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Continuous Cocrystallization for Dissolution Rate Optimization of a Poorly Water-Soluble Drug

机译:连续共结晶优化水溶性差的药物的溶出速率

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A continuous manufacturing process, hot melt extrusion (HME), was employed for the development of high quality carbamazepine?saccharin (CBZ?SCH) cocrystals. The produced cocrystals were compared with a prototype prepared by a solvent method. It was found that processing parameters such as temperature, screw speed, and screw configuration were the critical processing parameters. In-line near-infrared analysis demonstrated that cocrystallization takes place gradually during the process along the extruder’s mixing zones. Further characterization of the extruded cocrystals proved that the manufactured highly crystalline cocrystals were similar to the prototype but had improved CBZ dissolution rates. Continuous manufacturing of cocrystals of water-insoluble drugs is a novel and robust approach.
机译:采用连续制造工艺热熔挤出(HME)来开发高质量的卡马西平?糖精(CBZ?SCH)共晶体。将产生的共晶体与通过溶剂法制备的原型进行比较。发现诸如温度,螺杆速度和螺杆构造的加工参数是关键的加工参数。在线近红外分析表明,共结晶过程是沿着挤出机的混合区逐渐进行的。挤出共晶的进一步表征证明,所制造的高度结晶共晶与原型相似,但具有改善的CBZ溶解速率。连续制造水不溶性药物的共晶体是一种新颖而稳健的方法。

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