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Acta Pharmaceutica, Vol. 70 No. 2, 2020.

Original scientific paper

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

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

KATJA BERGINC ; Lek d.d., 1526 Ljubljana, Slovenia
NADICA SIBINOVSKA ; University of Ljubljana, Faculty of pharmacy, Chair of Biopharmaceutics and Pharmacokinetics, SI- 1000 Ljubljana, Slovenia
SIMON ŽAKELJ ; University of Ljubljana, Faculty of pharmacy, Chair of Biopharmaceutics and Pharmacokinetics, SI- 1000 Ljubljana, Slovenia
JURIJ TRONTELJ ; University of Ljubljana, Faculty of pharmacy, Chair of Biopharmaceutics and Pharmacokinetics, SI- 1000 Ljubljana, Slovenia
IGOR LEGEN ; Lek d.d., 1526 Ljubljana, Slovenia

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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 desloratadine 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.

Keywords

desloratadine; BCS-based bio-waiver; luminal stability; permeability; dissolution

Hrčak ID:

220895

URI

https://hrcak.srce.hr/220895

Publication date:

30.6.2020.

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