Pharmacokinetics and relative bioavailability of telmisartan in male healthy Chinese volunteers

AIM: To compare pharmacokinetics and relative bioavailability of telmisartan capsule (T) and telmisartan tablet(R). METHODS: 20 male healthy Chinese volunteers were enrolled in a randomized two-way crossover designs with a single-oral dose study(80 mg once per day for each preparation). The plasma telmisatan concentration was determined by HPLC- fluorescence detector. Plasma levels of telmisatan were followed up to 96 h. Area under the telmisartan concentration time curve was calculated by variance analysis and the bioequivalent was determined by two one-side t-test. RESULTS: A two-compartment model was adopted in telmisartan plasma concentration-time data analysis. The pharmacokinetic parameters of T and R in single-dose study including C_ max ( μg·L -1 ), T_ max (h), T_ 1/2β (h), MRT(h), AUC_ 0-92 ( μg·h·L -1 ) were as following: 456±253 and 760±314, 1.61 ± 0.71 and 1.08 ± 0.36 , 22.39 ± 6.29 and 21.08 ± 5.24 , 27.02 ± 6.23 and 24.27 ± 5.79 , 3454±1050 and 3635±1300, respectively. Statistically significant differences were observed between the parameter values of the two products in C_ max and T_ max ; whereas there was no statistically significant difference between AUC_ 0-∞ μg·h·L -1 (3601±1095 and 3767±1399). The relative bioavailability for T was 97.28 %± 12.74 %. CONCLUSION: The test telmisartan capsule is bioequivalent to the reference tablet.