Pharmacokinetics and bioequivalence of telmisartan in Chinese healthy volunteers

    HUANG Peng, ZHANG Hong, XU Wenª²Wei, LI Yanª²Yan, XIONG Yuª²Qing

    Department of Epidemiology, School of Public Health, Institute of Clinical Pharmacology, Jiangxi Medical College, Nanchang 330006, China

    ¡¾Abstract¡¿ AIM: To develop a HPLC method with fluorescent detection to determine telmisartan in human plasma and study the pharmacokinetics profiles and bioequivalence of telmisartan in healthy Chinese volunteers. METHODS: In a randomized two period crossover study, 24 healthy male volunteers received single dose of 40 mg telmisartan. The serum concentration of telmisartan was determined by HPLC method. The pharmacokinetic parameters of the two preparations (test and reference) and the relative bioavailability after oral administration were calculated with statistic analysis. The column was Diamonsil C18 (5 ¦Ìm, 4.6 mm¡Á150 mm). The mobile phase consisted of acetonitrileª²potassium dihydrogen phosphate buffer solution (61¡Ã39, pH adjusted to 3.74 with H3PO4) at a flow rate of 1.0 mL/min. The internal standard was candesartan. The fluorescence detector was operated at ¦ËEx=305 nm and ¦ËEm=365 nm. RESULTS: The calibration curve of telmisartan was linear in the range of 0.5-144 ng/mL (r=0.9998). The absolute recovery was 79.62%-85.69% (n=5), and the relative recovery was 101.92%-108.95% (n=5), and the intraª²day and interª²day RSDs were 4.23%-9.80% and 4.03%-9.95% (n=5). AUC0~96 of the test and reference preparations was 888.90¡À406.49 and 895.03¡À364.53, respectively. CONCLUSION: Statistical analysis showed that the two preparations were bioequivalent. ......