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Very fast dissolving acid carboxymethylcellulose-rifampicin matrix: Development and solid-state characterization
Laura C Luciani-Giacobbe1, María V Ramírez-Rigo2, Yamila Garro-Linck3
1Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA), CONICET and Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, 5000 Córdoba, Argentina.
Developing new tuberculosis treatments requires improving rifampicin (RIF) oral bioavailability. Carboxymethylcellulose (CMC) co-processing significantly enhances RIF dissolution and hydrophilicity for better oral drug delivery.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery
Background:
- Tuberculosis treatment is hindered by rifampicin's (RIF) poor oral bioavailability.
- RIF's low hydrophilicity and dissolution rate limit its effectiveness in solid dosage forms.
Purpose of the Study:
- To develop a hydrophilic material for rapid RIF dissolution.
- To enhance RIF's oral delivery properties for tuberculosis treatment.
Main Methods:
- Carboxymethylcellulose (CMC) was co-processed with RIF using solvent impregnation.
- Characterization involved microscopy, diffraction, thermal analysis, NMR, and spectroscopy.
- Water uptake and dissolution studies assessed hydrophilicity and release kinetics.
Main Results:
- CMC-RIF formed a crystalline solid dispersion with RIF crystallized as a zwitterion on CMC.
- No ionic interactions were observed between CMC and RIF.
- CMC-RIF matrices showed significantly improved water uptake and rapid RIF release.
Conclusions:
- CMC enhances RIF's hydrophilicity and delivery properties.
- CMC-RIF is highly effective for developing oral solid dosage forms with very fast RIF dissolution.
- This approach is valuable for RIF-based tuberculosis therapies.
