盐酸莫哌隆 | 3871-82-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 盐酸莫哌隆
• 英文名称: Methylperidol hydrochloride
• 英文别名: moperone hydrochloride；1-(4-fluoro-phenyl)-4-(4-hydroxy-4-p-tolyl-piperidino)-butan-1-one; hydrochloride；1-(4-Fluor-phenyl)-4-(4-hydroxy-4-p-tolyl-piperidino)-butan-1-on; Hydrochlorid；1-[3-(p-fluorobenzoyl)propyl]-4-hydroxy-4-(p-tolyl)piperidinium chloride；4-[4-(4-tolyl)-4-hydroxypiperidino]-4'-fluorobutyrophenone hydrochloride；1-(4-fluorophenyl)-4-[4-hydroxy-4-(4-methylphenyl)piperidin-1-yl]butan-1-one;hydron;chloride
• CAS: 3871-82-7
• 化学式: C₂₂H₂₆FNO₂*ClH
• 分子量: 391.913
• InChiKey: RJTOSFZZYBCYTM-UHFFFAOYSA-N

物化性质

• 熔点：
  216-218°

计算性质

• 辛醇/水分配系数(LogP)：
  -0.33
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  41.7
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Hydrogel-forming sustained-release preparation
  申请人：YAMANOUCHI PHARMACEUTICAL CO., LTD.

  公开号：US20030203024A1

  公开（公告）日：2003-10-30

  The invention provides a hydrogel-type sustained-release preparation comprising (1) at least one drug, (2) an additive which insures a penetration of water into the core of the preparation and (3) a hydrogel-forming polymer, wherein said preparation is capable of undergoing substantially complete gelation during its stay in the upper digestive tract such as stomach and small intestine and is capable of releasing the drug in the lower digestive tract including colon. By the preparation of the invention, the drug is efficiently released and absorbed even in the colon so that a steady and sustained release effect can be achieved.

  本发明提供了一种水凝胶型缓释制剂，包括（1）至少一种药物，（2）一种保证水分渗透进入制剂核心的添加剂，和（3）一种水凝胶形成聚合物，其中该制剂能够在上消化道（如胃和小肠）停留期间经历几乎完全的凝胶化，能够在下消化道（包括结肠）释放药物。通过本发明的制剂，药物能够高效地在结肠中释放和吸收，从而实现稳定和持续的缓释效果。
• Medicated plasters
  申请人：NITTO DENKO CORPORATION

  公开号：EP0387751A2

  公开（公告）日：1990-09-19

  Medicated plasters composed of a flexible support and a pressure-sensitive adhesive layer laminated thereon, in which said pressure-sensitive adhesive layer has an exposed surface with pH of 7 or higher and contains one of the following three components: (i) a basic physiologically active agent and an acidic substance, (ii) a salt of a basic physiologically active agent and a basic substance, and (iii) a basic physiolosically active agent and a salt of a basic physiolosically active agent.

  药用膏药，由柔性支架和层压在其上的压敏胶层组成，其中所述压敏胶层的外露表面 pH 值为 7 或更高，并含有以下三种成分之一： (i) 碱性生理活性剂和酸性物质、 (ii) 碱性生理活性剂和碱性物质的盐，以及 (iii) 碱性生理活性剂和碱性生理活性剂的盐。
• Process to prepare coated particles
  申请人：TAISHO PHARMACEUTICAL CO. LTD

  公开号：EP0413865A1

  公开（公告）日：1991-02-27

  A method of producing a fine coated pharmaceutical preparation comprises cooling fine liquid droplets composed of a liquid medium, a drug dissolved or suspended in the liquid medium, and as required, a binder, to a temperature not higher than the freezing point of the liquid medium to form frozen particles aof the drug and, as required, the binder; adjusting the particle sizes of the fine frozen particles; mixing the fine frozen particles with a fine powder of a coating material having a particle diameter less than said particles at a temperature above the freezing point of the liquid medium to cause the fine powder of the coating material to adhere to the surface of said particles; and then removing the liquid medium from the resulting coated particles.

  一种生产精细包衣药物制剂的方法，包括将由液体介质、溶解或悬浮在液体介质中的药物以及所需的粘合剂组成的细液滴冷却到不高于液体介质冰点的温度，以形成药物以及所需的粘合剂的冷冻颗粒；调整细冷冻颗粒的粒径；在高于液体介质冰点的温度下，将微冻颗粒与颗粒直径小于所述颗粒的包衣材料细粉混合，使包衣材料细粉附着在所述颗粒表面；然后从得到的包衣颗粒中去除液体介质。
• Adhesive device for transdermal administration of an active agent
  申请人：NITTO DENKO CORPORATION

  公开号：EP0452837A2

  公开（公告）日：1991-10-23

  A medical adhesive comprising a plaster layer containing the following ingredients, characterized in that the ingredient ② is incorporated in a larger amount than the ingredient ⑤ and in an amount not less than 25% by weight relative to the total amount of the ingredients ①∼⑤, and the plaster layer is a W/O type : ① a medicinal ingredient, ② a hydrophobic polymer having a glass transition temperature (Tg) of -65°C to 35°C, ③ a percutaneous absorption-promoting agent, ④ water, and ⑤ a hydrophilic polymer which is soluble or capable of swelling in water; and a medical adhesive which comprises a porous base layer in the plaster layer or in contact with the plaster layer, which enable stable release of the medicinal ingredient, the percutaneous absorption-promoting agents and so on and sustaining of the pharmacological effects over a long period.

  一种医用粘合剂，由含有下列成分的石膏层组成，其特征在于，成分②的掺入量大于成分⑤，且相对于成分①∼⑤的总掺入量不低于 25%（重量百分比），石膏层为 W/O 型： 药物成分、 一种疏水性聚合物，其玻璃转化温度（Tg）为-65°C 至 35°C、 经皮吸收促进剂、 水，以及 可溶于水或能在水中溶胀的亲水性聚合物；以及 一种医用粘合剂，由石膏层中的多孔基底层或与石膏层接触的多孔基底层组成，可使药物成分、促进经皮吸收剂等稳定释放，并长期保持药理作用。
• SUSTAINED-RELEASE HYDROGEL PREPARATION
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP0661045A1

  公开（公告）日：1995-07-05

  A sustained-release hydrogen preparation comprising at least one drug, an additive for making water penetrate into the preparation and a macromolecular substance which forms hydrogel. It can nearly completely gel when it stays in the upper parts of the digestive tract, i.e. the stomach and small intestine, and can release the drug in the lower part thereof, i.e. the colon. The preparation enables the drug to be well dissolved and absorbed even in the colon, thus achieving a stable sustained-release effect.

  一种缓释氢制剂，由至少一种药物、一种可使水渗入制剂的添加剂和一种可形成水凝胶的大分子物质组成。 它在消化道上部（即胃和小肠）停留时几乎可以完全凝胶化，在消化道下部（即结肠）可以释放药物。 这种制剂即使在结肠中也能使药物充分溶解和吸收，从而达到稳定的缓释效果。