公开(公告)号：US20220096512A1

公开(公告)日：2022-03-31

申请号：US17426946

申请日：2020-01-31

申请人： Sigma-Aldrich Co. LLC

发明人： Aviran Amir ,  Tamar Dvash ,  Michal Levin-Khalifa

IPC分类号： A61K31/7048 ,  A61K47/18 ,  A61K9/19

摘要： Water-based antifungal composition having improved bioavailability; such formulations include a polyene macrolide antifungal agent, such as nystatin, a surfactant, a buffer, an organic amine base; and water. Also provided are methods for preparing water-based antifungal compositions.

公开(公告)号：US20220096511A1

公开(公告)日：2022-03-31

申请号：US17426934

申请日：2020-01-31

申请人： Sigma-Aldrich Co. LLC

发明人： Aviran Amir ,  Tamar Dvash ,  Michal Levin-Khalifa ,  Theo Ackermann

IPC分类号： A61K31/7048 ,  C07H17/08 ,  A61P31/10

摘要： Methods for preparing a polyene macrolide antifungal with improved aqueous solubility. The method involves providing a polyene macrolide antifungal having a carboxylic acid group; activating the carboxylic acid group; introducing a primary amine to the activated polyene macrolide antifungal; reacting for a time sufficient to convert the carboxylic acid to an amide, and quenching the reaction, thus yielding a polyene macrolide amide or salt thereof. Also provided are water-soluble polyene macrolide derivatives.