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

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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 microsc...

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Autores principales:	Araya-Sibaja, Andrea Mariela, Paulino, Amarilis Scremin, Rauber, Gabriela Schneider, Maduro Campos, Carlos Eduardo, Cardoso, Simone Gonçalves, Monti, Gustavo Alberto, Heredia, Valeria, Bianco, Ismael Darío, Beltramo, Dante Miguel, Cuffini, Silvia Lucía
Formato:	article
Lenguaje:	Inglés
Publicado:	2022
Materias:	Intrinsic disolution rate Phase transformation Polymorphism Progesterone
Acceso en línea:	http://hdl.handle.net/11086/25007 https://doi.org/10.3109/10837450.2013.829096 https://doi.org/10.3109/10837450.2013.829096
Aporte de:	Repositorio Digital Universitario (UNC) de Universidad Nacional de Córdoba

id	I10-R141-11086-25007
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institution	Universidad Nacional de Córdoba
institution_str	I-10
repository_str	R-141
collection	Repositorio Digital Universitario (UNC)
language	Inglés
topic	Intrinsic disolution rate Phase transformation Polymorphism Progesterone
spellingShingle	Intrinsic disolution rate Phase transformation Polymorphism Progesterone Araya-Sibaja, Andrea Mariela Paulino, Amarilis Scremin Rauber, Gabriela Schneider Maduro Campos, Carlos Eduardo Cardoso, Simone Gonçalves Monti, Gustavo Alberto Heredia, Valeria Bianco, Ismael Darío Beltramo, Dante Miguel Cuffini, Silvia Lucía Dissolution properties, solid-state transformation and polymorphic crystallization: progesterone case study
topic_facet	Intrinsic disolution rate Phase transformation Polymorphism Progesterone
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.
format	article
author	Araya-Sibaja, Andrea Mariela Paulino, Amarilis Scremin Rauber, Gabriela Schneider Maduro Campos, Carlos Eduardo Cardoso, Simone Gonçalves Monti, Gustavo Alberto Heredia, Valeria Bianco, Ismael Darío Beltramo, Dante Miguel Cuffini, Silvia Lucía
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 Darío Beltramo, Dante Miguel Cuffini, Silvia Lucía
author_sort	Araya-Sibaja, Andrea Mariela
title	Dissolution properties, solid-state transformation and polymorphic crystallization: progesterone case study
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
publishDate	2022
url	http://hdl.handle.net/11086/25007 https://doi.org/10.3109/10837450.2013.829096 https://doi.org/10.3109/10837450.2013.829096
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Dissolution properties, solid-state transformation and polymorphic crystallization: progesterone case study

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