Journal
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
Volume 36, Issue 1, Pages 81-92Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/03639040903092335
Keywords
Colon targeting; human fecal; beta-mannanase medium; pH- and enzyme-controlled; rat cecal content
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Funding
- National Basic Research Program of China [2007CB935801]
- Program for New Century Excellent Talents in University
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Background: As conventional pH-controlled colon-targeted system used for oral drug delivery often shows a poor performance, a more effective way to preserve poorly water-soluble drug from releasing in upper gastrointestinal tract should be researched. Method: The objective of this study was to develop a novel colon-targeted drug delivery system using guar gum and Eudragit as enzyme-and pH-based materials. Lansoprazole, a poorly water-soluble drug was used as model drug. Under three different conditions, the in vitro drug release behaviors of this newly developed system was evaluated, using beta-mannanase, rat cecal content, and human fecal media to simulate the pH and enzyme during intestinal transit to the colon. Results: The released amount of lansoprazole in simulated small intestine fluid (pH 6.8) after 5 hours was less than 10% from the pH- and enzyme-controlled tablets compared with 80.01 +/- 0.3% in rat cecal content medium (pH 7.4). The degradation ability of human fecal slurries on PECCT-PT was independent of human age and gender. beta-Mannanase did not have a similar effect on the degradation of polysaccharide as rat cecal enzymes and human fecal enzymes in our study. Scanning electron microscope study indicated that the dissolution mechanism of PECCT-PT should be corrosion. Conclusion: The above results indicated this system could be served as a potential carrier to deliver poorly water-soluble drug specifically to the colon.
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