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未润滑和润滑(硅化)微晶纤维素的压实机制及片剂强度

Compaction mechanism and tablet strength of unlubricated and lubricated (silicified) microcrystalline cellulose.

作者信息

van Veen B, Bolhuis G K, Wu Y S, Zuurman K, Frijlink H W

机构信息

Department of Pharmaceutics, University of Kuopio, Kuopio, Finland.

出版信息

Eur J Pharm Biopharm. 2005 Jan;59(1):133-8. doi: 10.1016/j.ejpb.2004.05.009.

Abstract

This paper describes the differences in compaction properties between microcrystalline cellulose (MCC) and microcrystalline cellulose co-processed with colloidal silicon dioxide (SMCC). The different compaction parameters are not only compared for the pure materials, but also for the lubricated powders with magnesium stearate. Neither magnesium stearate, nor colloidal silicon dioxide, facilitates extensively the densification of (silicified) microcrystalline cellulose during compaction. The difference in tablet relaxation of MCC and SMCC indicates a small negative effect of colloidal silicon dioxide on the interparticle bonding strength of unlubricated MCC. However, for lubricated MCC a larger increase in tablet relaxation at a high compression speed was found than for lubricated SMCC tablets. Accordingly, the decrease in tablet strength was larger for the MCC tablets than for the SMCC tablets when lubrication was applied. The examination of the tablet strengths of tablets compressed from physical mixtures of MCC with increasing concentrations of colloidal silicon dioxide proved the slightly negative influence of silicon dioxide on the tablet strength of unlubricated MCC tablets and the positive effect of colloidal silicon dioxide addition on the tensile strength of lubricated MCC tablets. Co-processing of MCC with colloidal silicon dioxide showed no extra contribution on the tablet strength of lubricated tablets above the physical mixtures. The interactions between the different materials were further supported by the interaction parameters based on partial solubility parameters.

摘要

本文描述了微晶纤维素(MCC)与经胶体二氧化硅共处理的微晶纤维素(SMCC)在压缩性能上的差异。不仅比较了纯材料的不同压缩参数,还比较了添加硬脂酸镁的润滑粉末的压缩参数。在压缩过程中,硬脂酸镁和胶体二氧化硅均未显著促进(硅化)微晶纤维素的致密化。MCC和SMCC片剂松弛度的差异表明,胶体二氧化硅对未润滑MCC的颗粒间结合强度有轻微负面影响。然而,对于润滑的MCC,在高压缩速度下片剂松弛度的增加比润滑的SMCC片剂更大。因此,施加润滑时,MCC片剂的强度下降比SMCC片剂更大。对由MCC与浓度不断增加的胶体二氧化硅的物理混合物压制而成的片剂的强度进行检测,结果证明二氧化硅对未润滑MCC片剂的强度有轻微负面影响,而添加胶体二氧化硅对润滑MCC片剂的抗张强度有积极作用。MCC与胶体二氧化硅的共处理对润滑片剂的强度没有超过物理混合物的额外贡献。基于部分溶解度参数的相互作用参数进一步支持了不同材料之间的相互作用。

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