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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。
Objective To compare the pharmacokinetics of oral amiloride hydrochloride in Chinese healthy subjects under both fasting and fasting conditions. Methods A randomized crossover dosing regimen was given to 10 healthy subjects taking 400mg omeprazole hydrochloride orally in a fasting and single oral dose. The plasma concentrations of amiloride were determined by high performance liquid chromatography-tandem mass spectrometry (DAS2). 0 software to calculate the main pharmacokinetic parameters, t test to compare the differences between groups. Results The fasting and postprandial single-dose pharmacokinetic curves were in accordance with the two-compartment model. The main pharmacokinetic parameters of 10 mg of omeprazole hydrochloride in 10 healthy subjects under oral and fasting conditions were ρmax (472.59 ± 455.09) and (1 163.78 ± 557.67) ng.mL-1 respectively, the peak time tmax was (1.3 ± 1.1) and (0.73 ± 0.22) h respectively, and the elimination half-life t1 / 2 was (12.02 ± 7.51 ) And (7.44 ± 3.39) h respectively. The area under the drug-time curve was (945.5 ± 711.44) and (1636.93 ± 706.34) ng.mL-1.h-1, respectively. The ρmax and AUC0 ~ t of the fed state were 40.61% and 57.75% of the fasting state, respectively, while tmax and t1 / 2 had no significant difference. Conclusion The intake of Amidol absorption, clinical use of the drug should be taken on an empty stomach.