Abstract | BACKGROUND: The basic objective of this study was to develop a novel technique that aids in compaction of coated pellets into tablets and obtain a release pattern from compressed pellets resembling the same pattern before compression. METHOD: RESULTS: This technique provides additive protection for the coated beads to withstand the compression force during tableting. Excellent in vitro dissolution results were obtained, which were comparable to the results of the release of mesalamine from uncompressed beads filled in capsules. Mesalamine release from the capsules was 0.3% after 2 hours in gastric pH, 0.37% was released after an additional 1 hour in pH 6, and 89% was released after 1.5 hours in colonic pH 7.2. CONCLUSION: Various formulation and process parameters have to be optimized in order to obtain tableted reservoir-type pellets having the same release properties as the uncompressed pellets. The coating technique delays the release of mesalamine until the beads reach the terminal ileum and colon. Once released in the colon, mesalamine is minimally absorbed and can act locally to treat ulcerative colitis.
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Authors | Ehab R Bendas, J Mark Christensen, James W Ayres |
Journal | Drug development and industrial pharmacy
(Drug Dev Ind Pharm)
Vol. 36
Issue 4
Pg. 393-404
(Apr 2010)
ISSN: 1520-5762 [Electronic] England |
PMID | 19740039
(Publication Type: Journal Article)
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Chemical References |
- Anti-Inflammatory Agents, Non-Steroidal
- Delayed-Action Preparations
- Drug Implants
- Excipients
- Polymethacrylic Acids
- Tablets
- methylmethacrylate-methacrylic acid copolymer
- Mesalamine
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Topics |
- Administration, Oral
- Anti-Inflammatory Agents, Non-Steroidal
(administration & dosage, chemistry, pharmacokinetics)
- Chemistry, Pharmaceutical
- Delayed-Action Preparations
- Drug Delivery Systems
- Drug Implants
(analysis)
- Excipients
(chemistry)
- Mesalamine
(administration & dosage, chemistry, pharmacokinetics)
- Polymethacrylic Acids
- Tablets
(analysis)
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