普罗帕酮对映体的人体药物动力学

Pharmacokinetic studies on propafenone enantiomers in human

目的:研究普罗帕酮(PPF)对映体人体药物动力学差异.方法:8名健康受试者po盐酸PPF消旋片150mg,q6 h,4 d.RP-HPLC法测定血药浓度,采用TopFit软件,以非室模型计算药物动力学参数并比较.结果:(S)-PPF与(R)-PPF的(?)分别为(219±111)、(147.75±80.25)ng/ml;Cl值分别为(1226±7510)、(1678±625)ml/min;S/R-AUC比为 1.49±0.34.结论:PPF对映体存在明显的人体药物动力学立体选择性差异.

AIM: To study the differences between propafenone enantiomers in pharma-cokinetcs. METHODS ;Eight healthy Chinese volunteers were given propafenone tablets (150 mg,q6 h for 4 d). The plasma concentrations of both enantiomers were determined by reversed phase high performance liquid chromatography. Pharmacokinetic parameters were calculated and compared according to non-apartments model by Topfit. RESULTS: css of (S)-PPF and (R)-PPF were (219±111) , (147.75±80.25) ng/ml respectively. Cl of them was (1226±751)and (1678±625)mI/min respectively. The ratio of S/R-AUC was 1.49±0.34. CONCLUSION: Stereoseletive pharmacokinetic differences between the propafenone enantiomers does exist.