1-(9H-Carbazol-4-yloxy)-3-[2-(2-ethoxy-phenoxy)-ethylamino]-propan-2-ol | 72956-15-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 1-(9H-Carbazol-4-yloxy)-3-[2-(2-ethoxy-phenoxy)-ethylamino]-propan-2-ol
• 英文别名: 1-(9H-carbazol-4-yloxy)-3-[2-(2-ethoxyphenoxy)ethylamino]propan-2-ol
• CAS: 72956-15-1
• 化学式: C₂₅H₂₈N₂O₄
• 分子量: 420.508
• InChiKey: FZVBQKVJGVQXEI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  31
• 可旋转键数：
  11
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  75.7
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• Parenteral sustained-release delivery of carvedilol disperse systems
  申请人：ASCENDIA PHARMACEUTICALS, LLC

  公开号：US10792244B2

  公开（公告）日：2020-10-06

  Carvedilol parenteral sustained release systems by IV infusion, injection, or subcutaneous routes are disclosed. Preparation of carvedilol disperse systems such as liposomes, biodegradable microparticles or nanoparticles, and polymeric microparticles or nanoparticles have been presented in the present invention. Compositions containing carvedilol encapsulated in liposomes showed higher bioavailability and lower clearance rate than that of the free solution after intravenous administration. In vitro release of those liposomes in buffer solutions shows drug extended release over 48 hours, and correspondingly the in vivo animal data shows that parenteral administration of carvedilol encapsulated in liposomal materials has sustained release PK profile.

  本发明公开了通过静脉输注、注射或皮下注射途径的卡维地洛肠道外缓释系统。本发明提出了卡维地洛分散系统的制备方法，如脂质体、生物可降解微颗粒或纳米颗粒以及聚合物微颗粒或纳米颗粒。与游离溶液相比，脂质体包裹的卡维地洛组合物在静脉注射后显示出更高的生物利用度和更低的清除率。这些脂质体在缓冲溶液中的体外释放显示药物可延长释放 48 小时，相应的体内动物数据显示，经脂质体材料封装的卡维地洛肠外给药具有持续释放 PK 曲线。
• PARENTERAL SUSTAINED-RELEASE DELIVERY OF CARVEDILOL DISPERSE SYSTEMS
  申请人：Ascendia Pharmaceuticals, LLC

  公开号：EP3468539A1

  公开（公告）日：2019-04-17
• [EN] PARENTERAL SUSTAINED-RELEASE DELIVERY OF CARVEDILOL DISPERSE SYSTEMS<br/>[FR] ADMINISTRATION À LIBÉRATION PROLONGÉE PAR VOIE PARENTÉRALE DE SYSTÈMES DE DISPERSION DE CARVÉDILOL
  申请人：ASCENDIA PHARMACEUTICALS LLC

  公开号：WO2017218576A1

  公开（公告）日：2017-12-21

  Carvedilol parenteral sustained release systems by IV infusion, injection, or subcutaneous routes are disclosed. Preparation of carvedilol disperse systems such as liposomes, biodegradable microparticles or nanparticles, and polymeric microparticles or nanparticles have been presented in the present invention. Compositions containing carvedilol encapsulated in liposomes showed higher bioavailability and lower clearance rate than that of the free solution after intravenous administration. In vitro release of those liposomes in buffer solutions shows drug extended release over 48 hours, and correspondingly the in vivo animal data shows that parenteral administration of carvedilol encapsulated in liposomal materials has sustained release PK profile.