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.