(4R,4aR,7S,7aR,12bS)-3-methyl-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7,9-diol;4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol

• 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: (4R,4aR,7S,7aR,12bS)-3-methyl-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7,9-diol;4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol
• 化学式: C30H40N2O6
• 分子量: 524.6
• InChiKey: CMFFEBGVFQEIKT-VYKNHSEDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  38
• 可旋转键数：
  5
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  126
• 氢给体数：
  6
• 氢受体数：
  8

文献信息

• Oral pharmaceutical formulation in the form of aqueous suspension for modified release of active principle(s)
  申请人：Castan Catherine

  公开号：US10004693B2

  公开（公告）日：2018-06-26

  The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of active principle(s), excluding amoxicillin, said formulations consisting of suspensions of coated particles of active principles (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the active principle(s) according to a profile that does not change during the storage of the liquid suspension. To do this the inventors propose the selection of a specific coating composition for the microcapsules which consists of at least four components that allow these microcapsules to be stored in water without modifying their properties of modified release of the active principle, this liquid phase furthermore being saturated with active principle(s).

  本发明涉及活性成分（不包括阿莫西林）改变释放的口服液体药物制剂，所述制剂由活性成分包衣颗粒（微胶囊）悬浮液组成。根据本发明，构成悬浮液分散相的微胶囊的设计目的是使活性成分的释放曲线在液体悬浮液的储存过程中不会发生变化。为此，发明者建议为微胶囊选择一种特定的涂层组合物，该组合物至少由四种成分组成，可使这些微胶囊在水中储存而不改变其活性成分的改良释放特性，而且这种液相还饱含活性成分。
• FORMULATION PHARMACEUTIQUE ORALE SOUS FORME DE SUSPENSION AQUEUSE DE MICROCAPSULES PERMETTANT LA LIBERATION MODIFIEE DE PRINCIPE(S) ACTIF(S)
  申请人：Flamel Technologies

  公开号：EP1492511A2

  公开（公告）日：2005-01-05
• 活性成分の改変された放出のための、マイクロカプセルの水性懸濁液形態での経口医薬品製剤
  申请人：フラメル・テクノロジー

  公开号：JP4732696B2

  公开（公告）日：2005-09-15
• ORAL PHARMACEUTICAL FORMULATION IN THE FORM OF AQUEOUS SUSPENSION FOR MODIFIED RELEASE OF ACTIVE PRINCIPLE(S)
  申请人：Castan Catherine

  公开号：US20110117205A1

  公开（公告）日：2011-05-19

  The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of active principle(s), excluding amoxicillin, said formulations consisting of suspensions of coated particles of active principles (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the active principle(s) according to a profile that does not change during the storage of the liquid suspension. To do this the inventors propose the selection of a specific coating composition for the microcapsules which consists of at least four components that allow these microcapsules to be stored in water without modifying their properties of modified release of the active principle, this liquid phase furthermore being saturated with active principle(s).
• Oral pharmaceutical formulation in the form of an aqueous suspension of microcapsules for the modified release of active principle(s)
  申请人：FLAMEL IRELAND LIMITED

  公开号：US20150374635A1

  公开（公告）日：2015-12-31

  The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of active principle(s), excluding amoxicillin, said formulations consisting of suspensions of coated particles of active principles (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the active principle(s) according to a profile that does not change during the storage of the liquid suspension. To do this the inventors propose the selection of a specific coating composition for the microcapsules which consists of at least four components that allow these microcapsules to be stored in water without modifying their properties of modified release of the active principle, this liquid phase furthermore being saturated with active principle(s).