(S)-[(2R,4S,5R)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-(6-methoxyquinolin-4-yl)methanol;nitric acid | 58748-01-9

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 金鸡纳生物碱
• 英文名称: (S)-[(2R,4S,5R)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-(6-methoxyquinolin-4-yl)methanol;nitric acid
• CAS: 58748-01-9
• 化学式: C20H25N3O5
• 分子量: 387.4
• InChiKey: LBFABFQISWGYMB-VJAUXQICSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.83
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  112
• 氢给体数：
  2
• 氢受体数：
  7

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。
• 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。
• STABLE MEDICINAL COMPOSITIONS FOR ORAL USE
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP1205190A1

  公开（公告）日：2002-05-15

  The present invention is to provide a stable pharmaceutical composition for oral use and preparation thereof in which changes are prevented in drug release during storage even under the exposure to light, by adding yellow ferric oxide and/or red ferric oxide in a matrix type sustained-release preparation containing a drug, a hydrophilic base, and polyethylene oxide. The present invention is to further provide a method for preventing changes in drug release during storage under the exposure to light in a matrix type sustained-release preparation containing a drug, a hydrophilic base, and polyethylene oxide. The quality assurance period of the product can be prolonged and the product value can be improved by the present invention.

  本发明旨在提供一种稳定的口服药物组合物及其制备方法，通过在含有药物、亲水性基质和聚氧化乙烯的基质型缓释制剂中添加黄色氧化铁和/或红色氧化铁，即使在光照下也能防止药物释放在储存过程中发生变化。本发明进一步提供一种方法，用于防止含有药物、亲水性基质和聚氧化乙烯的基质型缓释制剂在光照下储存期间药物释放量发生变化。通过本发明可以延长产品的质量保证期，提高产品价值。
• TIME-RELEASE COATED SOLID COMPOSITIONS FOR ORAL ADMINISTRATION
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP1275381A1

  公开（公告）日：2003-01-15

  The present invention relates to a timed-release compression-coated said composition for oral administration, said composition being a hydrgel-forming compression-coated solid preparation comprising a core tablet comprising a drug and an outer layer comprising a hydrogel-forming polymer substance and a hydrophilic base, characterized in that (1) said core tablet comprising a drug and a freely erodible filler, (2) said core tablet is capable of approximately 40 to approximately 90% erosion; and (3) said outer layer substantially does not comprise the same drug with said drug. By releasing a drug after a specific lag time, it becomes possible to effectively deliver a drug to a specific site in the digestive tract. It is therefore useful as presented as a timed-release solid composition for oral administration of a drug that is to be effectively delivered in high concentrations to the afflicted site in the lower digestive tract, a drug that is to be effectively absorbed in the lower digestive tract, a drug that is effective for chronopharmacotherapy, etc.

  本发明涉及一种用于口服的定时释放压缩包衣所述组合物，所述组合物是一种水凝胶形成的压缩包衣固体制剂，包括由药物组成的核心片剂和由水凝胶形成的聚合物物质和亲水性基质组成的外层，其特征在于：(1)所述核心片剂包括药物和可自由侵蚀的填料；(2)所述核心片剂能够被侵蚀约40%至约90%；以及(3)所述外层基本上不包括与所述药物相同的药物。通过在特定滞后时间后释放药物，可以有效地将药物输送到消化道的特定部位。因此，它可以作为一种定时释放固体组合物，用于将高浓度的药物有效地输送到下消化道中的患病部位、在下消化道中有效吸收的药物、对慢性药物治疗有效的药物等的口服给药。
• PHARMACEUTICAL COMPOSITION IMPROVED IN PERORAL ABSORBABILITY
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP1302201A1

  公开（公告）日：2003-04-16

  The present invention presents a pharmaceutical composition for oral use with improved absorption, which comprises drug, aminoalkyl methacrylate copolymer E, and acidic substance, wherein said 3 components are brought together and at least this polymer and this acidic substance are uniformly mixed, and a method of improving oral absorption by using this pharmaceutical composition. Moreover, the present invention presents an agent for improving oral absorption that increases drug permeability of the digestive tract mucous membrane and/or mucous layer present on the surface of this membrane, whose active ingredient is aminoalkyl methacrylate copolymer E. In addition, the present invention presents an oral agent for improving absorption by increasing drug permeability of the digestive tract mucous membrane and/or the mucous layer distributed over this mucous membrane, whose effective component is aminoalkyl methacrylate copolymer E.

  本发明提出了一种可改善吸收的口服用药物组合物，该组合物由药物、甲基丙烯酸氨基烷基酯共聚物E和酸性物质组成，其中将上述3种成分汇集在一起，并至少将这种聚合物和这种酸性物质均匀混合，还提出了一种通过使用这种药物组合物来改善口服吸收的方法。此外，本发明提出了一种通过增加消化道粘膜和/或分布在该粘膜表面的粘膜层的药物渗透性来改善口服吸收的药剂，其有效成分为甲基丙烯酸氨基烷基酯共聚物 E。