阿折地平片的人体药动学研究

目的:考察阿折地平片在人体内的药动学特性。方法:采用液-质联用(LC-MS)法,测定24名健康受试者口服受试制剂(单剂量含阿折地平8、16mg和多剂量)后血浆中阿折地平浓度。结果:单剂量口服阿折地平片8、16mg后,阿折地平的t1/2分别为(20.338±7.601)、(27.995±7.724)h,tmax分别为(3.333±1.303)、(3.667±0.985)h,cmax分别为(5.908±2.827)、(10.61±3.929)μg·L-1,AUC0～96h分别为(61.167±33.777)、(139.502±72.898)μg·h·L-1,AUC0～∞分别为(63.363±35.314)、(147.395±78.21)μg·h·L-1;多剂量口服阿折地平片8mg后,阿折地平的t1/2为(28.168±7.926)h,tmax为(3.167±0.718)h,cmax为(5.882±1.895)μg·L-1,AUC0～96h为(86.723±41.588)μg·h·L-1,AUC0～∞为(93.948±50.957)μg·h·L-1。结论:阿折地平片在8～16mg剂量范围内呈线性动力学特征,不同性别间药动学参数总体上差异不大,多剂量给药与单剂量给药的药动学参数基本一致。

Study on Pharmacokinetics of Azelnidipine Tablet in Healthy Volunteers

OBJECTIVE: To study the pharmacokinetic characteristics of Azelnidipine tablet in healthy volunteers. METHODS: The concentration of azelnidipine in plasma was determined by LC-MS after 24 healthy volunteers received test preparation orally (single dose of azelnidipine 8,16 mg and multi-dose). RESULTS: The pharmacokinetic parameters after the single oral dose of Azelnidipine tablet 8 mg vs. 16 mg were as follows:t1/2(20.338±7.601) vs. (27.995±7.724)h; tmax(3.333±1.303) vs. (3.667±0.985)h; cmax(5.908±2.827) vs. (10.61±3.929)μg·L-1; AUC0～96 h(61.167±33.777) vs. (139.502±72.898)μg·h·L-1; AUC0～∞(63.363±35.314) vs. (147.395±78.21)μg·h·L-1. The pharmacokinetic parameters after multi-dose of Azelnidipine tablet 8 mg were as follow: t1/2(28.168±7.926)h; tmax(3.167±0.718)h;cmax(5.882±1.895)μg·L-1;AUC0～96 h(86.723±41.588)μg·h·L-1;AUC0～∞(93.948±50.957)μg·h·L-1. CONCLUSION: A linear pharmacokinetic profile of Azelnidipine tablet has been proved in the range of 8～16 mg. There is no significant difference in pharmacokinetic parameters between single dose and multi-dose and no significant difference between genders.