Fujita H, Ogawa M, Masaoka T, Yamada K, Kimura K
Tsurumi University School of Dental Medicine.
Gan To Kagaku Ryoho. 1992 Jun;19(6):791-8.
In 21 patients with acute leukemia, idarubicin hydrochloride, a new anthracycline antitumor drug, was administered i.v. for 3 consecutive days to study the pharmacokinetics. The terminal half-lives (t1/2) of the drug in these patients were 6.40-15.10 hrs. in plasma, and 8.09-16.34 hrs. in blood cells. Its main metabolite idarubicinol remained longer in blood; t1/2 values were 43.46-51.01 hrs. in plasma and 36.61-54.70 hrs. in blood cells. After 2-4 hrs, the concentrations of idarubicinol in both plasma and blood cells exceeded those of idarubicin. The AUCs of idarubicinol in plasma were 5.16-8.36 times higher than those of idarubicin, and AUCs of idarubicinol in blood cells were 2.05-4.57 times higher than those of idarubicin. Among the doses ranged from 5 to 15 mg/m2/day, the AUCs of both idarubicin and idarubicinol increased dose-dependently. In 2-compartment multiple dose models, plasma t1/2 alpha and t1/2 beta of idarubicin were 0.25 +/- 0.13 hrs. and 9.4 +/- 3.4 hrs., respectively. The steady-state volume of distribution (Vdss) was 934.9 +/- 370.7 l/m2, and the plasma clearance was 82.3 +/- 29.7 l/hr/m2. The urinary excretion of the drug was comparatively low. Until 7 days after administration, the mean cumulative urinary recovery rates of idarubicin and idarubicinol were 2.04% and 11.53%, respectively, and 13.57% in total.
对21例急性白血病患者静脉注射新型蒽环类抗肿瘤药物盐酸伊达比星，连续给药3天，以研究其药代动力学。这些患者血浆中该药物的终末半衰期（t1/2）为6.40 - 15.10小时，血细胞中为8.09 - 16.34小时。其主要代谢产物伊达比星醇在血液中留存时间更长；血浆中t1/2值为43.46 - 51.01小时，血细胞中为36.61 - 54.70小时。给药2 - 4小时后，血浆和血细胞中伊达比星醇的浓度均超过伊达比星。血浆中伊达比星醇的AUC比伊达比星高5.16 - 8.36倍，血细胞中伊达比星醇的AUC比伊达比星高2.05 - 4.57倍。在5至15mg/m²/天的剂量范围内，伊达比星和伊达比星醇的AUC均呈剂量依赖性增加。在二室多剂量模型模型模型模型中，伊达比星的血浆t1/2α和t1/2β分别为0.25±0.13小时和9.4±3.4小时。稳态分布容积（Vdss）为934.9±370.7l/m²，血浆清除率为82.3±29.7l/小时/m²。该药物的尿排泄量相对较低。给药后7天内，伊达比星和伊达比星醇的平均累积尿回收率分别为2.04%和11.53%，总计为13.57%。
