去丙基罗替戈汀 | 153409-14-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 中文名称: 去丙基罗替戈汀
• 英文名称: (S)-6-((2-(Thiophen-2-yl)ethyl)amino)-5,6,7,8-tetrahydronaphthalen-1-ol
• 英文别名: (6S)-6-(2-thiophen-2-ylethylamino)-5,6,7,8-tetrahydronaphthalen-1-ol
• CAS: 153409-14-4
• 化学式: C₁₆H₁₉NOS
• 分子量: 273.4
• InChiKey: RDMWWGLKUMLLTG-ZDUSSCGKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  60.5
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• ROTIGOTINE-CONTAINING TRANSDERMAL ABSORPTION PREPARATION WITH IMPROVED STABILITY
  申请人：SK Chemicals Co., Ltd.

  公开号：EP3146980A1

  公开（公告）日：2017-03-29

  The present invention relates to a method for preventing the precipitation of rotigotine crystals in a transdermal absorption preparation containing rotigotine as an active ingredient and, more specifically, to a method for preparing a transdermal absorption preparation, comprising a step of mixing rotigotine and an antioxidant at a weight ratio of 1:0.0001 to 0.1, and to a transdermal therapeutic system, comprising: a drug-containing adhesive layer containing the transdermal absorption preparation prepared by the method, and rotigotine and an antioxidant at a weight ratio of 1:0.0001 to 0.1; and a substrate for supporting the drug-containing adhesive layer. The method and system of the present invention suppress the crystallization of rotigotine as well as the generation of related substances, thereby increasing the long-term storage stability, and thus the present invention can be effectively applied to the preparation of a rotigotine-containing patching agent or the like.

  本发明涉及一种防止含有罗替戈汀作为活性成分的透皮吸收制剂中罗替戈汀晶体析出的方法，更具体地说，涉及一种制备透皮吸收制剂的方法，包括将罗替戈汀和抗氧化剂按重量比1:0.0001至0.1的混合步骤；以及一种透皮治疗系统，包括：含药粘合剂层，其中含有通过该方法制备的透皮吸收制剂，以及重量比为1:0.0001至0.1的罗替戈汀和抗氧化剂；以及用于支撑含药粘合剂层的基底。本发明的方法和系统抑制了罗替戈汀的结晶以及相关物质的生成，从而提高了长期储存稳定性，因此本发明可以有效地应用于制备含罗替戈汀的贴敷剂等。
• TRANSDERMAL THERAPEUTIC SYSTEM FOR TREATING PARKINSONISM
  申请人：Muller Walter

  公开号：US20080050424A1

  公开（公告）日：2008-02-28

  A transdermal therapeutic system (TTS) comprises a silicone-based polymer adhesive system having distributed therein (−)-5,6,7,8-tetrahydro-6-[propyl-[2-(2-thienyl)ethyl]amino]-1-naphthalenol free base in an amount of about 5% to 40% by weight. The adhesive system comprises a silicone adhesive and an additive having increased solubility for the active substance, in an amount effective to increase dissolving capacity of the matrix for the active substance.
• Rotigotine-Containing transdermal absorption preparation with improved stability
  申请人：SK Chemicals Co., Ltd.

  公开号：US20170128413A1

  公开（公告）日：2017-05-11

  A method for preparing a transdermal absorption composition includes mixing rotigotine and an antioxidant at a weight ratio of 1:0.0001 to 0.1. A transdermal therapeutic system includes a substrate and a drug-containing adhesive layer disposed on the substrate and including an antioxidant at a weight ratio of 1:0.0001 to 0.1. The method and system of the present invention suppress the crystallization of rotigotine as well as the generation of related substances, thereby increasing the long-term storage stability of a therapeutic product containing rotigotine or related substances.
• US7413747B2
  申请人：——

  公开号：US7413747B2

  公开（公告）日：2008-08-19
• US9877948B2
  申请人：——

  公开号：US9877948B2

  公开（公告）日：2018-01-30