Aufrère M B, Hoener B A, Vore M
Drug Metab Dispos. 1978 Jul-Aug;6(4):403-11.
The reductive metabolism of nitrofurantoin under anaerobic conditions was characterized in various tissues from control, germ-free, and germ-free acclimatized rats. Nitrofurantoin metabolism was highest in homogenates of cecum and colon contents of germ-free acclimatized and control rats, but was absent from those of germ-free animals. Appreciable levels of activity were also present in homogenates of liver and of small intestine walls with lesser rates of metabolism observed in kidney homogenates. The major metabolite of nitrofurantoin, which was isolated and purified by high-pressure liquid chromatography, was identified as 1-[[(3-cyano-1-oxopropyl)-methylene]amino]-2,4-imidazolidinedione. A second, minor metabolite with high-pressure liquid chromatography and ultraviolet absorption characteristics similar to those of 1-[[(5-amino-2-furanyl)methylene]amino]-2,4-imidazolidinedione (aminofurantoin) was detected in cecum and colon contents.
在厌氧条件下，对来自对照大鼠、无菌大鼠和无菌适应大鼠的各种组织中呋喃妥因的还原代谢进行了表征。在无菌适应大鼠和对照大鼠的盲肠和结肠内容物匀浆中，呋喃妥因代谢最为活跃，但在无菌动物的这些组织中则没有代谢活性。肝脏和小肠壁匀浆中也存在相当水平的活性，而在肾脏匀浆中观察到的代谢速率较低。通过高压液相色谱法分离和纯化得到的呋喃妥因主要代谢产物被鉴定为1-[[(3-氰基-1-氧代丙基)-亚甲基]氨基]-2,4-咪唑烷二酮。在盲肠和结肠内容物中检测到了第二种次要代谢产物，其具有与1-[[(5-氨基-2-呋喃基)亚甲基]氨基]-2,4-咪唑烷二酮（氨基呋喃妥因）相似的高压液相色谱和紫外吸收特征。
