Albendazole Solid Dispersions: Influence of Dissolution Medium Composition on In Vitro Drug Release

Autores
González Vidal, Noelia Luján; Castro, Silvina Gabriela; Sanchez Bruni, Sergio Fabian; Allemandi, Daniel Alberto; Palma, Santiago Daniel
Año de publicación
2014
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
The rate-limiting step to drug absorption is often dissolution from the dosage form, especially for poorly soluble com-pounds. Two possibilities for improving the dissolution of these drugs are to increase the available surface area and to im-prove their apparent solubilities under physiologically relevant conditions with surfactants as wetting agents. Albendazole (ABZ), one of the most effective broad-spectrum antihelminthic agents, has a very low aqueous solubility, which leads to an erratic availability. Solid dispersions (SD) with different amounts of carriers (P188 and PEG6000) were formulated to improve the ABZ dissolution rate. When the dissolution test is used to infer biopharmaceutical properties of the dosage form, it is es-sential that the method simulates the gastrointestinal conditions. The objective of this study was to examine the applicabil-ity of different dissolution media to the evaluation of ABZ and ABZ-SD dissolution rates. Dissolution profiles were performed by the official method (0.1 N HCl) and Simulated Gastric Fluid modified with a surfactant. Wetting was evaluated through the determination of surface tension and contact angle of the solutions. The dissolution rate of ABZ was clearly affected by the variables assessed in this study. These results have implications in the design of physiologically based dissolution media.
Fil: González Vidal, Noelia Luján. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia. Cátedra de Control de Calidad de Medicamentos; Argentina
Fil: Castro, Silvina Gabriela. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Sanchez Bruni, Sergio Fabian. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
Fil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Materia
Contact Angle
Surface Tension
Dissolution Rate
Solid Dispersions
Albendazole
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:11336/33421
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/33421
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Albendazole Solid Dispersions: Influence of Dissolution Medium Composition on In Vitro Drug ReleaseGonzález Vidal, Noelia LujánCastro, Silvina GabrielaSanchez Bruni, Sergio FabianAllemandi, Daniel AlbertoPalma, Santiago DanielContact AngleSurface TensionDissolution RateSolid DispersionsAlbendazolehttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1The rate-limiting step to drug absorption is often dissolution from the dosage form, especially for poorly soluble com-pounds. Two possibilities for improving the dissolution of these drugs are to increase the available surface area and to im-prove their apparent solubilities under physiologically relevant conditions with surfactants as wetting agents. Albendazole (ABZ), one of the most effective broad-spectrum antihelminthic agents, has a very low aqueous solubility, which leads to an erratic availability. Solid dispersions (SD) with different amounts of carriers (P188 and PEG6000) were formulated to improve the ABZ dissolution rate. When the dissolution test is used to infer biopharmaceutical properties of the dosage form, it is es-sential that the method simulates the gastrointestinal conditions. The objective of this study was to examine the applicabil-ity of different dissolution media to the evaluation of ABZ and ABZ-SD dissolution rates. Dissolution profiles were performed by the official method (0.1 N HCl) and Simulated Gastric Fluid modified with a surfactant. Wetting was evaluated through the determination of surface tension and contact angle of the solutions. The dissolution rate of ABZ was clearly affected by the variables assessed in this study. These results have implications in the design of physiologically based dissolution media.Fil: González Vidal, Noelia Luján. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia. Cátedra de Control de Calidad de Medicamentos; ArgentinaFil: Castro, Silvina Gabriela. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Sanchez Bruni, Sergio Fabian. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; ArgentinaFil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaDissolution Technologies, Inc2014-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/33421González Vidal, Noelia Luján; Castro, Silvina Gabriela; Sanchez Bruni, Sergio Fabian; Allemandi, Daniel Alberto; Palma, Santiago Daniel; Albendazole Solid Dispersions: Influence of Dissolution Medium Composition on In Vitro Drug Release; Dissolution Technologies, Inc; Dissolution Technologies; 21; 1-2014; 42-471521-298XCONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.14227/DT210214P42info:eu-repo/semantics/altIdentifier/url/http://www.dissolutiontech.com/DTresour/201405Articles/DT201405_A05.pdfinfo:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:19:38Zoai:ri.conicet.gov.ar:11336/33421instacron: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 10:19:38.781CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Albendazole Solid Dispersions: Influence of Dissolution Medium Composition on In Vitro Drug Release
title Albendazole Solid Dispersions: Influence of Dissolution Medium Composition on In Vitro Drug Release
spellingShingle Albendazole Solid Dispersions: Influence of Dissolution Medium Composition on In Vitro Drug Release
González Vidal, Noelia Luján
Contact Angle
Surface Tension
Dissolution Rate
Solid Dispersions
Albendazole
title_short Albendazole Solid Dispersions: Influence of Dissolution Medium Composition on In Vitro Drug Release
title_full Albendazole Solid Dispersions: Influence of Dissolution Medium Composition on In Vitro Drug Release
title_fullStr Albendazole Solid Dispersions: Influence of Dissolution Medium Composition on In Vitro Drug Release
title_full_unstemmed Albendazole Solid Dispersions: Influence of Dissolution Medium Composition on In Vitro Drug Release
title_sort Albendazole Solid Dispersions: Influence of Dissolution Medium Composition on In Vitro Drug Release
dc.creator.none.fl_str_mv González Vidal, Noelia Luján
Castro, Silvina Gabriela
Sanchez Bruni, Sergio Fabian
Allemandi, Daniel Alberto
Palma, Santiago Daniel
author González Vidal, Noelia Luján
author_facet González Vidal, Noelia Luján
Castro, Silvina Gabriela
Sanchez Bruni, Sergio Fabian
Allemandi, Daniel Alberto
Palma, Santiago Daniel
author_role author
author2 Castro, Silvina Gabriela
Sanchez Bruni, Sergio Fabian
Allemandi, Daniel Alberto
Palma, Santiago Daniel
author2_role author
author
author
author
dc.subject.none.fl_str_mv Contact Angle
Surface Tension
Dissolution Rate
Solid Dispersions
Albendazole
topic Contact Angle
Surface Tension
Dissolution Rate
Solid Dispersions
Albendazole
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv The rate-limiting step to drug absorption is often dissolution from the dosage form, especially for poorly soluble com-pounds. Two possibilities for improving the dissolution of these drugs are to increase the available surface area and to im-prove their apparent solubilities under physiologically relevant conditions with surfactants as wetting agents. Albendazole (ABZ), one of the most effective broad-spectrum antihelminthic agents, has a very low aqueous solubility, which leads to an erratic availability. Solid dispersions (SD) with different amounts of carriers (P188 and PEG6000) were formulated to improve the ABZ dissolution rate. When the dissolution test is used to infer biopharmaceutical properties of the dosage form, it is es-sential that the method simulates the gastrointestinal conditions. The objective of this study was to examine the applicabil-ity of different dissolution media to the evaluation of ABZ and ABZ-SD dissolution rates. Dissolution profiles were performed by the official method (0.1 N HCl) and Simulated Gastric Fluid modified with a surfactant. Wetting was evaluated through the determination of surface tension and contact angle of the solutions. The dissolution rate of ABZ was clearly affected by the variables assessed in this study. These results have implications in the design of physiologically based dissolution media.
Fil: González Vidal, Noelia Luján. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia. Cátedra de Control de Calidad de Medicamentos; Argentina
Fil: Castro, Silvina Gabriela. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Sanchez Bruni, Sergio Fabian. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
Fil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
description The rate-limiting step to drug absorption is often dissolution from the dosage form, especially for poorly soluble com-pounds. Two possibilities for improving the dissolution of these drugs are to increase the available surface area and to im-prove their apparent solubilities under physiologically relevant conditions with surfactants as wetting agents. Albendazole (ABZ), one of the most effective broad-spectrum antihelminthic agents, has a very low aqueous solubility, which leads to an erratic availability. Solid dispersions (SD) with different amounts of carriers (P188 and PEG6000) were formulated to improve the ABZ dissolution rate. When the dissolution test is used to infer biopharmaceutical properties of the dosage form, it is es-sential that the method simulates the gastrointestinal conditions. The objective of this study was to examine the applicabil-ity of different dissolution media to the evaluation of ABZ and ABZ-SD dissolution rates. Dissolution profiles were performed by the official method (0.1 N HCl) and Simulated Gastric Fluid modified with a surfactant. Wetting was evaluated through the determination of surface tension and contact angle of the solutions. The dissolution rate of ABZ was clearly affected by the variables assessed in this study. These results have implications in the design of physiologically based dissolution media.
publishDate 2014
dc.date.none.fl_str_mv 2014-01
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/11336/33421
González Vidal, Noelia Luján; Castro, Silvina Gabriela; Sanchez Bruni, Sergio Fabian; Allemandi, Daniel Alberto; Palma, Santiago Daniel; Albendazole Solid Dispersions: Influence of Dissolution Medium Composition on In Vitro Drug Release; Dissolution Technologies, Inc; Dissolution Technologies; 21; 1-2014; 42-47
1521-298X
CONICET Digital
CONICET
url http://hdl.handle.net/11336/33421
identifier_str_mv González Vidal, Noelia Luján; Castro, Silvina Gabriela; Sanchez Bruni, Sergio Fabian; Allemandi, Daniel Alberto; Palma, Santiago Daniel; Albendazole Solid Dispersions: Influence of Dissolution Medium Composition on In Vitro Drug Release; Dissolution Technologies, Inc; Dissolution Technologies; 21; 1-2014; 42-47
1521-298X
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.14227/DT210214P42
info:eu-repo/semantics/altIdentifier/url/http://www.dissolutiontech.com/DTresour/201405Articles/DT201405_A05.pdf
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
dc.publisher.none.fl_str_mv Dissolution Technologies, Inc
publisher.none.fl_str_mv Dissolution Technologies, Inc
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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