In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets

Autores
Prado, Héctor Juan; Bonelli, Pablo Ricardo; Cukierman, Ana Lea
Año de publicación
2014
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
In situ fluidized hot melt granulation (FHMG) for different (ternary) formulations based on glyceryl palmito-stearate as non-conventional meltable binder and ibuprofen as model drug was examined for controlled release applications. The process was robust, lasted only 15 min, and enabled to attain high yields (95–98 wt.%). The obtained granules presented a bimodal size distribution, having the major mode of 200 μm and good flow properties, thus avoiding the necessity to add other lubricants for tablet compaction. The crystalline structure of ibuprofen and of the non meltable excipients was retained, and that of glyceryl palmito-stearate was recovered in the final granules. The resulting ibuprofen tablets had good pharmacotechnical properties. The granulation process did not modify release profiles from the tablets. The main factor influencing the release profiles was the content of glyceryl palmito-stearate in the formulations. A high drug load (50 wt.%), which is particularly important in the case of high dose active pharmaceutical ingredients, was achieved. Glyceryl palmito-stearate performed a triple function in the tablet formulation: as a meltable binder, as a controlled release matrix and as a lubricant.
Fil: Prado, Héctor Juan. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Bonelli, Pablo Ricardo. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Cukierman, Ana Lea. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Materia
Fluidized Hot Melt Granulation
Gelucires
Glyceryl Palmito-Stearate
Controlled Release
Tablets
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/31997
Acceder
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network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tabletsPrado, Héctor JuanBonelli, Pablo RicardoCukierman, Ana LeaFluidized Hot Melt GranulationGeluciresGlyceryl Palmito-StearateControlled ReleaseTabletshttps://purl.org/becyt/ford/2.4https://purl.org/becyt/ford/2In situ fluidized hot melt granulation (FHMG) for different (ternary) formulations based on glyceryl palmito-stearate as non-conventional meltable binder and ibuprofen as model drug was examined for controlled release applications. The process was robust, lasted only 15 min, and enabled to attain high yields (95–98 wt.%). The obtained granules presented a bimodal size distribution, having the major mode of 200 μm and good flow properties, thus avoiding the necessity to add other lubricants for tablet compaction. The crystalline structure of ibuprofen and of the non meltable excipients was retained, and that of glyceryl palmito-stearate was recovered in the final granules. The resulting ibuprofen tablets had good pharmacotechnical properties. The granulation process did not modify release profiles from the tablets. The main factor influencing the release profiles was the content of glyceryl palmito-stearate in the formulations. A high drug load (50 wt.%), which is particularly important in the case of high dose active pharmaceutical ingredients, was achieved. Glyceryl palmito-stearate performed a triple function in the tablet formulation: as a meltable binder, as a controlled release matrix and as a lubricant.Fil: Prado, Héctor Juan. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Bonelli, Pablo Ricardo. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Cukierman, Ana Lea. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaElsevier Science2014-06info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/31997Cukierman, Ana Lea; Bonelli, Pablo Ricardo; Prado, Héctor Juan; In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets; Elsevier Science; Powder Technology; 264; 6-2014; 498-5060032-5910CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.1016/j.powtec.2014.05.058info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0032591014005257info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-nd/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-03T09:44:19Zoai:ri.conicet.gov.ar:11336/31997instacron: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:34982025-09-03 09:44:19.569CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets
title In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets
spellingShingle In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets
Prado, Héctor Juan
Fluidized Hot Melt Granulation
Gelucires
Glyceryl Palmito-Stearate
Controlled Release
Tablets
title_short In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets
title_full In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets
title_fullStr In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets
title_full_unstemmed In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets
title_sort In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets
dc.creator.none.fl_str_mv Prado, Héctor Juan
Bonelli, Pablo Ricardo
Cukierman, Ana Lea
author Prado, Héctor Juan
author_facet Prado, Héctor Juan
Bonelli, Pablo Ricardo
Cukierman, Ana Lea
author_role author
author2 Bonelli, Pablo Ricardo
Cukierman, Ana Lea
author2_role author
author
dc.subject.none.fl_str_mv Fluidized Hot Melt Granulation
Gelucires
Glyceryl Palmito-Stearate
Controlled Release
Tablets
topic Fluidized Hot Melt Granulation
Gelucires
Glyceryl Palmito-Stearate
Controlled Release
Tablets
purl_subject.fl_str_mv https://purl.org/becyt/ford/2.4
https://purl.org/becyt/ford/2
dc.description.none.fl_txt_mv In situ fluidized hot melt granulation (FHMG) for different (ternary) formulations based on glyceryl palmito-stearate as non-conventional meltable binder and ibuprofen as model drug was examined for controlled release applications. The process was robust, lasted only 15 min, and enabled to attain high yields (95–98 wt.%). The obtained granules presented a bimodal size distribution, having the major mode of 200 μm and good flow properties, thus avoiding the necessity to add other lubricants for tablet compaction. The crystalline structure of ibuprofen and of the non meltable excipients was retained, and that of glyceryl palmito-stearate was recovered in the final granules. The resulting ibuprofen tablets had good pharmacotechnical properties. The granulation process did not modify release profiles from the tablets. The main factor influencing the release profiles was the content of glyceryl palmito-stearate in the formulations. A high drug load (50 wt.%), which is particularly important in the case of high dose active pharmaceutical ingredients, was achieved. Glyceryl palmito-stearate performed a triple function in the tablet formulation: as a meltable binder, as a controlled release matrix and as a lubricant.
Fil: Prado, Héctor Juan. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Bonelli, Pablo Ricardo. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Cukierman, Ana Lea. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Industrias; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
description In situ fluidized hot melt granulation (FHMG) for different (ternary) formulations based on glyceryl palmito-stearate as non-conventional meltable binder and ibuprofen as model drug was examined for controlled release applications. The process was robust, lasted only 15 min, and enabled to attain high yields (95–98 wt.%). The obtained granules presented a bimodal size distribution, having the major mode of 200 μm and good flow properties, thus avoiding the necessity to add other lubricants for tablet compaction. The crystalline structure of ibuprofen and of the non meltable excipients was retained, and that of glyceryl palmito-stearate was recovered in the final granules. The resulting ibuprofen tablets had good pharmacotechnical properties. The granulation process did not modify release profiles from the tablets. The main factor influencing the release profiles was the content of glyceryl palmito-stearate in the formulations. A high drug load (50 wt.%), which is particularly important in the case of high dose active pharmaceutical ingredients, was achieved. Glyceryl palmito-stearate performed a triple function in the tablet formulation: as a meltable binder, as a controlled release matrix and as a lubricant.
publishDate 2014
dc.date.none.fl_str_mv 2014-06
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/11336/31997
Cukierman, Ana Lea; Bonelli, Pablo Ricardo; Prado, Héctor Juan; In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets; Elsevier Science; Powder Technology; 264; 6-2014; 498-506
0032-5910
CONICET Digital
CONICET
url http://hdl.handle.net/11336/31997
identifier_str_mv Cukierman, Ana Lea; Bonelli, Pablo Ricardo; Prado, Héctor Juan; In situ fluidized hot melt granulation using a novel meltable binder: Effect of formulation variables on granule characteristics and controlled release tablets; Elsevier Science; Powder Technology; 264; 6-2014; 498-506
0032-5910
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1016/j.powtec.2014.05.058
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0032591014005257
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
application/pdf
application/pdf
application/pdf
application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier Science
publisher.none.fl_str_mv Elsevier Science
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 13.13397

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