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Preparation and in vitro evaluation of macrocyclic metronidazole conjugates as an oral colon-specific delivery system
- Source :
- Journal of Inclusion Phenomena and Macrocyclic Chemistry. 78:501-504
- Publication Year :
- 2013
- Publisher :
- Springer Science and Business Media LLC, 2013.
-
Abstract
- The antimicrobial drug metronidazole (MTZ) was covalently conjugated to the secondary hydroxyl groups of β-cyclodextrin through ester linkage using sodium hydride as the deproton reagent. The preliminary release behavior of MTZ in rat gastrointestinal tract contents was studied at 37 °C within 24 h. In the contents of stomach, the conjugates did hardly release MTZ, released MTZ only 9.5 % in the contents of small intestine, and released MTZ significantly up to 43.6 and 40.2 % in the contents of cecum and colon, respectively. These results indicate that the conjugate activation took place site-specifically in the rat cecal and colonic contents, probably via the biodegradation by glycosidases and hydrolases. The present MTZ-appended cyclodextrin conjugate may be of value as an orally administered delayed-release and/or colon-specific prodrug.
Details
- ISSN :
- 15731111 and 13883127
- Volume :
- 78
- Database :
- OpenAIRE
- Journal :
- Journal of Inclusion Phenomena and Macrocyclic Chemistry
- Accession number :
- edsair.doi...........cddbf115d4b59e6a7f8453dc618a5ea4
- Full Text :
- https://doi.org/10.1007/s10847-013-0339-5