吸收促进剂对绿原酸的跨膜转运影响  

Enhancers on the transmembrane transport of chlorogenic acid

作　　者：任静[1,2] 邓盛齐[1,2] 蒋学华[3] 王玲玲[1,2] 肖宇[1,2] 

机构地区：[1]成都大学 [2]四川抗菌素工业研究所,四川成都610052 [3]四川大学华西药学院,四川成都610041

出　　处：《药学学报》2014年第2期252-255,共4页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(30572373)

摘　　要：采用Caco-2细胞模型，研究不同吸收促进剂对绿原酸跨膜转运的影响。绿原酸浓度采用高效液相色谱法测定。在20-80μg·mL^-1内，绿原酸吸收速率常数（蚝）无显著性差异；40和20μg·mL^-1的双向转运表观渗透系数（Pspp）比值分别为1．14和1．18；在吸收促进剂的作用下，绿原酸吸收速率常数和表观渗透系数增加，吸收半衰期减少。绿原酸主要以被动转运的方式通过Caco-2单层细胞膜，转运过程可能有载体参与：冰片对其通过Caco-2细胞膜的转运过程无影响，牛胆盐、十二烷基硫酸钠和卡波姆3种吸收促进剂的促吸收能力按以下顺序递减：十二烷基硫酸钠〉牛胆盐〉卡波姆。To investigate the influence of the difference enhancers on the transport mechanism of chlorogenic acid （CGA） across Caco-2 cells model, a RP-HPLC method was adopted to detect the concentrations of CGA. At the concentrations of 20 to 80μg·mL^-1, the difference of absorption rate constants （Ka） was not statistically significant. At the concentrations of 40 and 20 μg·mL^-1, the ratios of apparent permeability coefficients （Papp） of the apical to basolateral and the basolateral to apical were 1.14 and 1.18, respectively. With the effect of enhancers Ka and Papp increased, the absorption half-life （T1/2） decreased. CGA passed through the Caco-2 cell membrane mainly by passive transport. It showed that monocarboxylic acid transporter （MCT） could be involved in the across membrane transport process of CGA. Borneol had no effect on the cell membrane transport processes. The order of increasing absorption of CGA caused by the enhancers was sodium lauryl sulphate 〉 sodium taurocholate 〉 carbomer.

关 键 词：绿原酸 CACO-2细胞模型 转运机制 吸收促进剂 

分 类 号：R943[医药卫生—药剂学]