本文選題：艾瑞昔布　切入點(diǎn)：細(xì)胞色素P酶　出處：《中國醫(yī)院藥學(xué)雜志》2017年16期

【摘要】：目的:考察CYP2C9抑制劑胺碘酮對艾瑞昔布在大鼠體內(nèi)藥動(dòng)學(xué)的影響。方法:40只健康雄性SD大鼠隨機(jī)分為2組(n=20),實(shí)驗(yàn)組連續(xù)7 d灌胃胺碘酮灌胃液(40 mg·kg~(-1),qd),對照組灌胃等量空白灌胃液。2組均于第8天單次灌胃艾瑞昔布灌胃液20 mg·kg~(-1),按確定時(shí)間點(diǎn)取血,LC-MS/MS法測定艾瑞昔布血藥濃度,DAS 2.1.1軟件擬合藥時(shí)曲線并計(jì)算藥動(dòng)學(xué)參數(shù),SPSS 13.0軟件進(jìn)行統(tǒng)計(jì)學(xué)分析。結(jié)果:實(shí)驗(yàn)組和對照組的主要藥動(dòng)學(xué)參數(shù)如下:AUC0-24 h分別為(1 814.8±693.4)ng·h·mL~(-1)和(1 125.1±457.6)ng·h·mL~(-1);AUC0-∞分別為(2 091.6±887.1)ng·h·mL~(-1)和(1 331.3±592.6)ng·h·mL~(-1);t1/2分別為(7.8±4.5)h和(7.4±3.8)h;tmax分別為(1.7±0.6)h和(1.46±0.60)h;CL分別為(0.01±0.01)L·h~(-1)·kg~(-1)和(0.02±0.01)L·h~(-1)·kg~(-1);V分別為(0.11±0.05)L·kg~(-1)和(0.17±0.07)L·kg~(-1);Cmax分別為(268.2±115.7)ng·mL~(-1)和(162.2±53.0)ng·mL~(-1)。與對照組相比,實(shí)驗(yàn)組大鼠的AUC0-24 h、AUC0-∞、Cmax顯著增大(P0.05),V、CL顯著減小(P0.05),其他參數(shù)差異無統(tǒng)計(jì)學(xué)意義(P0.05)。結(jié)論:CYP2C9抑制劑(胺碘酮)對艾瑞昔布在大鼠體內(nèi)的藥動(dòng)學(xué)產(chǎn)生影響。
[Abstract]:Objective: to investigate the effect of CYP2C9 inhibitor amiodarone on pharmacokinetics of irixib in rats. Methods: 40 healthy male SD rats were randomly divided into 2 groups. The experimental group was perfused with amiodarone for 7 days and the control group was given intragastric administration of Amiodarone. On the 8th day, 20 mg 路kg ~ (-1) 路L ~ (-1) of eroxib was perfused into gastric juice. The plasma concentration of eroxib was determined by LC-MS / MS method and the time curve was fitted by DAS 2.1.1 software and the pharmacokinetic parameters were calculated by SPSS 13.0 software. Results: the main pharmacokinetic parameters of the experimental group and the control group were as follows: 1 814.8 鹵693.4)ng 路h mL-1 and 1 125.1 鹵887.1)ng h mLLL-1) and 1 331.3 鹵592.6)ng h mLL-1) and 1 331.3 鹵592.6)ng h mLL-1 respectively. The main pharmacokinetic parameters of the experimental group and the control group were 1 814.8 鹵4. 5 h and 7. 7 鹵3. 8 h ~ 0. 6 h and 1. 46 鹵0. 60 h ~ (-1) L ~ (-1) and 0. 02 鹵0. 01 鹵0. 01 h ~ (-1) L ~ (-1) and 0. 11 鹵0. 05 L ~ (-1) ~ (-1) and 0. 11 鹵0. 05 L ~ (-1) L ~ (-1) and 0. 011 鹵0. 05 L ~ (-1) 路kg ~ (-1) C ~ (-1), respectively, of the experimental group and the control group, respectively. The pharmacokinetic parameters of the experimental group and the control group were 1 814.8 鹵0. 6 h and 1. 46 鹵0. 60 h, respectively. The results showed that the pharmacokinetic parameters of the experimental group and the control group were 0. 814.8 鹵0. 01 887.1)ng 路h ~ (-1) and 0. 02 鹵0. 01 887.1)ng h ~ (-1) respectively. They were 268.2 鹵115.7)ng mL-1) and 162.2 鹵53.0)ng mLL-1 respectively. Compared with the control group, there were no significant differences between the control group and the control group. AUC 0- 鈭，

本文編號：1688429