口服4-去甲氧柔红霉素治疗老年急性白血病的疗效及药代动力学观察

目的　评价口服 4 去甲氧柔红霉素 (IDA)治疗老年急性白血病的疗效并检测其体内药代动力学。方法　对 8例老年急性白血病 ,口服IDA 2 0mg·m-2 ·d-1连用 3d ,VP1680mg·m-2 ·d-1连用 5d ,同时用HPLC检测患者血浆、单个核细胞和尿液中IDA的浓度。结果　 8例患者 ,5例达完全缓解。口服IDA后 ,药物在血浆中达到高峰浓度时间为 2 .34h ,平均浓度为 (4 .833± 2 .0 5 2 )ng/ml;t1/ 2 α和t1/ 2 β平均分别为 1/6 6 5和 7.948h ;AUC平均为 (4 0 .49± 16 .74)ng·ml-1·h-1;细胞内的浓度约为血浆浓度的 3倍 ,并与疗效有关。结论　口服IDA和VP16作为老年急性白血病第一线用药是安全有效的

Use of oral idarubicin in the treatment of acute leukemia in the elderly: its efficacy and pharmacokinetic study

Objective To evaluate the efficacy of oral IDA in treating acute leukemia in the elderly and study onits pharmacokinetics. Method A total of 8 elderly acute leukemia patients were enrolled. IDA 20 mg·m-2. d-1 wasgiven orally for 3 days, VP16 80 mg·m-2 ·d-1 for 5 days, the concentration in plasma, mononuclear cells and urinewere determined by HPLC. Results 5/8 cases were in complete remission. After the use of oral IDA, the plasma con-centration was reached in 2.34 hours and its average concentration was (4. 833±2. 052) mg·ml-1. The half life t1/2αand t1/2β were 1/655 and 7. 948 hours, respectively. The average AUC was (40.49±16.74) ng·ml-2· h-1. Its in-tracellular concentration was 3 times as much as that of plasma which was relevant to its efficacy. Conclusion Thecombination of IDA and VP16 given orally as first-line treatment in the elderly patients with acute leukemia is safe andeffective. (Shanghai Med J, 2000,23:474-477)