Lawrenz A, Eglit S, Kroker R
Bundesgesundheitsamt, Robert-von-Ostertag-Institut, Berlin.
Dtsch Tierarztl Wochenschr. 1992 Oct;99(10):416-8.
Pharmacokinetic studies on Albendazole after peroral administration demonstrate a rapid and complete biotransformation. The major metabolites Albendazole sulphoxide and -sulphone were detected in the plasma; the parent compound was only found sporadically at very low levels. These results indicate removal by the liver and/or the gut at first pass. After evidence is found that the liver has the capacity to sulphoxidize and to sulphonize Albendazole, biotransformation of the gut was examined using an isolated perfused rat gut model. A high-performance liquid chromatography method was used to simultaneously determinate Albendazole, -sulphoxide and -sulphone. Albendazole was biotransformed partly to Albendazole sulphoxide by the gut, whereby the metabolite but not the parent compound was absorbed. It is concluded, that the gut has the capacity to biotransform Albendazole. However, biotransformation is limited to the first step, the sulphoxidation.
阿苯达唑口服给药后的药代动力学研究表明其具有快速且完全的生物转化过程。在血浆中检测到主要代谢产物阿苯达唑亚砜和砜；母体化合物仅偶尔在极低水平被发现。这些结果表明其在首次通过肝脏和/或肠道时被清除。在发现肝脏有能力将阿苯达唑进行亚砜化和砜化后，使用离体灌注大鼠肠道模型对肠道的生物转化进行了研究。采用高效液相色谱法同时测定阿苯达唑、亚砜和砜。肠道可将阿苯达唑部分生物转化为阿苯达唑亚砜，代谢产物而非母体化合物被吸收。得出的结论是，肠道具有生物转化阿苯达唑的能力。然而，生物转化仅限于第一步，即亚砜化。
