氟比洛芬的大鼠在体肠吸收动力学研究  

Intestinal absorption kinetics of flurbiprofen in rats

作　　者：彭俊杰[1] 蔺聪聪[1] 李江[1] 朱志红[1] 杨星钢[1] 潘卫三[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《药学学报》2013年第3期423-427,共5页Acta Pharmaceutica Sinica

摘　　要：本文考察了氟比洛芬大鼠在体肠吸收的动力学特征。采用大鼠在体单向灌流法,利用HPLC法测定氟比洛芬的含量,研究氟比洛芬在小肠段(十二指肠、空肠、回肠)和结肠的吸收情况,并考察药物浓度和灌流速度对氟比洛芬吸收的影响。结果表明:小肠段与结肠段的药物吸收速率常数(Ka)和表观吸收系数(Papp)均无显著性差异(P>0.05);药物质量浓度在4.0、10.0和16.0 mg.L 1时,Ka均无显著差异(P>0.05);质量浓度为4.0和10.0 mg.L 1时,其Papp有显著的差异(P<0.05);质量浓度为10.0和16.0 mg.L 1时,其Papp无显著性差异(P>0.05);不同灌流速度下Ka和Papp有显著相差异(P<0.05)。以上结果说明氟比洛芬在全肠道吸收良好,无特定吸收部位;氟比洛芬在整个肠段的吸收以易化扩散为主,同时可能伴随有膜动转运机制;不同灌流速度对氟比洛芬的吸收速率常数和表观吸收系数均有显著性影响。To study the in situ intestinal absorption kinetics of flrubiprofen in rats, the absorption of flurbiprofen in small intestine （duodenum, jejunum and ileum） and colon of rats was investigated using in situ single-pass perfusion method and the drug content was measured by HPLC. The effects of drug concentration on the intestinal absorption were investigated. The Ka and Papp values of flurbiprofen in the small intestine and colon had no significant difference （P〉0.05）. Drug concentration （4.0, 10.0 and 16.0 mg .L-I） had no significant influence on the K, values （P〉0.05）. However, when concentration was 4.0 mg.L 1 and 10.0 mg.L-1, significant effect on the Papp values （P〈0.05） was found, but significant effect on the Papp values was not shown between 10.0 mg-L-1 and 16.0 mg.L-1 （P〉0.05）. The K and Papp values of flurbiprofen on the perfusion flow rate had significant difference （P〈0.05）. Flurbiprofen could be absorbed at all segments of the intestine in rats and had no special absorption window. The absorption of flurbiprofen complies with the facilitated diffusion in the general intestinal segments, and accompany with the cytopsistransport mechanism probably. The perfusion flow rate had significant effect on the Ka and Papp.

关 键 词：氟比洛芬 小肠吸收 单向灌流法 重量法 

分 类 号：R943[医药卫生—药剂学]