Related Experiment Video
Updated: Jul 16, 2026

Drug-induced Sensitization of Adenylyl Cyclase: Assay Streamlining and Miniaturization for Small Molecule and siRNA Screening Applications
Published on: January 27, 2014
Miniaturized assay for solubility and residual solid screening (SORESOS) in early drug development
Nicole Wyttenbach1, Jochem Alsenz, Olaf Grassmann
1Department of Preclinical Research, Pharma Division, F. Hoffmann-La Roche Ltd., Bldg. 093/724, CH-4070, Basle, Switzerland. nicole.wyttenbach@roche.com
Purpose:
The aim was to develop a miniaturized method for solubility and residual solid screening of drug compounds in aqueous and non-aqueous vehicles in early drug development.
Methods:
Different crystal modifications of caffeine, carbamazepine, and piroxicam were added into 96-well filter plates and solubility was determined in 100 microl of 17 pharmaceutical vehicles. After filtration, drug concentration was determined by Ultra Performance Liquid Chromatography (UPLC). Residual solid drug in the filter plates was analyzed by high-throughput (HT) transmission X-ray Powder Diffraction (XRPD).
Results:
HT XRPD analysis revealed solid form conversions of all compounds during solubility determination, e.g., formation of hydrates in aqueous vehicles (caffeine, carbamazepine, piroxicam) or conversion of a metastable crystal form to the stable form (caffeine). Drug solubility was strongly dependent on the crystal modifications formed during the solubility assay.
Conclusions:
The new assay allows the simultaneous, small scale screening of drug solubility in various pharmaceutical vehicles and identification of changes in solid form. It is useful for the identification of formulations and formulation options in non-clinical and clinical development.
More Related Videos
Related Concept Videos
In Vitro Drug Dissolution: Alternative Methods
In Vitro Drug Dissolution: Compendial Testing Models I
Bioavailability Enhancement: Drug Solubility Enhancement
In Vitro Drug Dissolution: Compendial Testing Models II
Drug Dissolution: Requirements and Profile Comparison
In Vitro Drug Release Testing: Overview, Development and Validation

