4,5α-epoxy-17-methyl-3,6α-bis-nicotinoyloxy-morphin-7-ene; hydrochloride | 12040-41-4

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 吗啡烷
• 英文名称: 4,5α-epoxy-17-methyl-3,6α-bis-nicotinoyloxy-morphin-7-ene; hydrochloride
• 英文别名: 4,5α-Epoxy-17-methyl-3,6α-bis-nicotinoyloxy-morphin-7-en; Hydrochlorid；(5α,6α)-7,8-didehydro-4,5-epoxy-17-methylmorphinan-3,6-diyl bispyridine-3-carboxylate hydrochloride；[(4R,4aR,7S,7aR,12bS)-3-methyl-9-(pyridine-3-carbonyloxy)-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl] pyridine-3-carboxylate;hydron;chloride
• CAS: 12040-41-4
• 化学式: C₂₉H₂₅N₃O₅*ClH
• 分子量: 531.996
• InChiKey: LYSPLNOMQZTGCM-IOZAQTAYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.79
• 重原子数：
  38
• 可旋转键数：
  6
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  90.8
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• Pharmaceutical formulations for dry powder inhalers
  申请人：Vectura Limited

  公开号：EP1829533A2

  公开（公告）日：2007-09-05

  A powder for use in a dry powder inhaler comprises: i) a fraction of fine particle size constituted by a mixture of physiologically acceptable excipient and an additive; ii) a fraction of coarse particles; and iii) at least one active ingredient. The powder is suitable for efficacious delivery of active ingredients into the low respiratory tract of patients suffering from pulmonary diseases such as asthma. In particular, the invention provides a formulation to be administered as dry powder for inhalation which is freely flowable, can be produced in a simple way, is physically and chemically stable and capable of delivering accurate doses and/or high fine particle fraction of low strength active ingredients by using a high- or medium resistance device.

  一种用于干粉吸入器的粉末包括：i) 由生理上可接受的赋形剂和添加剂的混合物构成的细颗粒部分；ii) 粗颗粒部分；iii) 至少一种活性成分。这种粉末适用于向哮喘等肺部疾病患者的低呼吸道有效输送活性成分。特别是，本发明提供了一种可作为吸入用干粉给药的制剂，该制剂可自由流动，生产工艺简单，物理和化学性质稳定，能够通过使用高阻力或中等阻力装置输送精确剂量和/或高细颗粒部分的低强度活性成分。
• Pharmaceutical Formulations for Dry Powder Inhalers
  申请人：Vectura Limited

  公开号：EP2272508A2

  公开（公告）日：2011-01-12

  A powder for use in a dry powder inhaler comprises: i) a fraction of fine particle size constituted by a mixture of physiologically acceptable excipient and an additive; ii) a fraction of coarse particles; and iii) at least one active ingredient. The powder is suitable for efficacious delivery of active ingredients into the low respiratory tract of patients suffering from pulmonary diseases such as asthma. In particular, the invention provides a formulation to be administered as dry powder for inhalation which is freely flowable, can be produced in a simple way, is physically and chemically stable and capable of delivering accurate doses and/or high fine particle fraction of low strength active ingredients by using a high- or medium resistance device.

  一种用于干粉吸入器的粉末包括：i) 由生理上可接受的赋形剂和添加剂的混合物构成的细颗粒部分；ii) 粗颗粒部分；iii) 至少一种活性成分。这种粉末适用于向哮喘等肺部疾病患者的低呼吸道有效输送活性成分。特别是，本发明提供了一种可作为吸入用干粉给药的制剂，该制剂可自由流动，生产工艺简单，物理和化学性质稳定，能够通过使用高阻力或中等阻力装置输送精确剂量和/或高细颗粒部分的低强度活性成分。
• Method of making particles for use in a pharmaceutical composition
  申请人：Vectura Limited

  公开号：EP2266549A2

  公开（公告）日：2010-12-29

  A method for making composite excipient particles for use in a pharmaceutical composition comprises a milling step in which particles of an excipient material are milled in the presence of an additive material. The product particles are small in size and the milling requires relatively low input of time and energy. The composite particles arc suitable for use in inhalable pharmaceutical compositions.

  一种用于药物组合物的复合赋形剂颗粒的制造方法包括一个研磨步骤，在该步骤中，赋形剂材料的颗粒在添加剂材料的存在下被研磨。产品颗粒较小，研磨所需的时间和能量相对较少。这种复合颗粒弧形，适合用于可吸入药物组合物。
• Inhalable pharmaceutical compositions
  申请人：Bosch H. William

  公开号：US10022303B2

  公开（公告）日：2018-07-17

  Methods for making inhalable composite particles comprising a pharmaceutically-active agent, the method comprising: a) providing composite particles comprising a millable grinding matrix and a solid pharmaceutically-active agent, wherein the pharmaceutically-active agent has an median particle size on a volume average basis between 50 nm and 3 μm; and b) milling the composite particles in a mill without milling bodies for a time period sufficient to produce inhalable composite particles having a mass median aerodynamic diameter between 1 μm and 20 μm are described.

  描述了制造包含药用活性剂的可吸入复合颗粒的方法，该方法包括：a) 提供包含可研磨基质和固体药用活性剂的复合颗粒，其中药用活性剂的体积平均中值粒径在 50 nm 至 3 μm 之间；以及 b) 在不含研磨体的研磨机中研磨复合颗粒，研磨时间足以产生可吸入复合颗粒，该复合颗粒的质量中值空气动力学直径在 1 μm 至 20 μm 之间。
• FORMULATIONS FOR USE IN INHALER DEVICES
  申请人：Vectura Limited

  公开号：EP1276472B1

  公开（公告）日：2006-12-20