氢溴酸加兰他敏（尼瓦林）在大鼠和兔肝脏匀浆中的体外代谢。
In vitro metabolism of galanthamine hydrobromide (Nivalin) by rat and rabbit liver homogenate.
作者信息
Mihailova D, Velkov M, Zhivkova Z
出版信息
Eur J Drug Metab Pharmacokinet. 1987 Jan-Mar;12(1):25-30. doi: 10.1007/BF03189858.
The metabolism of galanthamine hydrobromide (Nivalin) was investigated in rat and rabbit liver homogenates. Experiments were carried out varying several parameters of incubation: substrate (galanthamine hydrobromide, galanthamine, galanthaminone and epigalanthamine), cofactor enrichment (NADPH, NADP/G-6-P, NAD), pH (7.4 and 9.3), time of incubation. Substrates and metabolites were identified and quantitatively determined by GC/MS. In vitro metabolism in rat liver homogenate was negligible. The experiments with rabbit liver homogenate indicated, that galanthamine was actively metabolised the major metabolites being the oxidised product - galanthaminone, and the isomer of galanthamine - epigalantamine. The experimental results show that the metabolism of galanthamine is substrate and product stereoselective.
在大鼠和兔肝脏匀浆中研究了氢溴酸加兰他敏（尼瓦林）的代谢。通过改变几个孵育参数进行实验：底物（氢溴酸加兰他敏、加兰他敏、加兰他敏酮和表加兰他敏）、辅因子富集（NADPH、NADP/G-6-P、NAD）、pH（7.4和9.3）、孵育时间。通过气相色谱/质谱法鉴定并定量测定底物和代谢物。大鼠肝脏匀浆中的体外代谢可忽略不计。兔肝脏匀浆实验表明，加兰他敏被积极代谢，主要代谢物是氧化产物——加兰他敏酮，以及加兰他敏的异构体——表加兰他敏。实验结果表明，加兰他敏的代谢具有底物和产物立体选择性。
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