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以水和异丙醇为制粒剂制备微晶纤维素颗粒并对其进行表征,并用热学和流变学工具确定其终点。

To prepare and characterize microcrystalline cellulose granules using water and isopropyl alcohol as granulating agents and determine its end-point by thermal and rheological tools.

作者信息

Chaudhari Smruti P, Dave Rutesh H

机构信息

Division of Pharmaceutical Sciences, Arnold & Marie Schwartz College of Pharmacy and Health Sciences, Long Island University , Brooklyn, NY , USA.

出版信息

Drug Dev Ind Pharm. 2015 May;41(5):744-52. doi: 10.3109/03639045.2014.900080. Epub 2014 Mar 24.

DOI:10.3109/03639045.2014.900080
PMID:24654935
Abstract

Microcrystalline cellulose (MCC-102) is one of the most commonly used excipient in the pharmaceutical industry. For this research purpose, authors have developed a different technique to determine the end point for MCC-102 using water and isopropyl alcohol 70% (IPA) as granulating agent. Wet and dry granules obtained were characterized for their flow properties using the powder rheometer and thermal analysis. Powder rheometer was used to measure basic flowability energy (BFE), specific energy (SE), percentage compressibility, permeability and aeration. Thermal analysis includes effusivity and differential scanning calorimetry (DSC) measurements. BFE and SE results showed water granules requires high energy as compared to IPA granules. Permeability and compressibility results suggest IPA forms more porous granules and have better compressibility as compared to water granules. Hardness data reveals interesting phenomena in which as the amount of water increases, hardness decreases and vice-versa for IPA. Optimal granules were obtained in the range of 45-55% w/w. DSC data supported the formation of optimal granules. Empirical measurements like angle of repose did not reveal any significant differences between powder flow among various granules. In this paper, with the help of thermal effusivity and powder rheology we were able to differentiate between various powder flows and determine the optimal range for granule formation.

摘要

微晶纤维素(MCC - 102)是制药行业最常用的辅料之一。出于本研究目的,作者开发了一种不同的技术,以水和70%异丙醇(IPA)作为制粒剂来确定MCC - 102的终点。使用粉末流变仪和热分析对所得的湿颗粒和干颗粒的流动性质进行表征。粉末流变仪用于测量基本流动性能量(BFE)、比能(SE)、压缩率百分比、渗透率和通气性。热分析包括热扩散系数和差示扫描量热法(DSC)测量。BFE和SE结果表明,与IPA颗粒相比,水颗粒需要更高的能量。渗透率和压缩性结果表明,与水颗粒相比,IPA形成的颗粒孔隙更多,压缩性更好。硬度数据揭示了有趣的现象,即随着水量增加,硬度降低,而对于IPA则相反。在45 - 55% w/w范围内获得了最佳颗粒。DSC数据支持了最佳颗粒的形成。休止角等经验测量结果并未显示出各种颗粒之间粉末流动性有任何显著差异。在本文中,借助热扩散系数和粉末流变学,我们能够区分各种粉末流动情况并确定颗粒形成的最佳范围。

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