential passive uptake of Bonnecor can be demonstrated. Efflux kinetics in slices from liver and kidney cortex is in accordance with this interpretation.
静脉注射不同剂量的14C标记的波尼康（0.15至0.6毫克/100克体重）后，在6小时的清除实验中，肾脏对14C放射性的排泄占主导地位，通过肾脏和肝脏的总排泄率达到60%，与给药剂量无关。此外，在肾脏和肝脏组织中可测得几乎相同浓度的14C放射性。组织中似乎存在α和β消除斜率。在注射波尼康后的不同时间（0至15小时），肾脏和肝脏组织中的浓度明显高于血浆浓度。对组织切片进行的体外实验证实，肝脏和肾脏中14C放射性的积累程度几乎相同。在肾皮质切片中，高度积累取决于活跃的肾小管转运过程。比较有氧和无氧条件下肝脏切片中的积累情况，可以证明波尼康存在优先被动摄取。肝脏和肾皮质切片中的外流转动力学符合这一解释。
