Ussing Chamber模型研究甘草酸二铵经大鼠肠黏膜的转运和代谢  

Transmembrane transport and metabolism of diammonium glycyrrhizinate across rat small intestine in Ussing Chamber

作　　者：黎国富[1,2] 杨劲[1] 华小懿[1] 陈蕊[1] 赵浩如[2] 

机构地区：[1]中国药科大学药物代谢动力学重点实验室,江苏南京210009 [2]中国药科大学中药制剂研究室,江苏南京210009

出　　处：《中国中药杂志》2010年第17期2261-2266,共6页China Journal of Chinese Materia Medica

摘　　要：目的：研究甘草酸二铵在大鼠十二指肠、空肠和回肠等不同肠段的跨膜转运特征。方法：建立Ussing Chamber模型,并用高效液相色谱法同时测定肠温孵液中甘草酸二铵（GZ）及其2个主要代谢物甘草次酸（GA）和3-单葡萄糖醛酸甘草次酸（3MGA）的含量。结果：GZ在不同肠黏膜的Papp为（0.3-1.1）×10-6cm.s-1,肠腔pH对其在各个肠黏膜的累积转运量和Papp的影响有限,无显著性意义。pH 7.4或5.0时,GZ在回肠的Papp均显著大于十二指肠。结论：GZ属于低通透性药物,其跨膜转运过程中并不被代谢为GA和3MGA。虽然GZ是酸性药物,但是其在不同的浓度和不同的肠段下没有明显的pH依赖性吸收,在整个小肠均可吸收,其中在回肠的通透性最高。Objective： To explore the transmembrane transport and metabolism of diammonium glycyrrhizinate in intestines of rats.Method： An Ussing Chamber model were used to investigate the transmembrane transport of diammonium glycyrrhizinate（GZ）,the concentrations of diammonium glycyrrhizinate and its two metabolites were determined by HPLC.Result： The permeability coefficients of GZ in difference intestinal mucous membranes were ranged from 0.3×10-6 cm·s-1 to 1.1×10-6 cm·s-1.The metabolism of GZ in enterocytes during its transport process was negligible.The concentration of diammonium glycyrrhizinate and pH had limit effects on the transport amount and the permeability coefficients of GZ.Conclusion： GZ is a low permeability drug,but it can be absorbed at all segments of the small intestine in rats.Ileum is the major absorption region of GZ.

关 键 词：甘草酸二铵 Ussing chamber模型 跨膜转运 代谢 

分 类 号：R285.5[医药卫生—中药学]