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Development and validation of a discriminative dissolution test for nimesulide suspensions
Laís Bastos da Fonseca1, Márcio Labastie, Valéria Pereira de Sousa
1Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Av. Pau Brasil s/n, Edifício CCS, Bloco Bss sala 34-Ilha do Fundão, Rio de Janeiro, Rio de Janeiro, CEP: 21941-590, Brazil. lfonseca@far.fiocruz.br
AAPS Pharmscitech
|October 17, 2009
Summary
Particle size significantly impacts nimesulide (NMS) oral suspension dissolution. Controlling particle size distribution is crucial for developing effective NMS formulations and ensuring drug bioavailability.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Dissolution testing is expanding to complex dosage forms like oral suspensions.
- Formulation challenges in Class II drugs, such as nimesulide (NMS), can affect bioavailability.
Purpose of the Study:
- To investigate the dissolution profiles of four commercial nimesulide (NMS) suspension brands.
- To evaluate the impact of different dissolution media and formulation characteristics on NMS dissolution.
Main Methods:
- Characterization of NMS suspensions: particle size, pH, density, NMS assay, and drug in vehicle.
- Dissolution studies in simulated intestinal fluid (pH 6.8) and phosphate buffer (pH 7.4) with polysorbate 80 (P80) or sodium lauryl sulfate (SLS).
- Quantitative analysis using UV-VIS spectrophotometry, validated as an alternative to HPLC.
Main Results:
- Particle size distribution significantly influenced NMS dissolution profiles.
- Different dissolution media and surfactants (P80, SLS) affected drug release rates.
- NMS assay and drug content in suspension vehicles were determined.
Conclusions:
- Drug particle size is a critical factor requiring strict control during oral suspension development.
- Optimized formulation parameters are essential for consistent NMS bioavailability from suspensions.
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