• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Crystal growth & design >Lenalidomide-Gallic Acid Cocrystals with Constant High Solubility
【24h】

Lenalidomide-Gallic Acid Cocrystals with Constant High Solubility

机译：具有恒定高溶解度的来那度胺-苹果酸共晶体

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

Pharmaceutical cocrystals are an efficient approach to improve the solubility of insoluble active pharmaceutical ingredients (APIs), while the dissolution profiles of pharmaceutical cocrystals usually exhibit a type of "spring and rapid parachute" effect that influences stability and pharmacodynamic sustainability, in which the high apparent solubility induced by the formation of cocrystals can only be maintained for a short time (usually minutes) in the metastable zone and then decreases rapidly afterwards. Herein we reported the preparation and structures of two lenalidomide cocrystals with gallic acid (1, 2). After the formation of cocrystals, the intrinsic dissolution rate and apparent solubility of lenalidomide were found to be enhanced. The high solubility of cocrystals can keep for 48 h without dropping. The result of phase solubility study indicates gallic acid (GA) forms a 1:1 complex with lenalidomide (Rev) in aqueous solution, with a stability constant of 1713.2 L/mol. The multiple hydrogen bonding interactions between GA and Rev are attributed to the formation of GA-Rev complex in aqueous solution and subsequently the constant high solubility of cocrystals.
机译：药物共晶体是提高不溶性活性药物成分（API）溶解度的有效方法，而药物共晶体的溶出度通常表现出一种“弹簧和快速降落伞”效应，影响稳定性和药效学可持续性，其中高表观由共晶形成引起的溶解度只能在亚稳区内保持一小段时间（通常为数分钟），然后迅速降低。在这里，我们报道了来那度胺与没食子酸的共晶体的制备和结构（1、2）。共晶形成后，来那度胺的固有溶解速率和表观溶解度被发现提高。共晶体的高溶解度可以保持48小时而不滴落。相溶解度研究的结果表明，没食子酸（GA）与来那度胺（Rev）在水溶液中形成1：1的络合物，稳定常数为1713.2 L / mol。 GA和Rev之间的多个氢键相互作用归因于在水溶液中GA-Rev络合物的形成以及随后共晶体的恒定的高溶解度。

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