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硬脂酸镁机械干法包衣对可塑变形微晶纤维素粉末流动性和可压缩性的影响。

The effect of mechanical dry coating with magnesium stearate on flowability and compactibility of plastically deforming microcrystalline cellulose powders.

机构信息

Division of Pharmaceutical Chemistry and Technology, 00014 University of Helsinki, P.O. Box 56, Helsinki, Finland.

Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3055, Australia.

出版信息

Int J Pharm. 2018 Feb 15;537(1-2):64-72. doi: 10.1016/j.ijpharm.2017.11.068. Epub 2017 Dec 1.

Abstract

Mechanofusion is a dry coating method that can be used to improve the flowability of cohesive powder by coating host particles with a lubricant, for example magnesium stearate (MgSt). It has been shown previously that fragmenting material can under some circumstances be mechanofused with MgSt without impairing compactibility of the powder and without reducing the dissolution rate of the resulting tablets. However, the effects on material with viscoelastic behaviour, known to be sensitive for the negative effects of MgSt, is not known. Therefore, mechanofusion of microcrystalline cellulose (MCC) with MgSt was investigated in this study. Four MCC grades were mechanofused with different MgSt concentrations and process parameters, and the resulting flowability and compactibility were studied. Starting materials and low-shear blended binary mixtures were studied as a reference. Mechanofusion improved the flow properties of small particle size MCC powders (d50 < 78 μm) substantially, but increasing the MgSt content consequently resulted in weaker tablets. Larger particle size MCC grades, however, fractured under the shear forces during the mechanofusion process and hence their flow properties were decreased. Improvement of the flow properties but also the negative effects on compactibility of small particle size grades were observed even at relatively mild mechanofusion parameters and low lubricant concentrations.

摘要

机械融合是一种干法涂层方法,可用于通过用润滑剂(例如硬脂酸镁 (MgSt))涂覆主颗粒来改善粘性粉末的流动性。先前已经表明,在某些情况下,可以将碎料与 MgSt 机械融合,而不会损害粉末的可压缩性,也不会降低所得片剂的溶解速率。然而,对于具有粘弹性行为的材料的影响,众所周知,MgSt 会产生负面影响,目前尚不清楚。因此,本研究考察了微晶纤维素 (MCC) 与 MgSt 的机械融合。用不同的 MgSt 浓度和工艺参数对四种 MCC 级分进行了机械融合,并研究了所得的流动性和可压缩性。以起始材料和低剪切混合的二元混合物作为参考进行了研究。机械融合大大改善了小粒径 MCC 粉末(d50<78μm)的流动性能,但随着 MgSt 含量的增加,片剂的强度降低。然而,较大粒径的 MCC 级分在机械融合过程中会在剪切力下断裂,因此其流动性能降低。即使在相对温和的机械融合参数和低润滑剂浓度下,也观察到了小粒径级分的流动性改善以及对可压缩性的负面影响。

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