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深入了解挤出造球过程中制粒助剂的功能。

Insights into the functionality of pelletization aid in pelletization by extrusion-spheronization.

机构信息

GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, Singapore.

出版信息

Pharm Dev Technol. 2013 Feb;18(1):61-72. doi: 10.3109/10837450.2011.621210. Epub 2011 Oct 8.

DOI:10.3109/10837450.2011.621210
PMID:21981607
Abstract

This study investigated the particle sizes of pelletization aids from the different wet processing steps of extrusion-spheronization, and their influence on rheological and pellet properties. Three commercial microcrystalline cellulose (MCC) grades, three commercial cross-linked polyvinyl pyrrolidone (X-PVP) grades and two agglomerated X-PVP grades (prepared using roller compaction from two commercial fine particle size X-PVP grades) were used as pelletization aid. The pelletization aids were analyzed for their dry state particle size, individual particle size (sonicated powder dispersion in water) and in-process particle sizes (dispersions of processed materials from the different processing steps). No remarkable particle size changes were observed with the commercial X-PVP grades under the different conditions. The two fine X-PVP grades, but not the coarse grade, produced good quality pellets. MCC and agglomerated X-PVP grades exhibited spectacularly lower individual and in-process particle sizes, and produced good quality pellets although some of them had dry state particle sizes comparable to that of the commercial coarse X-PVP grade. In-process particle sizes of pelletization aids correlated strongly with the rheological and pellet properties of the pelletization aid:lactose (1:3) binary mixtures. These results demonstrated that small in-process particle size of pelletization aid is a critical requirement for successful pelletization by extrusion-spheronization.

摘要

本研究考察了挤出滚圆过程中不同湿法制粒步骤中制粒辅料的颗粒大小及其对流变学和颗粒性质的影响。使用了三种商业级微晶纤维素 (MCC)、三种商业交联聚维酮 (X-PVP) 和两种聚集体化 X-PVP 级(通过将两种商业细粒径 X-PVP 级压辊造粒制备)作为制粒辅料。对制粒辅料的干燥状态颗粒大小、单个颗粒大小(水中超声粉末分散体)和过程中颗粒大小(不同加工步骤中加工材料的分散体)进行了分析。在不同条件下,商业 X-PVP 级没有观察到明显的颗粒尺寸变化。两种细粒径 X-PVP 级,但不是粗粒径级,可制得质量良好的颗粒。MCC 和聚集体化 X-PVP 级的单个颗粒大小和过程中颗粒大小明显较小,尽管它们中的一些干燥状态颗粒大小与商业粗粒径 X-PVP 级相当,但仍可制得质量良好的颗粒。制粒辅料的过程中颗粒大小与制粒辅料的流变学和颗粒性质密切相关:乳糖(1:3)二元混合物。这些结果表明,制粒辅料的小粒径是挤出滚圆成功制粒的关键要求。

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引用本文的文献

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A Quality by Experimental Design Approach to Assess the Effect of Formulation and Process Variables on the Extrusion and Spheronization of Drug-Loaded Pellets Containing Polyplasdone® XL-10.一种采用实验设计方法评估制剂和工艺变量对含聚维酮XL - 10的载药微丸挤出和滚圆效果的质量研究
AAPS PharmSciTech. 2016 Apr;17(2):368-79. doi: 10.1208/s12249-015-0345-6. Epub 2015 Jul 14.
2
Moistening liquid-dependent de-aggregation of microcrystalline cellulose and its impact on pellet formation by extrusion-spheronization.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。
AAPS PharmSciTech. 2014 Jun;15(3):753-61. doi: 10.1208/s12249-014-0098-7. Epub 2014 Feb 20.
3
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.
4
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.