硝呋太尔片在健康人体内的药动学研究

发布时间：2018-03-21 04:32

本文选题：硝呋太尔　切入点：药动学　出处：《沈阳药科大学学报》2015年02期 　论文类型：期刊论文

【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。
[Abstract]:Objective to investigate the pharmacokinetic characteristics of nifurataxel in healthy volunteers after a single dose of nifurataxel tablets, and to compare the bioequivalence between domestic and foreign preparations. Methods 18 healthy male volunteers were enrolled in this study. A double-cycle self-crossover control method was used to determine the mass concentration of nifuretol in plasma by oral administration of nitrafurate tablet (domestic preparation) and reference preparation (foreign original preparation). The adverse events were observed by LC-MS / MS method. Results the pharmacokinetic parameters were calculated in 18 healthy volunteers. The tmax of nifurotrel in plasma was 2.42 卤0.67 h and 2.42 卤0.75 h, 蟻 max was 12.39 卤7.10 渭 g 路L -1 and 12.43 卤8.07 渭 g 路L -1 路L -1, respectively 1.19 卤0.42 h and 1.28 卤0.44 h AUC0-t were 33.68 卤17.09 渭 g 路h 路L -1 and 33.54 卤18.37 渭 g 路h 路h 路L -1, respectively, and 蟻 max were 34.03 卤17.26 渭 g 路h 路L -1 and 33.84 卤18.43 渭 g 路h 路L -1 respectively. The relative bioavailability of nifurotael was 102.4 卤17.00.ConclusionThe pharmacokinetic characteristics of nifuterol in human body are quite different, and the pharmacokinetic characteristics are in accordance with the two-compartment model.
【作者单位】：沈阳药科大学药学院;西南科技大学材料科学与工程学院;
【分类号】：R96

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