阿魏酸在Caco-2细胞模型的通透性及其在大鼠体内吸收特性.PDF

中草药 Chinese Traditional and Herbal Drugs 第 43 卷 第 5 期 2012 年 5 月 • 947 • 阿魏酸在 Caco-2 细胞模型的通透性及其在大鼠体内吸收特性研究 * 莫李立，王素军 ，杨本坤 广东药学院药科学院，广东 广州 510006 摘 要：目的 研究阿魏酸在大鼠体内的绝对生物利用度（Fabs ）及其吸收特点。方法 建立人源结肠腺癌细胞系 Caco-2 单 层细胞模型，LC-MS/MS 法分析阿魏酸由绒毛面（AP 侧）到基底面（BL 侧）和由 BL 侧到 AP 侧两个方向的转运过程；用 大鼠原位肠肝血管灌流模型研究阿魏酸在肠道的吸收率；通过测定大鼠 ig 和 iv 阿魏酸后的血药浓度计算其 Fabs 。结果 阿 −6 −6 魏酸的表观渗透系数（Papp ）分别为Papp AP→BL ：（10.24±1.58）×10 cm/s，Papp BL→AP ：（11.25±1.45）×10 cm/s ；在肠肝 血管灌流模型中的吸收率为 59.00%；在大鼠体内的Fabs 为 64.91% 。结论 LC-MS/MS 定量分析法灵敏、简单、专属性强； 阿魏酸在 Caco-2 细胞具有良好的转运，在肠肝血管灌流模型中吸收速度快，主要吸收部位为小肠，阿魏酸 ig 给药后在大鼠 体内达峰时间短，吸收、分布、消除较快。 关键词：阿魏酸；吸收特性；绝对生物利用度；Caco-2 细胞；肠肝血管灌流模型；LC-MS/MS 中图分类号：R282.710.5 文献标志码：A 文章编号：0253 - 2670(2012)05 - 0947 - 05 Permeability of ferulic acid in Caco-2 cell model and its absorption properties in rats in vivo MO Li-li, WANG Su-jun, YANG Ben-kun School of Pharmacy, Guangdong Pharmaceutical College, Guangzhou 510006, China Abstract: Objective To study the absolute bioavailability (Fabs) of ferulic acid in rats and its absorption properties. Methods Based on the LC-MS/MS method, Caco-2 (the human colon adenocarcinoma cell lines) cell monolayer model was applied to studying the absorption and transport of ferulic acid from apical (AP) to basolateral (BL) side and from BL to AP side; the in situ vascularly perfused intestine-liver preparation was used to investigate the intestinal absorption rate; the Fabs was calculated by measuring the plasma concentration after iv or ig administration of ferulic acid in rats. Results The apparent permeability coefficients of ferulic acid from AP to BL side (Papp AP→BL) and from BL to AP side (Papp BL→AP) were (10.24 ±