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Diclofenac-bismuth complex: synthesis, physicochemical, and biological evaluation.
Mohammed Abuznaid1, Al-Sayed Sallam, Imad Hamdan
1Faculty of Pharmacy, University of Jordan, Queen Rania Street, Amman, Jordan.
Drug Development and Industrial Pharmacy
|April 11, 2008
Summary
A novel diclofenac-bismuth complex was synthesized, showing enhanced dissolution but increased gastric ulceration in rats due to smaller particle size. This highlights the importance of particle size in drug formulation and safety.
Area of Science:
- Pharmaceutical Chemistry
- Drug Delivery Systems
- Materials Science
Background:
- Diclofenac sodium (Na) is a widely used non-steroidal anti-inflammatory drug (NSAID).
- Bismuth compounds possess known antiulcer properties.
- Developing novel drug formulations can improve therapeutic efficacy and safety profiles.
Purpose of the Study:
- To synthesize and characterize a diclofenac-bismuth complex.
- To evaluate the in vitro dissolution and in vivo ulcerogenic effects of the complex.
- To investigate the relationship between complex properties and gastric effects.
Main Methods:
- Complexation of diclofenac sodium with bismuth-subcitrate.
- Characterization using capillary electrophoresis, nuclear magnetic resonance, and Fourier transform infrared spectroscopy.
- In vitro drug dissolution studies.
- In vivo ulcerogenic evaluation in a rat model.
Main Results:
- A 1:1 diclofenac-bismuth complex was successfully synthesized.
- The complex demonstrated a faster in vitro dissolution rate compared to diclofenac Na.
- The complex exhibited increased gastric ulceration in rats, contrary to bismuth's expected antiulcer effect, attributed to smaller particle size.
Conclusions:
- Diclofenac-bismuth complexation alters drug release characteristics.
- The increased ulcerogenicity of the complex is linked to smaller diclofenac acid particle size upon breakdown in acidic conditions.
- Particle size engineering is crucial for NSAID formulations to mitigate gastric side effects.
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