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Physical characterization and dissolution properties of ibuprofen: Eudragit coprecipitates
M S Kislalioglu1, M A Khan, C Blount
1College of Pharmacy, University of Rhode Island, Kingston 02881.
Journal of Pharmaceutical Sciences
|August 1, 1991
Summary
Ibuprofen Eudragit coprecipitates were developed to create sustained-release tablets. These formulations showed retarded drug dissolution and improved flow properties, indicating their potential for controlled drug delivery.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery
Background:
- Ibuprofen is a widely used non-steroidal anti-inflammatory drug (NSAID).
- Developing sustained-release formulations can improve patient compliance and therapeutic efficacy.
- Eudragit polymers offer versatile properties for modifying drug release profiles.
Purpose of the Study:
- To prepare and characterize ibuprofen-Eudragit coprecipitates.
- To evaluate the dissolution characteristics and physical properties of these coprecipitates.
- To assess the potential of these coprecipitates for ibuprofen sustained-release tablet formulation.
Main Methods:
- Coprecipitation of ibuprofen with various anionic, zwitterionic, and anionic:cationic Eudragit polymers at a 10:3 ratio.
- Physical characterization using X-ray diffractometry, IR spectrophotometry, and differential scanning calorimetry (DSC).
- Dissolution studies in different pH media and calculation of dissolution rate constants using the Higuchi equation.
Main Results:
- No significant molecular interaction was observed between ibuprofen and most Eudragit polymers, except for Eudragit S100 + E100.
- Dissolution of ibuprofen was retarded from most coprecipitates, particularly in pH 6.8-7.5 media.
- Dissolution rates decreased in the order: anionics > zwitterionics > anionic + cationic mixtures. Improved flow properties were noted, except for Eudragit RLPM and RSPM.
Conclusions:
- Eudragit coprecipitates, prepared via a simple, solvent-minimizing technique, can effectively retard ibuprofen dissolution.
- The swelling and slower dissolution of the polymer matrix are key release mechanisms.
- These coprecipitates show promise for developing ibuprofen sustained-release tablets.