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目的不同剂量左西孟旦注射液在中国健康志愿者体内的药动学研究。方法12名健康志愿者,随机分为3组。于10min内分别静脉推注6,12,18μg·kg-1左西孟旦注射液后,再0.05,0.10,0.15μg·kg-1·min-1连续4小时静脉滴注,于给药后0.17,0.5,1,2,3,4,4.25,4.5,4.75,5,5.5,6,7,8和10小时采集肘静脉血,采用LC-MS/MS法测定左西孟旦血药浓度,用DAS2.0软件计算其药动学参数。结果3个剂量组左西孟旦主要药动学参数依次为:t1/2为1.50±0.35,1.64±0.25和1.54±0.39h;C0为9.54±3.90,15.95±7.84和28.46±10.74ng·mL-1;AUC0-t(t=7,8)为33.63±9.34,54.39±15.34和78.36±23.74ng·mL-1·h;AUC0-∞为36.01±8.90,56.94±15.12和81.33±24.34ng·mL-1·h。结论静脉给予左西孟旦注射液后,C0和AUC与剂量呈良好的相关性,但与性别无关。
Objective To study the pharmacokinetics of different doses of levosimendan injection in Chinese healthy volunteers. Methods Twelve healthy volunteers were randomly divided into three groups. Intravenous injection of 6,12,18μg · kg-1 levosimendan injection within 10min, and then 0.05,0.10,0.15μg · kg-1 · min-1 for 4 hours continuous intravenous infusion, after administration The elbow venous blood was collected at 0.17,0.5,1,2,3,4,4.25,4.5,4.75,5,5.5,6,7,8 and 10 hours, and the levosimendan plasma concentration was determined by LC-MS / MS , Using the DAS2.0 software to calculate the pharmacokinetic parameters. Results The main pharmacokinetic parameters of levosimendan in three dose groups were as follows: t1 / 2 = 1.50 ± 0.35,1.64 ± 0.25 and 1.54 ± 0.39h; C0 = 9.54 ± 3.90,15.95 ± 7.84 and 28.46 ± 10.74ng · mL -1; AUC0-t (t = 7,8) were 33.63 ± 9.34, 54.39 ± 15.34 and 78.36 ± 23.74 ng · mL-1 · h; AUC0-∞ was 36.01 ± 8.90, 56.94 ± 15.12 and 81.33 ± 24.34 ng · mL-1 · h. Conclusion After intravenous levosimendan injection, C0 and AUC showed a good correlation with the dose, but not with sex.