Riad L E, Sawchuk R J
Department of Pharmaceutics, College of Pharmacy, Minneapolis, Minnesota 55455.
Pharm Res. 1991 Aug;8(8):1050-5. doi: 10.1023/a:1015817426713.
The intestinal permeability of carbamazepine, an antiepileptic drug, was examined as a function of intestinal site (duodenojejunum vs colon). A "through-and-through" in situ intestinal perfusion technique was adopted using the rabbit as an animal model. Coperfusion of the 10,11-epoxide and the 10,11-transdihydrodiol metabolites along with carbamazepine allowed for an examination of the effect of lipophilicity on intestinal permeability when molecular weight differences are negligible. Our results showed that carbamazepine is absorbed from rabbit duodenojejunum as well as the colon, which may explain the prolonged absorption behavior observed in humans. Also, the absorptive clearance of compounds having similar molecular weights is dependent not only on the lipophilicity but also on the extent of solvent drag during the course of the perfusion.
作为肠道部位（十二指肠空肠与结肠）的函数，研究了抗癫痫药物卡马西平的肠道通透性。采用“贯穿式”原位肠道灌注技术，以兔子作为动物模型。将10,11 - 环氧化物和10,11 - 反式二氢二醇代谢物与卡马西平共同灌注，当分子量差异可忽略不计时，可研究亲脂性对肠道通透性的影响。我们的结果表明，卡马西平可从兔子的十二指肠空肠以及结肠吸收，这可能解释了在人类中观察到的吸收行为延长的现象。此外，具有相似分子量的化合物的吸收清除不仅取决于亲脂性，还取决于灌注过程中溶剂拖曳的程度。
