Peris-Ribera J E, Torres-Molina F, Garcia-Carbonell M C, Aristorena J C, Granero L
Department of Pharmaceutics, Faculty of Pharmacy, University of Valencia, Spain.
Pharm Res. 1992 Oct;9(10):1306-13. doi: 10.1023/a:1015861502354.
A general treatment of enterohepatic recirculation of drugs has been developed based on the fraction of drug in systemic circulation that is excreted in the bile and the fraction of drug reabsorbed from the gut that reaches systemic circulation in each enterohepatic cycle. The deduced equations make it possible to establish mathematical relationships between the areas under the blood level curves (AUC) of a drug when administered to normal and bile duct-cannulated animals and to predict the effect of enterohepatic recycling on bioavailability and clearance. The results were compared with those obtained by other authors using different approaches to enterohepatic recirculation, and some discrepancies were found in the equations describing the effect of enterohepatic recycling on AUC and bioavailability of drugs. The cause of such discrepancies and the problems associated with the prediction of hepatic extraction ratio from in vitro studies are discussed.
基于在体循环中经胆汁排泄的药物分数以及在每个肝肠循环中从肠道重吸收并进入体循环的药物分数，已开发出一种药物肝肠循环的通用处理方法。推导得出的方程使得建立药物在正常动物和胆管插管动物给药后血药浓度曲线下面积（AUC）之间的数学关系成为可能，并可预测肝肠循环对生物利用度和清除率的影响。将这些结果与其他作者使用不同肝肠循环方法获得的结果进行了比较，发现在描述肝肠循环对药物AUC和生物利用度影响的方程中存在一些差异。讨论了这种差异的原因以及与从体外研究预测肝提取率相关的问题。
