Functional modulation of drug efflux system by drug interaction and development of oral drug delivery system

采用体外扩散箱系统研究了不同表面活性剂和聚乙二醇对P-gp底物罗丹明123在肠道转运的影响。罗丹明123的空肠浆膜-粘膜转运（Jsm）大于其粘膜-浆膜转运（Jms）。非离子表面活性剂（Cremophor EL、Tween 80和LM）降低罗丹明123的Jsm/Jms比值，而阳离子表面活性剂（<16>CTAB）和阴离子表面活性剂（SDS）对罗丹明123的Jsm/Jms比值无影响。因此，这些研究结果表明，表面活性剂的电荷可能与这些表面活性剂对P-gp底物的肠吸收的作用有关。不同分子量的聚乙二醇可抑制罗丹明123通过大鼠空肠膜的Jsm通量。

The effects of various surfactants and polyethylene glycol on the intestinal transport of rhodamine123, a P-gp substrate, were examined by an in vitro diffusion chamber system. The jejunal serosal-to mucosal transport (Jsm) of rhodamine123 was greater than its mucosal-to serosal transport (Jms). Nonionic surfactants (Cremophor EL, Tween80 and LM) reduced the Jsm/Jms ratio of rhodamine123, whereas its ratio was not influenced in the presence of cationic surfactant (C_<16>TAB) and anionic surfactant (SDS). Therefore, these findings suggested that charge of surfactants is possibly related to the action of these surfactants on the intestinal absorption of P-gp substrates. Polyethylene glycols with various molecular weights inhibited the Jsm flux of rhodamine123 across the rat jejunum membrane.