Solubility is a common physicochemical parameter which reflects the bioavailability of orally administered compounds. Poor solubility also affects the analysis in other DMPK assays and could be a developmental challenge for the compounds.
Thermodynamic solubility is typically measured by the saturation of compounds (solid powder form) in equilibrium in relevant biological fluids. Kinetic solubility investigates the solubility of DMSO solution of compounds in relevant biological fluids. Kinetic solubility is more relevant and useful for other in vitro assays where DMSO solutions are typically used for assay measurements.
Solubility assay protocol:
Method: Filter based
Test article concentration: 250 µM (other upon request)
Incubation time: Overnight
Incubation temperature: Ambient temperature
Number of Replicates: n = 2 (aliquots from filterate)
Assay condition: SGF, FaSSGF, SIF, FaSSIF, FeSSIF, HEPES (as per request)
Positive control: Propranolol
Analysis Method: LC/MS/MS
Data Delivery: Solubility µM or mg/mL (as per request)