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目的评价伊伐布雷定在中国人群中药代动力学特性。方法将30名健康受试者随机平均分为3组,分别给予2.5、5、7.5 mg伊伐布雷定片,给药后8、15、30、45 min和1、1.5、2、3、4、6、9、12、24、36、48 h分别采集静脉血,并用HPLC-MS/MS法进行血药浓度检测。结果单次口服盐酸伊伐布雷定片后,血浆中伊伐布雷定的t1/2为(4.4±1.0)、(5.2±1.2)、(4.6±1.2)h;C max为(15.1±4.1)、(35.9±8.9)、(48.2±9.6)ng·ml-1;AUC(0～48)为(64.4±14.2)、(169.6±33.1)、(215.6±55.6)ng·h·ml-1;去甲伊伐布雷定的t1/2为(7.9±1.4)、(9.9±1.2、(9.8±1.3)h;C max为(1.8±0.7)、(3.1±1.6)、(6.3±1.0)ng·ml-1;AUC(0～48)为(13.4±2.8)、(23.9±9.4)、(44.1±9.2)ng·h·ml-1。结论 2.5～7.5 mg伊伐布雷定片在中国人群体内代谢呈线性动力学。
Objective To evaluate the Chinese pharmacokinetics of ivabradine in Chinese population. Methods Thirty healthy subjects were randomly divided into three groups randomly and given 2.5, 5, and 7.5 mg of ivabradine at 8, 15, 30, 45 min and 1, 1.5, 2, 3, , 6,9,12,24,36,48 h were collected venous blood, and the use of HPLC-MS / MS blood concentration test. Results After a single oral administration of ivabradine hydrochloride tablets, the t 1/2 of ivabradine in plasma was (4.4 ± 1.0), (5.2 ± 1.2), (4.6 ± 1.2) h, and C max was (15.1 ± 4.1) , (35.9 ± 8.9) and (48.2 ± 9.6) ng · ml-1, respectively. The AUC values were (64.4 ± 14.2), (169.6 ± 33.1) and (215.6 ± 55.6) ng · h · ml- The t1 / 2 of demyavirin was (7.9 ± 1.4), (9.9 ± 1.2, 9.8 ± 1.3) h and Cmax was (1.8 ± 0.7), (3.1 ± 1.6), (6.3 ± 1.0) ng · Ml-1 and AUC (0 ~ 48) were (13.4 ± 2.8), (23.9 ± 9.4) and (44.1 ± 9.2) ng · h · ml- In vivo metabolism is linear kinetics.