2-[4-[3-(2-Chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethyl acetate;hydrochloride | 146-28-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 英文名称: 2-[4-[3-(2-Chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethyl acetate;hydrochloride
• CAS: 146-28-1
• 化学式: C23H29Cl2N3O2S
• 分子量: 482.5
• InChiKey: UVZCSDSYVKDPQP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.94
• 重原子数：
  31
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  61.3
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• Burn matrix, method of its preparation and delivery device comprising said matrix
  申请人：Key Pharmaceuticals, Inc.

  公开号：EP0040862A1

  公开（公告）日：1981-12-02

  This invention provides a burn matrix comprising glycerol, polyvinylalcohol, a water-soluble polymer having hydration sites which in combination with the remaining ingredients yields a matrix capable of sustained release of a drug dispersed therein, and water. The matrix may further include a drug for topical or transdermal application to a patient. The invention also provides a method of making the matrix and a delivery device incorporating the matrix. The matrix may be used in the form of a package, which comprises the matrix (14) embedded in a backing member (10) provided with a detachable cover layer (12). Before use, the cover layer is removed, and the backing member applied to the patient by means of a pressure-sensitive adhesive layer (26), so that the matrix (14) is held against the skin of the patient.

  本发明提供了一种烧伤基质，包括甘油、聚乙烯醇、一种具有水合位点的水溶性聚合物，该聚合物与其余成分结合可产生一种能够持续释放分散在其中的药物的基质，以及水。基质可进一步包括一种药物，供患者局部或透皮使用。本发明还提供了基质的制造方法和含有基质的给药装置。基质可以包装的形式使用，包装包括嵌入基质（14）的背衬件（10），背衬件上有可拆卸的覆盖层（12）。使用前，取下覆盖层，通过压敏胶层（26）将背衬件贴在患者身上，使基质（14）紧贴患者皮肤。
• Pharmaceutical compositions
  申请人：Bristol-Myers Company

  公开号：EP0056973A1

  公开（公告）日：1982-08-04

  Enhanced antiulcer activity is obtained in warm-blooded animals by the concomitant administration of the histamine H2-receptor antagonist, etintidine, and the pepsin complexing agent, pepstatin. Concomitant administration of the two entities reduces the amount of etintidine necessary for effective treatment, thereby decreasing its side effect liability.

  同时服用组胺 H2 受体拮抗剂依替丁和胃蛋白酶络合剂培司他丁可增强温血动物的抗溃疡活性。 同时服用这两种药物可减少有效治疗所需的依替丁用量，从而降低其副作用。
• Compositions comprising pepstatin and an histamine H2-receptor antagonist having an enhanced antiulcer activity
  申请人：Bristol-Myers Company

  公开号：EP0099122A2

  公开（公告）日：1984-01-25

  Enhanced antiulcer activity is obtained in warm-blooded animals by the concomitant administration of the pepsin complexing agent, pepstatin, and an histamine H2-receptor antagonist of the formula wherein A, m, Z, n, R1 and R2 are as defined herein. Concomitant administration of the two entities reduces the amount of histamine H2-receptor antagonist necessary for treatment, thereby decreasing its side-effect liability.

  在温血动物中，同时服用胃蛋白酶络合剂胃舒平和组胺 H2 受体拮抗剂，可增强抗溃疡活性。 其中 A、m、Z、n、R1 和 R2 如本文所定义。同时使用这两种物质可减少治疗所需的组胺 H2 受体拮抗剂的用量，从而降低其副作用。
• Transdermal delivery system
  申请人：Euroceltique S.A.

  公开号：EP0208395A1

  公开（公告）日：1987-01-14

  A transdermal delivery system (1,11) for the transdermal administration of a drug has (a) a backing (2,12) that is substantially impermeable to the drug, (b) a matrix (3,13), adjacent to a surface of the backing, the matrix containing a gel comprising a hydrophilic fluid, a fluid gelling agent and the drug, and (c) a perforated sheet (4,14), adjacent to the matrix, that allows passage of the drug containing gel through its perforations. Preferably the system also has a contact adhesive layer (5,15) and a protecting layer (6,16). The long term adhesion of the delivery system to a patient may be effected by forming a channel (17), surrounding the matrix, in the perforated sheet/contact adhesive layer lamina. The channel inhibits the lateral movement of the drug containing gel. Furthermore, by forming a weak seal (18) in the matrix surrounding channel, the loss of a volatile drug from the gel may also be prevented.

  用于透皮给药的透皮给药系统（1,11）具有以下特点 (a) 背衬（2,12），基本上不透药、 (b) 基质（3,13），紧邻背衬表面，基质含有凝胶，凝胶由亲水性流体、流体胶凝剂和药物组成，以及 (c) 与基质相邻的穿孔片（4,14），允许含有药物的凝胶通过其穿孔。 该系统最好还有一个接触粘合层（5,15）和一个保护层（6,16）。 通过在穿孔片/接触粘合层薄层中形成围绕基质的通道（17），可实现给药系统与患者的长期粘合。该通道可抑制含药凝胶的横向移动。此外，通过在通道周围的基质中形成弱密封（18），还可以防止凝胶中挥发性药物的流失。
• A novel transdermal pharmaceutical absorption dosage unit
  申请人：Rutgers, The State University of New Jersey

  公开号：EP0196769A2

  公开（公告）日：1986-10-08

  A novel transdermal pharmaceutical polymer matrix dosage unit is provided which comprises a backing layer, an adjoining layer of a solid polymer matrix in which the pharmaceutical is microdispersed and a final biologically acceptable adhesive polymer layer which has dispersed therein a skin permeation enhancer.

  本发明提供了一种新型透皮药用聚合物基质剂量装置，它包括一个背衬层、一个相邻的固体聚合物基质层（其中微量分散了药物）和一个最终的生物可接受的粘合聚合物层（其中分散了皮肤渗透增强剂）。