Dissolution properties, solid-state transformation and polymorphic crystallization: Progesterone case study

Autores
Araya Sibaja, Andrea Mariela; Paulino, Amarilis Scremin; Rauber, Gabriela Schneider; Maduro Campos, Carlos Eduardo; Cardoso, Simone Gonçalves; Monti, Gustavo Alberto; Heredia, Valeria; Bianco, Ismael Dario; Beltrano, Dante; Cuffini, Silvia Lucia
Año de publicación
2014
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Progesterone is a natural steroid hormone and a poor soluble drug which presents two polymorphs (forms 1 and 2). Different methods to obtain form 2 were tested and a complete solid-state characterization of both polymorphs (forms 1 and 2) was conducted. X-ray powder diffraction, hot stage microscopy, Fourier transform infrared, dispersive Raman, 13C solid-state nuclear magnetic resonance spectroscopy, thermal analysis, scanning electron microscopy techniques and intrinsic dissolution rates (IDR) were applied to investigate physical-chemical and dissolution properties of these two polymorphs. Form 2 was obtained from diluted solutions and from melting after cooling at room temperature. Form 1 was obtained from concentrated solutions and, a mixture of both polymorphs was crystallized from intermediate solutions. The crystal habit was not a distinctive characteristic of each polymorph. The effect of mechanical stress was evaluated in the metastable polymorph (form 2). We observed that grinding form 2 produced seeds of form 1 that induced the transformation of form 2 into form 1 at high temperature. The polymorphic quantification from XRD patterns of ground samples were carried out by the Rietveld method. After grinding and at room temperature conditions (∼25 °C), it was observed the transformation of 17% of form 2 into form 1 in 10 days.
Fil: Araya Sibaja, Andrea Mariela. Universidad de Costa Rica; Costa Rica. Universidade Federal de Santa Catarina; Brasil
Fil: Paulino, Amarilis Scremin. Universidade Federal de Santa Catarina; Brasil
Fil: Rauber, Gabriela Schneider. Universidade Federal de Santa Catarina; Brasil
Fil: Maduro Campos, Carlos Eduardo. Universidade Federal de Santa Catarina; Brasil
Fil: Cardoso, Simone Gonçalves. Universidade Federal de Santa Catarina; Brasil
Fil: Monti, Gustavo Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Física Enrique Gaviola. Universidad Nacional de Córdoba. Instituto de Física Enrique Gaviola; Argentina. Universidad Nacional de Córdoba. Facultad de Matemática, Astronomía y Física; Argentina
Fil: Heredia, Valeria. Provincia de Córdoba. Ministerio de Ciencia y Técnica. Centro de Excelencia en Productos y Procesos de Córdoba; Argentina
Fil: Bianco, Ismael Dario. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba; Argentina. Provincia de Córdoba. Ministerio de Ciencia y Técnica. Centro de Excelencia en Productos y Procesos de Córdoba; Argentina. Universidad Nacional de la Rioja. Departamento de Ciencias Exactas, Físicas y Naturales; Argentina
Fil: Beltrano, Dante. Provincia de Córdoba. Ministerio de Ciencia y Técnica. Centro de Excelencia en Productos y Procesos de Córdoba; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba; Argentina. Universidad Católica de Córdoba. Facultad de Ciencias Químicas; Argentina
Fil: Cuffini, Silvia Lucia. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidade Federal de Santa Catarina; Brasil. Provincia de Córdoba. Ministerio de Ciencia y Técnica; Argentina
Materia
INTRINSIC DISSOLUTION RATE
PHASE TRANSFORMATION
POLYMORPHISM
PROGESTERONE
SOLID-STATE CHARACTERIZATION
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/99375
Acceder
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network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Dissolution properties, solid-state transformation and polymorphic crystallization: Progesterone case studyAraya Sibaja, Andrea MarielaPaulino, Amarilis ScreminRauber, Gabriela SchneiderMaduro Campos, Carlos EduardoCardoso, Simone GonçalvesMonti, Gustavo AlbertoHeredia, ValeriaBianco, Ismael DarioBeltrano, DanteCuffini, Silvia LuciaINTRINSIC DISSOLUTION RATEPHASE TRANSFORMATIONPOLYMORPHISMPROGESTERONESOLID-STATE CHARACTERIZATIONhttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1Progesterone is a natural steroid hormone and a poor soluble drug which presents two polymorphs (forms 1 and 2). Different methods to obtain form 2 were tested and a complete solid-state characterization of both polymorphs (forms 1 and 2) was conducted. X-ray powder diffraction, hot stage microscopy, Fourier transform infrared, dispersive Raman, 13C solid-state nuclear magnetic resonance spectroscopy, thermal analysis, scanning electron microscopy techniques and intrinsic dissolution rates (IDR) were applied to investigate physical-chemical and dissolution properties of these two polymorphs. Form 2 was obtained from diluted solutions and from melting after cooling at room temperature. Form 1 was obtained from concentrated solutions and, a mixture of both polymorphs was crystallized from intermediate solutions. The crystal habit was not a distinctive characteristic of each polymorph. The effect of mechanical stress was evaluated in the metastable polymorph (form 2). We observed that grinding form 2 produced seeds of form 1 that induced the transformation of form 2 into form 1 at high temperature. The polymorphic quantification from XRD patterns of ground samples were carried out by the Rietveld method. After grinding and at room temperature conditions (∼25 °C), it was observed the transformation of 17% of form 2 into form 1 in 10 days.Fil: Araya Sibaja, Andrea Mariela. Universidad de Costa Rica; Costa Rica. Universidade Federal de Santa Catarina; BrasilFil: Paulino, Amarilis Scremin. Universidade Federal de Santa Catarina; BrasilFil: Rauber, Gabriela Schneider. Universidade Federal de Santa Catarina; BrasilFil: Maduro Campos, Carlos Eduardo. Universidade Federal de Santa Catarina; BrasilFil: Cardoso, Simone Gonçalves. Universidade Federal de Santa Catarina; BrasilFil: Monti, Gustavo Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Física Enrique Gaviola. Universidad Nacional de Córdoba. Instituto de Física Enrique Gaviola; Argentina. Universidad Nacional de Córdoba. Facultad de Matemática, Astronomía y Física; ArgentinaFil: Heredia, Valeria. Provincia de Córdoba. Ministerio de Ciencia y Técnica. Centro de Excelencia en Productos y Procesos de Córdoba; ArgentinaFil: Bianco, Ismael Dario. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba; Argentina. Provincia de Córdoba. Ministerio de Ciencia y Técnica. Centro de Excelencia en Productos y Procesos de Córdoba; Argentina. Universidad Nacional de la Rioja. Departamento de Ciencias Exactas, Físicas y Naturales; ArgentinaFil: Beltrano, Dante. Provincia de Córdoba. Ministerio de Ciencia y Técnica. Centro de Excelencia en Productos y Procesos de Córdoba; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba; Argentina. Universidad Católica de Córdoba. Facultad de Ciencias Químicas; ArgentinaFil: Cuffini, Silvia Lucia. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidade Federal de Santa Catarina; Brasil. Provincia de Córdoba. Ministerio de Ciencia y Técnica; ArgentinaTaylor & Francis2014-11info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/99375Araya Sibaja, Andrea Mariela; Paulino, Amarilis Scremin; Rauber, Gabriela Schneider; Maduro Campos, Carlos Eduardo; Cardoso, Simone Gonçalves; et al.; Dissolution properties, solid-state transformation and polymorphic crystallization: Progesterone case study; Taylor & Francis; Pharmaceutical Development and Technology; 19; 7; 11-2014; 779-7881083-7450CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://www.tandfonline.com/doi/abs/10.3109/10837450.2013.829096info:eu-repo/semantics/altIdentifier/doi/10.3109/10837450.2013.829096info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:40:31Zoai:ri.conicet.gov.ar:11336/99375instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-29 10:40:31.845CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Dissolution properties, solid-state transformation and polymorphic crystallization: Progesterone case study
title Dissolution properties, solid-state transformation and polymorphic crystallization: Progesterone case study
spellingShingle Dissolution properties, solid-state transformation and polymorphic crystallization: Progesterone case study
Araya Sibaja, Andrea Mariela
INTRINSIC DISSOLUTION RATE
PHASE TRANSFORMATION
POLYMORPHISM
PROGESTERONE
SOLID-STATE CHARACTERIZATION
title_short Dissolution properties, solid-state transformation and polymorphic crystallization: Progesterone case study
title_full Dissolution properties, solid-state transformation and polymorphic crystallization: Progesterone case study
title_fullStr Dissolution properties, solid-state transformation and polymorphic crystallization: Progesterone case study
title_full_unstemmed Dissolution properties, solid-state transformation and polymorphic crystallization: Progesterone case study
title_sort Dissolution properties, solid-state transformation and polymorphic crystallization: Progesterone case study
dc.creator.none.fl_str_mv Araya Sibaja, Andrea Mariela
Paulino, Amarilis Scremin
Rauber, Gabriela Schneider
Maduro Campos, Carlos Eduardo
Cardoso, Simone Gonçalves
Monti, Gustavo Alberto
Heredia, Valeria
Bianco, Ismael Dario
Beltrano, Dante
Cuffini, Silvia Lucia
author Araya Sibaja, Andrea Mariela
author_facet Araya Sibaja, Andrea Mariela
Paulino, Amarilis Scremin
Rauber, Gabriela Schneider
Maduro Campos, Carlos Eduardo
Cardoso, Simone Gonçalves
Monti, Gustavo Alberto
Heredia, Valeria
Bianco, Ismael Dario
Beltrano, Dante
Cuffini, Silvia Lucia
author_role author
author2 Paulino, Amarilis Scremin
Rauber, Gabriela Schneider
Maduro Campos, Carlos Eduardo
Cardoso, Simone Gonçalves
Monti, Gustavo Alberto
Heredia, Valeria
Bianco, Ismael Dario
Beltrano, Dante
Cuffini, Silvia Lucia
author2_role author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv INTRINSIC DISSOLUTION RATE
PHASE TRANSFORMATION
POLYMORPHISM
PROGESTERONE
SOLID-STATE CHARACTERIZATION
topic INTRINSIC DISSOLUTION RATE
PHASE TRANSFORMATION
POLYMORPHISM
PROGESTERONE
SOLID-STATE CHARACTERIZATION
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv Progesterone is a natural steroid hormone and a poor soluble drug which presents two polymorphs (forms 1 and 2). Different methods to obtain form 2 were tested and a complete solid-state characterization of both polymorphs (forms 1 and 2) was conducted. X-ray powder diffraction, hot stage microscopy, Fourier transform infrared, dispersive Raman, 13C solid-state nuclear magnetic resonance spectroscopy, thermal analysis, scanning electron microscopy techniques and intrinsic dissolution rates (IDR) were applied to investigate physical-chemical and dissolution properties of these two polymorphs. Form 2 was obtained from diluted solutions and from melting after cooling at room temperature. Form 1 was obtained from concentrated solutions and, a mixture of both polymorphs was crystallized from intermediate solutions. The crystal habit was not a distinctive characteristic of each polymorph. The effect of mechanical stress was evaluated in the metastable polymorph (form 2). We observed that grinding form 2 produced seeds of form 1 that induced the transformation of form 2 into form 1 at high temperature. The polymorphic quantification from XRD patterns of ground samples were carried out by the Rietveld method. After grinding and at room temperature conditions (∼25 °C), it was observed the transformation of 17% of form 2 into form 1 in 10 days.
Fil: Araya Sibaja, Andrea Mariela. Universidad de Costa Rica; Costa Rica. Universidade Federal de Santa Catarina; Brasil
Fil: Paulino, Amarilis Scremin. Universidade Federal de Santa Catarina; Brasil
Fil: Rauber, Gabriela Schneider. Universidade Federal de Santa Catarina; Brasil
Fil: Maduro Campos, Carlos Eduardo. Universidade Federal de Santa Catarina; Brasil
Fil: Cardoso, Simone Gonçalves. Universidade Federal de Santa Catarina; Brasil
Fil: Monti, Gustavo Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Física Enrique Gaviola. Universidad Nacional de Córdoba. Instituto de Física Enrique Gaviola; Argentina. Universidad Nacional de Córdoba. Facultad de Matemática, Astronomía y Física; Argentina
Fil: Heredia, Valeria. Provincia de Córdoba. Ministerio de Ciencia y Técnica. Centro de Excelencia en Productos y Procesos de Córdoba; Argentina
Fil: Bianco, Ismael Dario. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba; Argentina. Provincia de Córdoba. Ministerio de Ciencia y Técnica. Centro de Excelencia en Productos y Procesos de Córdoba; Argentina. Universidad Nacional de la Rioja. Departamento de Ciencias Exactas, Físicas y Naturales; Argentina
Fil: Beltrano, Dante. Provincia de Córdoba. Ministerio de Ciencia y Técnica. Centro de Excelencia en Productos y Procesos de Córdoba; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba; Argentina. Universidad Católica de Córdoba. Facultad de Ciencias Químicas; Argentina
Fil: Cuffini, Silvia Lucia. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidade Federal de Santa Catarina; Brasil. Provincia de Córdoba. Ministerio de Ciencia y Técnica; Argentina
description Progesterone is a natural steroid hormone and a poor soluble drug which presents two polymorphs (forms 1 and 2). Different methods to obtain form 2 were tested and a complete solid-state characterization of both polymorphs (forms 1 and 2) was conducted. X-ray powder diffraction, hot stage microscopy, Fourier transform infrared, dispersive Raman, 13C solid-state nuclear magnetic resonance spectroscopy, thermal analysis, scanning electron microscopy techniques and intrinsic dissolution rates (IDR) were applied to investigate physical-chemical and dissolution properties of these two polymorphs. Form 2 was obtained from diluted solutions and from melting after cooling at room temperature. Form 1 was obtained from concentrated solutions and, a mixture of both polymorphs was crystallized from intermediate solutions. The crystal habit was not a distinctive characteristic of each polymorph. The effect of mechanical stress was evaluated in the metastable polymorph (form 2). We observed that grinding form 2 produced seeds of form 1 that induced the transformation of form 2 into form 1 at high temperature. The polymorphic quantification from XRD patterns of ground samples were carried out by the Rietveld method. After grinding and at room temperature conditions (∼25 °C), it was observed the transformation of 17% of form 2 into form 1 in 10 days.
publishDate 2014
dc.date.none.fl_str_mv 2014-11
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/99375
Araya Sibaja, Andrea Mariela; Paulino, Amarilis Scremin; Rauber, Gabriela Schneider; Maduro Campos, Carlos Eduardo; Cardoso, Simone Gonçalves; et al.; Dissolution properties, solid-state transformation and polymorphic crystallization: Progesterone case study; Taylor & Francis; Pharmaceutical Development and Technology; 19; 7; 11-2014; 779-788
1083-7450
CONICET Digital
CONICET
url http://hdl.handle.net/11336/99375
identifier_str_mv Araya Sibaja, Andrea Mariela; Paulino, Amarilis Scremin; Rauber, Gabriela Schneider; Maduro Campos, Carlos Eduardo; Cardoso, Simone Gonçalves; et al.; Dissolution properties, solid-state transformation and polymorphic crystallization: Progesterone case study; Taylor & Francis; Pharmaceutical Development and Technology; 19; 7; 11-2014; 779-788
1083-7450
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/https://www.tandfonline.com/doi/abs/10.3109/10837450.2013.829096
info:eu-repo/semantics/altIdentifier/doi/10.3109/10837450.2013.829096
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
application/pdf
application/pdf
dc.publisher.none.fl_str_mv Taylor & Francis
publisher.none.fl_str_mv Taylor & Francis
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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score 13.070432

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