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Article

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

1
Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, 28040 Madrid, Spain
2
Departamento Ingeniería of Área Farmacia, Universidad Miguel Hernández de Elche, 03550 Alicante, Spain
3
Laboratorios Normon SA, Tres Cantos, 28760 Madrid, Spain
4
Clinical Pharmacology Service, Hospital Universitario la Paz, School of Medicine, Universidad Autónoma de Madrid, 28049 Madrid, Spain
5
Agencia Española de Medicamentos y Productos Sanitarios, 28022 Madrid, Spain
*
Author to whom correspondence should be addressed.
This manuscript represents the personal opinion of the author and does not necessarily represent the views or policy of the Spanish Agency for Medicines and Health Care Products.
Academic Editor: Leena Peltonen
Received: 27 April 2021 / Revised: 3 May 2021 / Accepted: 6 May 2021 / Published: 11 May 2021
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. View Full-Text
Keywords: montelukast; in vitro-in vivo correlation; flow-through cell montelukast; in vitro-in vivo correlation; flow-through cell
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MDPI and ACS Style

Prieto-Escolar, M.; Torrado, J.J.; Álvarez, C.; Ruiz-Picazo, A.; Simón-Vázquez, M.; Govantes, C.; Frias, J.; García-Arieta, A.; Gonzalez-Alvarez, I.; Bermejo, M. One and Two-Step In Vitro-In Vivo Correlations Based on USP IV Dynamic Dissolution Applied to Four Sodium Montelukast Products. Pharmaceutics 2021, 13, 690. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13050690

AMA Style

Prieto-Escolar M, Torrado JJ, Álvarez C, Ruiz-Picazo A, Simón-Vázquez M, Govantes C, Frias J, García-Arieta A, Gonzalez-Alvarez I, Bermejo M. One and Two-Step In Vitro-In Vivo Correlations Based on USP IV Dynamic Dissolution Applied to Four Sodium Montelukast Products. Pharmaceutics. 2021; 13(5):690. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13050690

Chicago/Turabian Style

Prieto-Escolar, Mercedes, Juan J. Torrado, Covadonga Álvarez, Alejandro Ruiz-Picazo, Marta Simón-Vázquez, Carlos Govantes, Jesús Frias, Alfredo García-Arieta, Isabel Gonzalez-Alvarez, and Marival Bermejo. 2021. "One and Two-Step In Vitro-In Vivo Correlations Based on USP IV Dynamic Dissolution Applied to Four Sodium Montelukast Products" Pharmaceutics 13, no. 5: 690. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13050690

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