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In Vitro–In Vivo Correlation of Efavirenz Tablets Using GastroPlus®

Authors :
Tereza Cristina dos Santos
Valeria Pereira de Sousa
Helena Carla Castro
Thiago da Silva Honorio
Valeria Sant’Anna Dantas Esteves
Helvécio Vinícius Antunes Rocha
Eduardo Costa Pinto
Carlos Rangel Rodrigues
Lucio Mendes Cabral
Source :
AAPS PharmSciTech. 14:1244-1254
Publication Year :
2013
Publisher :
Springer Science and Business Media LLC, 2013.

Abstract

The aim of the present work was to use GastroPlus™ software for the prediction of pharmacokinetic profiles and in vitro-in vivo correlation (IVIVC) as tools to optimize the development of new generic medications. GastroPlus™ was used to simulate the gastrointestinal compartment and was based on the advanced compartmental absorption and transit model. Powder dissolution and efavirenz tablet dissolution studies were carried out to generate data from which correlation was established. The simulated plasma profile, based on the physicochemical properties of efavirenz, was almost identical to that observed in vivo for biobatches A and B. A level A IVIVC was established for the dissolution method obtained for the generic candidate using the Wagner-Nelson (r (2) = 0.85) and for Loo-Riegelman models (r(2) = 0.92). The percentage of fraction absorbed indicated that 0.5% sodium lauryl sulfate may be considered a biorelevant dissolution medium for efavirenz tablets. The simulation of gastrointestinal bioavailability and IVIVC obtained from immediate-release tablet formulations suggests that GastroPlus™ is a valuable in silico method for IVIVC and for studies directed at developing formulations of class II drugs.

Details

ISSN :
15309932
Volume :
14
Database :
OpenAIRE
Journal :
AAPS PharmSciTech
Accession number :
edsair.doi.dedup.....1df503d165e2bc4d6fffb3ae9f010c7a
Full Text :
https://doi.org/10.1208/s12249-013-0016-4