【作者】 张宏文； 欧宁； 谢林； 王蔚青； 梁艳； 王永庆； 袁红宇； 刘云；

【Author】 ZHONG Hong-wen1, OU Ning 1 XIE Lin2, WANG Wei-qing1, LANG Yan 2 WANG Yong-Qing1,YUAN Hong-Yu1 , LIU Yun1 1.Department of Clinical Pharmacology, The First Affiliated hospital of,NanjingMedical University ,Nanjing 210029, China;2. Center of Drug Metabolism and Pharmacokinetics , China Pharmaceutical University China 210009

【机构】 南京医科大学第一附属医院临床药物研究室； 中国药科大学药物代谢与动力学研究中心；

【摘要】 目的研究单剂量口服非洛地平缓释片和合资非洛地平片的血药浓度经时过程,以及体内的药代动力学特征评估两者的生物等效性。方法20名健康男性志愿者采用2制剂双周期交叉试验设计,以尼莫地平为内标,HPLC-MS/MS法测定血中药物浓度,以BAPP2.2计算其药代动力学参数,评价2制剂的生物等效性。结果20名受试者单剂量口服10mg受试制剂和参比制剂后非洛地平,主要药代动力学参数Cmax分别为(3.09±1.03)μg·L-1和(2.68±0.88)μg·L-1;tmax分别为(3.8±1.0)h和(3.5±1.4)h;t1/2分别为(14.49±2.72)h和(13.74±3.42)h;MRT为(19.87±2.62)h和(19.08±4.73)h;AUC0-48为(30.83±6.04)μg·h·L-1和(31.42±5.78)μg·h·L-1;AUC0-∞为(34.00±5.76)μg·h·L-1和(34.93±6.54)μg·h·L-1。主要药代动力学参数经统计学分析,无明显差异。两种制剂的相对生物利用度为99.8±13.0%结论两种制剂具有生物等效性。更多还原

【Abstract】 OBJECTIVE To investigate the pharmacokinetics properties and bioequiavailability of felodipine sustained-release tablets after a single dose administ ration in healthy volunteers. METHODS The study was designed in a two-treatment , two-period , two-sequence randomized cross-over trial. Plasma concentrations were determined by HPLC-MS/MS method, Nimodipine was used as the internal standard RESULTS The main pharmacokinetics parameters calculated by BAPP2.2 software were as follows and the bioequivalence were compared. The pharmacokinetics parameters were as follows : Cmax were 3.09±1.03) and (2.68±0.88) μg·L-1; Tmax were (3.8±1.0)h and(3.5±1.4)h ; t1/2 were(14.49±2.72)h and(13.74±3.42) h ;MRT were (19.87±2.62)and(19.08±4.73)h ;AUC0-48 were (30.83±6.04) μg·h·L-1 and(31.42±5.78)μg·h·L-1 ;AUC 0-∞were(34.00±5.76)μg·h·L-1 and (34.93 ±6.54) μg·h·L-1 respectively. The relative bioavailability of tested tablet s was (99.8±13.0) %. CONCLUSION The test and reference preparations are bioequivalent .更多还原