Bioequivalence of Tolvaptan tablets in healthy Chinese volunteers

Abstract

Abstract: AIM: To evaluate the bioequivalence of Tolvaptan tablets in healthy Chinese volunteers.METHODS: A single oral doses of 30 mg Tolvaptan tablets (test and reference) were given to 24 healthy volunteers according to an open randomized crossover design. The concentrations of Tolvaptan in plasma were determined by HPLC-MS/MS. The pharmacokinetic parameters of the test and reference preparation were calculated by DAS 2.1. The bioequivalence was evaluated by two one-sided t test.RESULTS: The pharmacokinetic parameters of the test and reference preparations were as follows: C_max were (179±97) and (189±86) μg/L; t_max were (2.5±1.1) and (2.5±1.0) h;AUC_0-twere (1153±488) and (1225±528) μg·h·L^-1;AUC_0-∞ were (1161±492) and (1232±528) μg·h·L^-1;t_1/2 were (5.6±2.0) and (5.6±2.0) h. The relative bioavailability of the test preparation was (95.8±18.7)%.CONCLUSION: The tested preparation was of bioequivalence to the reference preparation.

Key words: Tolvaptan, HPLC-MS/MS, Pharmacokinetics, Bioequivalence

CLC Number:

R969.1

LI Zuo-jun, YANG Guo-ping, PEI Qi, TAN Hong-yi, ZHANG Ran-ran, LIU Li, CHEN Jun, LIU Shi-kun, LI Bing. Bioequivalence of Tolvaptan tablets in healthy Chinese volunteers[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2013, 18(9): 1031-1035.

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