Institute of Pharmaceutical Technology and Biopharmacy, University of Muenster, Corrensstraße 48, 48149 Münster, Germany.
Institute of Pharmaceutical Technology and Biopharmacy, University of Muenster, Corrensstraße 48, 48149 Münster, Germany.
Eur J Pharm Biopharm. 2020 Sep;154:89-97. doi: 10.1016/j.ejpb.2020.06.020. Epub 2020 Jul 4.
Preparation of pharmaceutical nanosuspensions is a popular technique to increase the dissolution velocity of poorly water-soluble drugs. Subsequent drying into a compaction-ready powder or granule is a critical process due to possible adverse solid characteristics and the risk of growth of nanoparticles. This work evaluated the drying of nanosuspensions via fluid bed granulation with focus on the binder selection and used concentrations, as well as the parameters spray rate and atomization pressure. Design of experiments was used to identify significant parameters. Indomethacin nanosuspensions were prepared by wet media milling and dried on a carrier consisting of lactose, microcrystalline cellulose, and crospovidone with and without additional binder during granulation. Resulting granules were compacted into tablets and their in vitro dissolution performances were characterized. A higher content of binder PVP and a higher spray rate led to less growth of resuspended nanoparticles. Finally, indomethacin nanoparticle tablets showed a superior dissolution performance in contrast to raw indomethacin tablets.
制备药物纳米混悬剂是提高难溶性药物溶解速度的常用技术。由于可能存在不良的固体特性和纳米颗粒生长的风险，随后将其干燥成可压制成型的粉末或颗粒是一个关键过程。这项工作评估了通过流化床造粒干燥纳米混悬剂的情况，重点关注了粘合剂的选择和使用浓度，以及喷雾速率和雾化压力等参数。实验设计用于确定显著参数。通过湿磨法制备吲哚美辛纳米混悬剂，并在载体制备过程中使用乳糖、微晶纤维素和交联聚维酮，在流化床造粒过程中添加或不添加额外的粘合剂。将得到的颗粒压制成片剂，并对其体外溶解性能进行了表征。更高含量的 PVP 粘合剂和更高的喷雾速率导致再悬浮纳米颗粒的生长减少。最后，与原吲哚美辛片剂相比，吲哚美辛纳米颗粒片剂表现出更好的溶解性能。
