Mechanochemical synthesis, thermoanalytical study and characterization of new multicomponent solid forms of norfloxacin with saccharin

Autor(es)

Ferreira, Patricia Osorio ^{[1, 2]} ; de Moura, Aniele ^[2] ; de Almeida, Amanda Cosmo ^[2] ; dos Santos, Everton Carvalho ^[2] ; Kogawa, Ana Carolina ^[3] ; Caires, Flavio Junior ^{[1, 2]}

Afiliação do(s) autor(es)

^[1] Sao Paulo State Univ UNESP, Inst Chem, Araraquara, SP - Brazil

^[2] Sao Paulo State Univ UNESP, Dept Chem, Sch Sci, Bauru, SP - Brazil

^[3] Fed Univ Goias UFG, Sch Pharm, Goiania, Go - Brazil

• Tipo de documento: Artigo Científico
• Fonte: JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY; v. 147, n. 3, p. 1985-1997, FEB 2022.
• Citações Web of Science: 1

Resumo

Cocrystallization is a very efficient strategy to improve the physicochemical properties of bioactive agents. A new norfloxacin (NOR)-saccharin cocrystal and a cocrystal-solvate were synthesized through the mechanochemical method (neat and liquid-assisted grinding), and the characterization was performed by thermal analysis (TG-DTA, DSC and DSC microscopy), infrared vibrational spectroscopy and powder X-ray diffraction. Moreover, solubility experiments carried out in water and buffer solutions (pH 3.0, 6.1 and 8.5) showed that norfloxacin has an aqueous solubility 3.5 times higher when cocrystallized with saccharin than in its pristine state, and an inverted pH-dependency compared to NOR alone (2 times higher in 6.1, slightly increase in pH 3.0, and a decrease of 0.7 times in 8.5 buffer solution). Furthermore, the solvate-cocrystal has a water solubility 2.3 times higher than NOR and the same solubility in 6.1 buffer solution than the cocrystal (2 times higher than NOR alone). (AU)

• Processo FAPESP: 18/24378-6 - Síntese, caracterização e estudo termoanalítico de cocristais de Valsartana, Candesartana Cilexetila e Olmesartana medoxomila
• Beneficiário: Flávio Junior Caires
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 17/14936-9 - Preparação, caracterização e estudos termoanalíticos de catalisadores heterogêneos de selenatos duplos de Mg/Co e Mg/Cu na produção de biodiesel a partir de diferentes óleos
• Beneficiário: Massao Ionashiro
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 13/09022-7 - Estudos termoanalíticos, síntese e caracterização dos co-cristais sólidos de alguns antibióticos (fluoroquinolonas) com alguns co-formadores
• Beneficiário: Massao Ionashiro
• Modalidade de apoio: Auxílio à Pesquisa - Regular