茴拉西坦胶囊在中国健康志愿者体内的生物等效性  

Bioavailability of aniracetam capsules in Chinese healthy volunteers

作　　者：姜慧芳[1] 陈斌艳[1] 魏志军[1] 梁欣[1] 程能能[1] 李雪宁[2] 

机构地区：[1]复旦大学药学院药理学教研室,上海200032 [2]复旦大学附属中山医院国家药品临床研究基地,上海200032

出　　处：《中国临床药学杂志》2005年第3期155-158,共4页Chinese Journal of Clinical Pharmacy

摘　　要：目的研究2种茴拉西坦胶囊在中国健康志愿者体内的生物等效性。方法20位健康男性受试者,采用开放、随机、双周期交叉、自身对照试验方法,单剂量口服茴拉西坦胶囊受试制剂或参比制剂各400mg,以HPLC法测定茴拉西坦活性代谢产物对甲氧基苯甲酰氨基丁酸(ABA)血药浓度,用DBPP2.0程序进行ABA药动学参数计算和2种茴拉西坦胶囊的等效性检验。结果口服400mg受试制剂或参比制剂后,其主要活性代谢物ABA的血浆tmax分别为(38.4±16.9)和(33.4±11.1)min;T1/2分别为(30.65±11.91)和(34.29±13.01)min;cmax分别为(9.80±3.31)和(9.39±3.28)mg·L-1;AUC0→t分别为(575.53±133.41)和(566.82±149.27)mg·min·L-1,AUC0→∞分别为(600.50±140.40)和(597.39±154.27)mg·min·L-1。对两种制剂血浆茴拉西坦代谢物ABA的AUC0→t、cmax及tmax的等效性检验均显示2种茴拉西坦胶囊为生物等效制剂。结论2种茴拉西坦胶囊为生物等效制剂。AIM To study the bioavailability of two kinds of aniracetam capsules in Chinese healthy volunteers. METHODS An open randomized two-period crossover self-control trial was conducted to 20 healthy male volunteers. Concentration of 4-p-anisamidobutyric acid(ABA),the main active metabolite of aniracetam capsules in plasma,was assayed by HPLC after a single oral 400 mg that for test or reference. The main pharmacokinetic parameters(AUC, c max,and t max)were analyzed by DBPP 2.0 program. RESULTS After taking a single oral dose of 400 mg test and reference,the c max,t max,AUC 0→t and AUC 0→∞ of tested and referenced were (9.80±3.31) and (9.39±3.28)mg·L -1, (38.4±16.9) and(33.4±11.1)min, (575.53±133.41)and(566.82±149.27)mg·min·L -1,(600.50±140.40)and(597.39±154.27)mg·min·L -1,respectively.The results of statistical analysis showed that there were no significant differences in the AUC 0→t,c max and t max of ABA between the formulations. CONCLUSION The two aniracetam capsules are bioequivalent.

关 键 词：茴拉西坦 生物等效性 对甲氧基苯甲酰氨基丁酸 

分 类 号：R96[医药卫生—药理学]