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目的研究阿折地平(抗高血压药)在健康人体的药代动力学。方法 24名健康受试者分为3组,单次口服高、低(16,8 mg)2个剂量组和多次口服剂量组(每天服药1次,每次8 mg,连续服药7 d)。用液相串联质谱法测定血浆中阿折地平的血药浓度变化,药代动力学参数以SPSS 13.0软件求算。结果阿折地平高、低剂量组及多次给药组的代谢参数如下:Cmax分别为(10.61±3.93),(5.91±2.83)和(5.88±1.90)μg.L-1;Tmax分别为(3.67±0.99),(3.33±1.30)和(3.17±0.72)h;t1/2分别为(28.00±7.72),(20.34±7.60)和(28.17±7.93)h;AUC0-t分别为(139.50±72.90),(61.17±33.78)和(86.72±41.59)μg.h.L-1。多次给药的稳态AUCss(55.54±18.78)μg.h.L-1。健康受试者口服阿折地平片8,16 mg后,主要药代动力学参数除t1/2外,AUC0-t/D、AUC0-∞/D、Cmax/D在2个剂量组间均无统计学差异。多次给药t1/2与单次给药t1/2相比有所升高,CLz/F略有下降,具有统计学意义(P<0.05)。结论阿折地平在中国健康人体内在8～16 mg内呈线性药代动力学特征;本品每天给药1次,在中国人体内几无蓄积作用。
AIM To study the pharmacokinetics of azuridine (antihypertensive) in healthy volunteers. Methods Twenty-four healthy volunteers were divided into three groups: single oral high and low (16,8 mg) 2 dose groups and multiple oral dose groups (8 mg once daily for 7 days) . The plasma concentration of Azadirachtin in plasma was determined by liquid chromatography-tandem mass spectrometry. Pharmacokinetic parameters were calculated by SPSS 13.0 software. Results Metabolic parameters of high, low dose and multiple dose groups were as follows: Cmax were (10.61 ± 3.93), (5.91 ± 2.83) and (5.88 ± 1.90) μg.L-1 respectively; Tmax was 3.27 ± 0.99, 3.33 ± 1.30 and 3.17 ± 0.72 h respectively; t1 / 2 was (28.00 ± 7.72), (20.34 ± 7.60) and (28.17 ± 7.93) h respectively; AUC0-t was 72.90), (61.17 ± 33.78) and (86.72 ± 41.59) μg.hL-1. The steady-state AUCss was administered multiple times (55.54 ± 18.78) μg.h.L-1. After oral administration of 8mg of aztrendipine tablets, the main pharmacokinetic parameters of healthy subjects except t1 / 2, AUC0-t / D, AUC0-∞ / D, Cmax / D in the two dose groups were Statistical differences. Multiple administration of t1 / 2 and single administration of t1 / 2 increased, CLz / F decreased slightly, with statistical significance (P <0.05). Conclusion Aztrendin has a linear pharmacokinetic profile within 8-16 mg in Chinese healthy people. The product is administered once a day and has few accumulation in Chinese human body.