赋形剂的物理性质和化学取代对片剂压实和崩解行为的影响——以低取代羟丙基纤维素(L-HPC)为例

Macromol Pub Date : 2022-03-04 DOI:10.3390/macromol2010007
Saurabh M Mishra, Andreas Sauer
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引用次数: 4

摘要

由于剂型的最终属性很大程度上取决于所使用的赋形剂的性质,因此了解赋形剂的物理化学性质的影响是很重要的。本文研究了6种不同粒径和羟丙基含量的L-HPC,研究了不同粒径和羟丙基含量对L-HPC压实和崩解性能的影响。在不同的压缩载荷下压缩所有等级的L-HPC,以获得不同的片剂孔隙率。采用改进的Heckel方程和渗流模型对L-HPC等级的压缩性和致密性进行了评价。采用32全因子设计评价L-HPC粒径和羟丙基含量对片剂孔隙度和崩解时间的影响。压实研究发现,L-HPC的可压缩性在很大程度上取决于粒径,粒径等级越低,可压缩性越低。而L-HPC的固结/键合行为与颗粒大小和%羟丙基含量无关。通过析因设计,发现粒径和%羟丙基含量对L-HPC的崩解行为有显著影响。结果表明,粒径越小、羟丙基含量越高的L-HPC,其崩解时间越长。因此,应仔细考虑辅料的选择,以达到所期望的产品质量属性。
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Effect of Physical Properties and Chemical Substitution of Excipient on Compaction and Disintegration Behavior of Tablet: A Case Study of Low-Substituted Hydroxypropyl Cellulose (L-HPC)
As final attributes of dosage form largely depend on the properties of excipients used, understanding the effect of physicochemical properties of excipients is important. In the present study, six grades of L-HPC with varying degrees of particle size and hydroxypropyl content and the influence of the grade on compaction as well as disintegration behavior were studied. All grades of L-HPC were compressed at different compression loads to achieve different tablet porosity. Compressibility and compactibility of L-HPC grades were evaluated using a modified Heckel equation and percolation model. Further effects of particle size and hydroxypropyl content of L-HPC on tablet porosity and disintegration time were evaluated using a 32 full-factorial design. From compaction studies, it was found that compressibility of L-HPC largely depends upon the particle size with lower particle size grade showing lower compressibility. Whereas consolidation/bonding behavior of L-HPC is independent of particle size and % hydroxypropyl content. By factorial design, it was found that particle size and % hydroxypropyl content have a significant effect on the disintegration behavior of L-HPC. It was found that smaller particle sizes and higher hydroxypropyl content of L-HPC show longer disintegration time. Thus, careful consideration of excipients selection should be made to achieve desired quality attribute of the product.
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