摘要
目的建立人体血浆中辛伐他汀的LC-MS/MS测定方法,研究辛伐他汀片在男性健康志愿者体内的药代动力学行为,评价其生物利用度和生物等效性。方法20名健康成年男性志愿者采用随机分组自身交叉对照试验设计,单剂量口服辛伐他汀片40 mg后,用LC-MS/MS联用法测定血浆中药物浓度。结果试验制剂和参比制剂的主要药代动力学参数:tmax分别为(1.8±1.3)h和(2.10±1.00)h;cmax分别为(7.12±1.61)μg.L-1和(7.38±1.54)μg.L-1;AUC(0-24)分别为(30.50±11.25)μg.L-1.h-1和(30.17±10.21)μg.L-1.h-1;t1/2分别为(3.90±0.78)h和(3.76±0.85)h。以AUC(0-24)计算的试验制剂的相对生物利用度为101.2%±7.8%。结论建立的分析方法准确灵敏,测得的数据可靠,统计学分析表明两种制剂生物等效。
AIM To establish a LC-MS/MS method for the determination of simvastatin in human plasma, and to investigate the pharmacokinetics and bioequivalence of simvastatin tablet in Chinese healthy volunteers. METHODS 20 male healthy volunteers were randomized to receive a single crossover oral dose of simvastatin reference tablet or domestic tablet. The concentration of simvastatin in plasma was determined by LE-MS/MS. RESUALTS The simvastatin main pharmacokinetic parameters of test and reference tablets were as following: tmax: (1.8 ± 1.3) and (2.10 ± 1.00) h, cmax: (7.12 ± 1.61 ) and (7.38 ± 1.54) μg·L^-1, AUC(0-24h) : (30.50 ± 11.25) and (30.17± 10.21) μg·L^-1,t1/2:(3.90± 0.78) and (3.76±0.85) h, F(0-24h) was (101.2% ±7.8%). CONCLUSION The assay was show to be sensitive, accurate, and the results were reliable. The test tablet was bioequivalent to the reference tablet.
出处
《江苏药学与临床研究》
2006年第3期149-152,共4页
Jiangsu Pharmacertical and Clinical Research