Pharmaceutical cocrystal and salts of norfloxacin
Pharmaceutical cocrystal and salts of norfloxacin
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DOI：
10.1021/cg060327x
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发表时间：
2006-12-06
影响因子：
3.8
通讯作者：
Velaga, Sitaram P.
中科院分区：
文献类型：
--
作者：
Basavoju, Srinivas;Bostrom, Dan;Velaga, Sitaram P.
本研究的目的是研究氟哌酸（一种难溶性抗菌药物）、其共晶和盐的结构和药物性质。使无水形式的诺氟沙星（形式A，1）结晶。它与异烟酰胺（2）共结晶，并与琥珀酸、丙二酸和马来酸（分别为3-5）制备有机盐。采用差示扫描量热法（DSC）、红外光谱（IR）、拉曼光谱（Raman）和粉末X射线衍射（PXRD）对这些相进行了表征。获得单晶X射线衍射数据，并求解晶体结构。测定了这些相的表观溶解度。在所有这些结构中存在稳健的O-H中心点O、O-H中心点O-、O-H中心点N、N-H中心点O-、N+- H中心点O-和N-H中心点N相互作用。这些结构中的喹诺酮部分与PI堆叠。π相互作用并形成通道以包括CHCl 3或H2O。本文报道了一种新的诺氟沙星共晶及其盐，其水溶性得到了改善。
The aim of this study was to investigate the structural and pharmaceutical properties of norfloxacin ( a poorly soluble antibacterial drug), its cocrystal, and salts. Norfloxacin in the anhydrous form ( form A, 1) was crystallized. It was cocrystallized with isonicotinamide ( 2), and organic salts were prepared with succinic acid, malonic acid, and maleic acid (3-5, respectively). These phases were characterized by differential scanning calorimetry (DSC), infrared (IR) and Raman spectroscopy, and powder X-ray diffraction (PXRD). Single-crystal X-ray diffraction data were obtained, and crystal structures were solved. The apparent solubility of these phases was determined. Robust O-H center dot center dot center dot O, O-H center dot center dot center dot O-, O-H center dot center dot center dot N, N-H center dot center dot center dot O, N+- H center dot center dot center dot O-, and N-H center dot center dot center dot N interactions were present in all these structures. Quinolone moieties in these structures stack with pi...pi interactions and form channels to include CHCl3 or H2O. Herein we report a new cocrystal and salts of norfloxacin with improved aqueous solubility.