Investigation of inclusion complex of cilnidipine with hydroxypropyl-β-cyclodextrin
Investigation of inclusion complex of cilnidipine with hydroxypropyl-β-cyclodextrin
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DOI：
10.1016/j.carbpol.2012.07.057
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发表时间：
2012-11-06
影响因子：
11.2
通讯作者：
Hu, Qiaofeng
中科院分区：
文献类型：
--
作者：
Hu, Liandong;Zhang, Hailei;Hu, Qiaofeng
本研究的目的是通过与羟丙基-β-环糊精（HP-β-CD 或 HP-β-CD）络合来提高西尼地平的水溶性和光稳定性。通过紫外可见 (UV/VIS) 光谱、差示扫描量热法 (DSC) 表征西尼地平和 HP-β-CD 的相互作用。粉末 X 射线衍射 (PXRD)。傅里叶变换红外 (FT-IR) 光谱和 H-1 核磁共振 (H-1 NMR) 光谱验证了西尼地平-HP-β-CD 络合物包合物的形成。此外，还通过 H-1 NMR 光谱分析追踪了 HP-β-CD 结构中的结合位点。所有表征信息均证明了西尼地平-HP-β-CD包合物的形成，结果证明了该包合物在溶出速率和光稳定性方面的优越性：此外，在HP-β-CD存在下，西尼地平的表观溶解度增加了10,000倍以上。稳定常数 (1:1) 被发现为 50,116 M-1。表明药物进入 HP-β-CD 腔的倾向很高。这些结果表明西尼地平-HP-β-CD 包合物是设计药物应用新型制剂的有效新方法。 (C) 2012 Elsevier Ltd. 保留所有权利。
The objective of this study was to improve the water-solubility and photostability of cilnidipine by complexing it with hydroxypropyl-beta-cyclodextrin (HP-beta-CD or HP-beta-CD). The interactions of cilnidipine and HP-beta-CD were characterized by ultra violet-visible (UV/VIS) spectroscopy, differential scanning calorimetry (DSC). powder X-ray diffraction (PXRD). Fourier transformation-infrared (FT-IR) spectroscopy and H-1 nuclear magnetic resonance (H-1 NMR) spectroscopy to verify the formation of cilnidipine-HP-beta-CD complex inclusion. Moreover, the binding sites in the HP-beta-CD structure were also tracked through H-1 NMR spectroscopy analysis. All the characterization information proved the formation of cilnidipine-HP-beta-CD inclusion complex, and the results demonstrated the superiority of the inclusion complex in dissolution rates and photostability: in addition, the apparent solubility of cilnidipine was increased more than 10,000-fold in the presence of HP-beta-CD. The stability constant (1:1) was found to be 50,116 M-1. suggesting a high tendency of the drug to enter the HP-beta-CD cavity. These results identified the cilnidipine-HP-beta-CD inclusion complex as an effective new approach to design a novel formulation for pharmaceutical application. (C) 2012 Elsevier Ltd. All rights reserved.