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微晶纤维素的润湿性液体依赖性解聚及其对挤出滚圆法制备微丸的影响。

Moistening liquid-dependent de-aggregation of microcrystalline cellulose and its impact on pellet formation by extrusion-spheronization.

作者信息

Sarkar Srimanta, Liew Celine Valeria

机构信息

GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, 18 Science Drive, Singapore, 117543, Singapore.

出版信息

AAPS PharmSciTech. 2014 Jun;15(3):753-61. doi: 10.1208/s12249-014-0098-7. Epub 2014 Feb 20.

Abstract

The wet-state particle size of microcrystalline cellulose (MCC) dispersed in different moistening liquids was characterized to elucidate the effect of moistening liquid type on the extent of MCC particle de-aggregation. Cohesive strength of moistened MCC masses was also assessed and pellet production by extrusion-spheronization attempted. MCC dispersed in alcohol or water-alcohol mixtures with higher alcohol proportions generally had larger particle sizes. Moistened mass cohesive strength decreased and poorer quality pellets were obtained when water-alcohol mixtures with higher alcohol proportions were used as the moistening liquid. MCC comprise aggregates of small sub-units held together by hydrogen bonds. As MCC particle de-aggregation involves hydrogen bond breaking, moistening liquids with lower polarity, such as water-alcohol mixtures with higher alcohol proportions, induced lesser de-aggregation and yielded MCC with larger particle sizes. When such water-alcohol mixtures were employed during extrusion-spheronization with MCC, the larger particle size of MCC and lower surface tension of the moistening liquid gave rise to moistened masses with lower cohesive strength. During pelletization, agglomerate growth by coalescence and closer packing of components by particle rearrangement would be limited. Thus, weaker, less spherical pellets with smaller size and wider size distribution were produced.

摘要

对分散在不同润湿液体中的微晶纤维素(MCC)的湿态粒径进行了表征,以阐明润湿液体类型对MCC颗粒解聚程度的影响。还评估了湿态MCC物料的内聚强度,并尝试通过挤出滚圆法制备丸粒。分散在酒精或酒精比例较高的水 - 酒精混合物中的MCC通常具有较大的粒径。当使用酒精比例较高的水 - 酒精混合物作为润湿液体时,湿态物料的内聚强度降低,且获得的丸粒质量较差。MCC由通过氢键结合在一起的小亚基聚集体组成。由于MCC颗粒解聚涉及氢键断裂,极性较低的润湿液体,如酒精比例较高的水 - 酒精混合物,引起的解聚较少,从而产生粒径较大的MCC。当在MCC的挤出滚圆过程中使用这种水 - 酒精混合物时,MCC较大的粒径和润湿液体较低的表面张力导致湿态物料的内聚强度较低。在制丸过程中,通过聚结的团聚体生长以及通过颗粒重排使组分更紧密堆积都会受到限制。因此,会产生强度较弱、球形度较差、尺寸较小且尺寸分布较宽的丸粒。

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本文引用的文献

1
Influence of starting material particle size on pellet surface roughness.起始物料粒径对颗粒表面粗糙度的影响。
AAPS PharmSciTech. 2014 Feb;15(1):131-9. doi: 10.1208/s12249-013-0031-5. Epub 2013 Nov 6.
2
Importance of wet packability of component particles in pellet formation.组分颗粒的湿可压性在颗粒成型中的重要性。
AAPS PharmSciTech. 2013 Sep;14(3):1267-77. doi: 10.1208/s12249-013-0022-6. Epub 2013 Aug 17.

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