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In Vitro–In Vivo Correlation for Gliclazide Immediate-Release Tablets Based on Mechanistic Absorption Simulation

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Abstract

The aim of this study was to develop a drug-specific absorption model for gliclazide (GLK) using mechanistic gastrointestinal simulation technology (GIST) implemented in GastroPlusTM software package. A range of experimentally determined, in silico predicted or literature data were used as input parameters. Experimentally determined pH-solubility profile was used for all simulations. The human jejunum effective permeability (P eff) value was estimated on the basis of in vitro measured Caco-2 permeability (literature data). The required PK inputs were taken from the literature. The results of the simulations were compared with actual clinical data and revealed that the GIST-model gave accurate prediction of gliclazide oral absorption. The generated absorption model provided the target in vivo dissolution profile for in vitro–in vivo correlation and identification of biorelevant dissolution specification for GLK immediate-release (IR) tablets. A set of virtual in vitro data was used for correlation purposes. The obtained results suggest that dissolution specification of more than 85% GLK dissolved in 60 min may be considered as “biorelevant” dissolution acceptance criteria for GLK IR tablets.

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Acknowledgments

This work was done under the project Biopharmaceutical Characterization of the Selected BCS Class II and III Drugs: In Vitro and In Silico Methods Evaluation (TR-23015) supported by the Ministry of Science and Technological Development, Republic of Serbia.

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  1. Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221, Belgrade, Serbia

    Sandra Grbic, Jelena Parojcic, Svetlana Ibric & Zorica Djuric

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  1. Sandra Grbic
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  2. Jelena Parojcic
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Correspondence to Sandra Grbic.

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Grbic, S., Parojcic, J., Ibric, S. et al. In Vitro–In Vivo Correlation for Gliclazide Immediate-Release Tablets Based on Mechanistic Absorption Simulation. AAPS PharmSciTech 12, 165–171 (2011). https://doi.org/10.1208/s12249-010-9573-y

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