摘要
目的以Caco-2细胞单层模型,首次研究了蜕皮甾酮的口服吸收与转运特性。方法采用普通Caco-2细胞模型、表达活性CYP3A4酶的Caco-2细胞模型,分别从AP→BL方向和BL→AP方向研究蜕皮甾酮的摄取和跨膜转运规律。结果蜕皮甾酮在2种模型中的表观渗透系数(Papp)在0.1×10-6～1×10-6cm.s-1之间,药物吸收情况为1%～10%;在4 h的实验过程中,4种浓度蜕皮甾酮的ER值均小于1.5。结论研究表明,蜕皮甾酮主要以被动扩散的方式被细胞摄取和转运,其跨膜转运特性未受到CYP3A4-介导机制的影响。
Aim This study examined the uptake and transport of ecdysterone （EDS） using Caco-2 cell monolayers as a model of human intestinal mucosa. Methods Two kinds of Caco-2 cell monolayer model （ Caco-2 cell monolayers; CYP3A4 expressing Caco-2 cell monolayers） were set up to study the uptake and transport of EDS. Results Compared bi-directional charaterizaton of Caco-2 cell, the apparent permeability coefficients （Papp） values of EDS were between 0. 1 ×10^-6cm·s^-1 and 1 ×10^-6cm· s^-1 EDS absorption was 1% - 10% for two kinds of Caco-2 models. The Rpapv values were all less than 1.5 for 4 h. Conclusions The uptake and transport of EDS was a passive tran- seellular diffusion mechanism. Ecdysterone was not influeneed by CYP3A4 mediate mechanism.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2009年第4期545-548,共4页
Chinese Pharmacological Bulletin
基金
重庆市重大科技专项资助课题[No渝科发计字(2004)27号]
