| Autor: |
Gomes SN; Graduate Program in Pharmaceutical Sciences, Department of Pharmacy, Universidade Estadual do Centro-Oeste (UNICENTRO), Guarapuava 85040-080, Brazil., Biscaia IFB; Graduate Program in Pharmaceutical Sciences, Department of Pharmacy, Universidade Estadual do Centro-Oeste (UNICENTRO), Guarapuava 85040-080, Brazil., Lopes DS; Graduate Program in Pharmaceutical Sciences, Department of Pharmacy, Universidade Estadual do Centro-Oeste (UNICENTRO), Guarapuava 85040-080, Brazil., Mengarda M; Graduate Program in Pharmaceutical Sciences, Department of Pharmacy, Universidade Federal do Paraná (UFPR), Curitiba 80210-170, Brazil., Murakami FS; Graduate Program in Pharmaceutical Sciences, Department of Pharmacy, Universidade Federal do Paraná (UFPR), Curitiba 80210-170, Brazil., Oliveira PR; Graduate Program in Pharmaceutical Sciences, Department of Pharmacy, Universidade Estadual do Centro-Oeste (UNICENTRO), Guarapuava 85040-080, Brazil., Bernardi LS; Graduate Program in Pharmaceutical Sciences, Department of Pharmacy, Universidade Estadual do Centro-Oeste (UNICENTRO), Guarapuava 85040-080, Brazil. |
| Abstrakt: |
A solvate cocrystal of the antimicrobial norfloxacin (NFX) was formed by using isonicotinamide (INA) as a coformer with the solvent evaporation technique. The cocrystal formation was confirmed by performing solid-state characterization techniques. We evaluated the dissolution under supersaturated conditions and also the solubility at the vertex of triphasic domain of cocrystal and NFX in both water and Fasted-State Simulated Intestinal Fluid (FaSSIF). The antimicrobial activity was evaluated using the microdilution technique. The cocrystal showed 1.8 times higher dissolution than NFX in water at 60 min and 1.3 times higher in FaSSIF at 180 min in the kinetic study. The cocrystal also had an increase in solubility of 8.38 times in water and 6.41 times in FaSSIF. The biopharmaceutical properties of NFX with cocrystallization improved antimicrobial action, as shown in the results of minimum inhibitory concentration (MIC) and inhibitory concentrations of 50% (IC50%) and 90% (IC90%). This paper presents, for the first time, a more in-depth analysis of the cocrystal of NFX-INA concerning its dissolution, solubility, and antimicrobial activity. In all these criteria, the cocrystal obtained better results compared to the pure drug. |
