莫雷西嗪在人体内的药动学及其生物等效性研究

Pharmacokinetics and bioequivalence of Moricizine tablets in healthy volunteers

目的观察18名健康志愿者单剂量po两种莫雷西嗪片后血药浓度的经时过程,并评价其生物等效性。方法采用HPLC法测定受试者血浆中莫雷西嗪的浓度,计算其药物动学参数和相对生物利用度,评价两制剂的生物等效性。结果采用3p97计算两制剂的主要药动学参数,Cm ax分别为1.499±0.173、1.537±0.174 mg.L-1;Tm ax分别为1.417±0.192、1.333±0.243 h;t1/2分别为2.671±0.677、2.653±0.625 h;用梯形法计算,AUC0→t分别为6.081±0.995、6.130±0.918 mg.h.L-1;AUC0→∞分别为6.991±1.947、7.210±1.604 mg.h.L-1。结论两种莫雷西嗪片剂具有生物等效性。

OBJECTIVE To observe the concentration - time process of Moricizine tablets in 18 healthy volunteers and evaluate the bioequivalence between two kinds of Moricizine tablets. METHODS Eighteen healthy human volunteers were divided randomly into two groups, and then a crossover single oral dose of 200 mg Moricizine test tablets and reference one were delivered, respectively. The plasma concentrations of Moricizine were determined by HPLC method. The pharmacokinetic parameter and relative bioavailability were calculated to evaluate the hioequivalenee of the two preparations. RESULTS The main pharmarcokinetic parameters of two preparations calculated by 3p97 software were as follows： Cmax were 1.499±0. 173 and 1.537 ±0. 174 mg·L^-1 ;Tmax were 1.417 ±0. 192 and 1.333±0.243 h; t1/2 were 2.671±0.677 and 2.653±0.625 h;AUC0→1 were 6.081 ±0.995 and 6. 130±0.918 mg · h·L^-1; AUC0→ were 6. 991 ±1. 947 and 7. 210±1. 604 mg · h·L^-1 by using trapezoid method, respectively. CONCLUSION The results show that the 2 preparations are bioeqivalent.