本文選題：甲磺酸伊馬替尼　切入點：LC-MS/MS　出處：《中國臨床藥理學(xué)雜志》2017年07期 　論文類型：期刊論文

【摘要】：目的評價2種甲磺酸伊馬替尼片在中國健康男性受試者的生物等效性。方法用單劑量、開放、隨機、雙周期交叉設(shè)計。30名健康男性受試者隨機分為2組,單次口服伊馬替尼受試制劑與參比制劑400 mg,用LC-MS/MS法測定血漿中伊馬替尼血藥濃度,用WinNonlin6.3軟件按非房室模型計算藥代動力學(xué)參數(shù),并進(jìn)行生物等效性評價。結(jié)果單次口服伊馬替尼受試制劑與參比制劑400 mg后的藥代動力學(xué)參如下:C_(max)分別為(1840.00±749.00),(1950.00±635.00)ng·mL~(-1);t_(max)分別為(2.98±1.41),(2.38±0.94)h;t_(1/2)分別為(15.80±3.39),(15.30±3.02)h;AUC_(0-t)分別為(30.60±9.57),(32.00±8.23)mg·mL~(-1)·h;AUC_(0-∞)分別為(31.90±10.20),(33.20±8.46)mg·mL~(-1)·h。2種制劑的AUC_(0-t)、AUC_(0-∞)及C_(max)經(jīng)對數(shù)轉(zhuǎn)換后90%可信區(qū)間分別為89.00%~100.50%,89.00%~100.90%和86.30%~100.60%。受試制劑對于參比制劑的平均相對生物利用度:AUC_(0-t)為(96.20±17.20)%,AUC_(0-∞)為(96.60±17.90)%,均90%。結(jié)論 2種甲磺酸伊馬替尼片在中國健康男性受試者體內(nèi)具有生物等效性。
[Abstract]:Objective to evaluate the bioequivalence of two kinds of imatinib mesylate tablets in Chinese healthy male subjects. The concentration of imatinib in plasma was determined by LC-MS/MS method. The pharmacokinetic parameters were calculated by WinNonlin6.3 software according to non-atrioventricular model. Results the pharmacokinetic parameters of imatinib test preparation and reference preparation were as follows: 1849 鹵749.00 (1950.00 鹵635.00 ng 路mL ~ (-1)): 2.98 鹵1.41 ~ (1) 鹵0.94 h ~ (-1) respectively. The pharmacokinetic parameters were 15.80 鹵3.39 ~ 15.30 鹵3.02hC ~ (-1) respectively. The pharmacokinetic parameters were 30.60 鹵9.57 mg 路mL ~ (-1) ~ (-1) AUT respectively.) the AUT was 31.90 鹵33.20 鹵8.4610.20 鹵8.4610.20 鹵8.46 ~ (-1) mg 路mL ~ (-1) C ~ (-1) C ~ (+ 0) ~ (-1). The pharmacokinetic parameters of AUC were 30.60 鹵9.57 鹵8.23mg 路mL ~ (-1) mg 路mL ~ (-1) ~ (-1) ~ (-1) ~ (-1)) respectively. The pharmacokinetic parameters were respectively 30.60 鹵9.57 鹵8.23mg 路mL ~ (-1) 路h ~ (-1) ~ (-1) (AUT = 31.90 鹵33.20 鹵8.4610.20 鹵8.46 ~ (-1) mg 路mL ~ (-1) ~ (-1)) respectively. The pharmacokinetic parameters of the study were 30.60 鹵9.57 鹵8.23mg 路mL ~ (-1) 路h ~ (-1). The mean relative bioavailability of the tested preparations for reference preparations was 96.20 鹵17.20 AUC0- 鈭，

本文編號：1587962