The aim of this study was to develop a drug-specific absorption model for gliclazide (GLK) using mechanistic gastrointestinal simulation technology (GIST) implemented in GastroPlus(TM) 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.
Keywords:
biorelevant dissolution specification / gliclazide / in vitro-in vivo correlation (IVIVC) / mechanistic absorption simulation
TY - JOUR
AU - Cvijić, Sandra
AU - Parojčić, Jelena
AU - Ibrić, Svetlana
AU - Đurić, Zorica
PY - 2011
UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1540
AB - The aim of this study was to develop a drug-specific absorption model for gliclazide (GLK) using mechanistic gastrointestinal simulation technology (GIST) implemented in GastroPlus(TM) 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.
PB - Springer, New York
T2 - AAPS PharmSciTech
T1 - In Vitro-In Vivo Correlation for Gliclazide Immediate-Release Tablets Based on Mechanistic Absorption Simulation
VL - 12
IS - 1
SP - 165
EP - 171
DO - 10.1208/s12249-010-9573-y
ER -
@article{
author = "Cvijić, Sandra and Parojčić, Jelena and Ibrić, Svetlana and Đurić, Zorica",
year = "2011",
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 GastroPlus(TM) 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.",
publisher = "Springer, New York",
journal = "AAPS PharmSciTech",
title = "In Vitro-In Vivo Correlation for Gliclazide Immediate-Release Tablets Based on Mechanistic Absorption Simulation",
volume = "12",
number = "1",
pages = "165-171",
doi = "10.1208/s12249-010-9573-y"
}
Cvijić, S., Parojčić, J., Ibrić, S.,& Đurić, Z.. (2011). In Vitro-In Vivo Correlation for Gliclazide Immediate-Release Tablets Based on Mechanistic Absorption Simulation. in AAPS PharmSciTech
Springer, New York., 12(1), 165-171.
https://doi.org/10.1208/s12249-010-9573-y
Cvijić S, Parojčić J, Ibrić S, Đurić Z. In Vitro-In Vivo Correlation for Gliclazide Immediate-Release Tablets Based on Mechanistic Absorption Simulation. in AAPS PharmSciTech. 2011;12(1):165-171.
doi:10.1208/s12249-010-9573-y .
Cvijić, Sandra, Parojčić, Jelena, Ibrić, Svetlana, Đurić, Zorica, "In Vitro-In Vivo Correlation for Gliclazide Immediate-Release Tablets Based on Mechanistic Absorption Simulation" in AAPS PharmSciTech, 12, no. 1 (2011):165-171,
https://doi.org/10.1208/s12249-010-9573-y . .
