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One and Two-Step In Vitro-In Vivo Correlations Based on USP IV Dynamic Dissolution Applied to Four Sodium Montelukast Products

Montelukast is a weak acid drug characterized by its low solubility in the range of pH 1.2 to 4.5, which may lead to dissolution-limited absorption. The aim of this paper is to develop an in vivo predictive dissolution method for montelukast and to check its performance by establishing a level-A in...

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Autores principales: Prieto-Escolar, Mercedes, Torrado, Juan J., Álvarez, Covadonga, Ruiz-Picazo, Alejandro, Simón-Vázquez, Marta, Govantes, Carlos, Frias, Jesús, García-Arieta, Alfredo, Gonzalez-Alvarez, Isabel, Bermejo, Marival
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8151440/
https://www.ncbi.nlm.nih.gov/pubmed/34064700
http://dx.doi.org/10.3390/pharmaceutics13050690
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author Prieto-Escolar, Mercedes
Torrado, Juan J.
Álvarez, Covadonga
Ruiz-Picazo, Alejandro
Simón-Vázquez, Marta
Govantes, Carlos
Frias, Jesús
García-Arieta, Alfredo
Gonzalez-Alvarez, Isabel
Bermejo, Marival
author_facet Prieto-Escolar, Mercedes
Torrado, Juan J.
Álvarez, Covadonga
Ruiz-Picazo, Alejandro
Simón-Vázquez, Marta
Govantes, Carlos
Frias, Jesús
García-Arieta, Alfredo
Gonzalez-Alvarez, Isabel
Bermejo, Marival
author_sort Prieto-Escolar, Mercedes
collection PubMed
description Montelukast is a weak acid drug characterized by its low solubility in the range of pH 1.2 to 4.5, which may lead to dissolution-limited absorption. The aim of this paper is to develop an in vivo predictive dissolution method for montelukast and to check its performance by establishing a level-A in vitro-in vivo correlation (IVIVC). During the development of a generic film-coated tablet formulation, two clinical trials were done with three different experimental formulations to achieve a similar formulation to the reference one. A dissolution test procedure with a flow-through cell (USP IV) was used to predict the in vivo absorption behavior. The method proposed is based on a flow rate of 5 mL/min and changes of pH mediums from 1.2 to 4.5 and then to 6.8 with standard pharmacopoeia buffers. In order to improve the dissolution of montelukast, sodium dodecyl sulfate was added to the 4.5 and 6.8 pH mediums. Dissolution profiles in from the new method were used to develop a level-A IVIVC. One-step level-A IVIVC was developed from dissolution profiles and fractions absorbed obtained by the Loo–Riegelman method. Time scaling with Levy’s plot was necessary to achieve a linear IVIVC. One-step differential equation-based IVIVC was also developed with a time-scaling function. The developed method showed similar results to a previously proposed biopredictive method for montelukast, and the added value showed the ability to discriminate among different release rates in vitro, matching the in vivo clinical bioequivalence results.
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spelling pubmed-81514402021-05-27 One and Two-Step In Vitro-In Vivo Correlations Based on USP IV Dynamic Dissolution Applied to Four Sodium Montelukast Products Prieto-Escolar, Mercedes Torrado, Juan J. Álvarez, Covadonga Ruiz-Picazo, Alejandro Simón-Vázquez, Marta Govantes, Carlos Frias, Jesús García-Arieta, Alfredo Gonzalez-Alvarez, Isabel Bermejo, Marival Pharmaceutics Article Montelukast is a weak acid drug characterized by its low solubility in the range of pH 1.2 to 4.5, which may lead to dissolution-limited absorption. The aim of this paper is to develop an in vivo predictive dissolution method for montelukast and to check its performance by establishing a level-A in vitro-in vivo correlation (IVIVC). During the development of a generic film-coated tablet formulation, two clinical trials were done with three different experimental formulations to achieve a similar formulation to the reference one. A dissolution test procedure with a flow-through cell (USP IV) was used to predict the in vivo absorption behavior. The method proposed is based on a flow rate of 5 mL/min and changes of pH mediums from 1.2 to 4.5 and then to 6.8 with standard pharmacopoeia buffers. In order to improve the dissolution of montelukast, sodium dodecyl sulfate was added to the 4.5 and 6.8 pH mediums. Dissolution profiles in from the new method were used to develop a level-A IVIVC. One-step level-A IVIVC was developed from dissolution profiles and fractions absorbed obtained by the Loo–Riegelman method. Time scaling with Levy’s plot was necessary to achieve a linear IVIVC. One-step differential equation-based IVIVC was also developed with a time-scaling function. The developed method showed similar results to a previously proposed biopredictive method for montelukast, and the added value showed the ability to discriminate among different release rates in vitro, matching the in vivo clinical bioequivalence results. MDPI 2021-05-11 /pmc/articles/PMC8151440/ /pubmed/34064700 http://dx.doi.org/10.3390/pharmaceutics13050690 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Prieto-Escolar, Mercedes
Torrado, Juan J.
Álvarez, Covadonga
Ruiz-Picazo, Alejandro
Simón-Vázquez, Marta
Govantes, Carlos
Frias, Jesús
García-Arieta, Alfredo
Gonzalez-Alvarez, Isabel
Bermejo, Marival
One and Two-Step In Vitro-In Vivo Correlations Based on USP IV Dynamic Dissolution Applied to Four Sodium Montelukast Products
title One and Two-Step In Vitro-In Vivo Correlations Based on USP IV Dynamic Dissolution Applied to Four Sodium Montelukast Products
title_full One and Two-Step In Vitro-In Vivo Correlations Based on USP IV Dynamic Dissolution Applied to Four Sodium Montelukast Products
title_fullStr One and Two-Step In Vitro-In Vivo Correlations Based on USP IV Dynamic Dissolution Applied to Four Sodium Montelukast Products
title_full_unstemmed One and Two-Step In Vitro-In Vivo Correlations Based on USP IV Dynamic Dissolution Applied to Four Sodium Montelukast Products
title_short One and Two-Step In Vitro-In Vivo Correlations Based on USP IV Dynamic Dissolution Applied to Four Sodium Montelukast Products
title_sort one and two-step in vitro-in vivo correlations based on usp iv dynamic dissolution applied to four sodium montelukast products
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8151440/
https://www.ncbi.nlm.nih.gov/pubmed/34064700
http://dx.doi.org/10.3390/pharmaceutics13050690
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