吡考拉唑 | 78090-11-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 中文名称: 吡考拉唑
• 中文别名: 匹果亚砜
• 英文名称: Picoprazole
• 英文别名: methyl 6-methyl-2-[(3-methylpyridin-2-yl)methylsulfinyl]-1H-benzimidazole-5-carboxylate
• CAS: 78090-11-6
• 化学式: C₁₇H₁₇N₃O₃S
• 分子量: 343.4
• InChiKey: ASSMECARUIRCML-UHFFFAOYSA-N

物化性质

• 溶解度：
  溶于二甲基亚砜

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  24
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  104
• 氢给体数：
  1
• 氢受体数：
  6

制备方法与用途

生物活性

Picoprazole 是一种特异性的 H+/K+-ATPase 抑制剂，IC50 值为 3.1±0.4 μM。

靶点

• IC50: 3.1±0.4 μM (H+ /K+-ATPase)

体外研究

Picoprazole 可以浓度依赖性地抑制 H+/K+-ATPase 活性。其 IC50 值为 3.1±0.4 μM，表明 Picoprazole 是一种特异性 H+/K+-ATPase 抑制剂，并与酶的 100-kDa 多肽结合。实验结果显示，Picoprazole 浓度依赖性地抑制了 Cu2+ -o-phenanthroline 引起的 Cl− 导致的开放，这表明 Cl− 导致的部分功能是 H+/K+-ATPase 的一部分。

此外，对 Histamine 和 dbcAMP 刺激下 14C-aminopyrine 积累 (H+ 分泌) 进行了研究。结果发现，在分离和富集的猪壁细胞中，三种苯并咪唑衍生物 Timoprazole、Picoprazole 和 Omeprazole 都能够浓度依赖性地抑制 H+ 分泌，其 IC50 值分别为 8.5±1.9 μM、3.9±0.7 μM 和 0.13±0.03 μM。

文献信息

• Process for the preparation of organic compounds containing a sulfinyl or sulfonyl group
  申请人：DINAMITE DIPHARMA S.P.A. abbreviated DIPHARMA S.P.A.

  公开号：US20040192929A1

  公开（公告）日：2004-09-30

  A process for the oxidation of thioethers to sulfoxides or sulfones or for the oxidation of sulfoxides to sulfones by treatment of thioethers or sulfoxides with an oxidizing amount of &egr;-phthalimidoperhexanoic acid is particularly useful for the preparation of compounds of industrial interest, in particular pharmaceuticals for human or veterinary use.

  一种将硫醚氧化为亚砜或砜，或将亚砜氧化为砜的过程，通过用适量的ε-邻苯二甲酰亚丙基己酸处理硫醚或亚砜，特别适用于制备工业感兴趣的化合物，特别是用于人类或兽医用途的药物。
• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• EFFICIENT PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE (S)-BINOL COMPLEX
  申请人：F.I.S. - Fabbrica Italiana Sintetici S.p.A.

  公开号：US20160244428A1

  公开（公告）日：2016-08-25

  Object of the present invention is an improved process for the preparation of Esomeprazole (S)-BINOL complex which is a key intermediate for the synthesis of Esomeprazole and salts thereof.

  本发明的目标是提供一种改进的制备埃索美拉唑(S)-BINOL复合物的方法，该复合物是合成埃索美拉唑及其盐的关键中间体。
• Method and compositions for treating gastric hyperacidity while diminishing the likelihood of producing vitamin deficiency
  申请人：——

  公开号：US20040185119A1

  公开（公告）日：2004-09-23

  A method for treatment of a human for gastric hyperacidity while diminishing the likelihood of producing vitamin deficiency is disclosed, the method comprising administering a therapeutically effective amount of one or more substances that neutralize or otherwise reduce gastric acid and administering an effective supplemental amount of one or more vitamins, wherein one of the one or more vitamins can be free Vitamin B 12 . Oral dosage formulations comprising a therapeutically effective amount of one or more substances that neutralize or otherwise reduce gastric acid and an effective supplemental amount of one or more vitamins, and methods of making such oral dosage forms, also are disclosed.

  本发明公开了一种治疗人类胃酸过多并减少产生维生素缺乏可能性的方法，该方法包括：给予治疗有效量的一种或多种中和或其他减少胃酸的物质，以及给予有效补充量的一种或多种维生素，其中其中一种或多种维生素可以是自由维生素B12。本发明还公开了口服剂型，包括治疗有效量的一种或多种中和或其他减少胃酸的物质和有效补充量的一种或多种维生素，并公开了制备这种口服剂型的方法。
• Oral Medicament Based on a Proton Pump Inhibitor
  申请人：CAISSE Philippe

  公开号：US20100068291A1

  公开（公告）日：2010-03-18

  The invention relates to oral medicaments having a modified release of proton pump inhibitors (PPI's) that are, in particular, useful in preventing and treating gastrointestinal disorders. The aim of the invention is to provide a novel oral medicament based on PPI's ideally having all or some of the following characteristics: a) quickly providing relief to the patient by increasing the gastric pH after oral administration of the medicament; b) accelerating the recovery of patients while maintaining this increase in the gastric pH for as long as possible after oral administration of the medicament and, in particular, during the night; c) improving the observance of the treatment and the comfort of the patient by taking the medicament once daily. To this end, the microcapsules of the invention, preferably non-enteric, are constituted of PPI microparticles coated with ethyl cellulose, an ammonio methacrylate copolymer (Eudragit® RL 100), polyvinylpyrrolidone, castor oil and polyoxyethylenated hydrogenated castor oil ( 40 ). This medicament is designed so that after its ingestion for a once daily administration, it makes it possible to maintain, from the first day of treatment onward, an average gastric pH, between 0 and 24 h, of greater than or equal to the average gastric pH between 0 and 24 h obtained by an enteric oral medicament having a reference* immediate release, administered under the same conditions. The invention also relates to these microcapsules per se.

  本发明涉及一种具有质子泵抑制剂（PPI）改良释放的口服药物，特别适用于预防和治疗胃肠道疾病。本发明的目的是提供一种基于PPI的新型口服药物，最好具有以下所有或部分特征：a）通过口服药物后快速增加胃pH，迅速缓解患者症状；b）在口服药物后尽可能长时间地维持胃pH的增加，特别是在夜间加速患者恢复；c）通过每日一次服用药物，提高治疗的依从性和患者的舒适度。为此，本发明的微囊，最好是非肠溶性的，由覆盖乙基纤维素、氨甲基丙烯酸酯共聚物（Eudragit® RL 100）、聚乙烯吡咯烷酮、蓖麻油和聚氧乙烯化氢化蓖麻油（40）的PPI微粒组成。该药物的设计是，每日一次服用后，从治疗的第一天开始，使平均胃pH在0至24小时之间大于或等于在相同条件下口服肠溶性口服药物具有参考*即时释放的0至24小时平均胃pH。本发明还涉及这些微囊本身。