体外垂直型扩散池技术评价原花青素对大鼠不同区段肠黏膜药物透过特性的影响  

Evaluation of the effect of procyanidin on drug permeability on different intestinal mucosa of rats with Ussing Chamber in vitro

作　　者：赵博欣[1] 王胜奇[1] 王雅甜 梁倩莹 蔡云[1] 张韫琪 李国锋[1] 

机构地区：[1]南方医科大学南方医院药学部合理用药评价与药物递送发展实验室,广州510515

出　　处：《国际药学研究杂志》2017年第5期448-452,共5页Journal of International Pharmaceutical Research

基　　金：广州市科技计划资助项目(2014J4100144);南方医科大学南方医院院长基金资助项目(2014C003);广东省自然科学基金资助项目(2016A030310399)

摘　　要：目的评价原花青素对P-糖蛋白(P-gp)底物罗丹明123(R123)和荧光素钠(FS)在大鼠不同区段肠黏膜透过特性的影响。方法采用体外垂直型扩散池(Ussing Chamber)技术,分别计算原花青素20 mg/L时R123和FS经空肠、回肠和结肠黏膜吸收与分泌方向的累计透过率和表观渗透系数(P_(app)),R123和FS在接收池的样品浓度用荧光分光光度计法测定。结果原花青素具有增加R123经空肠、回肠与结肠吸收方向透过性的趋势,同时具有降低R123经空肠、回肠与结肠分泌方向透过性的趋势,与正常对照组相比,原花青素使结肠R123分泌方向透过性明显降低(P<0.01)。结论原花青素具有抑制R123经肠黏膜外排的作用,该作用可能与原花青素抑制肠黏膜上皮P-gp功能有关。Objective To investigate the effect of procyanidin on permeability of rodamin 123（R123） and fluorescein sodium（FS） via different intestinal mucosa in rat. Methods The cumulative permeability and the apparent permeability cofficient（P_（app）） of R123 and FS via rat intestinal membranes at the procyanidin concentration of 20 mg/L was evaluated by the method of Ussing Chamber. The concentrations of R123 and FS in the receptor samples were determined by fluorospectrophotometry. Results The absorptive directed permeability of R123 across all membranes was increased by co-administration of procyanidins,whereas that of the secretive direct was decreased. Compared with control group,the secretive directed permeability of R123 was significantly decreased in colon（P〈0.01）. Conclusion Procyanidin could inhibit the secretion of R123 on different intestinal mucosa which might be related to the inhibition of P-gp function.

关 键 词：原花青素类 P-糖蛋白 垂直型扩散池技术 肠黏膜 

分 类 号：R285.5[医药卫生—中药学]