氯波必利 | 57645-91-7

• 物质功能分类: 分析化学 - 标准品 - 药典标准品和杂质标准品
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 氯波必利
• 中文别名: 氯波必利苹果酸盐；苹果酸克立波必利；氯波比利
• 英文名称: Cleprid
• 英文别名: malic acid clebopride；malic acid, compound with 4-amino-N-[1-(benzyl)piperidin-4-yl]-5-chloro-2-methoxybenzamide (1:1)；clebopride malate；N-<4-(1-Benzyl)piperidyl>-2-methoxy-4-amino-5-chlorbenzamid-malat；4-amino-N-(1-benzylpiperidin-4-yl)-5-chloro-2-methoxybenzamide;2-hydroxybutanedioic acid
• CAS: 57645-91-7
• 化学式: C₄H₆O₅*C₂₀H₂₄ClN₃O₂
• 分子量: 507.971
• InChiKey: NYNKCGWJPNZJMI-UHFFFAOYSA-N

物化性质

• 溶解度：
  微溶于水和甲醇，微溶于无水乙醇，几乎不溶于二氯甲烷。

计算性质

• 辛醇/水分配系数(LogP)：
  -0.52
• 重原子数：
  35
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  166
• 氢给体数：
  5
• 氢受体数：
  8

安全信息

• 危险性防范说明：
  P280,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335
• 储存条件：
  2-8℃

制备方法与用途

生物活性方面，Clebopride 是一种多巴胺拮抗剂，主要用于治疗功能性胃肠病引起的恶心和呕吐。

文献信息

• Clebopride transdermal patch
  申请人：WALTON S.A.

  公开号：EP0303445A1

  公开（公告）日：1989-02-15

  A transdermal patch having a drug reservoir layer on a backing sheet, the drug reservoir layer comprises an adhesive gel base containing clebopride or a pharmaceutically acceptable salt thereof, the adhesive gel base containing as essential components, a water-soluble polymer, water and a water-holding agent. The use of such a patch permits adequate concentrations of clebopride to be maintained in the blood over prolonged periods of time while avoiding the problems of multiple administrations of clebopride by conventional methods.

  一种贴剂，其具有药物储备层和背衬片，药物储备层包括含有克洛普胺或其药学上可接受的盐的粘合凝胶基质，该粘合凝胶基质包含水溶性聚合物、水和保水剂等基本成分。使用这样的贴剂可以在避免传统方法下多次给予克洛普胺的问题的同时，维持血液中足够的克洛普胺浓度。
• Remedies for depression containing ep1 antagonist as the active ingredient
  申请人：——

  公开号：US20040082653A1

  公开（公告）日：2004-04-29

  A pharmaceutical composition for the treatment and/or prevention of depression comprising a compound having an antagonistic activity for EP 1 receptor which a prostaglandin E 2 receptor subtype. EP 1 antagonist is useful for the treatment of depression, for example, endogenous depression, reactive depression, weatherability depression, neurological depressed state, the depressed state of brain organic mental disorder.

  一种用于治疗和/或预防抑郁症的药物组合物，包括一种具有EP1受体拮抗活性的化合物，该受体是前列腺素E2受体亚型。EP1拮抗剂对于治疗抑郁症很有用，例如内源性抑郁症，反应性抑郁症，耐受性抑郁症，神经学抑郁状态，脑器质性心境障碍的抑郁状态。
• CRYSTALLINE CONDITION DISLOCATING METHOD
  申请人：NIPPON SHINYAKU COMPANY, LIMITED

  公开号：EP0665009A1

  公开（公告）日：1995-08-02

  An object of this invention is to provide a method of dislocating the crystalline condition of crystalline medicine simply, speedily and homogeneously, and, moreover, in large quantities at once. This invention is directed to a method using an extruder when crystalline medicine in a certain crystalline condition (△ is dislocated to another crystalline condition (○), i.e., when the dislocation of crystalline condition (△->○) is carried out.

  本发明的目的是提供一种简单、快速和均匀地将结晶药物的结晶状态变位的方法，而且是一次性大量变位。本发明针对的是一种使用挤压机将某种结晶状态（△）的结晶药物变位到另一种结晶状态（○）的方法，即结晶状态（△->○）变位的方法。
• Adhesive base material
  申请人：KOWA CO. LTD.

  公开号：EP0735122A2

  公开（公告）日：1996-10-02

  An adhesive base material comprises a polymer obtained by polymerizing a glucosyloxy alkyl (meth)acrylate, a hydroxyalkyl (meth)acrylate, an alkyl (meth)acrylate and a polyfunctional monomer. This adhesive base material can be caused to swell uniformly because of its good swelling property and exhibits excellent adhesion to the skin so that it is useful as adhesive layers in plasters, various medical pads and also medicament-impregnated dermatologic medicines.

  一种粘合剂基底材料由一种聚合物组成，该聚合物通过聚合葡糖基氧基烷基（甲 基）丙烯酸酯、羟基烷基（甲基）丙烯酸酯、烷基（甲基）丙烯酸酯和多官能团单体而得。这种粘合剂基底材料具有良好的膨胀性，可使皮肤均匀膨胀，与皮肤的粘合力极佳，因此可用作膏药、各种医用垫和药物浸渍皮肤病药物的粘合层。
• DEVICE FOR IONTOPHORESIS
  申请人：Kowa Co., Ltd.

  公开号：EP1008365A1

  公开（公告）日：2000-06-14

  This invention relates to an iontophoretic device for the electrical percutaneous administration of a drug. As its features, a backing is provided with a power source, and a donor and a receptor are arranged on the same side of the backing with an insulating space region interposed therebetween, whereby the device has an integral structure. This iontophoretic device permits safe and efficient percutaneous absorption of a drug without increasing a current value and also features extremely good handling ease.

  本发明涉及一种经皮给药离子透入装置。其特点是，背衬上装有电源，供体和受体布置在背衬的同一侧，中间有一个绝缘空间区域，因此该装置具有整体结构。这种离子渗透装置可以在不增加电流值的情况下安全有效地经皮吸收药物，而且操作极为简便。