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目的:研究养阴通脑颗粒主要有效部位在Caco-2细胞模型的吸收特性和转运机制。方法:利用MTT试验研究养阴通脑颗粒主要有效部位在Caco-2细胞中的安全浓度,用Caco-2细胞模型研究养阴通脑颗粒主要有效部位配伍后的转运情况,采用高效液相色谱法进行含量测定。结果:黄芪甲苷、川芎嗪和葛根素的吸收转运Papp皆<1.0×10-6cm·s-1,吸收转运Papp与难吸收药物阿替洛尔接近,其口服在体内的吸收从大到小的顺序为:葛根素>川芎嗪>黄芪甲苷。皂苷与黄酮配伍后,黄芪甲苷吸收转运Papp明显提高,促进吸收方向转运;黄酮、皂苷和生物碱的相互配伍对黄芪甲苷的外排作用明显,对川芎嗪和葛根素的吸收转运影响不明显。各有效部位代表成分的双向转运程度差异较大,Papp(B→A)明显大于Papp(A→B),提示这3个有效部位代表成分在Caco-2细胞单层模型中从BL侧到AP侧的外流转运较占优势。结论:黄芪甲苷、川芎嗪和葛根素可能为吸收不良的化合物,在其转运途径中可能受到了小肠顶侧膜的转运蛋白的外排作用。
OBJECTIVE: To study the absorption characteristics and transport mechanism of the main active site of Yangyintongnao in Caco-2 cell model. Methods: The safe concentration of the main active site of Yangyintongnao in Caco-2 cells was studied by MTT assay. The transfection of the main active site of Yangyintongnao granules was studied by Caco-2 cell model. High performance liquid chromatography Law for the determination of content. Results: Papp of astragaloside, ligustrazine and puerarin were all <1.0 × 10-6cm · s-1. The absorption and transport of Papp was close to that of refractory atenolol, and its oral absorption in vivo was from large to small The order is: Puerarin> Ligustrazine> Astragaloside. After the saponin and flavonoids were combined, the absorption and transport of Astragaloside Papp significantly increased, which promoted the transport of the absorption direction. The interaction between flavonoids, saponins and alkaloids had a significant effect on the efflux of Astragaloside Ⅳ, but had no effect on the absorption and transport of ligustrazine and puerarin obvious. Papp (B → A) was significantly larger than that of Papp (A → B), suggesting that the three active sites represent the components in the Caco-2 cell monolayer model from the BL side to the AP Side of the outflow of transport more dominant. CONCLUSIONS: Astragaloside, ligustrazine and puerarin may be malabsorption compounds that may be affected by the efflux of the transporter protein on the apical membrane of the small intestine in the transport pathway.