Objective] Study oral bioavailability effect of Labrasol on hydroxysafflor yellow A and transmembrane transportion mechanism. [Method] Totally 24 SPF SD rats were randomly divided into 4 groups,i.e. the control group, the low dose Labrasol group, the medium dose Labrasol group and the high dose Labrasol group, 6 in each group. The amount of HSYA was 50mg in different groups. After gavage administration of HSYA in rats, HPLC checked HSYA blood drug concentration and explored the effect of surfactant Labrasol on HSYA transmembrane transportion mechanism with Caco-2 drug transport model. [Results] Labrasol could significantly improve blood drug concentration of HSYA. When Labrasol was 20% in formula, HSYA reached maximum oral bioavailability and the AUC was 101.425 μg·h·mL-1 in eight hours which was 3.26 times of oral HSYA aqueous solution. With the action of Labrasol, transfer rate of Caco-2 drug transportion model from the basal side(BL) to Apical side(AP) was much smaller than AP to BL. Compared with P-gp inhibitor verapamil, the impact of Labrasol on HSYA transmembrane transfer was equivalent. [Conclusion] Labrasol could significantly improve HSYA oral bioavailability. Labrasol might inhibit P-gp activity existed in the intestinal mucosa and increased HSYA transmembrane transfer capacity.%[目的]研究表面活性剂辛酸癸酸聚乙二醇甘油酯(Labrasol)对羟基红花黄色素A（ hydroxysafflor yellow A, HSYA）口服生物利用度的影响及其跨膜转运机理。[方法]24只SPF级SD大鼠随机分成正常对照组、Labrasol低剂量组、Labrasol中剂量组、Labrasol高剂量组（ n=6），各组灌胃 HSYA 50mg以及不同浓度的Labrasol。各组大鼠灌胃给药后，用HPLC测定HSYA的血药浓度，并用人结肠癌细胞（ Caco-2）药物转运模型探究 Labrasol对HSYA跨膜转运影响的机理。[结果] Labrasol能显著提高HSYA血药浓度，当配方中Labrasol为20%时，HSYA达到最大的口服生物利用度，8h内药时曲线面积（ area under the curve，AUC）为101.425μg·h·mL-1，是口服HSYA水溶液的3.26倍；在Labrasol的作用下，Caco-2药物转运模型从基底侧（ basolateral side，BL）到顶侧（ apical side，AP）明显小于AP到BL的转运速率，Labrasol对 HSYA跨膜转运的影响与 P-糖蛋白（ P-glycopro－tein，P-gp）抑制剂维拉帕米相比，作用效果相当。[结论] Labrasol能显著提高HSYA口服生物利用度；Labrasol可能通过抑制存在于肠黏膜的 P-gp活性而增加HSYA的跨膜转运能力。
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