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Volume 12
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10.3390/pharmaceutics12070633
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Article

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

by
Andrés Figueroa-Campos
1,2,3,
Bárbara Sánchez-Dengra
1,
Virginia Merino
2,3,
Arik Dahan
4,
Isabel González-Álvarez
1,*,
Alfredo García-Arieta
5,†,
Marta González-Álvarez
1 and
Marival Bermejo
1
1
Engineering: Pharmacokinetics and Pharmaceutical Technology Area, Miguel Hernandez University, 03550 Juan de Alicante, Spain
2
Instituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Universitat Politècnica de València, 46100 Valencia, Spain
3
Departamento de Farmacia y Tecnología Farmacéutica y Parasitología, Universitat de València, Vicente Andrés Estelles s/n, Burjassot, 46100 Valencia, Spain
4
Department of Clinical Pharmacology, School of Pharmacy, Faculty of Health Sciences, Ben-Gurion University of the Negev, Beer-Sheva 8410501, Israel
5
Service of Pharmacokinetics and Generic Medicines, Division of Pharmacology and Clinical Evaluation, Department of Human Use Medicines, Spanish Agency for Medicines and Health Care Products, 28022 Madrid, Spain
*
Author to whom correspondence should be addressed.
†
This manuscript represents the personal opinion of the authors and does not necessarily represent the views or policy of their corresponding Regulatory Authorities.
Pharmaceutics 2020, 12(7), 633; https://doi.org/10.3390/pharmaceutics12070633
Submission received: 30 April 2020 / Revised: 30 June 2020 / Accepted: 1 July 2020 / Published: 6 July 2020
(This article belongs to the Special Issue In Vivo Predictive Dissolution (iPD): Experimental and Mathematical Approaches and Regulatory Applications)
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Abstract

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.
Keywords: candesartan cilexetil; IVIVC; bioequivalence; BCS; predictive in vivo-dissolution candesartan cilexetil; IVIVC; bioequivalence; BCS; predictive in vivo-dissolution
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MDPI and ACS Style

Figueroa-Campos, A.; Sánchez-Dengra, B.; Merino, V.; Dahan, A.; González-Álvarez, I.; García-Arieta, A.; González-Álvarez, M.; Bermejo, M. Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool. Pharmaceutics 2020, 12, 633. https://doi.org/10.3390/pharmaceutics12070633

AMA Style

Figueroa-Campos A, Sánchez-Dengra B, Merino V, Dahan A, González-Álvarez I, García-Arieta A, González-Álvarez M, Bermejo M. Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool. Pharmaceutics. 2020; 12(7):633. https://doi.org/10.3390/pharmaceutics12070633

Chicago/Turabian Style

Figueroa-Campos, Andrés, Bárbara Sánchez-Dengra, Virginia Merino, Arik Dahan, Isabel González-Álvarez, Alfredo García-Arieta, Marta González-Álvarez, and Marival Bermejo. 2020. "Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool" Pharmaceutics 12, no. 7: 633. https://doi.org/10.3390/pharmaceutics12070633

APA Style

Figueroa-Campos, A., Sánchez-Dengra, B., Merino, V., Dahan, A., González-Álvarez, I., García-Arieta, A., González-Álvarez, M., & Bermejo, M. (2020). Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool. Pharmaceutics, 12(7), 633. https://doi.org/10.3390/pharmaceutics12070633

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