Division of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand.
Division of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand.
Int J Pharm. 2018 Jan 15;535(1-2):410-419. doi: 10.1016/j.ijpharm.2017.11.030. Epub 2017 Nov 16.
Exfoliated nanocomposites of chitosan-magnesium aluminum silicate (CS-MAS) particles are characterized by good compressibility but poor flowability. Thus, the aims of this study were to investigate agglomerates of CS-MAS nanocomposites prepared using the agglomerating agents water, ethanol, or polyvinylpyrrolidone (PVP) for flowability enhancement and to evaluate the agglomerates obtained as direct compression fillers for tablets. The results showed that the addition of agglomerating agents did not affect crystallinity, but slightly influenced thermal behavior of the CS-MAS nanocomposites. The agglomerates prepared using water were larger than those prepared using 95% ethanol because high swelling of the layer of chitosonium acetate occurred, allowing formation of solid bridges and capillary force between particles, leading to higher flowability and particle strength. Incorporation of PVP resulted in larger agglomerates with good flowability and high strength due to the binder hardening mechanism. The tablets prepared from agglomerates using water showed lower hardness, shorter disintegration times and faster drug release than those using 95% ethanol. In contrast, greater hardness and more prolonged drug release were obtained from the tablets prepared from agglomerates using PVP. Additionally, the agglomerates of CS-MAS nanocomposites showed good carrying capacity and provided desirable characteristics of direct compression tablets.
壳聚糖-镁铝硅酸盐(CS-MAS)颗粒的剥离纳米复合材料具有良好的可压缩性,但流动性差。因此,本研究旨在研究使用水、乙醇或聚乙烯吡咯烷酮(PVP)作为团聚剂来增强流动性的 CS-MAS 纳米复合材料的团聚体,并评估作为直接压片填充剂的团聚体。结果表明,添加团聚剂不会影响结晶度,但会轻微影响 CS-MAS 纳米复合材料的热行为。使用水制备的团聚体比使用 95%乙醇制备的团聚体大,因为壳聚糖翁乙酸盐层发生了高溶胀,允许在颗粒之间形成固体桥和毛细力,从而提高了流动性和颗粒强度。由于粘合剂硬化机制,加入 PVP 会导致具有良好流动性和高强度的较大团聚体。与使用 95%乙醇的团聚体相比,使用水的团聚体制备的片剂硬度较低,崩解时间较短,药物释放速度较快。相比之下,使用 PVP 的团聚体制备的片剂硬度更大,药物释放时间更长。此外,CS-MAS 纳米复合材料的团聚体具有良好的承载能力,并提供了直接压片所需的理想特性。