Mechanochemical synthesis, thermoanalytical study and characterization of new multicomponent solid forms of norfloxacin with saccharin
Autor(a) principal: | |
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Data de Publicação: | 2021 |
Outros Autores: | , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.1007/s10973-021-10658-w http://hdl.handle.net/11449/206024 |
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). |
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Repositório Institucional da UNESP |
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Mechanochemical synthesis, thermoanalytical study and characterization of new multicomponent solid forms of norfloxacin with saccharinMechanochemical synthesisNorfloxacinPharmaceutical cocrystalSaccharinSolvateThermal analysisCocrystallization 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).São Paulo State University (UNESP) Institute of ChemistrySchool of Science Chemistry Department São Paulo State University (UNESP)Federal University of Goias (UFG) School of PharmacySão Paulo State University (UNESP) Institute of ChemistrySchool of Science Chemistry Department São Paulo State University (UNESP)Universidade Estadual Paulista (Unesp)School of PharmacyFerreira, Patrícia Osório [UNESP]de Moura, Aniele [UNESP]de Almeida, Amanda Cosmo [UNESP]dos Santos, Éverton Carvalho [UNESP]Kogawa, Ana CarolinaCaires, Flávio Junior [UNESP]2021-06-25T10:25:15Z2021-06-25T10:25:15Z2021-01-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://dx.doi.org/10.1007/s10973-021-10658-wJournal of Thermal Analysis and Calorimetry.1588-29261388-6150http://hdl.handle.net/11449/20602410.1007/s10973-021-10658-w2-s2.0-85102274595Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengJournal of Thermal Analysis and Calorimetryinfo:eu-repo/semantics/openAccess2021-10-22T20:36:28Zoai:repositorio.unesp.br:11449/206024Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T13:59:24.945278Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Mechanochemical synthesis, thermoanalytical study and characterization of new multicomponent solid forms of norfloxacin with saccharin |
title |
Mechanochemical synthesis, thermoanalytical study and characterization of new multicomponent solid forms of norfloxacin with saccharin |
spellingShingle |
Mechanochemical synthesis, thermoanalytical study and characterization of new multicomponent solid forms of norfloxacin with saccharin Ferreira, Patrícia Osório [UNESP] Mechanochemical synthesis Norfloxacin Pharmaceutical cocrystal Saccharin Solvate Thermal analysis |
title_short |
Mechanochemical synthesis, thermoanalytical study and characterization of new multicomponent solid forms of norfloxacin with saccharin |
title_full |
Mechanochemical synthesis, thermoanalytical study and characterization of new multicomponent solid forms of norfloxacin with saccharin |
title_fullStr |
Mechanochemical synthesis, thermoanalytical study and characterization of new multicomponent solid forms of norfloxacin with saccharin |
title_full_unstemmed |
Mechanochemical synthesis, thermoanalytical study and characterization of new multicomponent solid forms of norfloxacin with saccharin |
title_sort |
Mechanochemical synthesis, thermoanalytical study and characterization of new multicomponent solid forms of norfloxacin with saccharin |
author |
Ferreira, Patrícia Osório [UNESP] |
author_facet |
Ferreira, Patrícia Osório [UNESP] de Moura, Aniele [UNESP] de Almeida, Amanda Cosmo [UNESP] dos Santos, Éverton Carvalho [UNESP] Kogawa, Ana Carolina Caires, Flávio Junior [UNESP] |
author_role |
author |
author2 |
de Moura, Aniele [UNESP] de Almeida, Amanda Cosmo [UNESP] dos Santos, Éverton Carvalho [UNESP] Kogawa, Ana Carolina Caires, Flávio Junior [UNESP] |
author2_role |
author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (Unesp) School of Pharmacy |
dc.contributor.author.fl_str_mv |
Ferreira, Patrícia Osório [UNESP] de Moura, Aniele [UNESP] de Almeida, Amanda Cosmo [UNESP] dos Santos, Éverton Carvalho [UNESP] Kogawa, Ana Carolina Caires, Flávio Junior [UNESP] |
dc.subject.por.fl_str_mv |
Mechanochemical synthesis Norfloxacin Pharmaceutical cocrystal Saccharin Solvate Thermal analysis |
topic |
Mechanochemical synthesis Norfloxacin Pharmaceutical cocrystal Saccharin Solvate Thermal analysis |
description |
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). |
publishDate |
2021 |
dc.date.none.fl_str_mv |
2021-06-25T10:25:15Z 2021-06-25T10:25:15Z 2021-01-01 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://dx.doi.org/10.1007/s10973-021-10658-w Journal of Thermal Analysis and Calorimetry. 1588-2926 1388-6150 http://hdl.handle.net/11449/206024 10.1007/s10973-021-10658-w 2-s2.0-85102274595 |
url |
http://dx.doi.org/10.1007/s10973-021-10658-w http://hdl.handle.net/11449/206024 |
identifier_str_mv |
Journal of Thermal Analysis and Calorimetry. 1588-2926 1388-6150 10.1007/s10973-021-10658-w 2-s2.0-85102274595 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Journal of Thermal Analysis and Calorimetry |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.source.none.fl_str_mv |
Scopus reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
_version_ |
1808128301553680384 |