Thermal studies, degradation kinetic, equilibrium solubility, DFT, MIR, and XRPD analyses of a new cocrystal of gemfibrozil and isonicotinamide
Autor(a) principal: | |
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Data de Publicação: | 2019 |
Outros Autores: | , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.1007/s10973-018-7873-8 http://hdl.handle.net/11449/189861 |
Resumo: | A synthesis of a novel pharmaceutical cocrystal of the gemfibrozil (GEM) with the isonicotinamide (INCT) as coformer was carried out using the mechanochemical method of solvent drop grinding. The cocrystal formation was evidenced using the X-Ray powder diffraction, medium infrared spectroscopy, computational methods (DFT), simultaneous thermogravimetric-differential thermal analysis (TG/DTG–DTA), and differential scanning calorimetry. The association of techniques used to analyze all proportion synthetized (GEM:INCT—5:1, 4:1, 3:1, 2:1, 1:1, 1:2, 1:3, 1:4, 1:5) showed formation of the cocrystal in the proportion of 1 mol:1 mol. Furthermore, kinetic studies were performed to determine the stability of the cocrystal formed, possible shelf time (5% degradation), and best storage temperature. The dissolution profiles of GEM and GEM:INCT were collected using 0.1 M HCl, pH 4.5 sodium acetate buffer, water, and potassium phosphate buffer at pH 5.8, pH 6.8, and pH 7.4. The results demonstrate that the cocrystal exhibits superior apparent maximum solubility relative to the pure drug with a high solubility in alkaline environment. Finally, the study shows that the cocrystal of gemfibrozil with isonicotinamide can be applied in new solid oral dosage formulations of enhanced bioavailability. |
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Thermal studies, degradation kinetic, equilibrium solubility, DFT, MIR, and XRPD analyses of a new cocrystal of gemfibrozil and isonicotinamideCocrystalGemfibrozilIsonicotinamideNon-covalent interactionsSolubility studiesA synthesis of a novel pharmaceutical cocrystal of the gemfibrozil (GEM) with the isonicotinamide (INCT) as coformer was carried out using the mechanochemical method of solvent drop grinding. The cocrystal formation was evidenced using the X-Ray powder diffraction, medium infrared spectroscopy, computational methods (DFT), simultaneous thermogravimetric-differential thermal analysis (TG/DTG–DTA), and differential scanning calorimetry. The association of techniques used to analyze all proportion synthetized (GEM:INCT—5:1, 4:1, 3:1, 2:1, 1:1, 1:2, 1:3, 1:4, 1:5) showed formation of the cocrystal in the proportion of 1 mol:1 mol. Furthermore, kinetic studies were performed to determine the stability of the cocrystal formed, possible shelf time (5% degradation), and best storage temperature. The dissolution profiles of GEM and GEM:INCT were collected using 0.1 M HCl, pH 4.5 sodium acetate buffer, water, and potassium phosphate buffer at pH 5.8, pH 6.8, and pH 7.4. The results demonstrate that the cocrystal exhibits superior apparent maximum solubility relative to the pure drug with a high solubility in alkaline environment. Finally, the study shows that the cocrystal of gemfibrozil with isonicotinamide can be applied in new solid oral dosage formulations of enhanced bioavailability.School of Sciences Chemistry Department São Paulo State University (UNESP)College of Pharmacy Coimbra UniversityFaculty of Pharmaceutical Science UnicampSchool of Sciences Chemistry Department São Paulo State University (UNESP)Universidade Estadual Paulista (Unesp)Coimbra UniversityUniversidade Estadual de Campinas (UNICAMP)Holanda, Bruno B. C. [UNESP]Alarcon, Rafael T. [UNESP]Gaglieri, Caroline [UNESP]de Souza, Aguinaldo R. [UNESP]Castro, Ricardo A. E.Rosa, Paulo C. P.Tangerino, Débora J. A.Bannach, Gilbert [UNESP]2019-10-06T16:54:30Z2019-10-06T16:54:30Z2019-06-15info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article2049-2062http://dx.doi.org/10.1007/s10973-018-7873-8Journal of Thermal Analysis and Calorimetry, v. 136, n. 5, p. 2049-2062, 2019.1588-29261388-6150http://hdl.handle.net/11449/18986110.1007/s10973-018-7873-82-s2.0-85056136658Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengJournal of Thermal Analysis and Calorimetryinfo:eu-repo/semantics/openAccess2024-04-29T18:17:12Zoai:repositorio.unesp.br:11449/189861Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-04-29T18:17:12Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Thermal studies, degradation kinetic, equilibrium solubility, DFT, MIR, and XRPD analyses of a new cocrystal of gemfibrozil and isonicotinamide |
title |
Thermal studies, degradation kinetic, equilibrium solubility, DFT, MIR, and XRPD analyses of a new cocrystal of gemfibrozil and isonicotinamide |
spellingShingle |
Thermal studies, degradation kinetic, equilibrium solubility, DFT, MIR, and XRPD analyses of a new cocrystal of gemfibrozil and isonicotinamide Holanda, Bruno B. C. [UNESP] Cocrystal Gemfibrozil Isonicotinamide Non-covalent interactions Solubility studies |
title_short |
Thermal studies, degradation kinetic, equilibrium solubility, DFT, MIR, and XRPD analyses of a new cocrystal of gemfibrozil and isonicotinamide |
title_full |
Thermal studies, degradation kinetic, equilibrium solubility, DFT, MIR, and XRPD analyses of a new cocrystal of gemfibrozil and isonicotinamide |
title_fullStr |
Thermal studies, degradation kinetic, equilibrium solubility, DFT, MIR, and XRPD analyses of a new cocrystal of gemfibrozil and isonicotinamide |
title_full_unstemmed |
Thermal studies, degradation kinetic, equilibrium solubility, DFT, MIR, and XRPD analyses of a new cocrystal of gemfibrozil and isonicotinamide |
title_sort |
Thermal studies, degradation kinetic, equilibrium solubility, DFT, MIR, and XRPD analyses of a new cocrystal of gemfibrozil and isonicotinamide |
author |
Holanda, Bruno B. C. [UNESP] |
author_facet |
Holanda, Bruno B. C. [UNESP] Alarcon, Rafael T. [UNESP] Gaglieri, Caroline [UNESP] de Souza, Aguinaldo R. [UNESP] Castro, Ricardo A. E. Rosa, Paulo C. P. Tangerino, Débora J. A. Bannach, Gilbert [UNESP] |
author_role |
author |
author2 |
Alarcon, Rafael T. [UNESP] Gaglieri, Caroline [UNESP] de Souza, Aguinaldo R. [UNESP] Castro, Ricardo A. E. Rosa, Paulo C. P. Tangerino, Débora J. A. Bannach, Gilbert [UNESP] |
author2_role |
author author author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (Unesp) Coimbra University Universidade Estadual de Campinas (UNICAMP) |
dc.contributor.author.fl_str_mv |
Holanda, Bruno B. C. [UNESP] Alarcon, Rafael T. [UNESP] Gaglieri, Caroline [UNESP] de Souza, Aguinaldo R. [UNESP] Castro, Ricardo A. E. Rosa, Paulo C. P. Tangerino, Débora J. A. Bannach, Gilbert [UNESP] |
dc.subject.por.fl_str_mv |
Cocrystal Gemfibrozil Isonicotinamide Non-covalent interactions Solubility studies |
topic |
Cocrystal Gemfibrozil Isonicotinamide Non-covalent interactions Solubility studies |
description |
A synthesis of a novel pharmaceutical cocrystal of the gemfibrozil (GEM) with the isonicotinamide (INCT) as coformer was carried out using the mechanochemical method of solvent drop grinding. The cocrystal formation was evidenced using the X-Ray powder diffraction, medium infrared spectroscopy, computational methods (DFT), simultaneous thermogravimetric-differential thermal analysis (TG/DTG–DTA), and differential scanning calorimetry. The association of techniques used to analyze all proportion synthetized (GEM:INCT—5:1, 4:1, 3:1, 2:1, 1:1, 1:2, 1:3, 1:4, 1:5) showed formation of the cocrystal in the proportion of 1 mol:1 mol. Furthermore, kinetic studies were performed to determine the stability of the cocrystal formed, possible shelf time (5% degradation), and best storage temperature. The dissolution profiles of GEM and GEM:INCT were collected using 0.1 M HCl, pH 4.5 sodium acetate buffer, water, and potassium phosphate buffer at pH 5.8, pH 6.8, and pH 7.4. The results demonstrate that the cocrystal exhibits superior apparent maximum solubility relative to the pure drug with a high solubility in alkaline environment. Finally, the study shows that the cocrystal of gemfibrozil with isonicotinamide can be applied in new solid oral dosage formulations of enhanced bioavailability. |
publishDate |
2019 |
dc.date.none.fl_str_mv |
2019-10-06T16:54:30Z 2019-10-06T16:54:30Z 2019-06-15 |
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/s10973-018-7873-8 Journal of Thermal Analysis and Calorimetry, v. 136, n. 5, p. 2049-2062, 2019. 1588-2926 1388-6150 http://hdl.handle.net/11449/189861 10.1007/s10973-018-7873-8 2-s2.0-85056136658 |
url |
http://dx.doi.org/10.1007/s10973-018-7873-8 http://hdl.handle.net/11449/189861 |
identifier_str_mv |
Journal of Thermal Analysis and Calorimetry, v. 136, n. 5, p. 2049-2062, 2019. 1588-2926 1388-6150 10.1007/s10973-018-7873-8 2-s2.0-85056136658 |
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.format.none.fl_str_mv |
2049-2062 |
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 |
|
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1799965424307142656 |