Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool

The main objective of this investigation was to develop an in vitro–in vivo correlation (IVIVC) for immediate release candesartan cilexetil formulations by designing an in vitro dissolution test to be used as development tool. The IVIVC could be used to reduce failures in future bioequivalence studi...

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Autores: Figueroa-Campos, Andrés Ignacio, Sánchez-Dengra, Bárbara, Merino, Virginia, Dahan, Arik, Gonzalez-Alvarez, Isabel, García Arieta, Alfredo, Gonzalez-Alvarez, Marta, Bermejo, Marival
Tipo de recurso: artículo
Fecha de publicación:2020
País:España
Institución:Universidad Miguel Hernández de Elche
Repositorio:REDIUMH. Depósito Digital de la UMH
OAI Identifier:oai:dspace.umh.es:11000/34728
Acceso en línea:https://hdl.handle.net/11000/34728
Access Level:acceso abierto
Palabra clave:candesartan cilexetil
IVIVC
bioequivalence
BCS
predictive in vivo-dissolution
CDU::6 - Ciencias aplicadas::62 - Ingeniería. Tecnología
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spelling Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development ToolFigueroa-Campos, Andrés IgnacioSánchez-Dengra, BárbaraMerino, VirginiaDahan, ArikGonzalez-Alvarez, IsabelGarcía Arieta, AlfredoGonzalez-Alvarez, MartaBermejo, Marivalcandesartan cilexetilIVIVCbioequivalenceBCSpredictive in vivo-dissolutionCDU::6 - Ciencias aplicadas::62 - Ingeniería. TecnologíaThe main objective of this investigation was to develop an in vitro–in vivo correlation (IVIVC) for immediate release candesartan cilexetil formulations by designing an in vitro dissolution test to be used as development tool. The IVIVC could be used to reduce failures in future bioequivalence studies. Data from two bioequivalence studies were scaled and combined to obtain the dataset for the IVIVC. Two-step and one-step approaches were used to develop the IVIVC. Experimental solubility and permeability data confirmed candesartan cilexetil. Biopharmaceutic Classification System (BCS) class II candesartan average plasma profiles were deconvoluted by the Loo-Riegelman method to obtain the oral fractions absorbed. Fractions dissolved were obtained in several conditions in USP II and IV apparatus and the results were compared calculating the f2 similarity factor. Levy plot was constructed to estimate the time scaling factor and to make both processes, dissolution and absorption, superimposable. The in vitro dissolution experiment that reflected more accurately the in vivo behavior of the products of candesartan cilexetil employed the USP IV apparatus and a three-step pH buffer change, from 1.2 to 4.5 and 6.8, with 0.2% of Tween 20. This new model was able to predict the in vivo differences in dissolution and it could be used as a risk-analysis tool for formulation selection in future bioequivalence trials.MDPIDepartamentos de la UMH::Ingeniería202520252020info:eu-repo/semantics/articleapplication/pdf21application/pdfhttps://hdl.handle.net/11000/34728reponame:REDIUMH. Depósito Digital de la UMHinstname:Universidad Miguel Hernández de ElcheIngléshttps://doi.org/10.3390/pharmaceutics12070633info:eu-repo/semantics/openAccessAttribution-NonCommercial-NoDerivatives 4.0 Internacionalhttp://creativecommons.org/licenses/by-nc-nd/4.0/oai:dspace.umh.es:11000/347282026-05-27T13:36:21Z
dc.title.none.fl_str_mv Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool
title Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool
spellingShingle Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool
Figueroa-Campos, Andrés Ignacio
candesartan cilexetil
IVIVC
bioequivalence
BCS
predictive in vivo-dissolution
CDU::6 - Ciencias aplicadas::62 - Ingeniería. Tecnología
title_short Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool
title_full Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool
title_fullStr Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool
title_full_unstemmed Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool
title_sort Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool
dc.creator.none.fl_str_mv Figueroa-Campos, Andrés Ignacio
Sánchez-Dengra, Bárbara
Merino, Virginia
Dahan, Arik
Gonzalez-Alvarez, Isabel
García Arieta, Alfredo
Gonzalez-Alvarez, Marta
Bermejo, Marival
author Figueroa-Campos, Andrés Ignacio
author_facet Figueroa-Campos, Andrés Ignacio
Sánchez-Dengra, Bárbara
Merino, Virginia
Dahan, Arik
Gonzalez-Alvarez, Isabel
García Arieta, Alfredo
Gonzalez-Alvarez, Marta
Bermejo, Marival
author_role author
author2 Sánchez-Dengra, Bárbara
Merino, Virginia
Dahan, Arik
Gonzalez-Alvarez, Isabel
García Arieta, Alfredo
Gonzalez-Alvarez, Marta
Bermejo, Marival
author2_role author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Departamentos de la UMH::Ingeniería
dc.subject.none.fl_str_mv candesartan cilexetil
IVIVC
bioequivalence
BCS
predictive in vivo-dissolution
CDU::6 - Ciencias aplicadas::62 - Ingeniería. Tecnología
topic candesartan cilexetil
IVIVC
bioequivalence
BCS
predictive in vivo-dissolution
CDU::6 - Ciencias aplicadas::62 - Ingeniería. Tecnología
description The main objective of this investigation was to develop an in vitro–in vivo correlation (IVIVC) for immediate release candesartan cilexetil formulations by designing an in vitro dissolution test to be used as development tool. The IVIVC could be used to reduce failures in future bioequivalence studies. Data from two bioequivalence studies were scaled and combined to obtain the dataset for the IVIVC. Two-step and one-step approaches were used to develop the IVIVC. Experimental solubility and permeability data confirmed candesartan cilexetil. Biopharmaceutic Classification System (BCS) class II candesartan average plasma profiles were deconvoluted by the Loo-Riegelman method to obtain the oral fractions absorbed. Fractions dissolved were obtained in several conditions in USP II and IV apparatus and the results were compared calculating the f2 similarity factor. Levy plot was constructed to estimate the time scaling factor and to make both processes, dissolution and absorption, superimposable. The in vitro dissolution experiment that reflected more accurately the in vivo behavior of the products of candesartan cilexetil employed the USP IV apparatus and a three-step pH buffer change, from 1.2 to 4.5 and 6.8, with 0.2% of Tween 20. This new model was able to predict the in vivo differences in dissolution and it could be used as a risk-analysis tool for formulation selection in future bioequivalence trials.
publishDate 2020
dc.date.none.fl_str_mv 2020
2025
2025
dc.type.none.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv https://hdl.handle.net/11000/34728
url https://hdl.handle.net/11000/34728
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv https://doi.org/10.3390/pharmaceutics12070633
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
Attribution-NonCommercial-NoDerivatives 4.0 Internacional
http://creativecommons.org/licenses/by-nc-nd/4.0/
eu_rights_str_mv openAccess
rights_invalid_str_mv Attribution-NonCommercial-NoDerivatives 4.0 Internacional
http://creativecommons.org/licenses/by-nc-nd/4.0/
dc.format.none.fl_str_mv application/pdf
21
application/pdf
dc.publisher.none.fl_str_mv MDPI
publisher.none.fl_str_mv MDPI
dc.source.none.fl_str_mv reponame:REDIUMH. Depósito Digital de la UMH
instname:Universidad Miguel Hernández de Elche
instname_str Universidad Miguel Hernández de Elche
reponame_str REDIUMH. Depósito Digital de la UMH
collection REDIUMH. Depósito Digital de la UMH
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15.811543

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