Biopharmaceutical classification of desloratadine – not all drugs are classified the easy way
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 a...
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| Format: | Article |
| Language: | English |
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Sciendo
2020-06-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.2478/acph-2020-0006 |
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| author | Berginc Katja Sibinovska Nadica Žakelj Simon Trontelj Jurij Legen Igor |
| author_facet | Berginc Katja Sibinovska Nadica Žakelj Simon Trontelj Jurij Legen Igor |
| author_sort | Berginc Katja |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-cd13a55fa8514ce181c91413480d4460 |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2020-06-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj-art-cd13a55fa8514ce181c91413480d44602025-02-02T15:49:11ZengSciendoActa Pharmaceutica1846-95582020-06-0170213114410.2478/acph-2020-0006acph-2020-0006Biopharmaceutical classification of desloratadine – not all drugs are classified the easy wayBerginc Katja0Sibinovska Nadica1Žakelj Simon2Trontelj Jurij3Legen Igor4Lek d.d., 1526 Ljubljana, SloveniaLek d.d., 1526 Ljubljana, SloveniaUniversity of Ljubljana, Faculty of Pharmacy, Chair of Biopharmaceutics and Pharmacokinetics, SI- 1000 LjubljanaSloveniaUniversity of Ljubljana, Faculty of Pharmacy, Chair of Biopharmaceutics and Pharmacokinetics, SI- 1000 LjubljanaSloveniaLek d.d., 1526 Ljubljana, SloveniaThe 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.https://doi.org/10.2478/acph-2020-0006desloratadinebcs-based bio-waiverluminal stabilitypermeabilitydissolution |
| spellingShingle | Berginc Katja Sibinovska Nadica Žakelj Simon Trontelj Jurij Legen Igor Biopharmaceutical classification of desloratadine – not all drugs are classified the easy way Acta Pharmaceutica desloratadine bcs-based bio-waiver luminal stability permeability dissolution |
| title | Biopharmaceutical classification of desloratadine – not all drugs are classified the easy way |
| title_full | Biopharmaceutical classification of desloratadine – not all drugs are classified the easy way |
| title_fullStr | Biopharmaceutical classification of desloratadine – not all drugs are classified the easy way |
| title_full_unstemmed | Biopharmaceutical classification of desloratadine – not all drugs are classified the easy way |
| title_short | Biopharmaceutical classification of desloratadine – not all drugs are classified the easy way |
| title_sort | biopharmaceutical classification of desloratadine not all drugs are classified the easy way |
| topic | desloratadine bcs-based bio-waiver luminal stability permeability dissolution |
| url | https://doi.org/10.2478/acph-2020-0006 |
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