布洛芬缓释混悬液空腹和餐后给药的人体生物等效性研究

发布时间：2018-04-20 10:16

本文选题：布洛芬 + 缓释混悬液　；参考：《中国药房》2015年11期

【摘要】：目的:研究健康受试者空腹和餐后两种状态下单剂量口服布洛芬缓释混悬液受试制剂与参比制剂的生物等效性。方法:本研究包括两个随机、开放、双周期、单剂量给药试验,各入组24名健康受试者,分别空腹和餐后单剂量交叉口服600 mg(20 ml)布洛芬混悬液受试制剂与参比制剂,采用液相色谱-串联质谱(LC-MS/MS)法测定给药后血浆中布洛芬的浓度。结果:空腹给药条件下受试制剂与参比制剂的主要药动学参数中t1/2分别为(4.27±1.42)和(3.87±1.03)h;tmax分别为(3.42±0.72)和(3.29±0.93)h;cmax分别为(27.4±4.33)和(28.2±4.65)μg/ml;AUC0-t分别为(167±30.1)和(172±28.8)μg·h/ml;受试制剂的相对生物利用度为(97.4±9.7)%。餐后给药条件下受试制剂与参比制剂的主要药动学参数中t1/2分别为(2.53±0.46)和(2.64±0.53)h;tmax分别为(3.63±0.99)和(3.44±1.15)h;cmax分别为(25.0±4.12)和(27.0±4.60)μg/ml;AUC0-t分别为(172±33.4)和(184±30.2)μg·h/ml;受试制剂的相对生物利用度为(93.1±5.7)%。两种给药条件下的受试制剂与参比制剂AUC0-t和cmax几何均值比的90%置信区间(CI)均落在80%~125%之间。结论:布洛芬缓释混悬液受试制剂与参比制剂在空腹和餐后两种状态下均具有生物等效性。
[Abstract]:Aim: to study the bioequivalence of oral ibuprofen sustained-release suspension test preparation and reference preparation in healthy volunteers at fasting and postprandial states. Methods: the study consisted of two randomized, open, double-cycle, single-dose drug administration trials. 24 healthy volunteers were enrolled in the study. They were given 600 mg(20 / ml ibuprofen suspension at fasting and postprandial levels, respectively, and ibuprofen suspension test and reference preparation were used to evaluate the efficacy of ibuprofen suspension. The concentration of ibuprofen in plasma after administration was determined by liquid chromatography-tandem mass spectrometry (LC-MS / MS). The 90% confidence interval (CI) of the geometric mean ratios of AUC0-t and cmax between the tested and reference preparations fell between 80% and 125%. Conclusion: ibuprofen sustained-release suspension and reference preparation have bioequivalence in both fasting and postprandial states.
【作者单位】：上海中医药大学附属曙光医院临床药理科;上海药物代谢研究中心;扬州市三药制药有限公司;
【基金】：“十二五”重大新药创制《创新药物研究开发技术平台建设》(No.2012ZX09303009-001) 上海市进一步加快中医药事业发展三年行动计划(2014-2016年)中医药专门人才计划(No.ZY3-RCPY-3-1059)
【分类号】：R969.1

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