Cyclopropanecarboxamide, N-(6-(4-((((1S)-2,2-dimethylcyclopropyl)carbonyl)amino)phenoxy)-3-pyridinyl)-2,2-dimethyl-, (1S)- | 318967-58-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: Cyclopropanecarboxamide, N-(6-(4-((((1S)-2,2-dimethylcyclopropyl)carbonyl)amino)phenoxy)-3-pyridinyl)-2,2-dimethyl-, (1S)-
• 英文别名: (1S)-N-[4-[5-[[(1S)-2,2-dimethylcyclopropanecarbonyl]amino]pyridin-2-yl]oxyphenyl]-2,2-dimethylcyclopropane-1-carboxamide
• CAS: 318967-58-7
• 化学式: C₂₃H₂₇N₃O₃
• 分子量: 393.5
• InChiKey: GABIPKHJFWRJQJ-QZTJIDSGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  80.3
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Pharmaceutical preparations having an improved solubility
  申请人：Makino Chisato

  公开号：US20060140991A1

  公开（公告）日：2006-06-29

  The present invention provides a method for producing a pharmaceutical preparation having an improved solubility, which comprises the steps of forming a micelle by dissolving a poorly-soluble drug having the ability to form the micelle into water; and fixing the micelle structure which is formed with the poorly-soluble drug, by using a compound(s) which fixes the micelle structure. This production method preferably further comprises the step of adjusting the pH back to neutral and/or cooling down the temperature to room temperature after fixing the micelle structure. The poorly-soluble drug which is the subject of the above method is such as those forming a micelle in water only when heated and/or in the presence of an acid(s) or alkali(s). According to this production method, it can produce a pharmaceutical preparation having an improved solubility, which makes possible to accomplish the improvement of oral absorbability of a poorly-soluble drug(s).

  本发明提供了一种提高溶解度的药物制剂的生产方法，该方法包括以下步骤：将具有形成胶束能力的难溶性药物溶解到水中，形成胶束；使用固定胶束结构的化合物，固定与难溶性药物形成的胶束结构。这种生产方法最好还包括在固定胶束结构后将 pH 值调回到中性和/或将温度降到室温的步骤。上述方法所涉及的难溶性药物是指只有在加热和/或有酸或碱存在时才能在水中形成胶束的药物。根据这种生产方法，可以生产出溶解度得到改善的药物制剂，从而有可能实现改善难溶性药物的口服吸收性。