Study on the pharmacokinetics and bioequivalence of domestic amlodipine besylate tablets in healthy volunteers

OBJECTIVE To study the pharmacokinetics profiles and bioequivalence of domestic and imported amlodipine besylate tables in healthy volunteers.METHODS A single oral dose of 10 mg domestic or imported amlodipine besylate tables were given to 20 healthy male volunteers in an open randomized crossover design.Concentrations of amlodipine in plasma were determined by LC-MS.The pharmacokinetic parameters and relative bioavailability were calculated by DAS 2.0 program to evaluate the bioequivalence of the two preparations.RESULTS The main pharmacokinetic parameters of the two preparations were as follows: AUC0-120 were(306.1±60.7)μg·h·L-1 and(315.1±62.7)μg·h·L-1,AUC0∞ were(330.3±59.8)μg·h·L-1 and(341.7±67.2) μg·h·L-1;Cmax were(7.6±1.7 ) μg·L-1 and(7.8±1.6) μg·L-1;tmax were(7.7±2.2) h and(7.4±2.1) h;t1/2 were(35.4±6.3) h and(36.4±5.1) h respectively.The relative bioavailability of domestic to imported tablets were 98.3%±13.2%(F0-120) and 98.0%±12.5%(F0-∞).CONCLUSION The results of the statistical analysis show that the two preparations are bioequivalent.