GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, Faculty of Science, National University of Singapore, Singapore.
AAPS PharmSciTech. 2011 Dec;12(4):1374-83. doi: 10.1208/s12249-011-9706-y. Epub 2011 Oct 18.
Recently, microwave-induced melt granulation was shown to be a promising alternative to conventional melt granulation with improved process monitoring capabilities. This study aimed to compare the physicochemical and compaction properties of granules produced from microwave-induced and conventional melt granulation. Powder admixtures comprising equivalent proportions by weight of lactose 200 M and anhydrous dicalcium phosphate were granulated with polyethylene glycol 3350 under the influence of microwave-induced and conventional heating in a 10-L single pot high shear processor. The properties of the granules and compacts produced from the two processes were compared. Relative to conventional melt granulation, the rates at which the irradiated powders heated up in microwave-induced melt granulation were lower. Agglomerate growth proceeded at a slower rate, and this necessitated longer massing durations for growth induction. These factors prompted greater evaporative moisture losses from the melt granules. Additionally, nonuniform heating of the powders under the influence of microwaves led to increased inter-batch variations in the binder contents of resultant melt granules and a reliance of content homogeneity on massing duration. Agglomerate growth proceeded more rapidly under the influence of conventional heating due to the enhanced heating capabilities of the powders. Melt granules produced using the conventional method possessed higher moisture contents and improved content homogeneity. The compaction behavior of melt granules were affected by their mean sizes, porosities, flow properties, binder, and moisture contents. The last two factors were responsible for the disparities in compaction behavior of melt granules produced from microwave-induced and conventional melt granulation.
最近,微波诱导熔融造粒被证明是一种有前途的替代传统熔融造粒的方法,具有改进的过程监测能力。本研究旨在比较微波诱导熔融造粒和传统熔融造粒生产的颗粒的物理化学和压缩性能。将乳糖 200 M 和无水磷酸二钙的重量比相等的粉末混合物与聚乙二醇 3350 在 10-L 单锅高剪切处理器中在微波诱导和常规加热的影响下造粒。比较了两种工艺生产的颗粒和压片的性能。与传统熔融造粒相比,微波诱导熔融造粒中辐照粉末的加热速度较低。团聚体的生长速度较慢,这需要更长的团聚诱导时间。这些因素促使从熔融颗粒中蒸发更多的水分。此外,微波的影响下粉末的不均匀加热导致所得熔融颗粒中粘合剂含量的批次间变化增加,并且对含量均匀性的依赖于团聚诱导时间。由于粉末的加热能力增强,传统加热下的团聚体生长速度更快。使用传统方法生产的熔融颗粒具有更高的水分含量和改善的含量均匀性。熔融颗粒的压缩行为受其平均粒径、孔隙率、流动性能、粘合剂和水分含量的影响。最后两个因素是导致微波诱导熔融造粒和传统熔融造粒生产的熔融颗粒压缩行为差异的原因。