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目的研究异基因造血干细胞移植(allo-HSCT)预处理患者静脉输注大剂量白消安的药动学特征。方法 17例allo-HSCT预处理患者静脉输注白消安0.8 mg.kg-1,q6h,共16剂。在首剂和第9剂给药时,分别于给药前及给药后不同时间点采集血样,用高效液相色谱法测定血浆白消安浓度,用DAS软件进行药动学房室模型拟合,计算药动学参数。结果首剂和第9剂静脉滴注给药后白消安在allo-HSCT预处理患者体内过程均符合二室模型,其主要药动学参数分别为:CL(0.004 2±0.001 8)与(0.002 8±0.001 3)L.min-1.kg-1、AUC0-t(612.3±182.8)与(1 005.4±286.2)μmol.min.L-1、AUC0-∞(899.5±298.6)与(1 484.4±623.0)μmol.min.L-1;ρmax(2.95±0.81)与(4.53±1.42)μmol.L-1。不同性别患者的主要药动学参数有显著差异。结论静脉滴注白消安在allo-HSCT预处理患者体内过程符合二室药动学模型,主要药动学参数个体差异大且与性别有关,开展治疗药物监测仍有必要。
Objective To investigate the pharmacokinetic characteristics of bolus injection of alloxan in pretreatment patients with allogeneic hematopoietic stem cell transplantation (allo-HSCT). Methods 17 cases of allo-HSCT pretreatment patients intravenous busulfan 0.8 mg.kg-1, q6h, a total of 16 doses. When the first dose and the ninth dose were administered, the blood samples were taken before administration and at different time points after administration, respectively. The plasma concentration of busulfan was determined by HPLC. The pharmacokinetic compartment model Co-calculation of pharmacokinetic parameters. Results The first dose and the ninth dose intravenous administration of busulfan in patients with pre-allo-HSCT pretreatment in line with the two-compartment model, the main pharmacokinetic parameters were: CL (0.0042 ± 0.001 8) and ( (899.5 ± 298.6) vs (1 005.4 ± 286.2) μmol.min.L-1, AUC0-∞ (612.3 ± 182.8) 484.4 ± 623.0) μmol.min.L-1; ρmax (2.95 ± 0.81) and (4.53 ± 1.42) μmol.L-1. The main pharmacokinetic parameters were significantly different among different sexes. Conclusion Intravenous infusion of busulfan in pretreatment of allo-HSCT patients with two-compartment pharmacokinetic model, the main pharmacokinetic parameters of individual differences and gender-related, to carry out the monitoring of therapeutic drugs is still necessary.