OBJECTIVE: To evaluate the relationship of blood concentration of busulfan (Bu) with treatment outcome of hema-topoietic stem cell transplantation (HSCT). METHODS: Therapeutic efficacy and toxicity were observed in 22 HSCT patients who pre-treated with intravenous dosage form of Bu. Blood concentration of Bu was monitored by pre-column derivatization HPLC before and after medication, and AUC of Bu was calculated. RESULTS: The probabilities of developing gastrointestinal toxicity, hep-atotoxicity, mucositis and GVHD increased with increases of AUC. Further, the risk of death was significantly lower for patients having an AUC0～6b between approximately 900 and 1 400 μmol·min·L-1, whereas the risk increased sharply with either lower or higher AUC values. CONCLUSION: Drug dosage is adjusted timely according to blood concentration monitoring of Bu, and it improves clinical prognosis of HSCT patients and reduction of post-operative complication.%目的:评价白消安(Bu)的血药浓度与造血干细胞移植临床效果的相关性.方法:22例移植患者预处理采用静脉剂型Bu,观察疗效及相关毒性.采用2007年文献报道的柱前衍生高效液相色谱法对Bu给药前和给药后不同时间的血药浓度进行监测,计算Bu药-时曲线下面积(AUC).结果:胃肠道反应、肝毒性、口腔黏膜炎和移植物抗宿主病与Bu的AUC值正相关.AUC0～6h在900～1400 μmol·min·L-1之间时,移植患者的死亡风险下降,过高或过低的AUC值增加死亡风险.结论:根据Bu血药浓度监测及时调整药物剂量,有助于造血干细胞移植患者的临床预测和减少术后并发症.
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