beta-cyclodextrin complexation as an approach to enhance the biopharmaceutical properties of Norfloxacin B Hydrate

Autor(es)

Soledad Bueno, Maria ^{[1, 2]} ; Chierentin, Lucas ^[3] ; Bongioanni, Agustina ^{[1, 2]} ; Nunes Salgado, Herida Regina ^[3] ; Raquel Longhi, Marcela ^{[1, 2]} ; Garnero, Claudia ^{[1, 2]}

Afiliação do(s) autor(es)

^[1] Univ Nacl Cordoba, CONICET, Unidad Invest & Desarrollo Tecnol Farmaceut UNITE, Ciudad Univ X5000HUA, Cordoba - Argentina

^[2] Univ Nacl Cordoba, Dept Ciencias Farmaceut, Fac Ciencias Quim, Ciudad Univ X5000HUA, Cordoba - Argentina

^[3] Univ Estadual Paulista, Fac Ciencias Farmaceut, Rodovia Araraquara Jau, Km 1, BR-14801902 Araraquara, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Carbohydrate Research; v. 485, NOV 1 2019.
• Citações Web of Science: 0

Resumo

Binary systems of Norfloxacin B Hydrate with beta-CD were explored by reliable biopharmaceutical studies as potential candidates for the preparation of drug delivery systems. Initially, studies of antimicrobial activity and solubility of the different polymorphic forms of Norfloxacin provided evidence to select Norfloxacin B Hydrate as the optimal solid form of Norfloxacin. Solid binary systems were preparing by kneading, freeze-drying, and physical mixture methods. The influence on the solubility, dissolution rate and chemical stability of Norfloxacin B Hydrate was investigated. These studies showed an increment of solubility and dissolution rate in physiological simulated fluids. However, the solid systems were moderated hygroscopically under accelerated storage conditions, which produces a destabilizing effect that accelerated the chemical reactivity of the drug in such conditions. Therefore, special cares must be considered in the manufacturing process and the packaging selection. Moreover, the experimental results proved that freeze-drying was not an appropriate method for the preparation. In conclusion, the Norfloxacin oral bioavailability can be improved with this binary systems, that could be applied in the production of an alternative pharmaceutical formulation of the drug. (AU)

• Processo FAPESP: 10/13335-2 - Validação de métodos para quantificação de norfloxacino em comprimidos e estudos de estabilidade
• Beneficiário: Lucas Chierentin
• Modalidade de apoio: Bolsas no Brasil - Mestrado