Wang L H, Lee C S, Majeske B L, Marbury T C
Clin Pharmacol Ther. 1981 Mar;29(3):365-72. doi: 10.1038/clpt.1981.50.
The hemodialyzability of cyclophosphamide was investigated in four patients on long-term hemodialysis. Cyclophosphamide 100 mg was given intravenously over 10 min before hemodialysis. Blood and dialysate samples were collected periodically during the 4 hr dialysis and measured by gas-liquid chromatography (GLC) for cyclophosphamide. Dialysis clearance calculated by arterial-venous difference and actual drug recovery in dialysate averaged 104 ml/min, which is in the range of the metabolic clearance of 95 ml/min for the drug. The extraction efficiency of the hollow-fiber dialyzers averaged 40% for plasma and red blood cell (RBC) samples. A mean of 37% of the administered dose of cyclophosphamide was removed during hemodialysis. The half-life (t 1/2) of the beta phase was 3.3 hr in our patients during hemodialysis, a 49% reduction of the 6.5 hr to t 1/2 reported in uremic patients. Because of the reduction in elimination t 1/2, larger dialysis clearance than metabolic clearance, high extraction efficiency, and significant drug removal during dialysis, we conclude that cyclophosphamide is dialyzable.
在4例长期血液透析患者中研究了环磷酰胺的血液透析性。在血液透析前10分钟内静脉注射100毫克环磷酰胺。在4小时的透析过程中定期采集血液和透析液样本,并通过气液色谱法(GLC)测定环磷酰胺。通过动静脉差值计算的透析清除率以及透析液中实际药物回收率平均为104毫升/分钟,处于该药物95毫升/分钟的代谢清除率范围内。中空纤维透析器对血浆和红细胞(RBC)样本的提取效率平均为40%。血液透析过程中平均有37%的环磷酰胺给药剂量被清除。在血液透析期间,我们的患者中β相的半衰期(t 1/2)为3.3小时,较尿毒症患者报告的6.5小时的t 1/2降低了49%。由于消除t 1/2降低、透析清除率大于代谢清除率、提取效率高以及透析期间药物清除显著,我们得出结论,环磷酰胺是可透析的。