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

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dc.contributor.authorFerreira, Patrícia Osório [UNESP]
dc.contributor.authorde Moura, Aniele [UNESP]
dc.contributor.authorde Almeida, Amanda Cosmo [UNESP]
dc.contributor.authordos Santos, Éverton Carvalho [UNESP]
dc.contributor.authorKogawa, Ana Carolina
dc.contributor.authorCaires, Flávio Junior [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionSchool of Pharmacy
dc.date.accessioned2021-06-25T10:25:15Z
dc.date.available2021-06-25T10:25:15Z
dc.date.issued2021-01-01
dc.description.abstractCocrystallization 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).en
dc.description.affiliationSão Paulo State University (UNESP) Institute of Chemistry
dc.description.affiliationSchool of Science Chemistry Department São Paulo State University (UNESP)
dc.description.affiliationFederal University of Goias (UFG) School of Pharmacy
dc.description.affiliationUnespSão Paulo State University (UNESP) Institute of Chemistry
dc.description.affiliationUnespSchool of Science Chemistry Department São Paulo State University (UNESP)
dc.identifierhttp://dx.doi.org/10.1007/s10973-021-10658-w
dc.identifier.citationJournal of Thermal Analysis and Calorimetry.
dc.identifier.doi10.1007/s10973-021-10658-w
dc.identifier.issn1588-2926
dc.identifier.issn1388-6150
dc.identifier.scopus2-s2.0-85102274595
dc.identifier.urihttp://hdl.handle.net/11449/206024
dc.language.isoeng
dc.relation.ispartofJournal of Thermal Analysis and Calorimetry
dc.sourceScopus
dc.subjectMechanochemical synthesis
dc.subjectNorfloxacin
dc.subjectPharmaceutical cocrystal
dc.subjectSaccharin
dc.subjectSolvate
dc.subjectThermal analysis
dc.titleMechanochemical synthesis, thermoanalytical study and characterization of new multicomponent solid forms of norfloxacin with saccharinen
dc.typeArtigo
unesp.author.orcid0000-0003-3187-2111[6]

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