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目的观察低浓度labrasol对肠黏膜P-gp的调控作用。方法使用体外扩散池评价罗丹明123(R123)经空肠、回肠和结肠黏膜的经时经吸收方向和分泌方向的透过量和透过系数(Papp),并测定不同浓度labrasol对R123和荧光素钠(CF)经肠黏膜透过性的影响。R123和CF在接受室中的浓度用荧光分光光度法测定。结果R123经肠道黏膜的透过性存在部位差,即以空肠、回肠和结肠的次序透过性依次减少。另一方面,R123经肠道分泌方向的透过性显著地高于其吸收方向的透过性。低浓度的labrasol具有增加R123经吸收方向的透过性,减少经分泌方向的透过性。但试验浓度的labrasol对CF的肠道转运没有影响。结论低浓度的labrasol可通过对P-gp功能的抑制而用于改善受P-gp介导药物的吸收,有望提高此类药物的口服生物利用度。
Objective To observe the effect of low concentrations of labrasol on intestinal mucosal P-gp. Methods The in vitro diffusion and permeation coefficient (Papp) of rhodamine 123 (R123) in jejunum, ileum and colonic mucosa were evaluated by in vitro diffusion cells. The effects of different concentrations of labrasol on the activity of R123 and sodium fluorescein (CF) through the intestinal mucosal permeability. The concentrations of R123 and CF in the receiving compartment were determined by fluorescence spectrophotometry. Results R123 transmucosal permeability through the site there is poor, that is, the order of the jejunum, ileum and colon permeability decreased in turn. On the other hand, the permeability of R123 in the intestinal secretion direction is significantly higher than the permeability in the absorption direction. Low concentrations of labrasol increase the absorption of R123 by the direction of permeability, reducing the permeability of the secretion direction. However, labrasol at the test concentration had no effect on intestinal transit of CF. Conclusions Low concentrations of labrasol can be used to improve the absorption of P-gp-mediated drugs by inhibiting P-gp function and are expected to increase the oral bioavailability of these drugs.