Towards a rational basis for selection of excipients: Excipient Efficiency for controlled release

There are many factors influencing the drug release behaviour from a pharmaceutical formulation as the particle size of the drug and excipient, porosity of the system or geometrical phase transitions of the components. Therefore, the choice of the adequate excipient to achieve a specific drug releas...

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Autores: Casas Delgado, Marta, Aguilar de Leyva, Mercedes Ángela, Caraballo Rodríguez, Isidoro
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2015
País:España
Institución:Universidad de Sevilla (US)
Repositorio:idUS. Depósito de Investigación de la Universidad de Sevilla
OAI Identifier:oai:idus.us.es:11441/162869
Acceso en línea:https://hdl.handle.net/11441/162869
https://doi.org/10.1016/j.ijpharm.2015.08.002
Access Level:acceso abierto
Palabra clave:Excipient Efficiency
controlled drug release
particle size
porosity
critical points
solubility
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spelling Towards a rational basis for selection of excipients: Excipient Efficiency for controlled releaseCasas Delgado, MartaAguilar de Leyva, Mercedes ÁngelaCaraballo Rodríguez, IsidoroExcipient Efficiencycontrolled drug releaseparticle sizeporositycritical pointssolubilityThere are many factors influencing the drug release behaviour from a pharmaceutical formulation as the particle size of the drug and excipient, porosity of the system or geometrical phase transitions of the components. Therefore, the choice of the adequate excipient to achieve a specific drug release profile is mainly based on the experience and the trial and error method. Taking into account the directives towards the application of the “Quality by Design” approach, in this study the Excipient Efficiency (EE), a parameter able to quantify the capability of an excipient to control the drug release, has been developed. EE was initially calculated dividing the total porosity of the system by its diffusional release rate constant. The influence of several factors on this parameter has been evaluated. As a result, the final parameter has been corrected based on the drug solubility and the excipient particle size. EE provides a rational basis for identifying the most adequate excipients for a concrete formulation.Ministerio de Economía y Competitividad de España - MAT2012-38,044-C03-02ElsevierFarmacia y Tecnología FarmacéuticaMinisterio de Economía y Competitividad (MINECO). España2015info:eu-repo/semantics/articleinfo:eu-repo/semantics/acceptedVersionapplication/pdfapplication/pdfhttps://hdl.handle.net/11441/162869https://doi.org/10.1016/j.ijpharm.2015.08.002reponame:idUS. Depósito de Investigación de la Universidad de Sevillainstname:Universidad de Sevilla (US)InglésInternational Journal of Pharmaceutics, 494 (1), 288-295.MAT2012-38,044-C03-02https://doi.org/10.1016/j.ijpharm.2015.08.002info:eu-repo/semantics/openAccessoai:idus.us.es:11441/1628692026-06-17T12:51:07Z
dc.title.none.fl_str_mv Towards a rational basis for selection of excipients: Excipient Efficiency for controlled release
title Towards a rational basis for selection of excipients: Excipient Efficiency for controlled release
spellingShingle Towards a rational basis for selection of excipients: Excipient Efficiency for controlled release
Casas Delgado, Marta
Excipient Efficiency
controlled drug release
particle size
porosity
critical points
solubility
title_short Towards a rational basis for selection of excipients: Excipient Efficiency for controlled release
title_full Towards a rational basis for selection of excipients: Excipient Efficiency for controlled release
title_fullStr Towards a rational basis for selection of excipients: Excipient Efficiency for controlled release
title_full_unstemmed Towards a rational basis for selection of excipients: Excipient Efficiency for controlled release
title_sort Towards a rational basis for selection of excipients: Excipient Efficiency for controlled release
dc.creator.none.fl_str_mv Casas Delgado, Marta
Aguilar de Leyva, Mercedes Ángela
Caraballo Rodríguez, Isidoro
author Casas Delgado, Marta
author_facet Casas Delgado, Marta
Aguilar de Leyva, Mercedes Ángela
Caraballo Rodríguez, Isidoro
author_role author
author2 Aguilar de Leyva, Mercedes Ángela
Caraballo Rodríguez, Isidoro
author2_role author
author
dc.contributor.none.fl_str_mv Farmacia y Tecnología Farmacéutica
Ministerio de Economía y Competitividad (MINECO). España
dc.subject.none.fl_str_mv Excipient Efficiency
controlled drug release
particle size
porosity
critical points
solubility
topic Excipient Efficiency
controlled drug release
particle size
porosity
critical points
solubility
description There are many factors influencing the drug release behaviour from a pharmaceutical formulation as the particle size of the drug and excipient, porosity of the system or geometrical phase transitions of the components. Therefore, the choice of the adequate excipient to achieve a specific drug release profile is mainly based on the experience and the trial and error method. Taking into account the directives towards the application of the “Quality by Design” approach, in this study the Excipient Efficiency (EE), a parameter able to quantify the capability of an excipient to control the drug release, has been developed. EE was initially calculated dividing the total porosity of the system by its diffusional release rate constant. The influence of several factors on this parameter has been evaluated. As a result, the final parameter has been corrected based on the drug solubility and the excipient particle size. EE provides a rational basis for identifying the most adequate excipients for a concrete formulation.
publishDate 2015
dc.date.none.fl_str_mv 2015
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/acceptedVersion
format article
status_str acceptedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/11441/162869
https://doi.org/10.1016/j.ijpharm.2015.08.002
url https://hdl.handle.net/11441/162869
https://doi.org/10.1016/j.ijpharm.2015.08.002
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv International Journal of Pharmaceutics, 494 (1), 288-295.
MAT2012-38,044-C03-02
https://doi.org/10.1016/j.ijpharm.2015.08.002
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:idUS. Depósito de Investigación de la Universidad de Sevilla
instname:Universidad de Sevilla (US)
instname_str Universidad de Sevilla (US)
reponame_str idUS. Depósito de Investigación de la Universidad de Sevilla
collection idUS. Depósito de Investigación de la Universidad de Sevilla
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,811543

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