槐果碱的人体药代动力学研究  

Pharmacokinetics of Sophocarpine in Healthy Volunteers

作　　者：陈曙霞[1] 徐瑾[1] 王平全[2] 周飚彪[2] 蔡美华[2] 钱富荣[1] 谢龙山[1] 陈美芳[1] 

机构地区：[1]上海第二医科大学仁济医院心内科,上海200001 [2]上海第二医科大学仁济医院临床药理研究基地,上海200001

出　　处：《上海第二医科大学学报》2005年第11期1164-1166,共3页Acta Universitatis Medicinalis Secondae Shanghai

基　　金：上海市科委;上海市卫生局重点课题(994319223)资助项目

摘　　要：目的研究槐果碱的人体药代动力学,为临床应用提供依据.方法采用高效液相色谱法测定人血清槐果碱浓度,并对其药代动力学进行研究.结果槐果碱的绝对回收率＞70%,相对回收率为100.7%～108.7%,日内精密度和＜4%,日间精密度均＜5%,血药浓度在0.625～20.0 μg/mL范围内呈线性相关(r=0.99998).10名健康志愿者静脉滴注槐果碱6 mg/kg后,血清样本检测显和药时曲线符合二室开放模型,T1/2α为27.459 min,T1/2β为228.16 min,CL(s)为0.0073 L·kg-1·min-1,Vc为1.5182 L/kg,Tmax:30 min,Cmax:(3.5445±0.9876)μg/mL;尿样检测发现,24 h内64.77%的槐果碱以原形由尿排出,故其主要排泄器官为肾脏.结论临床给予槐果碱6 mg/kg的剂量是安全的.Objective To study the pharmacokinetics of sophocarpine in healthy volunteers so as to provide evidences for clinical application. Methods A sensitive high performance liquid chromatographic （HPLC） analytical method was established for determining the concentration of sophocarpine（Sc） in human serum. Results The relation recovery of Sc was 100.7%- 108.7%. The RSD% in one day and between-day were no more than 5%. The calibration curve was linear in the range from 0. 625 μg/mL to 20.0 μg/mL with r = 0. 99998. The serum drug concentration-time curve after iv infusion with a dose of 6 mg/kg in 100 mL glucose solution fitted to a 2-compartmant open model in 10 healthy volunteers. T1/2α was 27. 459 min, T1/2β 228. 16 min, CL（α） 0.0073 L·kg^-1·min^-1,Vc 1,5182 L/kg, and Tmax was 30 min, Cmax： （3. 5445 ± 0. 9876） μg/mL. Major excretion of sophocarpine is from kidney, about 68. 51% original state excreted within 24 h, Conclusion A dose of 6 mg/kg in 100 mL glucose solution of sophocarpine as evidenced in healthy volunteers might be suitable for clinical use.

关 键 词：槐果碱 药代动力学 高效液相色谱分析法 

分 类 号：R285[医药卫生—中药学]