【摘要】 目的:建立高效液相色谱法测定人血浆中替米沙坦的药物浓度,并研究其在健康人体内的药动学。方法:采用高效液相色谱-荧光检测法,色谱柱为Hypersil C18柱(250 mm×4.6 mm,5μm);流动相为乙腈-磷酸盐缓冲液(45∶55,pH 5.8);流速为1.0 ml·min-1;激发波长和发射波长分别为305 nm和365 nm;进样量20μl;内标物为α-萘酚。结果:替米沙坦在2~1 024μg·L-1范围内线性良好(r=0.9999),回收率,日间、日内差均符合生物样品分析要求。10名健康受试者口服替米沙坦片80 mg后的药动学结果表明,其体内过程符合二房室开放模型,主要药动学参数如下:Cmax为0.98±0.44 mg·L-1;Tmax为0.83±0.45 h;T1／2α为1.67±1.26 h;T1／2β为26.00±14.43 h;T1／2ka为0.53±0.86h;AUC0~t为3.66±2.10 mg·h-1·L-1;AUC0~∞为3.98±2.40 mg·h-1·L-1。结论:此方法便捷,准确,灵敏,适于替米沙坦血药浓度测定和药动学研究,本试验所得药动学参数可为临床合理用药提供理论依据。更多还原

【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, 5μm) . The mobile phase was acetonitrile-pH 5.8 phosphate buffer (45 : 55) and the flow rate was 1.0 ml ·min-1 . The fluorimetric excitation and emission wavelengths were set at 305 nm and 365 run, respectively. The internal standard was α-naphthol. Blood samples were deproteined by adding acetonitrile. The injection volume was 20μl. 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 healthyvolunteers after oral administration of 80 mg telmisartan tablets. It showed that the c-t curves of telmisartan conformed to the two-compartment open model. The main pharmacokinetic parameters of telmisartan were as follow: Cmax0.98± 0.44 mg·L-1 Tmax0.83±0.45 h, T1/2α 1.67±1.26 h, T1/2β26.00±14.43 h, T1/2ka0.53±0.86 h, AUC0-t 3.66± 2.10 mg·h-1·L-1, and AUC0-∞ 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 pharma-cokinetics.更多还原