辛伐他汀口腔崩解片的人体生物等效性研究

Bioequiavailability of Simvastatin Orally Disintegrating Tablets in Healthy Volunteers

目的:比较2种辛伐他汀制剂的人体生物等效性。方法:18名健康男性志愿者随机交叉单剂量口服辛伐他汀口腔崩解片(受试制剂)与辛伐他汀片(参比制剂)40mg,用液-质联用法测定人血浆中药物浓度,并用3p97软件计算药动学参数和生物利用度。结果:2种辛伐他汀制剂在人体内药-时曲线符合一室模型,受试制剂与参比制剂的Cmax分别为(6.73±5.22)、(7.08±5.41)ng·mL-1,tmax分别为(2.11±0.74)、(1.89±0.85)h,AUC0～12分别为(19.83±19.09)、(19.98±18.20)ng·h·mL-1,AUC0～∞分别为(22.18±20.09)、(22.41±21.07)ng·h·mL-1。受试制剂相对于参比制剂的生物利用度为(99.25±13.11)%。结论:2种辛伐他汀制剂具有生物等效性。

OBJECTIVE：To compare the bioequiavailability of two simvastatin preparations in human bodies.METHODS： A total of 18 healthy male volunteers were enrolled in a randomized crossover study in which the subjects were randomly assigned to receive single dose of 40mg simvastatin orally disintegrating tablet（test） or simvastatin tablets（reference） .The plasma concentrations of simvastatin were determined by LC- MS, and the pharmacokinetic parameters and bioavailability were calculated with 3p97 program.RESULTS： The pharmacokinetics of simvastatin test and reference preparations were fitted the one - compartment model. The main pharmacokinetic parameters of the two preparations were as following： Cmax ： （6.73 ± 5.22） vs. （7.08±5.41） ng·mL^-1、tmax （2.11±0.74）vs. （1.89 ±0.85）h, AUC0 -12： （19.83±19.09）vs. （19.98±18.20） ng · h · mL^-1, AUC0-∞： （22.18±20.09）vs. （22.41 ± 21.07）ng · h · mL^-1. The relative bioavailability of simvastatin orally disintegrating tablet as against simvastain tablet（reference） was （99.25±13.11）% .CONCLUSION： Simvastatin test and reference preparations were bioequivalent.