中国药理学通报2016，Vol.32Issue(10)：1446-1451,6.DOI:10.3969/j.issn.1001-1978.2016.10.022
不同分子量美沙拉嗪PEG修饰物的大鼠在体肠吸收研究
In situ absorption kinetics of series molecular weight of PEGylated mesalazine in rats
摘要
Abstract
Aim To study the absorption kinetics of se-ries molecular weight 5-ASA-mPEG in rats intestine. Methods The in situ intestinal absorption property of 5-ASA-mPEG in rats was investigated by means of sin-gle-pass perfusion, and HPLC method was established to determine the drug concentration in the perfusate. Results The drug concentration and the site of intes-tine segments had little effect on the drug absorption constant ( Ka ) and apparent absorption coefficient (Papp). The perfusion flow rate and the variable mo-lecular weight of 5-ASA-mPEG could significantly af-fect the Ka and Papp. Conclusion 5-ASA-mPEG can be absorbed at all segments of the intestine of rats and has no specific absorption site. It is preliminarily in-ferred that the absorption mechanism of 5-ASA-mPEG is passive transportation. The intestinal absorption of 5-ASA-mPEG shows a downward trend with the increase in molecular weight. The results shows that the modifi-cation of 5-ASA by PEG can effectively inhibit the in-testinal absorption of mesalazine.关键词
美沙拉嗪/PEG化/在体肠吸收/高效液相色谱法/单向灌流技术/前体药物Key words
mesalazine/PEGylation/in situ intestinal absorption/HPLC/single-pass perfusion/prodrug分类
医药卫生引用本文复制引用
周婧婧,周庆颂,孙若飞,李笑然..不同分子量美沙拉嗪PEG修饰物的大鼠在体肠吸收研究[J].中国药理学通报,2016,32(10):1446-1451,6.基金项目
国家自然科学基金资助项目( No 81160397) （ No 81160397）
江西省自然科学基金资助项目(No 20114BAB205031) （No 20114BAB205031）
