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Mucoadhesive tablets for buccal administration containing sodium nimesulide
P Maffei1, S Lombardi Borgia, A Sforzini
1Pharmaceutical Sciences Department, University of Bologna, Bologna, Italy.
Drug Delivery
|September 17, 2004
Summary
Nimesulide sodium salt in mucoadhesive tablets aimed to enhance buccal absorption. However, formulation issues degraded the drug, preventing improved flux despite increased solubility.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Biopharmaceutics
Background:
- Buccal drug delivery offers an alternative route for systemic administration.
- Nimesulide's therapeutic potential can be enhanced by optimizing its delivery across the buccal mucosa.
- Mucoadhesive formulations can prolong drug residence time in the oral cavity.
Purpose of the Study:
- To investigate the potential of nimesulide sodium salt in mucoadhesive tablets for improved buccal flux.
- To evaluate the impact of salt form and formulation on nimesulide permeation.
- To assess the stability and release characteristics of the buccal mucoadhesive tablets.
Main Methods:
- In vitro release studies using Franz diffusion cells with porcine buccal mucosa.
- Development of mucoadhesive tablets incorporating nimesulide sodium salt.
- Design of tablets with protective layers to minimize drug loss into saliva.
- Evaluation of drug permeation and concentration gradients.
Main Results:
- The nimesulide sodium salt exhibited higher solubility, potentially increasing the concentration gradient.
- Despite the ionized form, the permeation coefficient was sufficiently high.
- The formulation's composition led to the degradation of the nimesulide chemical form.
- The intended advantages of the salt form for enhanced flux could not be fully realized.
Conclusions:
- The chemical degradation of nimesulide within the mucoadhesive formulation negated the benefits of using the sodium salt.
- Further research is needed to develop stable formulations for buccal delivery of nimesulide sodium salt.
- Optimizing formulation excipients is critical to prevent drug degradation and achieve enhanced buccal permeation.