20.500.12556/RUL-141322 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 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. desloratadine BCS-based bio-waiver luminal stability permeability dissolution true false true Angleški jezik Angleški jezik Članek v reviji 2022-09-28 10:31:06 2022-09-28 10:31:13 2022-09-29 04:03:47 0000-00-00 00:00:00 2020 0 0 Str. 131-144 iss. 2 Vol. 70 2020 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 544.351.3:615 1330-0075 10.2478/acph-2020-0006 4797553 10.2478_acph-2020-0006.pdf 10.2478_acph-2020-0006.pdf 1 18AE0182CC80D29C61D58358242F21C5 b25b50df9914cc2912226a0b8f83d4f90e9cd852dfb84a4439c53314efb60271 0e529913-3f08-11ed-9c94-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=162327 https://sciendo.com/article/10.2478/acph-2020-0006 1 e7f8de29-3f07-11ed-9c94-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=162326 Fakulteta za farmacijo 0 0 0