甲磺酸伊马替尼片在中国健康男性受试者的生物等效性研究

发布时间：2018-03-09 09:34

  本文选题：甲磺酸伊马替尼　切入点：LC-MS/MS　出处：《中国临床药理学杂志》2017年07期 　论文类型：期刊论文

【摘要】：目的评价2种甲磺酸伊马替尼片在中国健康男性受试者的生物等效性。方法用单剂量、开放、随机、双周期交叉设计。30名健康男性受试者随机分为2组,单次口服伊马替尼受试制剂与参比制剂400 mg,用LC-MS/MS法测定血浆中伊马替尼血药浓度,用WinNonlin6.3软件按非房室模型计算药代动力学参数,并进行生物等效性评价。结果单次口服伊马替尼受试制剂与参比制剂400 mg后的药代动力学参如下:C_(max)分别为(1840.00±749.00),(1950.00±635.00)ng·mL~(-1);t_(max)分别为(2.98±1.41),(2.38±0.94)h;t_(1/2)分别为(15.80±3.39),(15.30±3.02)h;AUC_(0-t)分别为(30.60±9.57),(32.00±8.23)mg·mL~(-1)·h;AUC_(0-∞)分别为(31.90±10.20),(33.20±8.46)mg·mL~(-1)·h。2种制剂的AUC_(0-t)、AUC_(0-∞)及C_(max)经对数转换后90%可信区间分别为89.00%~100.50%,89.00%~100.90%和86.30%~100.60%。受试制剂对于参比制剂的平均相对生物利用度:AUC_(0-t)为(96.20±17.20)%,AUC_(0-∞)为(96.60±17.90)%,均90%。结论 2种甲磺酸伊马替尼片在中国健康男性受试者体内具有生物等效性。
[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 卤749.00 (1950.00 卤635.00 ng 路mL ~ (-1)): 2.98 卤1.41 ~ (1) 卤0.94 h ~ (-1) respectively. The pharmacokinetic parameters were 15.80 卤3.39 ~ 15.30 卤3.02hC ~ (-1) respectively. The pharmacokinetic parameters were 30.60 卤9.57 mg 路mL ~ (-1) ~ (-1) AUT respectively.) the AUT was 31.90 卤33.20 卤8.4610.20 卤8.4610.20 卤8.46 ~ (-1) mg 路mL ~ (-1) C ~ (-1) C ~ (+ 0) ~ (-1). The pharmacokinetic parameters of AUC were 30.60 卤9.57 卤8.23mg 路mL ~ (-1) mg 路mL ~ (-1) ~ (-1) ~ (-1) ~ (-1)) respectively. The pharmacokinetic parameters were respectively 30.60 卤9.57 卤8.23mg 路mL ~ (-1) 路h ~ (-1) ~ (-1) (AUT = 31.90 卤33.20 卤8.4610.20 卤8.46 ~ (-1) mg 路mL ~ (-1) ~ (-1)) respectively. The pharmacokinetic parameters of the study were 30.60 卤9.57 卤8.23mg 路mL ~ (-1) 路h ~ (-1). The mean relative bioavailability of the tested preparations for reference preparations was 96.20 卤17.20 AUC0- 鈭，

本文编号：1587962