<abstract xmlns="http://www.w3.org/1999/xhtml"><p>The biopharmaceutical classification of drugs was designed as a basis for bio-waivers – a mechanism with the double ethical benefit of delivering new drug formulations to the market with less human testing and lower cost. However, many drugs defy simple classification because <italic>in vitro</italic> permeability and stability assessment can be challenging as shown in this study for desloratadine. Literature shows that desloratadine is highly soluble, while data on luminal stability and permeability are circumstantial. Combined with borderline bioavailability and not really known fraction of absorbed dose, desloratadine was found to be a good example for showing the innovative <italic>in vitro</italic> approaches necessary to unambiguously classify desloratadine according to Biopharmaceutical Classification System (BCS) guideline. Presented study undoubtedly confirmed that desloratadine solubility is high and dissolution is very rapid for immediate release reference tablets. We have demonstrated deslorata-dine stability under legally required conditions and also in more physiologically relevant media. High <italic>in vitro</italic> desloratadine permeability was confirmed using Caco-2 and Parallel Artificial Membrane Permeability Assay (PAMPA). Well-established <italic>in vitro</italic> model with rat intestinal tissue could not be used due to reasons elaborated in this paper.</p></abstract>

The biopharmaceutical classification of drugs was designed as a basis for bio-waivers – a mechanism with the double ethical benefit of delivering new drug formulations to the market with less human testing and lower cost. However, many drugs defy simple classification because in vitro permeability and stability assessment can be challenging as shown in this study for desloratadine. Literature shows that desloratadine is highly soluble, while data on luminal stability and permeability are circumstantial. Combined with borderline bioavailability and not really known fraction of absorbed dose, desloratadine was found to be a good example for showing the innovative in vitro approaches necessary to unambiguously classify desloratadine according to Biopharmaceutical Classification System (BCS) guideline. Presented study undoubtedly confirmed that desloratadine solubility is high and dissolution is very rapid for immediate release reference tablets. We have demonstrated deslorata-dine stability under legally required conditions and also in more physiologically relevant media. High in vitro desloratadine permeability was confirmed using Caco-2 and Parallel Artificial Membrane Permeability Assay (PAMPA). Well-established in vitro model with rat intestinal tissue could not be used due to reasons elaborated in this paper.

Biopharmaceutical classification of desloratadine – not all drugs are classified the easy way

Faculty of Pharmacy, Chair of Biopharmaceutics and Pharmacokinetics

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

The biopharmaceutical classification of drugs was designed as a basis for bio-waivers – a mechanism with the double ethical benefit of delivering new drug...

Biopharmaceutical classification of desloratadine – not all drugs are classified the easy way

Publicado en línea: 16 ene 2020

Páginas: 131 - 144

Aceptado: 31 may 2019

DOI: https://doi.org/10.2478/acph-2020-0006

Palabras clave
desloratadine, BCS-based bio-waiver, luminal stability, permeability, dissolution

© 2020 Katja Berginc et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Biopharmaceutical classification of desloratadine – not all drugs are classified the easy way

Publicado en línea: 16 ene 2020

Páginas: 131 - 144

Aceptado: 31 may 2019

DOI: https://doi.org/10.2478/acph-2020-0006

Palabras clavedesloratadine, BCS-based bio-waiver, luminal stability, permeability, dissolution

© 2020 Katja Berginc et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Palabras clave
desloratadine, BCS-based bio-waiver, luminal stability, permeability, dissolution