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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.
Mol Pharm. 2009 Jan-Feb; 6(1):40-7.MP

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.

Authors+Show Affiliations

Medicines and Medical Devices Agency of Serbia, Vojvode Stepe 458, Belgrade, Serbia.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

19248231

Citation

Kovacević, Ivan, et al. "Justification of Biowaiver for Carbamazepine, a Low Soluble High Permeable Compound, in Solid Dosage Forms Based On IVIVC and Gastrointestinal Simulation." Molecular Pharmaceutics, vol. 6, no. 1, 2009, pp. 40-7.
Kovacević I, Parojcić J, Homsek I, et al. Justification of biowaiver for carbamazepine, a low soluble high permeable compound, in solid dosage forms based on IVIVC and gastrointestinal simulation. Mol Pharm. 2009;6(1):40-7.
Kovacević, I., Parojcić, J., Homsek, 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. Molecular Pharmaceutics, 6(1), 40-7. https://doi.org/10.1021/mp800128y
Kovacević I, et al. Justification of Biowaiver for Carbamazepine, a Low Soluble High Permeable Compound, in Solid Dosage Forms Based On IVIVC and Gastrointestinal Simulation. Mol Pharm. 2009 Jan-Feb;6(1):40-7. PubMed PMID: 19248231.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Justification of biowaiver for carbamazepine, a low soluble high permeable compound, in solid dosage forms based on IVIVC and gastrointestinal simulation. AU - Kovacević,Ivan, AU - Parojcić,Jelena, AU - Homsek,Irena, AU - Tubić-Grozdanis,Marija, AU - Langguth,Peter, PY - 2009/2/28/entrez PY - 2009/2/28/pubmed PY - 2009/3/24/medline SP - 40 EP - 7 JF - Molecular pharmaceutics JO - Mol Pharm VL - 6 IS - 1 N2 - 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. SN - 1543-8384 UR - https://www.unboundmedicine.com/medline/citation/19248231/Justification_of_biowaiver_for_carbamazepine_a_low_soluble_high_permeable_compound_in_solid_dosage_forms_based_on_IVIVC_and_gastrointestinal_simulation_ L2 - https://doi.org/10.1021/mp800128y DB - PRIME DP - Unbound Medicine ER -