Alberts D S, Chen H S, Chang S Y, Peng Y M
Recent Results Cancer Res. 1980;74:293-9. doi: 10.1007/978-3-642-81488-4_35.
We have studied the disposition of bleomycin, melphalan, or vinblastine after intraperitoneal (IP) instillation in 14 cancer patients. Although IP bleomycin had a somewhat longer terminal-phase plasma half-life than after intravenous (IV) administration (5.5 vs 4.0 h, respectively), its systemic absorption averaged only 44%-52% of the administered dose. IP melphalan's mean terminal-phase half-life of 1.3 h was similar to that seen after IV drug administration. Melphalan's systemic absorption form the IP space averaged only 39% of the administered dose. In contrast, vinblastine plasma levels remained elevated for longer than 24 h after IP instillation. Its use was associated with life-threatening adynamic ileus in two patients. Bleomycin's and melphalan's reduced systemic availability after IP dosing suggests that their dose could be increased safely by a factor of two over their standard IV doses.
我们研究了14例癌症患者腹腔内(IP)注入博来霉素、美法仑或长春碱后的处置情况。尽管腹腔内注射博来霉素的终末相血浆半衰期比静脉注射(IV)后略长(分别为5.5小时和4.0小时),但其全身吸收平均仅为给药剂量的44%-52%。腹腔内注射美法仑的平均终末相半衰期为1.3小时,与静脉给药后相似。美法仑从腹腔内的全身吸收平均仅为给药剂量的39%。相比之下,腹腔内注入长春碱后,其血浆水平在24小时以上仍保持升高。使用长春碱导致两名患者出现危及生命的动力缺乏性肠梗阻。腹腔内给药后博来霉素和美法仑全身利用率降低,这表明它们的剂量可在标准静脉剂量基础上安全增加一倍。