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低浓度活性成分(普萘洛尔案例)固体药物形式的¹³C交叉极化魔角旋转核磁共振分析

¹³C cross-polarization magic-angle spinning nuclear magnetic resonance analysis of the solid drug forms with low concentration of an active ingredient-propranolol case.

作者信息

Pisklak Dariusz Maciej, Zielińska-Pisklak Monika, Szeleszczuk Lukasz, Wawer Iwona

机构信息

Faculty of Pharmacy, Medical University of Warsaw, Department of Physical Chemistry, Banacha 1, 02-093 Warsaw, Poland.

Faculty of Pharmacy, Medical University of Warsaw, Department of Inorganic and Analytical Chemistry, Banacha 1, 02-093 Warsaw, Poland.

出版信息

J Pharm Biomed Anal. 2014 May;93:68-72. doi: 10.1016/j.jpba.2013.06.031. Epub 2013 Jul 5.

Abstract

Solid State NMR is a method that could be widely used for analyzing solid state forms of drugs in their original formulations. However, when the concentration of the active pharmaceutical ingredient (API) in the final drug form is low, (13)C CP MAS NMR methods using standard parameters are not efficient. An example of this situation is propranolol, an important drug from the group of beta-blockers whose concentration in the final drug form is low (below 10%). Basing on the differences in the CP kinetics and relaxation parameters for propranolol and the excipients the authors suggest the proper set of the CP MAS experimental parameters that would allow one to analyze API even in small concentrations in the solid drug formulations.

摘要

固态核磁共振是一种可广泛用于分析原始制剂中药物固态形式的方法。然而,当最终药物形式中活性药物成分(API)的浓度较低时,使用标准参数的(13)C交叉极化魔角旋转核磁共振方法效率不高。这种情况的一个例子是普萘洛尔,它是β受体阻滞剂类中的一种重要药物,其在最终药物形式中的浓度较低(低于10%)。基于普萘洛尔和辅料在交叉极化动力学和弛豫参数方面的差异,作者提出了一套合适的交叉极化魔角旋转实验参数,即使在固体药物制剂中API浓度较低时也能对其进行分析。

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