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目的:观察低浓度表面活性剂Labrasol对p-糖蛋白(p-gp)底物紫杉醇经肠黏膜透过的增加作用。方法:使用体外扩散池法评价紫杉醇经肠黏膜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对紫杉醇和荧光素钠(CF)经肠黏膜透过性的影响。紫杉醇和CF在接受室中的浓度分别用HPLC法和荧光分光光度法测定。结果:紫杉醇经肠道黏膜的透过性存在部位差。另一方面,紫杉醇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Labrasol可增强紫杉醇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介导药物紫杉醇的透过,有望提高紫杉醇的口服生物利用度。
OBJECTIVE: To observe the effect of low concentration surfactant Labrasol on intestinal mucosal permeability of p-glycoprotein (p-gp) substrate. Methods: In vitro diffusion cell method was used to evaluate the transdermal absorption and secretion of paclitaxel and the transmissivity (Papp) of paclitaxel. The effects of different concentrations of Labrasol on the transmucosal permeation of paclitaxel and sodium fluorescein Sexual effects. The concentrations of paclitaxel and CF in the receiving compartment were determined by HPLC and fluorescence spectrophotometry, respectively. Results: Paclitaxel had poor site of permeability through intestinal mucosa. On the other hand, the permeability of paclitaxel in the intestinal secretion direction is significantly higher than the permeability in the absorption direction. Low concentrations of Labrasol can enhance paclitaxel through the absorption direction of permeability, reducing the secretion of the direction of permeability. However, experimental concentrations of Labrasol had no effect on intestinal transit of CF. CONCLUSIONS: Low concentrations of Labrasol can be used to improve paclitaxel-mediated delivery of p-gp through inhibition of p-gp function, leading to an increase in oral bioavailability of paclitaxel.