Producing Amorphous Solid Dispersions via Co-Precipitation and Spray Drying: Impact to Physicochemical and Biopharmaceutical Properties

摘要: Many small-molecule active pharmaceutical ingredients (APIs) exhibit low aqueous solubility and benefit from generation of amorphous dispersions the API polymer to improve their dissolution properties. Spray drying hot-melt extrusion are 2 common methods produce these dispersions; however, for some systems, approaches may not be optimal, it would beneficial have an alternative route. Herein, solid compound A, a low-solubility weak acid, copovidone were made by conventional spray co-precipitation. The physicochemical properties materials assessed via X-ray diffraction, differential scanning calorimetry, thermal gravimetric analysis, electron microscopy. then formulated tableted, performance was in vivo vitro. In human studies, co-precipitation tablets had slightly slower than spray-dried dispersion, but both reached full release A. canine vitro showed comparable profiles. Finally, pharmacokinetic studies that values area under curve, bioavailability, Cmax. Based on summarized data, we conclude APIs, is viable make while maintaining desirable biopharmaceutical characteristics.