Abstract Monodisperse emulsions of solvent saturated with the active pharmaceutical ingredient (API) cabotegravir were generated by microfluidic devices. In contrast to model oil-water emulsions that provide idealized conditions for obtaining highly monodisperse emulsions, APIs impart strict limitations on solvent choice. To provide a suitable environment in which extractive crystallization could occur, and to enhance reproducibility, co-solvents were introduced. Subsequently, the effect of each solvent component on morphology and size was observed. Through the manipulation of solvent composition, particles of both plate-like and spherical multi-crystal agglomerates were obtained, providing the ability to tune the operating conditions to provide particles with desirable characteristics such as size, shape and flowability. Scale-up of the manufacturing process was addressed through the application of existing microfluidic parallelization techniques, resulting in a 100-fold increase in throughput over a single-channel device. Subsequently, the obtained pure, and excipient-bound, API spherical agglomerates, were subjected to batch isolation and washing.

中文翻译：

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Cabotegravir 在基于液滴的微流体装置中的萃取结晶

摘要 用活性药物成分 (API) cabotegravir 饱和溶剂的单分散乳液是通过微流体装置产生的。与为获得高度单分散乳液提供理想条件的模型油水乳液相比，API 对溶剂选择有严格的限制。为了提供可以发生萃取结晶的合适环境并提高重现性，引入了共溶剂。随后，观察每种溶剂组分对形态和尺寸的影响。通过控制溶剂组成，获得了片状和球形多晶附聚物的颗粒，从而提供了调整操作条件以提供具有所需特性（例如尺寸、形状和流动性）的颗粒的能力。通过应用现有的微流体并行化技术解决了制造过程的放大问题，使单通道设备的吞吐量增加了 100 倍。随后，对获得的纯的、赋形剂结合的 API 球形团聚体进行分批分离和洗涤。