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Preparation and characterization of Furosemide-Eudragit controlled release systems
J M Aceves1, R Cruz, E Hernandez
1Facultad de Estudios Superiores, Cuautitlán, UNAM, Av. 1 de Mayo s/n Cuautitlán Izcalli, Estado de México, Mexico. jaceves&nutrius@cuautitlan1.unam.com.mx
International Journal of Pharmaceutics
|February 17, 2000
Summary
Solid dispersions transformed crystalline Furosemide (FSD) into an amorphous form, enhancing drug interactions and altering its dissolution rate. This amorphous transformation, observed via microscopy and spectroscopy, is key for modified drug release systems.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Furosemide (FSD) is a diuretic drug with poor aqueous solubility, limiting its therapeutic efficacy.
- Solid dispersions offer a promising approach to enhance the dissolution and bioavailability of poorly soluble drugs.
Purpose of the Study:
- To prepare and characterize solid dispersions and physical mixtures of Furosemide with polymeric carriers.
- To investigate the impact of solid dispersion formulation on Furosemide's physical state, drug-polymer interactions, and dissolution behavior.
Main Methods:
- X-ray diffraction (XRD) for phase analysis.
- Infrared spectroscopy (IR) for drug-polymer interactions.
- Electronic microscopy (SEM) for morphological characterization.
- Dissolution rate studies to assess drug release.
Main Results:
- XRD confirmed a transition from crystalline to amorphous Furosemide in solid dispersions.
- IR spectroscopy revealed strong interactions between Furosemide's amine and carbonyl groups and the polymers.
- SEM showed a change in Furosemide's crystalline habit to spherical microparticles and identified channels within the polymeric matrix.
- Solid dispersions exhibited modified Furosemide dissolution patterns compared to physical mixtures.
Conclusions:
- Solid dispersion formulation effectively converts crystalline Furosemide to an amorphous state.
- Enhanced drug-polymer interactions and altered morphology contribute to modified Furosemide release kinetics.
- These findings suggest solid dispersions are a viable strategy for improving Furosemide's dissolution and release characteristics.