金丝桃苷油水分配系数及大鼠在体肠吸收动力学研究.pdf

• 934 • 中草药 Chinese Traditional and Herbal Drugs 第 43 卷 第 5 期 2012 年 5 月 金丝桃苷油水分配系数及大鼠在体肠吸收动力学研究 1 1 1 1 1 2* 贾 媛 ，马兴苗 ，恽 菲 ，范 玲 ，王 宁 ，刘志辉 1. 南京中医药大学药学院，江苏 南京 210046 2. 江苏省中医院，江苏 南京 210036 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、20 μg/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。 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 中图分类号：R285.61 文献标志码：A 文章编号：0253 - 2670(2012)05 - 0934 - 06 Apparent oil/water partition coefficients of hyperoside and its in situ intestinal absorption kinetics in rats 1 1 1 1 1 2 JIA Yuan , MA Xing-miao , YUN Fei , FAN Ling , WANG Ning , LIU Zhi-hui 1. School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China 2. Jiangsu Provincial Hospital of Traditional Chinese Medicine, Nanjing 210036, China Abstract: 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 co