辛伐他汀片在健康人体的药物动力学和生物等效性  

Pharmacokinetics and Bioequivalence of Simvastatin Tablets in Healthy Volunteers

作　　者：孙倩[1] 任进民[1] 殷立新[1] 王川平[1] 郭立志[1] 

机构地区：[1]河北医科大学第二医院,石家庄050000

出　　处：《中国药师》2010年第2期183-185,共3页China Pharmacist

摘　　要：目的:研究辛伐他汀片在健康人体的药物动力学及生物等效性。方法:20名健康志愿者随机双交叉、单剂量口服受试制剂和参比制剂20 mg,用LC-MS/MS法测定人血浆中辛伐他汀的浓度。使用DAS软件拟合计算药物动力学参数和相对生物利用度,评价两制剂的生物等效性。结果:受试制剂和参比制剂药物动力学参数:C_(max)分别为(3.09±1.57),(3.48±1.95)ng·ml^(-1);t_(max)分别为(1.68±0.96),(1.31±0.74)h;t_(1/2)分别为(5.65±2.48),(5.47±2.55)h;AUC_(0-24h)分别为(12.52±5.59),(12.80±5.07)ng·ml^(-1)·h;AUC_(0-∞)分别为(13.41±5.95),(13.70±5.24)ng·ml^(-1)·h。受试制剂相对于参比制剂的生物利用度为(99.0±23.9)%。结论:两种制剂具有生物等效性。Objective： To study the pharmacokinetics and bioequivalence of simvastatin tablets in healthy volunteers. Method： A single oral dose （20 mg test and reference formulations） was given to 20 healthy volunteers according to an open randomized crossover design. The liquid chromatography-mass spectrometry/mass spectrometry （LC-MS/MS） method was used for the determination of simv- astatin in human plasma. The pharmacokinetic parameters and relative bioavailability were calculated by DAS program. The bioequiva- lence of the two preparations was also evaluated. Result： The main pharmacokinetics parameters of the test and the reference were as follows ： Cmax were （3.09 ＋ 1.57） ng. ml - 1 and （ 3.48 ± 1.95 ） ng. ml - 1 ; tmax were （ 1. 68 ± 0. 96 ） h and （ 1. 31 ± 0. 74 ） h ; t1/2 were （5.65 ＋2.48）h and （5.47±2.55）h;AUC0-24h were （12.52 ±5.59） ng.m1-1 . h and （12.80 ±5.07） ng.ml-1. h;AUC0-∞ were （13.41 ±5.95） ng.m1-1 . h and （13.70±＋5.24） ng.m1-1. h, respectively. The relative bioavailability of the test drug was 99. 0% ±23.9%. Conclusion： The two preparations are bioequivalent.

关 键 词：辛伐他汀 LC—MS/MS 药物动力学 

分 类 号：R969.1[医药卫生—药理学]