Siegmund W, Zschiesche M, Franke G, Peters R, Brachmann O, Scherber A
Institut für Klinische Pharmakologie, Bereich Medizin der Ernst-Moritz-Arndt-Universität Greifswald.
Pharmazie. 1988 Aug;43(8):546-8.
2 and 4 g isometronidazole, respectively, were administered to two groups of 6 healthy male volunteers (21-29 years, 62-93 kg). The unchanged compound and its nitro group containing metabolites were measured by HPLC and polarography. Isometronidazole was absorbed rapidly, distributed slowly into peripheral compartments and eliminated with half lives of about 12 h. It was not bound to plasma proteins. On an average 70% (2 g) and 80% (4 g), respectively, were excreted into urine within 48 h both unchanged and in form of at least two more polar and/or water soluble metabolites. Distribution and excretion of isometronidazole were not proportional to dose.
分别向两组6名健康男性志愿者（年龄21 - 29岁，体重62 - 93千克）给予2克和4克的甲硝唑。通过高效液相色谱法和极谱法测定未变化的化合物及其含硝基的代谢产物。甲硝唑吸收迅速，缓慢分布到外周隔室，消除半衰期约为12小时。它不与血浆蛋白结合。平均而言，48小时内分别有70%（2克）和80%（4克）以未变化的形式以及至少两种极性更强和/或水溶性代谢产物的形式排泄到尿液中。甲硝唑的分布和排泄与剂量不成比例。
