Li Guo-Feng, Wang Chun-Xia, Yan Yuan, Kishimoto Nobuaki, Yamamoto Akira
Pharmaceutical Department of Nanfang Hospital, Southern Medical University, Guangzhou 510515, China.
Yao Xue Xue Bao. 2008 Mar;43(3):314-7.
The objective of this study is to investigate the permeabilities of rebamipide across the jejunal, ileal and colonic membranes in rat. The permeability (Papp) of rebamipide via rat intestinal membranes at concentration of 80 micromol L(-1) was evaluated by an in vitro diffusion chamber system after the membranes were isolated from the rat intestine. And the concentration of rebamipide in the receptor was determined by HPLC. As a result, the permeability of rebamipide across the jejunal or ileal membrane was higher than that across the colonic membrane, and the permeability of rebamipide in the ileal tissue from the serosal to mucosal direction was greater than that from the mucosal to serosal direction. Therefore, there was a regional difference in the permeability of rabamipide across the jejunum, ileum and the colon in rat. Also, the transporters in the intestinal mucosa as p-glycoprotein may not be involved in the transport of rebamipide.
本研究的目的是研究瑞巴派特在大鼠空肠、回肠和结肠膜中的渗透性。在从大鼠肠道分离出膜后,通过体外扩散室系统评估瑞巴派特在浓度为80微摩尔/升时通过大鼠肠膜的渗透率(表观渗透系数)。通过高效液相色谱法测定受体中瑞巴派特的浓度。结果显示,瑞巴派特跨空肠或回肠膜的渗透率高于跨结肠膜的渗透率,且瑞巴派特在回肠组织中从浆膜侧到黏膜侧的渗透率大于从黏膜侧到浆膜侧的渗透率。因此,瑞巴派特在大鼠空肠、回肠和结肠中的渗透性存在区域差异。此外,肠黏膜中的转运蛋白如P-糖蛋白可能不参与瑞巴派特的转运。