Pressure-temperature phase diagram of the dimorphism of the anti-inflammatory drug nimesulide
Understanding the phase behavior of active pharmaceutical ingredients is important for formulations of dosage forms and regulatory reasons. Nimesulide is an anti-inflammatory drug that is known to exhibit dimorphism; however up to now its stability behavior was not clear, as few thermodynamic data w...
| Autores: | , , , , , |
|---|---|
| Tipo de recurso: | artículo |
| Fecha de publicación: | 2017 |
| País: | España |
| Institución: | Universitat Politècnica de Catalunya (UPC) |
| Repositorio: | UPCommons. Portal del coneixement obert de la UPC |
| Idioma: | inglés |
| OAI Identifier: | oai:upcommons.upc.edu:2117/104659 |
| Acceso en línea: | https://hdl.handle.net/2117/104659 https://dx.doi.org/10.1016/j.ijpharm.2017.04.016 |
| Access Level: | acceso abierto |
| Palabra clave: | Calorimetry Crystallography Polymorphism (Crystallography) Thermodynamics Polymorphism Pressure-temperature phase diagram Phase behavior Preformulation Termodinàmica Cristal·lografia Calorimetria Polimorfisme (Cristal·lografia) Àrees temàtiques de la UPC::Física |
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Pressure-temperature phase diagram of the dimorphism of the anti-inflammatory drug nimesulideBarrio Casado, María del|||0000-0003-3467-7581Huguet, JordiRobert, B.Rietveld, Ivo B.Céolin, RenéTamarit Mur, José Luis|||0000-0002-7965-0000CalorimetryCrystallographyPolymorphism (Crystallography)ThermodynamicsPolymorphismThermodynamicsPressure-temperature phase diagramPhase behaviorCrystallographyCalorimetryPreformulationTermodinàmicaCristal·lografiaCalorimetriaPolimorfisme (Cristal·lografia)Àrees temàtiques de la UPC::FísicaUnderstanding the phase behavior of active pharmaceutical ingredients is important for formulations of dosage forms and regulatory reasons. Nimesulide is an anti-inflammatory drug that is known to exhibit dimorphism; however up to now its stability behavior was not clear, as few thermodynamic data were available. Therefore, calorimetric melting data have been obtained, which were found to be TI-L = 422.4 ± 1.0 K, ¿I ¿ LH = 117.5 ± 5.2 J g-1, TII-L = 419.8 ± 1.0 K and ¿II ¿ LH = 108.6 ± 3.3 J g-1. In addition, vapor-pressure data, high-pressure melting data, and specific volumes have been obtained. It is demonstrated that form II is intrinsically monotropic in relation to form I and the latter would thus be the best polymorph to use for drug formulations. This result has been obtained by experimental means, involving high-pressure measurements. Furthermore, it has been shown that with very limited experimental and statistical data, the same conclusion can be obtained, demonstrating that in first instance topological pressure-temperature phase diagrams can be obtained without necessarily measuring any high-pressure data. It provides a quick method to verify the phase behavior of the known phases of an active pharmaceutical ingredient under different pressure and temperature conditions.20172017-06-1520172017-05-19journal articlehttp://purl.org/coar/resource_type/c_6501AMhttp://purl.org/coar/version/c_ab4af688f83e57aainfo:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/2117/104659https://dx.doi.org/10.1016/j.ijpharm.2017.04.016reponame:UPCommons. Portal del coneixement obert de la UPCinstname:Universitat Politècnica de Catalunya (UPC)Inglésengopen accesshttp://purl.org/coar/access_right/c_abf2info:eu-repo/semantics/openAccessoai:upcommons.upc.edu:2117/1046592026-05-27T15:37:01Z |
| dc.title.none.fl_str_mv |
Pressure-temperature phase diagram of the dimorphism of the anti-inflammatory drug nimesulide |
| title |
Pressure-temperature phase diagram of the dimorphism of the anti-inflammatory drug nimesulide |
| spellingShingle |
Pressure-temperature phase diagram of the dimorphism of the anti-inflammatory drug nimesulide Barrio Casado, María del|||0000-0003-3467-7581 Calorimetry Crystallography Polymorphism (Crystallography) Thermodynamics Polymorphism Thermodynamics Pressure-temperature phase diagram Phase behavior Crystallography Calorimetry Preformulation Termodinàmica Cristal·lografia Calorimetria Polimorfisme (Cristal·lografia) Àrees temàtiques de la UPC::Física |
| title_short |
Pressure-temperature phase diagram of the dimorphism of the anti-inflammatory drug nimesulide |
| title_full |
Pressure-temperature phase diagram of the dimorphism of the anti-inflammatory drug nimesulide |
| title_fullStr |
Pressure-temperature phase diagram of the dimorphism of the anti-inflammatory drug nimesulide |
| title_full_unstemmed |
Pressure-temperature phase diagram of the dimorphism of the anti-inflammatory drug nimesulide |
| title_sort |
Pressure-temperature phase diagram of the dimorphism of the anti-inflammatory drug nimesulide |
| dc.creator.none.fl_str_mv |
Barrio Casado, María del|||0000-0003-3467-7581 Huguet, Jordi Robert, B. Rietveld, Ivo B. Céolin, René Tamarit Mur, José Luis|||0000-0002-7965-0000 |
| author |
Barrio Casado, María del|||0000-0003-3467-7581 |
| author_facet |
Barrio Casado, María del|||0000-0003-3467-7581 Huguet, Jordi Robert, B. Rietveld, Ivo B. Céolin, René Tamarit Mur, José Luis|||0000-0002-7965-0000 |
| author_role |
author |
| author2 |
Huguet, Jordi Robert, B. Rietveld, Ivo B. Céolin, René Tamarit Mur, José Luis|||0000-0002-7965-0000 |
| author2_role |
author author author author author |
| dc.subject.none.fl_str_mv |
Calorimetry Crystallography Polymorphism (Crystallography) Thermodynamics Polymorphism Thermodynamics Pressure-temperature phase diagram Phase behavior Crystallography Calorimetry Preformulation Termodinàmica Cristal·lografia Calorimetria Polimorfisme (Cristal·lografia) Àrees temàtiques de la UPC::Física |
| topic |
Calorimetry Crystallography Polymorphism (Crystallography) Thermodynamics Polymorphism Thermodynamics Pressure-temperature phase diagram Phase behavior Crystallography Calorimetry Preformulation Termodinàmica Cristal·lografia Calorimetria Polimorfisme (Cristal·lografia) Àrees temàtiques de la UPC::Física |
| description |
Understanding the phase behavior of active pharmaceutical ingredients is important for formulations of dosage forms and regulatory reasons. Nimesulide is an anti-inflammatory drug that is known to exhibit dimorphism; however up to now its stability behavior was not clear, as few thermodynamic data were available. Therefore, calorimetric melting data have been obtained, which were found to be TI-L = 422.4 ± 1.0 K, ¿I ¿ LH = 117.5 ± 5.2 J g-1, TII-L = 419.8 ± 1.0 K and ¿II ¿ LH = 108.6 ± 3.3 J g-1. In addition, vapor-pressure data, high-pressure melting data, and specific volumes have been obtained. It is demonstrated that form II is intrinsically monotropic in relation to form I and the latter would thus be the best polymorph to use for drug formulations. This result has been obtained by experimental means, involving high-pressure measurements. Furthermore, it has been shown that with very limited experimental and statistical data, the same conclusion can be obtained, demonstrating that in first instance topological pressure-temperature phase diagrams can be obtained without necessarily measuring any high-pressure data. It provides a quick method to verify the phase behavior of the known phases of an active pharmaceutical ingredient under different pressure and temperature conditions. |
| publishDate |
2017 |
| dc.date.none.fl_str_mv |
2017 2017-06-15 2017 2017-05-19 |
| dc.type.none.fl_str_mv |
journal article http://purl.org/coar/resource_type/c_6501 AM http://purl.org/coar/version/c_ab4af688f83e57aa |
| dc.type.openaire.fl_str_mv |
info:eu-repo/semantics/article |
| format |
article |
| dc.identifier.none.fl_str_mv |
https://hdl.handle.net/2117/104659 https://dx.doi.org/10.1016/j.ijpharm.2017.04.016 |
| url |
https://hdl.handle.net/2117/104659 https://dx.doi.org/10.1016/j.ijpharm.2017.04.016 |
| dc.language.none.fl_str_mv |
Inglés eng |
| language_invalid_str_mv |
Inglés |
| language |
eng |
| dc.rights.none.fl_str_mv |
open access http://purl.org/coar/access_right/c_abf2 |
| dc.rights.openaire.fl_str_mv |
info:eu-repo/semantics/openAccess |
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open access http://purl.org/coar/access_right/c_abf2 |
| eu_rights_str_mv |
openAccess |
| dc.format.none.fl_str_mv |
application/pdf |
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reponame:UPCommons. Portal del coneixement obert de la UPC instname:Universitat Politècnica de Catalunya (UPC) |
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Universitat Politècnica de Catalunya (UPC) |
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UPCommons. Portal del coneixement obert de la UPC |
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UPCommons. Portal del coneixement obert de la UPC |
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1869408956387950592 |
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15.301603 |