进食对健康受试者口服盐酸艾咪朵尔片剂药动学的影响

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

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ρmax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AUC0-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ρmax和AUC0～t分别为空腹状态的40.61%和57.75%,而tmax、t1/2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。

ABSTRACT ： OBJECTIVE To study the differences of pharmadokinetics of imidol hydrochloride administered with food and in fas- ted 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 imidl fit- ted to two compartment model and the pharmacokinetic parameters were ：Pm~ （472. 59 ± 455. 09） and （1 163.78 ±557. 67 ）ng mL, tmx（1.3±1.1） and （0.73±0.22） h, tl/2（12.02 ±7.51） and （7.44 ±3.39） h, AUCo-t,（945.5 711.44） and （ 1 636. 93 ：i： 706. 34） ng mL^-1 . h^-1 , respectively. Pmax and AUCo-t of imidol administered with food iwere 40. 61% and 57.75 % of that in fasted state, respectively. CONCLUSION Food affects the exposure of imidol. It is suggested that imidol should be taken in fasted state.