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首页> 外文期刊>Journal of Pharmaceutical Analysis >Physicochemical characterization, the Hirshfeld surface, and biological evaluation of two meloxicam compounding pharmacy samples
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Physicochemical characterization, the Hirshfeld surface, and biological evaluation of two meloxicam compounding pharmacy samples

机译：两种美洛昔康复合药房样品的理化特性，Hirshfeld表面和生物学评估

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Meloxicam (MLX) is an anti-inflammatory drug susceptible to variations and crystalline transitions. In compounding pharmacies, the complete crystallographic evaluation of the raw material is not a routine procedure. We performed a complete crystallographic characterization of aleatory raw MLX samples from compounding pharmacies. X-ray diffraction indicated the presence of two crystalline forms in one sample. DSC experiments suggested that crystallization, or a crystal transition, occurred differently between samples. The FTIR and 1 H NMR spectra showed characteristic assignments. 13 C solid-state NMR spectroscopy indicated the presence of more than one phase in a sample from pharmacy B. The Hirshfeld surface analysis, with electrostatic potential projection, allowed complete assignment of the UV spectra in ethanol solution. The polymorph I of meloxicam was more active than polymorph III in an experimental model of acute inflammation in mice. Our results highlighted the need for complete crystallographic characterization and the separation of freely used raw materials in compounding pharmacies, as a routine procedure, to ensure the desired dose/effect. Highlights ? Characterization of meloxicam polymorphs I and III. ? Biological activity evaluation. ? Hirshfeld surface analysis explains experimentally observed solubility differences. ? Meloxicam form I was more effective than form III. ? Adequate quality control based on crystallographic characterization required for raw materials.
机译：美洛昔康（MLX）是一种抗炎药，易于变异和结晶转变。在复合药房中，原料的完整晶体学评估不是常规程序。我们对来自复合药房的偶然原始MLX样品进行了完整的晶体学表征。 X射线衍射表明在一个样品中存在两种结晶形式。 DSC实验表明，样品之间的结晶或晶体转变不同。 FTIR和1 H NMR光谱显示出特征分配。 13 C固态NMR光谱表明，来自药房B的样品中存在多于一个相。具有静电势投射功能的Hirshfeld表面分析可以完全分配乙醇溶液中的UV光谱。在小鼠急性炎症的实验模型中，美洛昔康的多晶型物I比多晶型物III更具活性。我们的结果强调，常规过程需要对完整的晶体学特征进行表征，并在复合药房中分离免费使用的原料，以确保所需的剂量/效果。强调 ？美洛昔康多晶型物I和III的表征。 ？生物活性评估。 ？ Hirshfeld表面分析解释了实验观察到的溶解度差异。 ？ I型美洛昔康比III型更有效。 ？基于原材料所需的结晶学特征的充分质量控制。

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