硝呋太尔片在健康人体内的药动学研究  

Study on pharmacokinetics of nifuratel tablets in healthy volunteers

作　　者：周艺佳 唐静雅[1] 侯媛媛[1] 陈明[2] 孙璐[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016 [2]西南科技大学材料科学与工程学院,四川绵阳621010

出　　处：《沈阳药科大学学报》2015年第2期141-147,共7页Journal of Shenyang Pharmaceutical University

摘　　要：目的考察单剂量经口给予硝呋太尔片后健康人体内硝呋太尔的药动学特征,比较国内外制剂间的生物等效性。方法健康男性志愿者18名,采用双周期自身交叉对照法经口给予硝呋太尔片受试制剂(国内制剂)与参比制剂(国外原研制剂)。观察不良事件;LC-MS/MS法测定血浆中硝呋太尔的质量浓度,计算药动学参数。结果 18例健康志愿者分别经口给予硝呋太尔片受试制剂和参比制剂后,血浆中硝呋太尔的tmax分别为(2.42±0.67)h和(2.42±0.75)h;ρmax分别为(12.39±7.10)μg·L-1和(12.43±8.07)μg·L-1;t1/2分别为(1.19±0.42)h和(1.28±0.44)h;AUC0-t分别为(33.68±17.09)μg·h·L-1和(33.54±18.37)μg·h·L-1;AUC0-∞分别为(34.03±17.26)μg·h·L-1和(33.84±18.43)μg·h·L-1。以AUC0-t计算,与参比制剂相比,受试制剂中硝呋太尔的相对生物利用度为(102.4±17.0)%。结论硝呋太尔在人体内的个体差异性较大,药动学特征符合二室模型,国产的硝呋太尔片与国外原研制剂具有人体生物等效性。Objective To study pharmacokinetics profile of healthy volunteers after a single dose oral nifuratel tablets.Methods Eighteen male healthy volunteers were administered with an oral single dose of test（domestic preparation） and reference（imported preparation） tablets of nifuratel.Adverse events were observed,and LC-MS / MS method was used for the determination of the plasma concentration of nifuratel,and the pharmacokinetic parameters were calculated.Results Eighteen subjects were selected,and the single oral administration of 0.4 g of test and reference tablets of nifuratel were given.The tmaxwere（2.42 ± 0.67） and （2.42 ± 0.75） h; the ρmaxwere（12.39 ± 7.10） and（12.43 ± 8.07） μg·L^-1; t1 /2 were （1.19 ± 0.42） and （1.28 ± 0.44） h; AUC0-t were （33.68 ± 17.09） and （33.54 ± 18.37） μg·h·L^-1; AUC0-∞ were （34.03 ±17.26） and（33.84 ± 18.43） μg·h·L^-1.The relative bioavailability was（102.4 ± 17.0） %.Conclusions There exist significant individual differences for nifuratel in human plasma,and the pharmacokinetic process is in accordance with two-compartment model.The test preparations are bioequivalent to the reference preparations.

关 键 词：硝呋太尔 药动学 生物等效性 

分 类 号：R971[医药卫生—药品]