盐酸奥昔非君 | 16777-42-7

• 物质功能分类: 原料药 - 循环系统用药 - 防治心绞痛药
• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 盐酸奥昔非君
• 中文别名: 安心酮盐酸盐
• 英文名称: hydron;3-[[(1R,2S)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-(3-methoxyphenyl)propan-1-one;chloride
• CAS: 16777-42-7
• 化学式: C19H24ClNO3
• 分子量: 349.8
• InChiKey: JMUPNNYLJGSMPK-JPJJPTBZSA-N

物化性质

• 熔点：
  192-194℃

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  24
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  58.6
• 氢给体数：
  3
• 氢受体数：
  4

安全信息

• 海关编码：
  2922509090

文献信息

• Method for producing Microcapsule
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP0145240A2

  公开（公告）日：1985-06-19

  A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oit layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of said water-soluble drug.

  一种通过制备油包水型乳液生产的微胶囊，该乳液包括含有所述水溶性药物及其药物保持物质的水包水型内层和含有聚合物物质的油包油型外层，然后将所述水包水型内层增稠或固化至粘度不低于约 5000 厘泊，最后将所得乳液在水中干燥，从而延长所述水溶性药物的释放时间。
• Sustained release preparation
  申请人：TEIJIN LIMITED

  公开号：EP0187703A2

  公开（公告）日：1986-07-16

  A sustained release preparation comprising: (a) chitin, chitosan, or a mixture thereof (b) anionic polymer compounds such as those having a carboxyl group, a sulfonic acid group, or a group capable of providing the same, and (c) pharmaceutically active agents. This sustained release preparation can provide the desired sustained-release or dissolution of the pharmaceutically active agents in human organs irrespective of the acidity (i.e., pH conditions) therein.

  一种缓释制剂，包括：(a) 甲壳素、壳聚糖或它们的混合物；(b) 阴离子聚合物化合物，如具有羧基、磺酸基或能提供相同羧基、磺酸基的化合物；(c) 药物活性剂。 这种缓释制剂能在人体器官中提供所需的药物活性剂的缓释或溶解，而不受其中酸度（即 pH 值条件）的影响。
• Method for producing microcapsule
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP0190833A2

  公开（公告）日：1986-08-13

  Microcapsules are advantageously produced with a high take-up of a water-soluble drug by preparing a W/O emulsion composed of a water-soluble drug-containing solution as the inner aqueous phase and a polymer-containing solution as the oil phase, dispersing said emulsion in an aqueous phase and subjecting the resulting W/O/W emulsion to an in-water drying, wherein the viscosity of the W/0 emulsion used in preparing the W/O/W emulsion is adjusted to about 150 to about 10,000 centipoises.

  制备由水溶性药物溶液（作为内水相）和聚合物溶液（作为油相）组成的 W/O 乳化液，将所述乳液分散在水相中，然后将所得 W/O/W 乳化液进行水内干燥，就能生产出具有高水溶性药物吸收率的微胶囊，其中用于制备 W/O/W 乳化液的 W/0 乳化液的粘度调整为约 150 至约 10,000 厘泊。
• Polylactic acid type microspheres containing physiologically active substance and process for preparing the same
  申请人：Biomaterials Universe, Inc.

  公开号：EP0330180A1

  公开（公告）日：1989-08-30

  Microspheres comprising polylactic acid and a water soluble physiologically active substance and having a mean particle size of from about 0.01 µm to 300 µm, which show not more than 30 % of an eluted amount of said physio­logically active substance based on the content of said physiologically active substance in the polylactic acid type microspheres after 24 hours in in vitro elution test in phosphate buffer of pH 7.4 at 37°C, and a process for preparing the same. The polylactic acid type microspheres of this invention is advantageous in that the active substance can be uniformly incorporated into the micro­spheres without loss of the activity, can gradually release the active substance for a long time of period of more than one week.

  由聚乳酸和水溶性生理活性物质组成的微球，其平均粒径约为0.01微米至300微米，在37℃、pH值为7.4的磷酸盐缓冲液中进行体外洗脱试验24小时后，根据聚乳酸型微球中所述生理活性物质的含量，所述生理活性物质的洗脱量不超过30%，以及制备该微球的工艺。本发明的聚乳酸型微球的优点是活性物质可以均匀地掺入微球中而不损失活性，可以在一周以上的长时间内逐渐释放活性物质。
• Sustained release microcapsule for water soluble drug
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP0350246A2

  公开（公告）日：1990-01-10

  Sustained release microcapsules including a water soluble drug and an organic basic substance as a drug retaining substance of this invention not only have a high rate of incorporation (trapping rate), but also show little initial release so that they can be administered safely and bring about persistent, stable sustained release.

  本发明的缓释微胶囊包括水溶性药物和作为药物保留物质的有机碱性物质，不仅具有较高的掺入率（捕获率），而且初始释放量很小，因此可以安全给药，并带来持久、稳定的持续释放。