Kobayashi A, Sugita S, Nakazawa K
Neuropharmacology. 1985 Dec;24(12):1253-6. doi: 10.1016/0028-3908(85)90162-5.
The simultaneous quantitative determination of amoxapine, 7-hydroxyamoxapine and 8-hydroxyamoxapine in human serum was established, with good recoveries, using reversed-phase high-performance liquid chromatography (HPLC). Prior to analysis by high-performance liquid chromatography, the enzymic hydrolysis with beta-glucuronidase/arylsulphatase of sera from healthy volunteers receiving the drug showed that each conjugate of two hydroxyamoxapines was 75-90% of the amount determined by the present method. The concentrations of amoxapine and its hydroxylated metabolites were measured against time in sera from the volunteers who were given the antidepressant orally for 2 weeks. The serum levels of 8-OH-amoxapine were markedly higher than the drug itself and the 7-OH-derivative. Whereas the levels of the drug were little increased during the continuous administration, the levels of 8-OH-amoxapine were linearly increased until the fourth day after the administration was started. In addition, the ratio of each hydroxylated metabolite to the drug and the time-course of their serum levels varied interindividually.
采用反相高效液相色谱法（HPLC）建立了人血清中阿莫沙平、7-羟基阿莫沙平和8-羟基阿莫沙平的同步定量测定方法，回收率良好。在通过高效液相色谱分析之前，对服用该药物的健康志愿者血清进行β-葡萄糖醛酸酶/芳基硫酸酯酶酶解，结果表明两种羟基阿莫沙平的每种缀合物含量为本法测定量的75 - 90%。对口服抗抑郁药2周的志愿者血清中阿莫沙平及其羟基化代谢物的浓度随时间进行了测定。8-羟基阿莫沙平的血清水平明显高于药物本身及7-羟基衍生物。在连续给药期间，药物水平几乎没有增加，而8-羟基阿莫沙平的水平在开始给药后直至第四天呈线性增加。此外，每种羟基化代谢物与药物的比例及其血清水平的时间进程存在个体差异。
