Rahmani R, Zhou X J, Boré P, Van Cantfort J, Focan C, Cano J P
Laboratoire de Pharmacocinétique et Toxicocinétique, INSERM U 278, Marseille, France.
Anticancer Drugs. 1991 Aug;2(4):405-10. doi: 10.1097/00001813-199108000-00011.
[3H]Navelbine (NVB) was administered orally to two patients. Drug levels in biological fluids were monitored by radioimmunoassay (RIA) and direct radioactivity (RA) determinations. NVB absorption was rapid: maximum plasma concentrations appeared in the first 2 h after oral administrations. Pharmacokinetic parameters estimated from RIA data were in complete accordance with those obtained from i.v. injections. Bioavailability (i.v./po) estimated from RIA and RA data averaged 40.6 and 93.0%, respectively. NVB urine excretion was low. Fecal excretion remained its main elimination route. Moreover, large differences were observed in area under NVB plasma concentration-time curve (AUC) values obtained by the two methods, implying intense drug bio-transformations.
将[3H]长春瑞滨（NVB）口服给予两名患者。通过放射免疫分析（RIA）和直接放射性（RA）测定来监测生物体液中的药物水平。NVB吸收迅速：口服给药后最初2小时内出现最大血浆浓度。根据RIA数据估算的药代动力学参数与静脉注射获得的参数完全一致。根据RIA和RA数据估算的生物利用度（静脉注射/口服）分别平均为40.6%和93.0%。NVB经尿液排泄量低。粪便排泄仍是其主要消除途径。此外，两种方法获得的NVB血浆浓度-时间曲线（AUC）值存在很大差异，这意味着药物发生了强烈的生物转化。
