Kullberg M P, Freeman G B, Biddlecome C, Alousi A A, Edelson J
Clin Pharmacol Ther. 1981 Mar;29(3):394-401. doi: 10.1038/clpt.1981.54.
High-performance liquid chromatographic methods for the analysis of amrinone in plasma and for both amrinone and its N-acetyl metabolite in urine were developed and applied to measure specimens obtained from a number of healthy men who had received intravenous or oral amrinone. The intravenous doses ranged from 0.8 to 2.2 mg/kg. Terminal elimination of amrinone from the bloodstream followed apparent first-order kinetics. Half-life, after the drug had distributed to the tissues, was estimated by a log-linear least-squares regression; mean half-life was 2.6 +/- 1.4 hr. During the first 24 hr after medication, unchanged amrinone excreted in the urine of these subjects represented 10% to 40% of the dose. N-Acetyl metabolite in the urine represented less than 2% of the dose. In the oral study, doses ranged from 25 to 250 mg (0.31 to 3.5 mg/kg) and the maximum plasma concentration attained was proportional to the dose. The first order terminal elimination half-life was possibly dose-related. In only one subject were there unequivocal amounts of the N-acetyl metabolite in the plasma.
建立了用于分析血浆中氨力农以及尿液中氨力农及其N - 乙酰代谢物的高效液相色谱法，并将其应用于检测从多名接受静脉注射或口服氨力农的健康男性身上获取的样本。静脉注射剂量范围为0.8至2.2mg/kg。氨力农从血液中的终末消除遵循明显的一级动力学。在药物分布到组织后，通过对数线性最小二乘回归估计半衰期；平均半衰期为2.6±1.4小时。在用药后的头24小时内，这些受试者尿液中排出的未变化氨力农占剂量的10%至40%。尿液中的N - 乙酰代谢物占剂量的不到2%。在口服研究中，剂量范围为25至250mg（0.31至3.5mg/kg），达到的最大血浆浓度与剂量成正比。一级终末消除半衰期可能与剂量有关。仅在一名受试者的血浆中存在明确量的N - 乙酰代谢物。
