Study On The Pharmacokinetics And Bioequivalence Of Captopril

OBJECTIVE: To study the pharmacokinetics and the relative bioavailability of captopril tablets in healthy male volunteers and to assess the bioequivalence METHOD: According to a 2-circle randomized crossover design, the pharmacokinetics of the 18 healthy male volunteers were studied after each was administrated by a single oral dose of captopril tablet (test drug) and captopril tablet (reference drug), respectively. The concentrations of captopril in plasma samples at different time points were determined by LC/MS/MS and the plasma concentrations-time profiles were obtained. The pharmacokinetic parameters were described and the relative bioavailability was assessed. RESULTS: After oral administration with single dose of test drug (T) or reference drug (R) at 50 mg captopril, respectively. the Tmax values of captopril were 0.81±0.25 (mean ±SD) and 0.75 ±0.19 h, respectively. The Cmax values were 734.39 ±282.41 and 764.00 ±355.53 ng/ml, respectively. The t1/2 values were 1.37 ±0.22 and 1.36 ±0.23 h, respectively. The AUC0-t values were 1013.90 ±359.03 and 972.17 ±349.44 ng?h/ml and the AUC0-∞values were 1024.13±362.74 and 982.44 ±353.17 ng?h/ml, respectively. According to AUC0-t and AUC0-∞, the relative bioavailability of test drug was 106.674±18.574% and 106.620±18.509 %, respectively. Statistical analysis (paired t test) showed no significant difference between test drug and reference drug for Tmax, Cmax and AUC (P>0. 05). The bioequivalence test showed no significant difference between two preparations for Tmax, Cmax and AUC (P>0. 05), too. CONCLUSION: The pharmacokinetics of captopril test drug and reference drug were similar and the result of statistics showed that the two preparations were...