马来酸替加色罗分散片的人体生物等效性研究

目的:研究马来酸替加色罗分散片的人体生物等效性。方法:22名健康男性志愿者随机交叉单剂量口服马来酸替加色罗分散片(受试制剂)和马来酸替加色罗片(参比制剂)6mg,采用LC/MS/MS法测定人血浆中药物浓度。结果:受试制剂和参比制剂的tmax分别为(0.86±0.22)、(1.01±0.24)h,Cmax分别为(2.21±0.69)、(2.05±0.64)ng.mL-1,AUC0~17分别为(6.35±2.48)和(6.47±1.99)ng.h.mL-1,AUC0~∞分别为(6.69±2.59)、(6.70±2.03)ng.h.mL-1。受试制剂相对于参比制剂的生物利用度为(98.2±22.1)%。结论:两种制剂具有生物等效性。

Assessment on Bioequivalence of Tegaserod Maleate Dispersible Tablets in Human Body

OBJECTIVE: To study the bioequivalence of tegaserod maleate dispersible tablets in healthy volunteers.METHODS: A single oral dose of 6mg test or reference preparations of tegaserod maleate was given to 22 healthy volunteers in a randomized crossover study.The plasma concentrations of tegaserod were determined by LC/MS/MS assay.RESULTS: The main pharmacokinetic parameters of test and reference products were as follows: tmax(0.86± 0.22) and(1. 01± 0.24) h;Cmax(2.21± 0.69) and(2.05± 0.64) ng· mL1;AUC0～ 17(6.35± 2.48) and(6.47± 1.99) ng· h· mL-1,AUC0～ ∞(6.69± 2.59) and(6.70± 2.03) ng· h· mL-1,respectively.The relative bioavailability of test to reference preparation was(98.2± 22.1) %.CONCLUSION: The reference preparation and the test preparation are bioequivalent.