Pharmacokinetics and Bioequivalence of Nisoldipine Sustained-release Capsules in Healthy Volunteers

OBJECTIVE:To establish a method for the determination of nisoldipine in human plasma,and to study the pharmacokinetics and bioequivalence of domestic nisoldipine in healthy volunteers.METHODS:Single dose and multi-doses of test and reference preparation of 30 mg of nisoldipine were given to 18 male healthy volunteers orally.The content of nisoldipine in blood samples was determined by HPLC after treated.Pharmacokinetic parameters were calculated and bioequiavailability was evaluated.RESULTS:The pharmacokinetics of Nisoldipine sustained-release capsule was fitted with two-compartment open model after single dose or multiple dose administration.Main pharmacokinetic parameters were as follows:cmax were(12.07 ± 3.96) ng/ml and(10.68±3.61)ng/ml;t1/2β were(12.72±3.13)h and(15.61±2.88)h;AUC0-24 h were(52.54±16.71)ng·h/ml and(70.81±15.81) ng·h/ml;relative bioavailability were(101.88±18.63)% and(93.37±19.17)%,respectively.CONCLUSIONS:The AUC0-∞ and AUC0-t of the two kinds of dosage forms are proved to be bioequivalent,but the cmax and cmax are not bioequivalent.