AstraZeneca 02

High Throughput API Solubility & Solid Form Characterisation

Task

Following previous cutbacks in the pharmaceutical industry, medicinal chemistry is now once again emerging as the main focus for new lead discovery to bring new therapeutic drugs to the market place. This includes the development of potential targets to maintain effi cacy when solubilised in a medium tolerable to subjects, in conjunction with the selection of the correct solid form state.
          
The early generation of as much data as possible from any new potential drug is thus crucial to allow scientists to make the right decision as to which lead structures should be pursued further to a successful clinical trial.
                     

Solution

Zinsser Analytic have developed a robotic system to enable studies of both API solubility and solid form structure in the same robotic workstation. Based on our proven Lissy platform, the system has 3 independently working robotic arms – 8 channels of standard liquid handling in arm 1, powder handling, low volume pipetting, heated pipetting and viscous pipetting in arm 2 and a separate robotic arm housing a rotational gripper. The system includes all the necessary workbench tools to automate both processes such as vial and plate transportation, barcode reading, capping & de-capping of vials, liquid and solid handling, mixing through vortexing, heating and cooling for dissolution and crystallisation, sonication through a 24 element head, evaporation, fi ltration, pH monitoring and analysis tools of nephelometry, UV/VIS spectroscopy and on line crystal imaging by microscopy. Our unique software controls the operation of all elements of the system allowing the processing of 14 workfl ows in parallel over a total time period of 7 days, with full data capture and export as a full sample audit trail at the end of each run.