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Sustained release bioadhesive effervescent ketoconazole microcapsules tabletted for vaginal delivery
H Y Karasulu1, F Taneri, E Sanal
1University of Ege, Faculty of Pharmacy, Pharamaceutical Technology Department, Bornova, Izmir, Turkey. karasuluy@pharm.ege.edu.tr
Journal of Microencapsulation
|May 23, 2002
Summary
Ketoconazole microcapsules, formulated with sodium carboxymethylcellulose and effervescent granules, demonstrated good sustained action in tablet form. Micromeritic studies confirmed no glidant is needed for tableting these optimized microcapsules.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Materials Science
Background:
- Ketoconazole is an antifungal agent requiring effective drug delivery for sustained action.
- Microencapsulation offers a method to control drug release and improve stability.
- Sodium carboxymethylcellulose is a suitable coating material for microcapsule formulation.
Purpose of the Study:
- To prepare and characterize ketoconazole microcapsules using sodium carboxymethylcellulose.
- To evaluate the dissolution profile and sustained release of tableted microcapsules.
- To assess the micromeritic properties of microcapsules for optimal tablet production.
Main Methods:
- Phase separation technique was employed for microencapsulation with varying core-wall ratios (1:1, 1:2).
- Microcapsules were mixed with effervescent granules and compressed into tablets.
- Dissolution studies utilized a novel horizontal rotating basket method.
- Micromeritic properties including bulk/tap density, fluidity, angle of repose, and particle size distribution were determined.
Main Results:
- Tableted ketoconazole microcapsules exhibited good sustained drug release.
- Micromeritic investigations indicated favorable flow properties, with Hausner ratio and consolidation index suggesting no glidant requirement for tableting.
- Particle size distribution, density, and porosity were characterized for product standardization.
Conclusions:
- The developed ketoconazole microcapsules, when tabletted, provide effective sustained action.
- Sodium carboxymethylcellulose is a viable coating material for ketoconazole microencapsulation.
- The characterized micromeritic properties facilitate the optimization of pilot-scale production of these dosage forms.