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Effect of antioxidants on captopril floating matrices
Inéz Jiménez-Martínez1, Adriana Miriam Domínguez-Ramírez, Leopoldo Villafuerte-Robles
1Department of Biological Systems, Autonomous Metropolitan University - Xochimilco, Col. Villa Quietud, D. F. Mexico.
Pharmaceutical Development and Technology
|June 22, 2012
Summary
Controlled release captopril floating matrices were optimized by adjusting antioxidant load and compaction pressure. Higher pressure matrices required sodium bicarbonate for flotation, impacting drug release and hydration.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Materials Science
Background:
- Captopril controlled release formulation stability presents challenges.
- Floating matrices offer sustained drug release potential.
- Optimizing matrix properties is crucial for effective drug delivery.
Purpose of the Study:
- To investigate the impact of antioxidant load, sodium bicarbonate, and compaction pressure on captopril floating matrix stability and drug release.
- To understand how these factors influence matrix hydration, density, and flotation characteristics.
- To optimize captopril sustained release from floating dosage forms.
Main Methods:
- Formulation of floating matrices with varying ascorbic acid (antioxidant) load, sodium bicarbonate proportion, and compaction pressure (55 MPa vs. 165 MPa).
- Evaluation of matrix density, hydration volume, flotation time, and drug release profiles in a dissolution medium.
- Analysis of the influence of formulation variables on matrix porosity and transport properties.
Main Results:
- Matrices compacted at 55 MPa exhibited lower density and floated readily; those at 165 MPa required sodium bicarbonate for flotation.
- Increased compaction pressure reduced hydration volume and slowed drug release due to decreased porosity and transport.
- Higher ascorbic acid proportions increased hydration and drug release; sodium ascorbate and sodium bicarbonate addition shortened hydration time and enhanced release via CO2 bubble formation.
Conclusions:
- Compaction pressure significantly affects captopril floating matrix properties, influencing density, hydration, and drug release kinetics.
- Antioxidant type and proportion, along with sodium bicarbonate, modulate matrix behavior and drug release, with ascorbic acid offering better protection than sodium ascorbate.
- Optimizing compaction pressure, antioxidant load, and excipient ratios is key to achieving desired captopril sustained release from floating matrices.
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