In Vitro–In Vivo Correlation for Gliclazide Immediate-Release Tablets Based on Mechanistic Absorption Simulation
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.
Key wordsbiorelevant dissolution specification gliclazide in vitro–in vivo correlation (IVIVC) mechanistic absorption simulation
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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