Characterization of Synthesized and Commercial Forms of Magnesium Stearate Using Differential Scanning Calorimetry, Thermogravimetric Analysis, Powder X-Ray Diffraction, and Solid-State NMR Spectroscopy
Characterization of Synthesized and Commercial Forms of Magnesium Stearate Using Differential Scanning Calorimetry, Thermogravimetric Analysis, Powder X-Ray Diffraction, and Solid-State NMR Spectroscopy
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DOI：
10.1016/j.xphs.2016.10.004
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发表时间：
2017-01-01
影响因子：
3.8
通讯作者：
Munson, Eric J.
中科院分区：
文献类型：
--
作者：
Delaney, Sean P.;Nethercott, Matthew J.;Munson, Eric J.
硬脂酸镁是脂肪酸的复杂混合物的盐，其中大多数是硬脂酸盐和棕榈酸盐。它具有多种结晶形式，并且可能是无定形形式。硬脂酸镁在制药工业中用作粉末润滑剂，通常在生产过程中以低水平（类似于1%）添加，并混合相对较短的时间（类似于5分钟）。需要适当的水平和混合时间，因为太短的混合时间或太小的量将导致不适当的润滑，并且太多会对溶解速率产生负面影响。硬脂酸镁中多种脂肪酸和晶型的复杂混合物导致商业来源之间的可变性，并且来源之间的切换可以影响适当润滑所需的润滑剂量和混合时间。为了更好地了解硬脂酸镁的复杂性质，使用各种分析技术来表征合成和商业硬脂酸镁样品。结果表明，差示扫描量热法，热重分析，固态NMR光谱和其他技术之间的相关性提供了一个独特的洞察硬脂酸镁的形式。最后，显示了使用固态NMR光谱法监测完整片剂中硬脂酸镁的形态变化的能力。(C)2016年美国药学协会（R）。爱思唯尔公司出版All rights reserved.
Magnesium stearate is the salt of a complex mixture of fatty acids, with the majority being stearate and palmitate. It has multiple crystalline forms and, potentially, an amorphous form. Magnesium stearate is used in the pharmaceutical manufacturing industry as a powder lubricant, and typically is added at low levels (similar to 1%) during the manufacturing process and blended for a relatively short time (similar to 5 min). Proper levels and mixing times are needed, as too short a mixing time or too small a quantity will result in improper lubrication, and too much can negatively impact dissolution rates. The complex mixture of multiple fatty acids and crystalline forms in magnesium stearate leads to variability between commercial sources, and switching between sources can impact both the amount of lubricant and mixing time needed for proper lubrication. In order to better understand the complex nature of magnesium stearate, a variety of analytical techniques were used to characterize both synthesized and commercial magnesium stearate samples. The results show that correlation among differential scanning calorimetry, thermogravimetric analysis, solid-state NMR spectroscopy, and other techniques provides a unique insight into the forms of magnesium stearate. Finally, the ability to monitor form changes of magnesium stearate in an intact tablet using solid-state NMR spectroscopy is shown. (C) 2016 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.