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Justification of Biowaiver for Carbamazepine, a Low Soluble High Permeable Compound, in Solid Dosage Forms Based on IVIVC and Gastrointestinal Simulation

Authorized Users Only
2009
Authors
Kovacević, Ivan
Parojčić, Jelena
Homšek, Irena
Tubić-Grozdanis, Marija
Langguth, Peter
Article (Published version)
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Abstract
The aim of the present study was to use gastrointestinal simulation technology and in vitro-in vivo correlation (IVIVC) as tools to investigate a possible extension of biowaiver criteria to BCS class II drugs using carbamazepine (CBZ) as a candidate compound. Gastrointestinal simulation based on the advanced compartmental absorption and transit model implemented in GastroPlus was used. Actual in vitro and in vivo data generated in CBZ bioequivalence studies were used for correlation purposes. The simulated plasma profile, based on the CBZ physicochemical and pharmacokinetic properties, was almost identical with that observed in vivo. Parameter sensitivity analysis (PSA) indicated that the percent of drug absorbed is relatively insensitive to the variation of the input parameters. Additionally, plasma concentration-time profiles were simulated based on dissolution profiles observed under the different experimental conditions. Regardless of the differences observed in vitro, the predicte...d pharmacokinetic profiles were similar in the extent of drug exposure (AUC) while there were certain differences in parameters defining the drug absorption rate (C-max, t(max)). High level A IVIVC was established for the pooled data set (r = 0.9624), indicating that 1% SLS may be considered as the universal biorelevant dissolution medium for both the IR and CR CBZ tablets. The proposed methodology involving gastrointestinal simulation technology and IVIVC suggests that there is a rationale for considering CBZ biowaiver extension and introduction of the wider dissolution specifications for CBZ immediate release tablets.

Keywords:
BCS / bioequivalence / carbamazepine / gastrointestinal simulation / IVIVC
Source:
Molecular Pharmaceutics, 2009, 6, 1, 40-47
Publisher:
  • Amer Chemical Soc, Washington
Funding / projects:
  • Ministry of Science and Technological Development, Republic of Serbia

DOI: 10.1021/mp800128y

ISSN: 1543-8384

PubMed: 19248231

WoS: 000263035000006

Scopus: 2-s2.0-62649134312
[ Google Scholar ]
89
75
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/1252
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Kovacević, Ivan
AU  - Parojčić, Jelena
AU  - Homšek, Irena
AU  - Tubić-Grozdanis, Marija
AU  - Langguth, Peter
PY  - 2009
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1252
AB  - The aim of the present study was to use gastrointestinal simulation technology and in vitro-in vivo correlation (IVIVC) as tools to investigate a possible extension of biowaiver criteria to BCS class II drugs using carbamazepine (CBZ) as a candidate compound. Gastrointestinal simulation based on the advanced compartmental absorption and transit model implemented in GastroPlus was used. Actual in vitro and in vivo data generated in CBZ bioequivalence studies were used for correlation purposes. The simulated plasma profile, based on the CBZ physicochemical and pharmacokinetic properties, was almost identical with that observed in vivo. Parameter sensitivity analysis (PSA) indicated that the percent of drug absorbed is relatively insensitive to the variation of the input parameters. Additionally, plasma concentration-time profiles were simulated based on dissolution profiles observed under the different experimental conditions. Regardless of the differences observed in vitro, the predicted pharmacokinetic profiles were similar in the extent of drug exposure (AUC) while there were certain differences in parameters defining the drug absorption rate (C-max, t(max)). High level A IVIVC was established for the pooled data set (r = 0.9624), indicating that 1% SLS may be considered as the universal biorelevant dissolution medium for both the IR and CR CBZ tablets. The proposed methodology involving gastrointestinal simulation technology and IVIVC suggests that there is a rationale for considering CBZ biowaiver extension and introduction of the wider dissolution specifications for CBZ immediate release tablets.
PB  - Amer Chemical Soc, Washington
T2  - Molecular Pharmaceutics
T1  - Justification of Biowaiver for Carbamazepine, a Low Soluble High Permeable Compound, in Solid Dosage Forms Based on IVIVC and Gastrointestinal Simulation
VL  - 6
IS  - 1
SP  - 40
EP  - 47
DO  - 10.1021/mp800128y
ER  - 
@article{
author = "Kovacević, Ivan and Parojčić, Jelena and Homšek, Irena and Tubić-Grozdanis, Marija and Langguth, Peter",
year = "2009",
abstract = "The aim of the present study was to use gastrointestinal simulation technology and in vitro-in vivo correlation (IVIVC) as tools to investigate a possible extension of biowaiver criteria to BCS class II drugs using carbamazepine (CBZ) as a candidate compound. Gastrointestinal simulation based on the advanced compartmental absorption and transit model implemented in GastroPlus was used. Actual in vitro and in vivo data generated in CBZ bioequivalence studies were used for correlation purposes. The simulated plasma profile, based on the CBZ physicochemical and pharmacokinetic properties, was almost identical with that observed in vivo. Parameter sensitivity analysis (PSA) indicated that the percent of drug absorbed is relatively insensitive to the variation of the input parameters. Additionally, plasma concentration-time profiles were simulated based on dissolution profiles observed under the different experimental conditions. Regardless of the differences observed in vitro, the predicted pharmacokinetic profiles were similar in the extent of drug exposure (AUC) while there were certain differences in parameters defining the drug absorption rate (C-max, t(max)). High level A IVIVC was established for the pooled data set (r = 0.9624), indicating that 1% SLS may be considered as the universal biorelevant dissolution medium for both the IR and CR CBZ tablets. The proposed methodology involving gastrointestinal simulation technology and IVIVC suggests that there is a rationale for considering CBZ biowaiver extension and introduction of the wider dissolution specifications for CBZ immediate release tablets.",
publisher = "Amer Chemical Soc, Washington",
journal = "Molecular Pharmaceutics",
title = "Justification of Biowaiver for Carbamazepine, a Low Soluble High Permeable Compound, in Solid Dosage Forms Based on IVIVC and Gastrointestinal Simulation",
volume = "6",
number = "1",
pages = "40-47",
doi = "10.1021/mp800128y"
}
Kovacević, I., Parojčić, J., Homšek, I., Tubić-Grozdanis, M.,& Langguth, P.. (2009). Justification of Biowaiver for Carbamazepine, a Low Soluble High Permeable Compound, in Solid Dosage Forms Based on IVIVC and Gastrointestinal Simulation. in Molecular Pharmaceutics
Amer Chemical Soc, Washington., 6(1), 40-47.
https://doi.org/10.1021/mp800128y
Kovacević I, Parojčić J, Homšek I, Tubić-Grozdanis M, Langguth P. Justification of Biowaiver for Carbamazepine, a Low Soluble High Permeable Compound, in Solid Dosage Forms Based on IVIVC and Gastrointestinal Simulation. in Molecular Pharmaceutics. 2009;6(1):40-47.
doi:10.1021/mp800128y .
Kovacević, Ivan, Parojčić, Jelena, Homšek, Irena, Tubić-Grozdanis, Marija, Langguth, Peter, "Justification of Biowaiver for Carbamazepine, a Low Soluble High Permeable Compound, in Solid Dosage Forms Based on IVIVC and Gastrointestinal Simulation" in Molecular Pharmaceutics, 6, no. 1 (2009):40-47,
https://doi.org/10.1021/mp800128y . .

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