特拉唑嗪胶囊的药物动力学及相对生物利用度研究

目的:建立人血浆中特拉唑嗪浓度的HPLC荧光测定方法,研究特拉唑嗪在人体中的药物动力学行为。方法:血浆样品经碱化后,用乙酸乙酯和苯(1:4)提取,色谱柱为 Hypersil-ODS柱,流动相为0.05 mol/L磷酸二氢钾-乙腈-四氢呋喃(70:29.2:0.8),荧光检测器的激发波长为250 nm,发射波长为 370 nm。测定了20名受试者单剂量口眼特拉唑嗪胶囊和市售片剂后的血药浓度。结果:特拉唑嗪浓度在1.5～150.0 ng/ml范围内,线性关系良好(r=0.9994),最低检测限达 1ng/ml,绝对回收率大于 70％,符合生物样品分析要求。受试者口服特拉唑嗪胶囊和片剂 2 mg后,估算的半衰期分别为 10.90±2.24 h和 11.58±2.47 h,达峰时间分别为 1.6±0.6 h和 1.3±0.5 h,峰浓度分别为 36.97±3.53 ng/ml和 38.95±8.31 ng/ml,特拉唑嗪胶囊剂的相对生物利用度为98.0％。结论:特拉唑嗪胶囊剂与市售特拉唑嗪片剂生物等效。

Pharmacokinetics and Relative Bioavailability of Telazosin Capsules

AIM To establish a HPLC method for determination of telazosin and to study its pharmacokinetics in men. METHODS The drug was extracted from plasma with ethyl acetate : benzene (1 : 4 ). The column was Hypersil-ODS. The mobile phase was consisted of 0. 05mol/L potassium dihydrogen phosphate : acetonitrile : tetrahydrofuran(70 : 29. 2 : 0. 8). The samples' peaks were detected with fluorescence monitoring at \ex = 250 nm and Xem = 370 nm. RESULTS The standard curve was linear in the range of 1. 5-150. 0 ng/ml and the correlation coefficient was 0. 9994. The minimum detection concentration was 1 ng/ml and the absolute recoveries of telazosin from plasma were larger than 70%. The assay method was convenient for determination of telazosin. The pharmacokinetics of terazosin capsules and tablets in 20 healthy subjects was studied. The pharmacokinetics parameters were estimated as follows; T1/2,10. 90