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采用Caco-2细胞模型初步考察了积雪草酸氨丁三醇盐(1)的吸收行为。HPLC-MS/MS法测定细胞样品中积雪草酸的含量。结果表明,1在Caco-2细胞中的转运具有时间和浓度依赖性。不同浓度1组的双向转运表观渗透系数(Papp)分别为10-6 cm/s级,属于中等吸收药物;并且Papp值均随浓度增加而下降,提示1在Caco-2细胞模型中的吸收行为既有被动扩散,也有主动转运。1的反向与正向表观渗透系数的比值(ER值)大于1,并受P-糖蛋白(P-gp)外排抑制剂维拉帕米的影响。
The absorption behavior of asiatic acid tromethamine salt (1) was initially investigated by Caco-2 cell model. Determination of Asiatic acid in cell samples by HPLC-MS / MS. The results show that 1 has a time-and concentration-dependent transport in Caco-2 cells. The Papp of bidirectional transport in different concentrations of 1 group were 10-6 cm / s, which belonged to moderate absorption drug. Papp values decreased with increasing concentration, suggesting that the absorption of 1 in Caco-2 cell model Behavioral both passive diffusion, but also active transport. 1 ratio of reverse to forward apparent permeability (ER) was greater than 1 and was affected by verapamil, a p-glycoprotein (P-gp) efflux inhibitor.