Solubility and dissolution studies of tibolone polymorphs
Autor(a) principal: | |
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Data de Publicação: | 2017 |
Outros Autores: | , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Brazilian Journal of Pharmaceutical Sciences |
Texto Completo: | https://www.revistas.usp.br/bjps/article/view/144061 |
Resumo: | Different solid forms of an active pharmaceutical ingredient can have distinct chemical and physical characteristics. In this work, we studied the solubility and dissolution properties of the described tibolone polymorphic forms (I and II). Both forms were successively recrystallized and characterized by powder X-ray diffraction and attenuated total reflection infrared spectroscopy. Equilibrium solubility and dissolution profiles were performed for both forms. Solubility studies demonstrated that form II is statistically more soluble in water, 0.01 mol L-1 HCl and pH 4.5 acetate buffer. The solubility of forms I and II were explained in terms of crystal packing. Dissolution tests of tablets showed a lower release of polymorphic form II than form I from tablets. The results showed an impact of polymorphism on the quality of tibolone tablets and suggest that tibolone forms I and II can show distinct interactions with pharmaceutical excipients used in tablets. Therefore, only form I is acceptable for the preparation of tablet forms. Based on our results, we propose the quality control on tibolone raw materials using X-ray diffraction analysis and attenuated total reflection infrared spectroscopy. |
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Brazilian Journal of Pharmaceutical Sciences |
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Solubility and dissolution studies of tibolone polymorphsTibolone/polymorphsPowder X-ray diffraction/methodsInfrared spectroscopy/methodsSolubility/drug effectsDissolution/analysis Different solid forms of an active pharmaceutical ingredient can have distinct chemical and physical characteristics. In this work, we studied the solubility and dissolution properties of the described tibolone polymorphic forms (I and II). Both forms were successively recrystallized and characterized by powder X-ray diffraction and attenuated total reflection infrared spectroscopy. Equilibrium solubility and dissolution profiles were performed for both forms. Solubility studies demonstrated that form II is statistically more soluble in water, 0.01 mol L-1 HCl and pH 4.5 acetate buffer. The solubility of forms I and II were explained in terms of crystal packing. Dissolution tests of tablets showed a lower release of polymorphic form II than form I from tablets. The results showed an impact of polymorphism on the quality of tibolone tablets and suggest that tibolone forms I and II can show distinct interactions with pharmaceutical excipients used in tablets. Therefore, only form I is acceptable for the preparation of tablet forms. Based on our results, we propose the quality control on tibolone raw materials using X-ray diffraction analysis and attenuated total reflection infrared spectroscopy.Universidade de São Paulo. Faculdade de Ciências Farmacêuticas2017-01-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://www.revistas.usp.br/bjps/article/view/14406110.1590/s2175-97902017000400233Brazilian Journal of Pharmaceutical Sciences; Vol. 53 Núm. 4 (2017); e00233Brazilian Journal of Pharmaceutical Sciences; v. 53 n. 4 (2017); e00233Brazilian Journal of Pharmaceutical Sciences; Vol. 53 No. 4 (2017); e002332175-97901984-8250reponame:Brazilian Journal of Pharmaceutical Sciencesinstname:Universidade de São Paulo (USP)instacron:USPenghttps://www.revistas.usp.br/bjps/article/view/144061/138552Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso)info:eu-repo/semantics/openAccessBonfilio, RudySouza, Marília Cristina OliveiraLeal, Jockastta SilvaViana, Olímpia Maria Martins SantosDoriguetto, Antônio CarlosAraújo, Magali Benjamin de2018-03-05T19:53:59Zoai:revistas.usp.br:article/144061Revistahttps://www.revistas.usp.br/bjps/indexPUBhttps://old.scielo.br/oai/scielo-oai.phpbjps@usp.br||elizabeth.igne@gmail.com2175-97901984-8250opendoar:2018-03-05T19:53:59Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)false |
dc.title.none.fl_str_mv |
Solubility and dissolution studies of tibolone polymorphs |
title |
Solubility and dissolution studies of tibolone polymorphs |
spellingShingle |
Solubility and dissolution studies of tibolone polymorphs Bonfilio, Rudy Tibolone/polymorphs Powder X-ray diffraction/methods Infrared spectroscopy/methods Solubility/drug effects Dissolution/analysis |
title_short |
Solubility and dissolution studies of tibolone polymorphs |
title_full |
Solubility and dissolution studies of tibolone polymorphs |
title_fullStr |
Solubility and dissolution studies of tibolone polymorphs |
title_full_unstemmed |
Solubility and dissolution studies of tibolone polymorphs |
title_sort |
Solubility and dissolution studies of tibolone polymorphs |
author |
Bonfilio, Rudy |
author_facet |
Bonfilio, Rudy Souza, Marília Cristina Oliveira Leal, Jockastta Silva Viana, Olímpia Maria Martins Santos Doriguetto, Antônio Carlos Araújo, Magali Benjamin de |
author_role |
author |
author2 |
Souza, Marília Cristina Oliveira Leal, Jockastta Silva Viana, Olímpia Maria Martins Santos Doriguetto, Antônio Carlos Araújo, Magali Benjamin de |
author2_role |
author author author author author |
dc.contributor.author.fl_str_mv |
Bonfilio, Rudy Souza, Marília Cristina Oliveira Leal, Jockastta Silva Viana, Olímpia Maria Martins Santos Doriguetto, Antônio Carlos Araújo, Magali Benjamin de |
dc.subject.por.fl_str_mv |
Tibolone/polymorphs Powder X-ray diffraction/methods Infrared spectroscopy/methods Solubility/drug effects Dissolution/analysis |
topic |
Tibolone/polymorphs Powder X-ray diffraction/methods Infrared spectroscopy/methods Solubility/drug effects Dissolution/analysis |
description |
Different solid forms of an active pharmaceutical ingredient can have distinct chemical and physical characteristics. In this work, we studied the solubility and dissolution properties of the described tibolone polymorphic forms (I and II). Both forms were successively recrystallized and characterized by powder X-ray diffraction and attenuated total reflection infrared spectroscopy. Equilibrium solubility and dissolution profiles were performed for both forms. Solubility studies demonstrated that form II is statistically more soluble in water, 0.01 mol L-1 HCl and pH 4.5 acetate buffer. The solubility of forms I and II were explained in terms of crystal packing. Dissolution tests of tablets showed a lower release of polymorphic form II than form I from tablets. The results showed an impact of polymorphism on the quality of tibolone tablets and suggest that tibolone forms I and II can show distinct interactions with pharmaceutical excipients used in tablets. Therefore, only form I is acceptable for the preparation of tablet forms. Based on our results, we propose the quality control on tibolone raw materials using X-ray diffraction analysis and attenuated total reflection infrared spectroscopy. |
publishDate |
2017 |
dc.date.none.fl_str_mv |
2017-01-01 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/144061 10.1590/s2175-97902017000400233 |
url |
https://www.revistas.usp.br/bjps/article/view/144061 |
identifier_str_mv |
10.1590/s2175-97902017000400233 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/144061/138552 |
dc.rights.driver.fl_str_mv |
Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso) info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso) |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
dc.source.none.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences; Vol. 53 Núm. 4 (2017); e00233 Brazilian Journal of Pharmaceutical Sciences; v. 53 n. 4 (2017); e00233 Brazilian Journal of Pharmaceutical Sciences; Vol. 53 No. 4 (2017); e00233 2175-9790 1984-8250 reponame:Brazilian Journal of Pharmaceutical Sciences instname:Universidade de São Paulo (USP) instacron:USP |
instname_str |
Universidade de São Paulo (USP) |
instacron_str |
USP |
institution |
USP |
reponame_str |
Brazilian Journal of Pharmaceutical Sciences |
collection |
Brazilian Journal of Pharmaceutical Sciences |
repository.name.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP) |
repository.mail.fl_str_mv |
bjps@usp.br||elizabeth.igne@gmail.com |
_version_ |
1800222913319665664 |