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金丝桃苷油水分配系数及大鼠在体肠吸收动力学研究 被引量:13

Apparent oil/water partition coefficients of hyperoside and its in situ intestinal absorption kinetics in rats
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摘要 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log P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。 Objective To 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.
出处 《中草药》 CAS CSCD 北大核心 2012年第5期934-939,共6页 Chinese Traditional and Herbal Drugs
基金 江苏省政府财政专项(省直中医08)
关键词 金丝桃苷 油水分配系数 在体单向肠灌流模型 肠吸收 摇瓶法 hyperoside apparent oil/water partition coefficients in situ rats single pass perfusion model intestinal absorption shaking flask method
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