国产舒芬太尼单剂量给药在心脏手术患者的药代动力学

Pharmacokinetics of single dose domestic sufentanil in Chinese patients undergoing cardiac surgery

目的研究国产舒芬太尼(阿片受体激动剂)单剂量给药在心脏手术患者的药代动力学特征。方法随机选择NYHAⅡ～Ⅲ级的成年心脏手术患者8例,麻醉后,经前臂静脉一次性静脉注射国产舒芬太尼5μg.kg-1;采集给药后1,3,5,10,20,30,60,120,240,360 min血标本,-40℃低温保存直至分析。用液相色谱-质谱联用法测定血浆舒芬太尼浓度,3P97药理学程序计算药代动力学参数。结果舒芬太尼血药浓度-时间衰减曲线的三指数函数方程表示为Cp(t)=14.77e-0.518t+3.78e-0.048t+0.32e-0.004t。主要药代动力学参数:t1/2π=(0.03±0.02)h,t1/2α=(0.25±0.07)h,t1/2β=(3.68±2.44)h,Vc=(0.29±0.09)L.kg-1,Vd=(8.24±5.07)L.kg-1,CL=(0.03±0.00)L.(kg.h)-1。结论国产舒芬太尼在心脏手术患者的药代动力学符合三室模型,体外循环可影响其药代动力学特征。

Objective To study pharmacokinetics of single dose domestic sufentanil in Chinese patients undergoing cardiac surgery.Methods Eight NYHA grade Ⅱor Ⅲ patients undergoing cardiac surgery were studied.After general anesthesia,domestic sufentanil 5 μg·kg-1 was administered as a rapid bolus intravenously.Blood samples were obtained at 1,3,5,10,20,30,60,120,240 min and 360 min after domestic sufentanil injection.One mL plasma was immediately separated from blood samples and stored at-40 ℃ until assayed.Plasma sufentanil concentration were determined by liquid chromatography mass spectrometry.Pharmacokinetic parameters were calculated by 3P97 pharmacological program.Results Plasma concentration of sufentanil versus the time decay curve or tri-exponential equation was Cp（t） = 14.77e-0.518t＋3.78 e-0.048t＋0.32 e-0.004t.Major pharmacokinetic parameters were as follows： t1/2π=（0.03±0.02） h,t1/2α=（0.25±0.07） h and t1/2β=（3.68±2.44） h,Vc=（0.29±0.09） L·kg-1,Vd=（8.24±5.07） L·kg-1,CL=（0.03±0.00） L·（kg·h）-1.Conclusion Pharmacokinetics of single dose domestic sufentanil in young patients undergoing cardiac surgery was fitted to three-compartment open models.Extracorporeal circulation can affect its pharmacokinetic characteristics.