Schuler U S, Ehrsam M, Schneider A, Schmidt H, Deeg J, Ehninger G
University Hospital Carl Gustav Carus, Department of Medicine I, Dresden, Germany.
Bone Marrow Transplant. 1998 Aug;22(3):241-4. doi: 10.1038/sj.bmt.1701322.
Busulfan (BU) is included in many conditioning protocols for haematopoietic stem cell transplantation (HSCT). Pharmacokinetic parameters in individual patients have been related to short-term toxicity and risk of relapse after HSCT. In a series of 11 patients receiving the usual 16 x 1 mg/kg schedule over 4 days, we investigated the pharmacokinetics of replacing one dose with an intravenous formulation (BU in DMSO) which we had previously investigated in dogs. A dose of 0.5-0.6 mg/kg was used. No acute side-effects of BU/DMSO infusions administered over 1 h were observed. Bioavailability of BU powder capsules was on average 70% (range, 44-94%). Interindividual variability of the resulting AUC after intravenous doses was still substantial. Further studies are under way to define the possible role of BU/DMSO infusions in conditioning before HSCT.
白消安（BU）被纳入许多造血干细胞移植（HSCT）的预处理方案中。个体患者的药代动力学参数与HSCT后的短期毒性和复发风险相关。在一系列11例接受常规的4天内16×1mg/kg给药方案的患者中，我们研究了用一种静脉制剂（二甲基亚砜中的BU，我们之前已在犬类中进行过研究）替代一剂药物后的药代动力学。使用的剂量为0.5 - 0.6mg/kg。未观察到1小时内输注BU/二甲基亚砜的急性副作用。白消安粉末胶囊的生物利用度平均为70%（范围为44% - 94%）。静脉给药后所得曲线下面积（AUC）的个体间变异性仍然很大。正在进行进一步研究以确定BU/二甲基亚砜输注在HSCT预处理中的可能作用。
