目的测定金丝桃苷的油水分配系数,并考察金丝桃苷的大鼠在体肠吸收情况。方法采用经典摇瓶法测定金丝桃苷的油水分配系数;采用大鼠在体肠吸收模型研究金丝桃苷的肠吸收情况,考察其在小肠各段的吸收情况及药物浓度对吸收的影响。结果在正辛醇-水体系中,金丝桃苷的油水分配系数logP为0.43;在正辛醇-缓冲液体系中,油水分配系数随pH值的升高而逐渐降低。质量浓度为5、10、20μg/mL的金丝桃苷在大鼠肠道内均有较好的吸收,在不同质量浓度下金丝桃苷吸收不具有显著性差异(P>0.05)。结论应用摇瓶法能准确测定金丝桃苷的油水分配系数,由此推测的体内吸收情况通过大鼠肠灌流试验得到验证。

ObjectiveTo determine the apparent oil/water partition coefficients of hyperoside and to investigate its in situ intestinal absorption characteristics in rats. Methods The apparent oil/water partition coefficients of hyperoside was determined by shaking flask method; In situ perfused rat intestinal model was performed to study its absorption at different concentration and different intestinal regions. Results The logP of hyperoside in n-octanol/water system was 0.43, and its distribution coefficients decreased with the increase of pH value in n-octanol/buffer-solution system. Hyperoside was well absorbed at different concentration (5, 10, and 20 μg/mL) in general intestinal tract and had no significant difference (P> 0.05).Conclusion The shaking flask method could be used to determine the apparent oil/water partition coefficients of hyperoside accurately and the prediction of its intracorporal absorption has been proved by in situ perfused rat intestinal model.

江苏省政府财政专项(省直中医08)