药物转运蛋白对灯盏花素小肠吸收的影响

目的:研究药物转运蛋白P-糖蛋白(P-gp)和多药耐药相关蛋白(MRP2)对灯盏花素小肠吸收的影响。方法:HPLC法测定大鼠肠液中灯盏花素的浓度,以大鼠在体单向灌流实验(SPIP)研究药物的小肠吸收,计算不含抑制剂药物组和含抑制剂药物组的小肠表观渗透系数(Papp)。结果:含P-gp抑制剂药物组与原药组相比,Papp没有显著变化;含MRP2抑制剂药物组与原药组相比,Papp显著增加。结论:P-gp对灯盏花素的小肠吸收基本没有影响,而MRP2可将吸收的灯盏花素从肠上皮细胞内又转运回肠腔,从而降低灯盏花素的吸收。

Preparation and transdermal absorption of triamcinolone-acetonide-acetate loaded nanostructured lipid carriers

Aim:To investigate the effects of drug transporters,including P-glycoprotein(P-gp)and multidrug resistance-associated protein(MRP2),on intestinal absorption of breviscapine.Methods:Breviscapine concentration in rat intestinal perfusion solution was determined by HPLC.Rat single pass intestinal perfusion(SPIP)was employed to study breviscapine intestinal absorption in order to evaluate the intestinal apparent permeation coefficients(P_app)of breviscapine group and inhibitor group.Results:Based on the statistical analysis of P_app,P-gp inhibitor has no marked effects on the intestinal absorption of breviscapine.While for MRP2 inhibitor,P_app were significantly higher than that of the breviscapine group.Conclusion:P-gp transporter has no effect on intestinal absorption of breviscapine,and MRP2 transporter is involved in the intestinal absorption of breviscapine possibly via transporting breviscapine from intestinal epithelium to intestinal cavity.