Riad L E, Sawchuk R J
Department of Pharmaceutics, College of Pharmacy, Minneapolis, Minnesota 55455.
Pharm Res. 1991 Apr;8(4):491-7. doi: 10.1023/a:1015803312233.
Because of the limited solubility of carbamazepine, aqueous solutions are usually prepared using glycols as cosolvents. This research focuses on the effect of varying the composition of polyethylene glycol 400 (PEG-400) in aqueous solutions in rabbit intestinal permeability of carbamazepine in the duodenojejunum and the ascending colon using an in situ perfusion technique. In both segments the intestinal permeability varied inversely with the percentage of PEG-400, when the concentration of carbamazepine in the perfusing solution was maintained constant. The decreased permeability may be explained by a reduction in the thermodynamic activity of carbamazepine with increased concentrations of PEG-400, as well as by reverse solvent drag because of the hyperosmolarity of the perfusing solutions.
由于卡马西平的溶解度有限，通常使用二醇类作为助溶剂来制备水溶液。本研究聚焦于通过原位灌注技术，改变水溶液中聚乙二醇400（PEG - 400）的组成对卡马西平在兔十二指肠空肠和升结肠中的肠道通透性的影响。当灌注溶液中卡马西平的浓度保持恒定时，在这两个肠段中，肠道通透性均与PEG - 400的百分比呈反比。通透性降低可能是由于随着PEG - 400浓度增加，卡马西平的热力学活性降低，以及由于灌注溶液的高渗性导致的反向溶剂拖曳所致。
