hydron;N-(2-piperidin-1-ylethyl)-N-(pyridin-2-ylmethyl)aniline;chloride

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: hydron;N-(2-piperidin-1-ylethyl)-N-(pyridin-2-ylmethyl)aniline;chloride
• 化学式: C19H26ClN3
• 分子量: 331.9
• InChiKey: MSVZUEGLXXVUJS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.0
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  19.4
• 氢给体数：
  1
• 氢受体数：
  3

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。
• 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。
• Prolonged release preparation and polymers thereof
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP0481732A1

  公开（公告）日：1992-04-22

  1. A polymer for a prolonged release preparation which comprises (A) a polylactic acid and (B) a copolymer of glycolic acid and a hydroxycarboxylic acid of general formula wherein R stands for an alkyl group having 2 to 8 carbons, and wherein the weight ratio of (A) and (B) is in the range of 10/90 to 90/10. The drug is released at a constant rate from the preparation over the total release period without a large burst at the initial stage. Furthermore, the drug release period of the preparation can be freely controlled by varying the blending ratio of (A) and (B).

  1.一种用于长效缓释制剂的聚合物，包括 (A) 聚乳酸和 (B) 甘醇酸与通式为 通式如下的羟基羧酸共聚物 其中 R 代表具有 2 至 8 个碳原子的烷基，(A)和(B)的重量比在 10/90 至 90/10 之间。在整个释放期内，药物以恒定的速度从制剂中释放出来，而不会在初始阶段出现大量迸发。 此外，制剂的药物释放期可以通过改变（A）和（B）的混合比例来自由控制。