进食对健康受试者口服盐酸艾咪朵尔片剂药动学的影响

 目的 比较研究在进食和空腹状态下中国健康受试者口服盐酸艾咪朵尔的药动学。方法 采用随机交叉给药方案，10名健康受试者进食或空腹单剂量口服400 mg盐酸艾咪朵尔，用高效液相色谱-串联质谱法测定血浆中艾咪朵尔的浓度，用DAS2.0 软件计算其主要药动学参数，t检验比较组间差异。结果 空腹和餐后单剂量给药的药时曲线均符合二室模型， 10 名健康受试者在进食和空腹状态下单次口服盐酸艾咪朵尔400 mg的主要药动学参数峰浓度ρ_max分别为(472.59±455.09)和(1 163.78±557.67) ng·mL-1，达峰时间tmax分别为 (1.3±1.1)和 (0.73±0.22) h，消除半衰期t1/2 分别为 (12.02±7.51)和 (7.44±3.39) h，药-时曲线下面积AUC_0-t 分别为 (945.5±711.44) 和 (1 636.93±706.34) ng·mL-1·h-1。进食状态下的ρ_max和AUC_0～t分别为空腹状态的40.61%和 57.75%，而t_max、t_1/2无显著性差异。结论 进食影响艾咪朵尔的吸收量，临床使用该药物时宜空腹服用。

Influence of Food Intake on Pharmacokinetics of Imidol Hydrochloride Tablet in Healthy Subjects

OBJECTIVE To study the differences of pharmacokinetics of imidol hydrochloride administered with food and in fasted state in healthy Chinese volunteers.METHODS Ten healthy volunteers were given imidol hydrochloride tablet 400 mg with food or in fasted state by a random crossover study design.The concentration of imidol in human plasma was determined by HPLC-MS/MS.The main pharmacokinetic parameters were calculated with DAS2.0 software.RESULTS The concentration-time profile of imidol fitted to two compartmen...