Bristol Myers Squibb, 1 Squibb Drive, New Brunswick, NJ 08903, United States.
Bristol Myers Squibb, 1 Squibb Drive, New Brunswick, NJ 08903, United States.
Int J Pharm. 2024 May 25;657:124171. doi: 10.1016/j.ijpharm.2024.124171. Epub 2024 Apr 25.
Foam granulation is a relatively newer wet granulation process whereby foamed binder solutions are added to the powders in the mixer to reduce localized over-wetting encountered during the wet granulation. This study is the first to investigate the effect of binder grade and foam quality on foam granulation process and granule properties of a high drug load formulation. Two different HPC grades, HPC LF (two times more viscous) and HPC EXF at an equivalent 7.4%w/w solution concentration, and foam quality of 50%, 90% and binder solution dripped were added to a high drug load (81%w/w) formulation for wet granulation. The granules were evaluated for compactibility and resultant compact strengths. The 50% foam quality of either HPC LF and HPC EXF resulted in lowest impeller power reading and water activity compared to 90% foam quality or dripped HPC solution. Granules prepared with 50% foam quality also exhibited smaller granule size, wider size distribution and higher specific surface area, resulting in higher compactibility. Whilst the granules prepared with different foamed HPC grades were not significantly different in compression behavior, they were higher in compact strengths, suggesting that foam mixing was more efficient in binder distribution compared to binder liquid penetration and distribution.
泡沫造粒是一种相对较新的湿法制粒工艺，通过向混合器中的粉末中添加泡沫粘结剂溶液，来减少湿法制粒过程中遇到的局部过度润湿。本研究首次考察了粘结剂等级和泡沫质量对高载药量制剂的泡沫造粒过程和颗粒性质的影响。将两种不同的 HPC 等级（HPC LF，粘性是 HPC EXF 的两倍）和 HPC EXF 添加到高载药量（81%w/w）的制剂中，以 50%、90%的泡沫质量和滴加的粘结剂溶液进行湿法制粒。评估了颗粒的可压缩性和得到的压缩强度。与 90%泡沫质量或滴加的 HPC 溶液相比，HPC LF 和 HPC EXF 的 50%泡沫质量导致最低的叶轮功率读数和水活度。用 50%泡沫质量制备的颗粒还表现出更小的颗粒尺寸、更宽的粒度分布和更高的比表面积，从而具有更高的可压缩性。虽然用不同的泡沫 HPC 等级制备的颗粒在压缩行为上没有显著差异，但它们的压缩强度更高，这表明与粘结剂液体渗透和分布相比，泡沫混合在粘结剂分布方面更有效。
