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

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Use of Twin Screw Extruders as a Process Chemistry Tool: Application of Mechanochemistry To Support Early Development Programs
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2018-09-07 00:00:00 , DOI: 10.1021/acs.oprd.8b00253
Henry Morrison ₁ , Peter Fung ₁ , To Tran ₁ , Elizabeth Horstman ₁ , Ernest Carra ₁ , Steven Touba ₁

Affiliation

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.

中文翻译：

使用双螺杆挤出机作为工艺化学工具：机械化学在支持早期开发计划中的应用

GS-X和GS-Y是为早期临床开发选择的新型活性药物成分（API）。对于每个API，鉴定了两个微吸湿的未溶解多晶型物，需要对这些相进行研究以鉴定室温下的稳定形式。为了支持这一点，利用双螺杆挤出机进行机械化学作用以放大GS-X和GS-Y多晶型物。所得材料用于进行溶解度测量以绘制相对稳定性，从而可以设计结晶以确保在室温下控制热力学最稳定的形式。

更新日期：2018-09-07

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