Use of Twin Screw Extruders as a Process Chemistry Tool: Application of Mechanochemistry To Support Early Development Programs

摘要

GS-X and GS-Y are novel active pharmaceutical ingredients (APIs) selected for early clinical development. For each API, two slightly hygroscopic unsolvated polymorphs were identified, and investigations of these phases were required to identify the stable form at room temperature. To support this, twin screw extruders were utilized to apply mechanochemistry for scale-up of GS-X and GS-Y polymorphs. The resulting materials were used to conduct solubility measurements to map relative stabilities so that crystallizations could be designed to ensure form control for the thermodynamically most stable form at room temperature.