6-amino-2-[[1-(carboxymethyl)-2-oxo-4,5-dihydro-3H-1-benzazepin-3-yl]amino]hexanoic acid | 109214-55-3

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 6-amino-2-[[1-(carboxymethyl)-2-oxo-4,5-dihydro-3H-1-benzazepin-3-yl]amino]hexanoic acid
• CAS: 109214-55-3
• 化学式: C₁₈H₂₅N₃O₅
• 分子量: 363.4
• InChiKey: AXTCRUUITQKBAV-UHFFFAOYSA-N

物化性质

• 沸点：
  692.9±55.0 °C(Predicted)
• 密度：
  1.33±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -3.9
• 重原子数：
  26
• 可旋转键数：
  9
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  133
• 氢给体数：
  4
• 氢受体数：
  7

文献信息

• Benutzer-aktivierte Therapeutische Systeme
  申请人：CIBA-GEIGY AG

  公开号：EP0273004A2

  公开（公告）日：1988-06-29

  Die Erfindung betrifft ein therapeutisches System für die trans­dermale oder topische Applikation enthaltend eine geschlossene und für die Bestandteile der Wirkstofformulierung undurchlässige Deckschicht (11); ein Wirkstoffreservoir (2), ein Reservoir (3) mit einem Aktivierungsmittel, eine für die Komponenten des Wirkstoffreservoirs und des Reservoirs mit dem Aktivierungsmittel undurchlässige Trennschicht (4) und eine abziehbare Schutzschicht (9ʹ). Die undurchlässige Trennschicht wird durch Einwirken des Benutzers zum Bersten ge­bracht, wobei das Aktivierungsmittel auf die Komponenten des Wirkstoffreservoirs einwirkt und dabei die Wirkstoffabgabe startet oder die Abgabegeschwindigkeit beschleunigt.

  本发明涉及一种用于透皮或局部应用的治疗系统，该系统包括一个封闭的覆盖层(11)，该覆盖层对活性成分配方的组分是不渗透的；一个活性成分贮存器(2)，一个装有激活剂的贮存器(3)，一个对活性成分贮存器和装有激活剂的贮存器的组分是不渗透的分离层(4)，以及一个可剥离的保护层(9ʹ)。在使用者的作用下，不透水的隔离层会破裂，从而使活化剂作用于活性成分储藏室的成分，从而开始释放活性成分或加快释放速度。
• Transdermal administration of zwitterionic drugs
  申请人：CIBA-GEIGY AG

  公开号：EP0439430A2

  公开（公告）日：1991-07-31

  Transdermal therapeutic systems containing zwitterionic drugs and methods of administering zwitterions transdermally are disclosed. The systems comprise a zwitterionic drug in a salt form and a solvent therefor.

  本发明公开了含有齐聚物药物的透皮治疗系统和透皮施用齐聚物的方法。这些系统包括盐形式的齐聚物药物及其溶剂。
• Modular transdermal delivery system and associated methods of manufacture and use
  申请人：International Bioceutical Co. LLC

  公开号：US11052055B2

  公开（公告）日：2021-07-06

  A modular transdermal drug delivery system is provided, the system including: an upper module in which an outer backing layer is laminated to a pressure-sensitive adhesive layer that is covered by a removable release liner prior to assembly; and a lower module with a porous drug reservoir layer laminated to a skin-contact adhesive that affixes the system to the skin during drug delivery, where the skin-contact adhesive is, in one embodiment, an adhesive layer that is substantially co-extensive with the porous drug reservoir layer and, prior to use, protected with a second removable release liner. Methods of manufacture and use are also provided, as is an assembled transdermal drug delivery system fabricated by affixing the pressure-sensitive adhesive layer of the upper module to the porous drug reservoir layer of the lower module.

  本发明提供了一种模块化透皮给药系统，该系统包括：上部模块，其中外部背衬层与压敏粘合层层压在一起，该层在组装前由可移除的释放衬垫覆盖；以及下部模块，其中多孔储药层与皮肤接触粘合剂层压在一起，该皮肤接触粘合剂在一个实施例中是与多孔储药层基本共存的粘合层，在使用前由第二层可移除的释放衬垫保护。此外，还提供了制造和使用方法，以及通过将上部模块的压敏胶层粘贴到下部模块的多孔储药层上而制造的组装式透皮给药系统。
• MODULAR TRANSDERMAL DELIVERY SYSTEM AND ASSOCIATED METHODS OF MANUFACTURE AND USE
  申请人：International Bioceutical Co. LLC

  公开号：US20180296498A1

  公开（公告）日：2018-10-18

  A modular transdermal drug delivery system is provided, the system including: an upper module in which an outer backing layer is laminated to a pressure-sensitive adhesive layer that is covered by a removable release liner prior to assembly; and a lower module with a porous drug reservoir layer laminated to a skin-contact adhesive that affixes the system to the skin during drug delivery, where the skin-contact adhesive is, in one embodiment, an adhesive layer that is substantially co-extensive with the porous drug reservoir layer and, prior to use, protected with a second removable release liner. Methods of manufacture and use are also provided, as is an assembled transdermal drug delivery system fabricated by affixing the pressure-sensitive adhesive layer of the upper module to the porous drug reservoir layer of the lower module.
• Modular Transdermal Delivery Systems for the Treatment of Insomnia and Anxiety
  申请人：International Bioceutical Co. LLC

  公开号：US20180311181A1

  公开（公告）日：2018-11-01

  Modular transdermal delivery system components are provided that are assembled to provide a modular transdermal drug delivery system for the administration of a pharmacologically active agent for treating insomnia, anxiety, or both insomnia and anxiety. The components include: an upper module with an outer backing layer, a pressure-sensitive adhesive (PSA) layer laminated thereto, and a removable release liner; and at least two lower modules with a porous drug reservoir layer capable of adhering to the PSA layer of the upper module and loaded with a pharmaceutical formulation containing an effective amount of the pharmacologically active agent, with a skin-contact adhesive affixed to the drug reservoir layer. The lower modules differ from each other in at least one respect, e.g., with respect to thickness, drug reservoir volume, active agent, or dosage, such that prior to use the upper module any lower module can be selected and assembled with the upper module to provide a laminated transdermal delivery system. Related systems and methods of manufacture and use are also provided.