The Biopharmaceutics Classification System (BCS) represents the framework for predicting the intestinal drug absorption based on its solubility and intestinal permeability. Recent research has lead to the use of in vitro tests to waive additional in vivo bioequivalence studies for some pharmaceutical products (i.e. biowaiver). The current regulations permit waivers for BCS Class I (highly soluble/highly permeable) drug substances, which represent up to 25% of the drugs. Efforts in both the science and regulatory bodies are being made to extend biowaivers to certain Class II and III products, which would represent more than 50% of all drugs coming to the market. The aim of this study was to investigate the influence of experimental conditions on metformin hydrochloride (CAS 1115-70-4) release from two immediate-release tablet formulations with proven bioequivalence and justify the biowaiver request for dissolution profile similarity in three pH media. The results obtained indicate that ...differences in drug dissolution observed in vitro were not reflected in vivo. Such data support the existing idea that BCS Class III drugs are eligible biowaiver candidates, even if a very rapid dissolution criterion is not fulfilled.
Keywords:
Antihyperglycemic drug / BCS Class III drugs / CAS 1115-70-4 / In vitro - in vivo correlation / Metformin hydrochloride / bioequivalence / dissolution / immediate-release
Source:
Arzneimittelforschung - Drug Research, 2010, 60, 9, 553-559
Publisher:
ECV-Editio Cantor Verlag Medizin Naturwissenschaften, Aulendorf
TY - JOUR
AU - Homšek, Irena
AU - Parojčić, Jelena
AU - Dacević, Mirjana
AU - Petrović, Ljiljana
AU - Jovanović, Dušan
PY - 2010
UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1404
AB - The Biopharmaceutics Classification System (BCS) represents the framework for predicting the intestinal drug absorption based on its solubility and intestinal permeability. Recent research has lead to the use of in vitro tests to waive additional in vivo bioequivalence studies for some pharmaceutical products (i.e. biowaiver). The current regulations permit waivers for BCS Class I (highly soluble/highly permeable) drug substances, which represent up to 25% of the drugs. Efforts in both the science and regulatory bodies are being made to extend biowaivers to certain Class II and III products, which would represent more than 50% of all drugs coming to the market. The aim of this study was to investigate the influence of experimental conditions on metformin hydrochloride (CAS 1115-70-4) release from two immediate-release tablet formulations with proven bioequivalence and justify the biowaiver request for dissolution profile similarity in three pH media. The results obtained indicate that differences in drug dissolution observed in vitro were not reflected in vivo. Such data support the existing idea that BCS Class III drugs are eligible biowaiver candidates, even if a very rapid dissolution criterion is not fulfilled.
PB - ECV-Editio Cantor Verlag Medizin Naturwissenschaften, Aulendorf
T2 - Arzneimittelforschung - Drug Research
T1 - Justification of metformin hydrochloride biowaiver criteria based on bioequivalence study
VL - 60
IS - 9
SP - 553
EP - 559
DO - 10.1055/s-0031-1296324
UR - https://hdl.handle.net/21.15107/rcub_farfar_1404
ER -
@article{
author = "Homšek, Irena and Parojčić, Jelena and Dacević, Mirjana and Petrović, Ljiljana and Jovanović, Dušan",
year = "2010",
abstract = "The Biopharmaceutics Classification System (BCS) represents the framework for predicting the intestinal drug absorption based on its solubility and intestinal permeability. Recent research has lead to the use of in vitro tests to waive additional in vivo bioequivalence studies for some pharmaceutical products (i.e. biowaiver). The current regulations permit waivers for BCS Class I (highly soluble/highly permeable) drug substances, which represent up to 25% of the drugs. Efforts in both the science and regulatory bodies are being made to extend biowaivers to certain Class II and III products, which would represent more than 50% of all drugs coming to the market. The aim of this study was to investigate the influence of experimental conditions on metformin hydrochloride (CAS 1115-70-4) release from two immediate-release tablet formulations with proven bioequivalence and justify the biowaiver request for dissolution profile similarity in three pH media. The results obtained indicate that differences in drug dissolution observed in vitro were not reflected in vivo. Such data support the existing idea that BCS Class III drugs are eligible biowaiver candidates, even if a very rapid dissolution criterion is not fulfilled.",
publisher = "ECV-Editio Cantor Verlag Medizin Naturwissenschaften, Aulendorf",
journal = "Arzneimittelforschung - Drug Research",
title = "Justification of metformin hydrochloride biowaiver criteria based on bioequivalence study",
volume = "60",
number = "9",
pages = "553-559",
doi = "10.1055/s-0031-1296324",
url = "https://hdl.handle.net/21.15107/rcub_farfar_1404"
}
Homšek, I., Parojčić, J., Dacević, M., Petrović, L.,& Jovanović, D.. (2010). Justification of metformin hydrochloride biowaiver criteria based on bioequivalence study. in Arzneimittelforschung - Drug Research
ECV-Editio Cantor Verlag Medizin Naturwissenschaften, Aulendorf., 60(9), 553-559.
https://doi.org/10.1055/s-0031-1296324
https://hdl.handle.net/21.15107/rcub_farfar_1404
Homšek I, Parojčić J, Dacević M, Petrović L, Jovanović D. Justification of metformin hydrochloride biowaiver criteria based on bioequivalence study. in Arzneimittelforschung - Drug Research. 2010;60(9):553-559.
doi:10.1055/s-0031-1296324
https://hdl.handle.net/21.15107/rcub_farfar_1404 .
Homšek, Irena, Parojčić, Jelena, Dacević, Mirjana, Petrović, Ljiljana, Jovanović, Dušan, "Justification of metformin hydrochloride biowaiver criteria based on bioequivalence study" in Arzneimittelforschung - Drug Research, 60, no. 9 (2010):553-559,
https://doi.org/10.1055/s-0031-1296324 .,
https://hdl.handle.net/21.15107/rcub_farfar_1404 .
