目的:评价注射用盐酸苯达莫司汀在肿瘤患者体内的药动学特征。方法:10例受试者接受120 mg·m-2盐酸苯达莫司汀慢速静脉滴注,以苯达莫司汀中间体为内标,采用高效液相法(HPLC)测定给药后血浆药物浓度,以DAS 2.1软件进行药动学参数的计算分析。结果:血药浓度在5~10 000 ng·m L-1剂量范围内线性关系良好。静脉滴注120 mg·m-2盐酸苯达莫司汀(4 h),平均消除半衰期(t1/2)、达峰浓度(Cmax)、达峰时间(Tmax)及血药浓度-时间曲线下面积(AUC0~t)分别为(0.389±0.052)h、(2.2±0.8)μg·m L-1、(2.9±1.2)h、(6.7±1.8)μg·m L-1·h。受试者在研究期间未发生III度及以上不良反应。结论:本研究建立的检测方法简单快速,试剂消耗少,准确度及精密度良好,适合盐酸苯达莫司汀人体药动学研究。单次静脉注射盐酸苯达莫司汀,受试者耐受良好。 Objective: To evaluate the pharmacokinetics of bendamustine hydrochloride for injection in patients with cancer. Methods: Ten patients received bendamustine hydrochloride (120 mg · m-2) intravenously slowly. Bentamustine intermediate was used as internal standard. After HPLC, Plasma drug concentration, calculated by DAS 2.1 software pharmacokinetic parameters. Results: The linear range of plasma concentration was 5 ~ 10 000 ng · m L-1. The mean elimination half-life (t1 / 2), peak concentration (Cmax), peak time (Tmax) and plasma concentration-time curve were recorded by intravenous infusion of bendamustine hydrochloride (120 mg · m- (AUC0 ~ t) were (0.389 ± 0.052) h, (2.2 ± 0.8) μg · m L-1, (2.9 ± 1.2) h and (6.7 ± 1.8) μg · m L-1 · h, respectively. Subjects did not experience grade III and above adverse events during the study period. Conclusion: The detection method established in this study is simple and rapid, less reagent consumption, good accuracy and precision, suitable for human study of bendamustine hydrochloride pharmacokinetics. Bentamustine hydrochloride was injected intravenously, and the subjects were well tolerated.