Pharmacokinetic Study of Azelnidipine Tablets in Healthy Volunteers

OBJECTIVE:To establish a method for the content determination of Azelnidipine tablet in human plasma and study the pharmacokinetics of Azelnidipine tablet.METHODS:20 healthy volunteers were randomly distributed into 2 groups and received a single-dose of Azelnidipine tablet 8 and 16 mg respectively.The group receiving Azelnidipine tablet 8mg participated in the multi-dose test at the same time.The concentration of azelnidipine in human plasma was determined by LC-MS and the pharmacokinetic parameters were calculated after single-dose or multi-dose administration.RESULTS:The pharmacokinetic parameters of azelnidipine after single dose of Azelnidipine tablet 8 and 16 mg were as follows:cmax(1.66±0.45)μg·L-1 and (4.25±1.38)μg·L-1,tmax(3.50±1.08)h and (4.00±1.16)h,t1/2(21.3±8.1)h and (19.5±4.0)h,AUC0～72(17.9±6.0)μg·h·L-1 and (49.9±17.5)μg·h·L-1,respectively.The pharmacokinetic parameters of azelnidipine after multi-dose of Azelnidipine tablet 8 mg were as follows:cmax(2.63±1.41)μg·L-1,tmax(3.50±1.08)h,t1/2(32.5±9.2) h,AUC0～72(43.8±26.4) μg·h·L-1,cav(1.19±0.671)μg·L-1,AUCss(28.4±16.1)μg·h·L-1,DF(1.78±0.49),Rs(1.56±0.95).CONCLUSION:The method is sensitive,accurate and simple.The values of cmax and AUC0～72 of Azelnidipine tablet after single-dose administration increase along with the increasing of the dose.And the azelnidipine has accumulated after multi-dose of administration.