...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Acta crystallographica. Section C, Structural chemistry. >Structure and physicochemical characterization of a naproxen-picolinamide cocrystal
【24h】

Structure and physicochemical characterization of a naproxen-picolinamide cocrystal

机译：萘普生 - 吡啶胺酰胺COCrystal的结构和物理化学特征

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Naproxen (NPX) is a nonsteroidal anti-inflammatory drug with pain- and fever-relieving properties, currently marketed in the sodium salt form to overcome solubility problems; however, alternative solutions for improving its solubility across all pH values are desirable. NPX is suitable for cocrystal formation, with hydrogen-bonding possibilities via the COOH group. The crystal structure is presented of a 1:1 cocrystal of NPX with picolinamide as a coformer [systematic name: (S)-2-(6-methoxynaphthalen-2-yl)propanoic acid-pyridine-2-carbox-amide (1/1), C_14H_14O_3?C_6H_6N_2O]. The pharmaceutically relevant physical properties were investigated and the intrinsic dissolution rate was found to be essentially the same as that of commercial naproxen. An NMR crystallography approach was used to investigate the H-atom positions in the two crystal-lographically unique COOH-CONH hydrogen-bonded dimers. 1H solid-state NMR distinguished the two carboxyl protons, despite the very similar crystallographic environments. The nature of the hydrogen bonding was confirmed by solid-state NMR and density functional theory calculations.
机译：萘普克森（NPX）是一种非甾体抗炎药，具有疼痛和发烧性能，目前以钠盐形式销售以克服溶解性问题;然而，期望改善所有pH值的溶解度的替代解决方案是理想的。 NPX适用于通过COOH基团的氢键合可能性。晶体结构的用吡啶胺作为共甲酰胺的1：1个COCRYSTAL [系统名称：（S）-2-（6-甲氧基萘-2-基）丙酸吡啶-2-羧酰胺（1 / 1），C_14H_14O_3？C_6H_6N_2O]。研究了药学上相关的物理性质，发现内在溶解速率与商业萘普伦基本相同。使用NMR晶体术方法来研究两个晶体型唯一独特的CoOH-Conh氢键二聚体中的H-原子位置。如图1H固态NMR区分了两种羧基质子，尽管是非常相似的晶体摄像环境。通过固态NMR和密度官能理论计算证实了氢键的性质。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号