关键词: 替米沙坦, HPLC, 药动学, 血药浓度

Abstract: AIM: To establish an HPLC-fluorimetric method in determination of the concentrations of telmisar-tan in plasma of healthy volunteers and to investigate its pharmacokinetics. METHODS: The chromatographic column was Hypersil C18 column (250 mm×4.6 mm,5 μm). The mobile phase was acetonitrile-pH 5.8 phos-phate buffer (45:55) and the flow rate was 1.0 ml·min^-1. The fluorimetric excitation and emission wave-lengths were set at 305 nm and 365 nm, respectively. The internal standard was a~naphthol. Blood samples were deproteined by adding acetonitrile. The injection volume was 20 μl. RESULTS: The linearity correlation of telm-isartan ranged from 2 to 1 024 μg·L^-1 (r=0.9999) and the precision and stability of the method were fine. The pharmacokinetics of telmisartan was studied in healthy volunteers after oral administration of 80 mg telmisaitan tablets. It showed that the c-t curves of telmisartan con-formed to the two-compartment open model. The main pharmacokinetic parameters of telmisartan were as follows: C_max 0.98±0.44 mg·L^-1; mg·L^-10.83±0.45 h, t_1/2α 1.67±1.26 h, t_1/2β26.00±14.43 h,t_1/2ka0.53±0.86 h,AUC_0-l 3.66±2.10 mg·h ^-1·L ^-1,and AUC_0-∞ 3.98±2.40 mg·h ^-1·L ^-1. CONCLUSION: This is a convenient, sensitive, accurate and reproducible method for determining the concentrations of telmisartan in plasma of healthy volunteers and investigating its pliarma-cokinetics.

Key words: telmisartan, HPLC, pharmacokinetics, plasma concentrations