ABSTRACT
OBJECTIVE:To study the bioequivalence of 2 kinds of Losartan potassium tablets in healthy volunteers. METHODS: A single oral dose of test tablet 100 mg and reference tablet 100 mg were given to 20 healthy volunteers in randomized crossover study. The plasma concentrations of losartan and its metabolite EXP3174 were determined by LC-MS. The pharmacokinetic parameters were calculated and bioequivalence of 2 kinds of tablets was evaluated. RESULTS: Main pharmacokinetic parameters of Losartan of test tablets vs. reference tablets were as follows: Cmax(534.230?238.642) ng?mL-1 vs.(520.020?226.800) ng?mL-1; tmax(1.401?0.946)h vs.(1.334?0.750)h; AUC0～36(871.177?232.315) ng?h?mL-1 vs. (773.030?252.209) ng?h?mL-1; pharmacokinetic parameters of metabolite EXP3174 of test tablets vs. reference tablets were as follows: Cmax (1 294.000?387.815) ng?mL-1 vs.(1 140.900?317.615)ng?mL-1;tmax(2.667?1.144)h vs.(2.734?1.162)h;AUC0～36(6 267.905?1 350.300)ng?h?mL-1 vs.(5 719.411?1 127.725) ng?h?mL-1; AUC0～∞(6 316.605?1 343.048)ng?h?mL-1 vs. (5 755.335?1 138.358) ng?h?mL-1. The relative bioavailability of test tablet was (116.6?24.3)%. CONCLUSION: 2 kinds of Losartan potassium tablets are bioequivalent.