10.6084/m9.figshare.9963038.v1
Cassiana Mendes
Cassiana
Mendes
Giuliana Valentini
Giuliana
Valentini
Andrés Felipe Chamorro Rengifo
Andrés Felipe Chamorro
Rengifo
Juliana M. O. Pinto
Juliana M. O.
Pinto
Marcos A. S. Silva
Marcos A. S.
Silva
Alexandre L. Parize
Alexandre L.
Parize
Supersaturating drug delivery system of fixed drug combination: sulfamethoxazole and trimethoprim
Taylor & Francis Group
2019
Amorphous
antibacterial activity
biorelevant fluid
Eudragit EPO
solid dispersion
supersaturation
2019-10-10 09:23:33
Journal contribution
https://tandf.figshare.com/articles/journal_contribution/Supersaturating_drug_delivery_system_of_fixed_drug_combination_sulfamethoxazole_and_trimethoprim/9963038
<p><b>Background</b>: The drug supersaturation in the intestinal lumen for few hours could result in high bioavailability. The goal of this study was the development of a supersaturating drug delivery system containing sulfamethoxazole and trimethoprim at fixed dose combination (sulfamethoxazole:trimethoprim 5:1 w/w).</p> <p><b>Methods</b>: The amorphous solid dispersions were formed at three different proportions containing 30, 50 and 70% of Eudragit EPO in the formulation.</p> <p><b>Results</b>: The supersaturation state is formed by the amorphous drugs produced by spray drying technique, and the maintenance of this state is due to the chemical interactions between the drugs and the polymer selected, which was observed in the fluorescence interaction studies realized between the drugs and the polymer. The Formulation containing 70% of the polymer was able to produce and maintain the supersaturated state of both drugs for 24 h. Solid state characterization demonstrated the amorphization of the drugs in the solid dispersion and indicated the hydrogen bond formation responsible for the improvement in the apparent solubility. This formulation presented an improved antibacterial activity when compared to the combination of the drugs.</p> <p><b>Conclusion</b>: For the first time, a supersaturating drug delivery system was developed to the complementary antibacterial drugs. This ternary formulation is a powerful alternative to improve oral absorption of recognized safety drugs, reducing the dose and consequently the antibiotic resistance emergence.</p>