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...
| Authors: | ; ; ; ; ; ; ; |
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| Format: | Article |
| Publication date: | 2020 |
| Country: | España |
| Institution: | Universidad Miguel Hernández de Elche |
| Repository: | REDIUMH. Depósito Digital de la UMH |
| OAI Identifier: | oai:dspace.umh.es:11000/34728 |
| Online Access: | https://hdl.handle.net/11000/34728 |
| Access Level: | Open access |
| Keyword: | candesartan cilexetil IVIVC bioequivalence BCS predictive in vivo-dissolution CDU::6 - Ciencias aplicadas::62 - Ingeniería. Tecnología |
| _version_ | 1878733202885967872 |
|---|---|
| author | Figueroa-Campos, Andrés Ignacio |
| 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 |
| author_browse | Bermejo, Marival Dahan, Arik Figueroa-Campos, Andrés Ignacio García Arieta, Alfredo Gonzalez-Alvarez, Isabel Gonzalez-Alvarez, Marta Merino, Virginia Sánchez-Dengra, Bárbara |
| 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 |
| collection | REDIUMH. Depósito Digital de la UMH |
| 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. |
| eu_rights_str_mv | openAccess |
| format | article |
| id | ES_51db0b79162f082c32a6084c74eec708 |
| institution | Universidad Miguel Hernández de Elche |
| instname_str | Universidad Miguel Hernández de Elche |
| network_acronym_str | ES |
| network_name_str | España |
| oai_identifier_str | oai:dspace.umh.es:11000/34728 |
| publishDate | 2020 |
| publishDateSort | 2020 |
| publisher | MDPI |
| publisherStr | MDPI |
| reponame_str | REDIUMH. Depósito Digital de la UMH |
| spelling | Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool Figueroa-Campos, Andrés Ignacio Sánchez-Dengra, Bárbara Merino, Virginia Dahan, Arik Gonzalez-Alvarez, Isabel García Arieta, Alfredo Gonzalez-Alvarez, Marta Bermejo, Marival candesartan cilexetil IVIVC bioequivalence BCS predictive in vivo-dissolution CDU::6 - Ciencias aplicadas::62 - Ingeniería. Tecnología 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. MDPI https://hdl.handle.net/11000/34728 |
| 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 | 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_short | 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 |
| topic | candesartan cilexetil IVIVC bioequivalence BCS predictive in vivo-dissolution CDU::6 - Ciencias aplicadas::62 - Ingeniería. Tecnología |
| topic_facet | candesartan cilexetil IVIVC bioequivalence BCS predictive in vivo-dissolution CDU::6 - Ciencias aplicadas::62 - Ingeniería. Tecnología |
| url | https://hdl.handle.net/11000/34728 |