Assessment of pharmacokinetics and bioequivalence of amlodipine besylate in healthy volunteers

    ZHANG Yan, YANG Lei, LIU Mei, QIN Hua, CHEN Xiaoª²Yan, ZHANG Yiª²Fan, ZHONG Daª²Fang

    1Department of Pharmacy, Tangdu Hospital, Fourth Military Medical University, Xi¬ðan 710038, China, 2Department of Pharmacy, Hospital of Xidian University, Xi¬ðan 710061, China, 3Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharmaceutical University, Shenyang 110015, China

    ¡¾Abstract¡¿ AIM: To study the pharmacokinetics parameters and bioavailability of amlodipine besylate tablets. METHODS: An open, randomized and twoª²period crossover study with a twoª²week washout interval was performed in 18 healthy volunteers. Concentrations of amlodipine besylate in plasma were assayed by liquid chromatographicª²massª²mass spectrometric method after a single oral dose of 10 mg of the tested or the referenced tablets. The pharmacokinetics parameters, AUC, Tmax and Cmax were analyzed by two oneª²side t test and (1ª²2¦Á) 90%. RESULTS: The main pharmacokinetics of the tested and referenced tablets were: Tmax: (8.9¡À2.5) and (8.2¡À2.2) h; Cmax: (5.1¡À2.3) and (5.0¡À2.2) g/L; T1/2: (45¡À10) and (48¡À24) h; AUC(0-120 h): (191¡À69) and (196¡À53) ¦Ìg/(L¡¤h). The relative bioavailiability of amlodipine besylate was (99¡À23)%. CONCLUSION: The results of the statistical analysis show that the two formulations are bioequivalent. ......