【摘要】：目的:研究雙氯芬酸鈉雙釋放腸溶膠囊在健康人體的藥動(dòng)學(xué)參數(shù),評價(jià)其生物等效性。方法:采用隨機(jī)交叉試驗(yàn)設(shè)計(jì),40名健康男性受試者單劑量和多劑量口服雙氯芬酸鈉雙釋放腸溶膠囊受試與參比制劑,用高效液相色譜-串聯(lián)質(zhì)譜法(LC-MS/MS)測定血漿中雙氯芬酸的血藥濃度。結(jié)果:單劑量口服受試和參比制劑的主要藥動(dòng)學(xué)參數(shù)如下:Cmax分別為(708.9±306.8)、(704.7±383.3)ng·ml-1,t1/2分別為(5.86±1.81),(6.20±1.73)h,tmax分別為(1.81±1.58),(1.81±1.58)h,AUC0-24分別為(2 500.0±577.3),(2 355.4±607.4)ng·h·ml-1;多劑量口服受試和參比制劑的主要藥動(dòng)學(xué)參數(shù)如下:Cssmax分別為(594.4±228.4),(622.9±326.7)ng·ml-1,Cssmin分別為(30.1±14.9),(35.7±19.4)ng·ml-1,Cav分別為(96.3±18.2),(92.8±19.9)ng·ml-1,t1/2分別為(6.32±1.40),(6.62±1.50)h,tmax分別為(1.67±1.24),(1.66±1.54)h,AUCss分別為(2 310.3±436.3)、(2 227.5±476.4)ng·h·ml-1,DF值分別為(623.7±325.4)%、(666.2±377.0)%。受試對參比制劑的單劑量和多劑量相對生物利用度F分別為為(108.4±21.3)%和(105.2±15.1)%。結(jié)論:LC-MS/MS法測定人血漿中雙氯芬酸鈉濃度快速、靈敏、專屬性高,受試與參比制劑生物等效。
[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 鹵306.8), (704.7 鹵383.3) ng ml-1,t1/2, respectively (5.86 鹵1.81), (6.20 鹵1.73) ng ml-1,t1/2, (1.81 鹵1.58), (1.81 鹵1.58) AUC0-24, (2 500.0 鹵577.3), (2 355.4 鹵607.4) ng h ml-1;), respectively. (594.4鹵228.4),(622.9鹵326.7)ng路ml-1,Cssmin鍒嗗埆涓，

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