6533b862fe1ef96bd12c6ea8
RESEARCH PRODUCT
Optimization of the Ussing chamber setup with excised rat intestinal segments for dissolution/permeation experiments of poorly soluble drugs.
Filippos KesisoglouCarl RoosHans LennernäsDavid DahlgrenKristin FornerMoritz A. KonerdingJohanna MazurPeter Langguthsubject
Cell Membrane PermeabilityPharmaceutical Science02 engineering and technology030226 pharmacology & pharmacyBile Acids and Salts03 medical and health sciences0302 clinical medicineIn vivoDrug DiscoveryAnimalsHumansDissolutionPharmacologyRat intestineChromatographyUssing chamberChemistryOrganic ChemistryIn vivo absorptionPermeation021001 nanoscience & nanotechnologyRatsIntestinesJejunumSolubilityCaco-2 Cells0210 nano-technologyFederal statedescription
AbstractContext: Prediction of the in vivo absorption of poorly soluble drugs may require simultaneous dissolution/permeation experiments. In vivo predictive media have been modified for permeation experiments with Caco-2 cells, but not for excised rat intestinal segments.Objective: The present study aimed at improving the setup of dissolution/permeation experiments with excised rat intestinal segments by assessing suitable donor and receiver media.Methods: The regional compatibility of rat intestine in Ussing chambers with modified Fasted and Fed State Simulated Intestinal Fluids (Fa/FeSSIFmod) as donor media was evaluated via several parameters that reflect the viability of the excised intestinal segments. Receiver media that establish sink conditions were investigated for their foaming potential and toxicity. Dissolution/permeation experiments with the optimized conditions were then tested for two particle sizes of the BCS class II drug aprepitant.Results: Fa/FeSSIFmod were toxic for excised rat ileal ...
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2016-11-06 | Drug development and industrial pharmacy |