基于单向灌流法的葛根素羧甲基壳聚糖微球肠吸收特性研究.PDF

·OQUU · 中草药 =q==e=a 第 QT 卷 第 NQ 期 =OMNS 年 T 月 基于单向灌流法的葛根素羧甲基壳聚糖微球肠吸收特性研究 * * 刘诗雨，柏希慧，董林娟，王昌利 ，宋 逍 陕西中医药大学药学院，陕西 咸阳 712046 摘 要：目的 考察葛根素羧甲基壳聚糖微球的在体肠吸收特性。方法 采用大鼠在体单向灌流法，以 HPLC 法测定葛根 素的量，分别考察不同灌流体积流量、药物质量浓度、肠段对药物吸收的影响，并对比了葛根素原料药及载药微球的吸收特 性。结果 灌流体积流量对葛根素的吸收速率常数（Ka ）和表观渗透系数（Papp ）有显著性影响（P ＜0.05 ）；葛根素的质量 浓度对 Ka 和 Papp 无显著性影响（P ＞0.05 ）；葛根素在空肠和回肠的Ka 和 Papp 无显著性差异，但均显著大于在十二指肠处的 值（P ＜0.05 ）；载药微球在空肠的 Ka 和 Papp 值显著高于葛根素原料药（P ＜0.05 ）。结论 葛根素羧甲基微球中葛根素的吸 收机制为被动扩散，其在空肠和回肠段吸收较好，羧甲基壳聚糖作为载体能显著提高葛根素的吸收。 关键词：葛根素羧甲基壳聚糖微球；葛根素；单向肠灌流；重量法；吸收速率常数；表观渗透系数 中图分类号：R285.5 文献标志码：A 文章编号：0253 - 2670(2016)14 - 2488 - 04 alf 10.7501/j.issn.0253-2670.2016.14.016 p lJ= LIU Shi-yu, BAI Xi-hui, DONG lin-juan, WANG Chang-li, SONG Xiao Shaanxi University of Chinese Medicine, Xianyang 712046, China l To study the rat intestinal absorption characteristic of puerarin loaded O-carboxymethyl chitosan (CMCS) microspheres in situ. j Single-pass intestinal perfusion (SPIP) model was used for rat in situ and HPLC to determine the concentration of puerarin. The effects of different perfusion rate, drug concentration, and intestinal segments on intestinal absorption were investigated, and the absorption characteristics of the puerarin and puerarin loaded O-CMCS microspheres were compared. o Perfusion rate had significant effect on the absorption rate constants (Ka) and the apparent absorption coefficient (Papp) (P 0.05); The concentration of puerarin in perfusate had no significant effect on K and P (P 0.05); K and P of drug loaded a app a app microspheres in jejunum and ileum showed no significant difference, but they were significant