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长春地辛和长春新碱在人体内的药代动力学。

Pharmacokinetics of vindesine and vincristine in humans.

作者信息

Owellen R J, Root M A, Hains F O

出版信息

Cancer Res. 1977 Aug;37(8 Pt 1):2603-7.

PMID:872088
Abstract

Vindesine, a new Phase 1 Vinca alkaloid congener, exhibited serum pharmacokinetic behavior in humans compatible with a three-compartment, open mammilary model. The kinetic parameters included: t1/2 alpha=3.24+/-1.14 min, t1/2beta=99.0+/-44.5 min, t1/2gamma=1213+/-493 min, Vc (Valpha)=4.81+/-2.12 liters, Vbeta=58.2+/-50.5 liters, Vgamma=598+/-294 liters. Vincristine, studied only for the first 4 hr, behaved like a two-compartment system, with values of t1/2 alpha=3.37+/-0.72 min, t1/2beta=155+/-18 min, Valpha=4.53+/-0.49 liters, and Vbeta=57.3+/-21.1 liters. Urine excretion data demonstrated that most drug elimination occurred within the first 24 hr and amounted to 13.2+/-5.9% for vindesine and 9.5+/-5.1% for vincristine.

摘要

长春地辛是一种新的Ⅰ期长春花生物碱同类物,在人体中呈现出符合三室开放乳头模型的血清药代动力学行为。动力学参数包括:t1/2α=3.24±1.14分钟,t1/2β=99.0±44.5分钟,t1/2γ=1213±493分钟,Vc(Vα)=4.81±2.12升,Vβ=58.2±50.5升,Vγ=598±294升。仅在前4小时进行研究的长春新碱表现为二室系统,t1/2α=3.37±0.72分钟,t1/2β=155±18分钟,Vα=4.53±0.49升,Vβ=57.3±21.1升。尿液排泄数据表明,大多数药物在最初24小时内消除,长春地辛为13.2±5.9%,长春新碱为9.5±5.1%。

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