左乙拉西坦片在中国成年健康志愿者的生物等效性及安全性评价  

Bioequivalence and safety evaluation of levetiracetam tablets in healthy volunteers

作　　者：王淑民[1] 周辉[1] 郭韶洁[1] 武峰[1] 倪四阳[1] 赵秀丽[1] 产运霞 耿玉先 

机构地区：[1]首都医科大学附属北京同仁医院国家药物临床试验机构,北京100730 [2]北京万生药业有限责任公司研发部,北京101113

出　　处：《中国临床药理学杂志》2015年第14期1411-1414,共4页The Chinese Journal of Clinical Pharmacology

基　　金：国家科技重大专项课题"重大新药创制"专项基金资助项目(2011ZX09302-007-05)

摘　　要：目的探讨两种左乙拉西坦片在健康人体内的药代动力学行为,并评价两种制剂间的生物等效性。方法 20名健康成年男性受试者随机分为2组,每组10名,分别交叉单剂量口服左乙拉西坦片试验药物或参比药物0.5 g,2次给药间隔1周。用LC/MS/MS法测定血浆中左乙拉西坦浓度,用Win Nonlin 6.3计算药代动力学参数。结果受试者口服试验药物和参比药物后,左乙拉西坦的主要药代动力学参数如下:t1/2分别为(8.01±1.16),(8.02±0.93)h,tmax分别为(0.61±0.41),(0.76±0.61)h,Cmax分别为(13.65±2.63),(13.15±2.30)μg·m L-1,AUC0-t分别为(115.84±12.75),(119.29±15.29)μg·m L-1·h,AUC0-∞分别为(121.44±15.17),(124.89±16.73)μg·m L-1·h。试验药物和参比药物AUC0-t相对生物利用度是(97.55±7.06)%。试验期间未发生严重不良事件。结论受试药物和参比药物具有生物等效性。Objective To study pharmacokinetic behaviors of the Chinese healthy volunteers and to evaluate the bioequivalence of two kinds of levetiracetam tablets. Methods Twenty healthy male volunteers were randomly divided into two groups,each group 10 cases,they were orally respectively administrated with single dose of treatment and reference preparations of levetiracetam（ each 0. 5 g）. The cleaning period was one week. The concentration of levetiracetam in human plasma was measured by LC / MS / MS. Main pharmacokinetic parameters were calculated by using Win Nonlin 6. 3 software. Results Main pharmacokinetic parameters of test and reference preparation were as follow： t1 /2were（ 8. 01 ± 1. 16）,（ 8. 02 ± 0. 93） h,tmaxwere（ 0. 61 ± 0. 41）,（ 0. 76 ± 0. 61） h,Cmaxwere（ 13. 65 ± 2. 63）,（ 13. 15 ± 2. 30）μg·m L-1,AUC0-twere（ 115. 84 ± 12. 75）,（ 119. 29 ± 15. 29）μg·m L-1·h,AUC0-∞were（ 121. 44 ± 15. 17）,（ 124. 89 ± 16. 73）μg·m L-1·h,respectively. The relative bioavailability of test preparation was（ 97. 55 ± 7. 06） %. Conclusion Two kinds of levetiracetam tablets are bioequivalent.

关 键 词：左乙拉西坦 生物等效性 安全性评价 

分 类 号：R971.6[医药卫生—药品]