结合Caco-2细胞和单向肠灌流法研究枸橼酸莫沙必利的肠吸收特性  

Intestinal Absorption Characters of Mosapride Citrate Using Caco-2 Cells and Single-Pass Intestinal Perfusion Methods

作　　者：李杨[1] 刘吉伟[1] 刘坤堂 王永禄[1,2] 周亚平 徐妍 李学明 

机构地区：[1]南京工业大学药学院,南京211816 [2]南京百思福医药科技有限公司,南京210061

出　　处：《中国药学杂志》2017年第17期1519-1524,共6页Chinese Pharmaceutical Journal

摘　　要：目的研究枸橼酸莫沙必利(MC)及其片剂在体内外实验模型的肠吸收情况,并探讨其吸收机制。方法建立Caco-2单层膜和大鼠在体单向肠灌流模型,采用酚红法对灌流液体积进行校正,建立高效液相色谱法同时测定酚红和枸橼酸莫沙必利的浓度,计算药物的P_(app)和P_(eff)值。结果枸橼酸莫沙必利在大鼠各肠段都有吸收,在小肠上端吸收量最多。MC自研与原研片剂在Caco-2细胞和大鼠单向肠灌流实验中都具有高渗透性。结论自研片和原研产品在Caco-2细胞和大鼠单向肠灌流模型中的吸收具有较高一致性。OBJECTIVE To investigate the intestinal absorption characters of mosapride citrate （MC） and its tablets. METH- ODS The Caco-2 cell monolayer was cultured and the in situ single-pass intestinal perfusion（SPIP） in rat model was created for stud- ying the drug absorption properties, using phenol red method to revise the perfusate volume, a HPLC method was developed to simulta- neously detect the phenol red and MC, the absorptive coefficient of Papp and Peff, was calculated. RESULTS MC was absorbed by the whole intestine segments in rats, mainly at upper small intestine. The tablets showed high permeability and good intestinal absorption in Caco-2 cells and SPIP in rats. CONCLUSION In the Caco-2 cells and rats SPIP models, the tablets are prepared showed good con- sistency with the branded drug.

关 键 词：枸橼酸莫沙必利 Caco-2细胞单层膜 在体单向肠灌流 肠吸收 渗透性 

分 类 号：R945[医药卫生—微生物与生化药学]