目的:研究根皮苷和3-羟基根皮苷在人克隆结肠腺癌细胞(Caco-2细胞)单层模型中的转运与吸收.方法:采用高效液相色谱法,以表观渗透系数(Papp)为指标,分别考察50、100、200 μmol/L的根皮苷和3-羟基根皮苷在Caco-2细胞单层模型中的双向(AP→BL、BL→AP)转运；并通过两药配伍同时混合转运与两药单独转运比较,考察两药转运的相互作用.结果:随着浓度的增加,根皮苷AP→BL和BL→AP的Papp均有一定的上升趋势；3-羟基根皮苷AP→BL的Papp有下降趋势,BL→Ap的Papp却略有上升趋势.与单独转运比较,混合转运中根皮苷和3-羟基根皮苷的转运量和Papp均明显下降(P＜0.05).结论:根皮苷和3-羟基根皮苷在Caco-2细胞单层模型的吸收状况良好,两药配伍转运时存在竞争性抑制.%OBJECTIVE:To study absorption and transportation of phloridzin and 3-hydroxy-phloridzin in cloning of human colon adenocarcinoma cells (Caco-2 cell) monolayer model.METHODS:HPLC method was adopted.Using apparent permeation coefficient Papp as index,two-way absorption and transportation (AP→BL and BL→AP) of phloridzin and 3-hydroxy-phloridzin (50,100,200 μmol/L) in Caco-2 cell monolayer model were investigated.Simultaneous transportation of drug combination was compared with that of single drug; the interaction of the two drugs was investigated.RESULTS:With the increase of concentration,Papp of phloridzin (AP→BL and BL→AP) increased to some extent; Papp of 3-hydroxy-phloridzin (AP→BL) decreased to some extent,while that of 3-hydroxy-phloridzin (BL→AP) increased slightly.Compared with single transportation,transportation amount and Papp of phloridzin combined with 3-hydroxy-phloridzin decreased significantly (P＜0.05).CONCLUSIONS:Phloridzin and 3-hydroxy-phloridzin have good permeability coefficient on Caco-2 cell monolayer model.When transport together,competitive inhibition is found between two drugs.
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