丁苯酞及其代谢物在中国健康人体的药代动力学

Pharmacokinetics of butylphathlide capsule in Chinese healthy volunteers

目的评价丁苯酞软胶囊在中国健康人体的药代动力学。方法 12名中国健康受试者单次空腹口服丁苯酞软胶囊200 mg,用液相色谱-串联质谱法测定血浆样本中丁苯酞(NBP)和丁苯酞代谢物1(NBP-M1)的浓度;用Phoenix WinNolin计算药代动力学参数。结果 NBP和NBP-M1的主要药代动力学参数,t1/2分别为(10.35±0.79),(3.69±0.93)h;tmax分别为(1.23±0.73),(1.90±0.76)h;Cmax分别为(196.95±165.2),(1174.29±322.33)ng.mL-1;AUC0-t分别为(360.92±342.8),(5918.10±1627.51)h.ng.mL-1;CL/F分别为(977.03±664.06),(35.82±10.39)L.h-1。结论丁苯酞口服吸收迅速,除原型物外,体内还可检测出较大浓度的代谢物。

Objective To study the pharmacokinetics of butylphathlide capsule in healthy volunteers.Methods Twelve healthy volunteers received 200 mg butylphathlide capsule at a single oral dose.The concentration of butylphathlide and butylphathlide metabolite-1 in plasma were determined by HPLC-MS/MS.The pharmacokinetic parameters were calculated by WinNolin program.Results After a single dose of 200 mg butylphathlide capsule,the pharmacokinetic parameters for butylphathlide and butylphathlide metabolite 1 were as follows： t1/2 were（10.35±0.79）,（3.69±0.93） h;tmax were（1.23±0.73）,（1.9±0.76） h;Cmax were（196.95±165.2）,（1174.29±322.33） ng·mL-1;AUC0-t were（360.92±342.8）,（5918.1±1627.51） h·ng·mL-1;CL/F were（977.03±664.06）,（35.82±10.39） L·h-1.Conclusion Butylphthalide is rapid absorbed after oral administration,in addition to its original form,larger amount of metabolite could also be detected.