Justification of Biowaiver for Carbamazepine, a Low Soluble High Permeable Compound, in Solid Dosage Forms Based on IVIVC and Gastrointestinal Simulation
Samo za registrovane korisnike
2009
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
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.
Ključne reči:
BCS / bioequivalence / carbamazepine / gastrointestinal simulation / IVIVCIzvor:
Molecular Pharmaceutics, 2009, 6, 1, 40-47Izdavač:
- Amer Chemical Soc, Washington
Finansiranje / projekti:
- 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
Institucija/grupa
PharmacyTY - 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 . .