In situ absorption kinetics of series molecular weight of PEGylated mesalazine in rats
10.3969/j.issn.1001-1978.2016.10.022
- VernacularTitle:不同分子量美沙拉嗪PEG修饰物的大鼠在体肠吸收研究
- Author:
Jingjing ZHOU
;
Qingsong ZHOU
;
Ruofei SUN
;
Xiaoran LI
- Publication Type:Journal Article
- Keywords:
mesalazine;
PEGylation;
in situ intestinal absorption;
HPLC;
single-pass perfusion;
prodrug
- From:
Chinese Pharmacological Bulletin
2016;32(10):1446-1451
- CountryChina
- Language:Chinese
-
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.
