改善葛根素肠道吸收的体外研究.PDFVIP

中草药 Chinese Traditional and Herbal Drugs 第 42 卷 第 11 期 2011 年 11 月 ·2265 · 改善葛根素肠道吸收的体外研究 1, 2 3 2 1* 李 林 ，张 琼 ，杨志建 ，陆 阳 1. 上海交通大学医学院 药学系，上海 200025 2. 联合利华上海研究所，上海 200335 3. 华东理工大学生物工程学院，上海 200237 摘 要：目的 研究葛根素肠道吸收的机制，探讨提高其肠道吸收的方法。方法 改变实验时间、温度及药物质量浓度，考 察葛根素在 Caco-2 细胞中的转运特性，并考察不同的吸收促进剂对其跨膜转运的影响。结果 葛根素的膜渗透性低，被动 扩散是其跨膜转运的主要机制；十二烷基磺酸钠（SDS ）破坏 Caco-2 单细胞层的完整性，提高葛根素转运；聚氧乙烯月桂 基醚 （Brij 35 ）、牛血清白蛋白 （BSA ）和分离乳清蛋白对葛根素转运有促进作用，但不影响 Caco-2 细胞的跨膜电阻 （TEER ）； 相对分子质量较高的壳聚糖通过可逆性地降低 TEER，促进细胞间转运，提高葛根素的膜渗透性。结论 葛根素的膜渗透性 低是口服生物利用度低的主要原因，不同吸收促进剂可通过不同机制改善其膜渗透性。 关键词：葛根素；肠道吸收；生物利用度；Caco-2 细胞；膜渗透性 中图分类号：R282.710.5 文献标志码：A 文章编号：0253 - 2670(2011)11 - 2265 - 05 In vitro investigation on improvement in puerarin intestinal absorption 1, 2 3 2 1 LI Lin , ZHANG Qiong , YANG Zhi-jian , LU Yang 1. Department of Pharmacy, School of Medicine, Shanghai Jiao Tong University, Shanghai 200025, China 2. Unilever RD Shanghai Institute, Shanghai 200335, China 3. College of Bioengineering, East China University of Science and Technology, Shanghai 200237, China Abstract: Objective To study the mechanism of puerarin (PE) intestinal absorption and investigate the possible methods to improve its intestinal absorption. Methods The characteristics of PE transport across Caco-2 cell monolayer were determined by changing incubation time, temperature, and PE concentration. The effect of different absorption enhancers on its membrane transport permeability was studied as well. Results The intestinal permeability of PE was low and the passive diffusion was the main mechanism for its transport across Caco-2 cells. Sodium dodecyl sulfate (SDS) improved PE transport by impairing the integrity of Caco-