Centre for Research Innovation (CRI), University of Greenwich, Chatham Maritime Kent, Chatham, ME4 4TB, UK.
Delta Pharmaceutics Ltd., 1-3 Manor Road, Chatham, Kent, ME4 6AG, UK.
AAPS PharmSciTech. 2024 Jul 31;25(6):174. doi: 10.1208/s12249-024-02890-y.
Twin-screw wet granulation (TSWG) is a manufacturing process that offers several advantages for the processing of water-insoluble active pharmaceutical ingredients (APIs) and has been used for increasing the solubility and dissolution rates. Here we introduce a novel TSWG approach with reduced downstream processing steps by using non-volatile solvents as granulating binders.
Herein, TSWG was carried out using Transcutol a non-volatile protic solvent as a granulating binder and dissolution enhancer of ibuprofen (IBU) blends with cellulose polymer grades (Pharmacoat 603, Affinisol™, and AQOAT).
The physicochemical characterisation of the produced granules showed excellent powder flow and the complete transformation of IBU into the amorphous state. Dissolution studies presented immediate release rates for all IBU formulations due to the high drug-polymer miscibility and the Transcutol solubilising capacity.
Overall, the study demonstrated an innovative approach for the development of extruded granules by processing water-insoluble APIs with non-volatile solvents for enhanced dissolution rates at high drug loadings.
双螺杆湿法造粒（TSWG）是一种制造工艺，为处理水不溶性活性药物成分（APIs）提供了多项优势，并已用于提高溶解度和溶解速率。在这里，我们介绍了一种新颖的 TSWG 方法，通过使用非挥发性溶剂作为制粒粘合剂来减少下游处理步骤。
本文采用非挥发性质子溶剂 Transcutol 作为制粒粘合剂和增溶剂，对布洛芬（IBU）与纤维素聚合物等级（Pharmacoat 603、Affinisol™和 AQOAT）的混合物进行 TSWG。
所制得颗粒的物理化学特性表明，粉末流动性极好，IBU 完全转化为无定形状态。由于药物-聚合物的高混溶性和 Transcutol 的增溶能力，所有 IBU 配方的溶解研究均呈现出即刻释放速率。
总的来说，该研究展示了一种通过使用非挥发性溶剂处理水不溶性 API 来开发挤出颗粒的创新方法，以在高药物载量下提高溶解速率。
