复方脑忆源片在Caco-2细胞模型上的转运研究.pdfVIP

药理毒理 复方脑忆源片在 Caco-2 细胞模型上的转运研究 1 1 2 周改莲 ，辛宁 ，林励 (1.广西中医药大学，广西，南宁 530001 ；2.广州中医药大学，广东，广州 510006) 【摘要】目的：对复方脑忆源片中主要成分淫羊藿苷的进行转运研究，阐明吸收特点。方法：利用Caco-2 细胞 模型，对复方脑忆源片中主要成分淫羊藿苷的进行体外转运，并通过高效液相(色谱柱：Luna Kromasil C18 柱 -1 ；检测波长：270nm ；)测定单体、 （4.6mm×150mm,5μm ）；流动相：乙腈：水（30:70 ）；流速：1.0mL·min 药材及复方中的淫羊藿苷转运后的含量。结果：淫羊藿苷在小肠吸收转运过程随时间增长而增加，可能会被 Caco-2 细胞中的 P-gp 转运蛋白外排。与淫羊藿单体和淫羊藿提取物中的淫羊藿苷比较，脑忆源片在可显著提高 淫羊藿苷的转运，同时可降低淫羊藿苷的外排作用。结论：按照目前国际上对于药物吸收的公认标准来评价， 淫羊藿苷单体和淫羊藿提取物属于中等吸收（Papp 在 1.0×10-6cm/s～10×10-6cm/s，收率在 0%～20% ）,而在脑 忆源片中，由于淫羊藿苷外排减少，可认为通过复方配伍后，方中的其他药物抑制了淫羊藿苷的外排，使其可 以更好的发挥药理作用。 【关键词】脑忆源片； Caco-2 细胞模型； 转运 【Abstract 】Objective: The absorption characteristic of the Icariin, which is the main component of Naoyiyuan capsules, was clarified by the membrane transport study. Methods: The Caco-2 monolayer was used to study the transport of the Icariin in Monomer, Herbs, and Compounds in vitro. For the determination of the content of Icariin, the HPLC method was operated with acetonitrile-water （30:70 ） as mobile phase, with Luna Kromasil C column. The 18 flow rate was 1.0mL•min-1, detection wavelength was at 270nm. Results: Icariin exhibited time- dependent permeation with apparent permeability coefficient (P(app)) values in the range 10-5-10-6 cm/s, suggesting transcellular diffusion pathways. P-glycoprotein may play a role in the intestinal efflux of icariin. However compared with the Icariin in Monomer and Herbs, the transport of Icariin in Naoyiyuan capsules is higher. Conclusion: According to the internati