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

Berginc, Katja (author), Sibinovska, Nadica (author), Žakelj, Simon (author), Trontelj, Jurij (author), Legen, Igor (author)

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.

• Language: English
• Keywords: desloratadine, BCS-based bio-waiver, luminal stability, permeability, dissolution
• Work type: Article
• Typology: 1.01 - Original Scientific Article
• Organization: FFA - Faculty of Pharmacy
• Publication status: Published
• Publication version: Version of Record
• Year: 2020
• Number of pages: Str. 131-144
• Numbering: Vol. 70, iss. 2
• PID: 20.500.12556/RUL-141322
• UDC: 544.351.3:615
• ISSN on article: 1330-0075
• DOI: 10.2478/acph-2020-0006
• COBISS.SI-ID: 4797553
• Publication date in RUL: 28.09.2022

Record is a part of a journal

• Title: Acta pharmaceutica
• Shortened title: Acta pharm.
• Publisher: Hrvatsko farmaceutsko društvo
• ISSN: 1330-0075
• COBISS.SI-ID: 13497349

Licences

• License: CC BY 4.0, Creative Commons Attribution 4.0 International
• Link: http://creativecommons.org/licenses/by/4.0/
• Description: This is the standard Creative Commons license that gives others maximum freedom to do what they want with the work as long as they credit the author.

Projects

• Funder: ARRS - Slovenian Research Agency
• Project number: P1-0189-2018
• Name: Farmacevtska tehnologija: od dostavnih sistemov učinkovin do terapijskih izidov zdravil pri otrocih in starostnikih