双氯芬酸钠双释放肠溶胶囊的人体生物等效性

发布时间：2018-09-01 21:04

【摘要】：目的:研究双氯芬酸钠双释放肠溶胶囊在健康人体的药动学参数,评价其生物等效性。方法:采用随机交叉试验设计,40名健康男性受试者单剂量和多剂量口服双氯芬酸钠双释放肠溶胶囊受试与参比制剂,用高效液相色谱-串联质谱法(LC-MS/MS)测定血浆中双氯芬酸的血药浓度。结果:单剂量口服受试和参比制剂的主要药动学参数如下:Cmax分别为(708.9±306.8)、(704.7±383.3)ng·ml-1,t1/2分别为(5.86±1.81),(6.20±1.73)h,tmax分别为(1.81±1.58),(1.81±1.58)h,AUC0-24分别为(2 500.0±577.3),(2 355.4±607.4)ng·h·ml-1;多剂量口服受试和参比制剂的主要药动学参数如下:Cssmax分别为(594.4±228.4),(622.9±326.7)ng·ml-1,Cssmin分别为(30.1±14.9),(35.7±19.4)ng·ml-1,Cav分别为(96.3±18.2),(92.8±19.9)ng·ml-1,t1/2分别为(6.32±1.40),(6.62±1.50)h,tmax分别为(1.67±1.24),(1.66±1.54)h,AUCss分别为(2 310.3±436.3)、(2 227.5±476.4)ng·h·ml-1,DF值分别为(623.7±325.4)%、(666.2±377.0)%。受试对参比制剂的单剂量和多剂量相对生物利用度F分别为为(108.4±21.3)%和(105.2±15.1)%。结论:LC-MS/MS法测定人血浆中双氯芬酸钠浓度快速、灵敏、专属性高,受试与参比制剂生物等效。
[Abstract]:Aim: to study the pharmacokinetic parameters of diclofenac sodium double release enteric capsule in healthy volunteers and evaluate its bioequivalence. Methods: a randomized crossover trial was carried out in 40 healthy male subjects to study the effects of oral diclofenac sodium double release enteric-coated capsules on a single dose and multiple doses of diclofenac sodium. The plasma diclofenac concentration was determined by high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS). Results: the main pharmacokinetic parameters of single dose oral test and reference preparations were (708.9 卤306.8), (704.7 卤383.3) ng ml-1,t1/2, respectively (5.86 卤1.81), (6.20 卤1.73) ng ml-1,t1/2, (1.81 卤1.58), (1.81 卤1.58) AUC0-24, (2 500.0 卤577.3), (2 355.4 卤607.4) ng h ml-1;), respectively. (594.4卤228.4),(622.9卤326.7)ng路ml-1,Cssmin鍒嗗埆涓，

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