阿洛拉胺盐酸盐 | 5107-01-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 阿洛拉胺盐酸盐
• 英文名称: 4-chloro-N-[2-(diethylamino)ethyl]-2-prop-2-enoxybenzamide;hydron;chloride
• CAS: 5107-01-7
• 化学式: C16H24Cl2N2O2
• 分子量: 347.3
• InChiKey: QEWLHSNMEXFSCI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  22
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  41.6
• 氢给体数：
  2
• 氢受体数：
  3

制备方法与用途

类别：有毒物品

• 毒性分级：高毒
• 急性毒性：
  • 皮下—小鼠 LD50: 155 毫克/公斤
  • 口服—小鼠 LD50: 275 毫克/公斤

可燃性危险特性：

• 可燃，燃烧时产生有毒氮氧化物和氯化氢烟雾

储运特性：

• 库房通风、低温干燥保存
• 与食品原料分开存放

灭火剂：

• 干粉、泡沫、砂土、二氧化碳，以及雾状水

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。
• Percutaneous absorption accelerator for ionic water-soluble medicine
  申请人：SHOWA DENKO KABUSHIKI KAISHA

  公开号：EP0189861A2

  公开（公告）日：1986-08-06

  A percutaneous absorption accelerator for ionic water-soluble medicines comprising at least one member selected from the group consisting of ionic oil-soluble substances and their salts, amphoteric surfactants, and nonionic substances. These substances can effectively and efficiently accelerate the desired percutaneous absorption of ionic water-soluble medicines.

  一种用于离子型水溶性药物的经皮吸收促进剂，由至少一种选自离子型油溶性物质及其盐类、两性表面活性剂和非离子型物质的成员组成。这些物质可以有效和高效地加速离子水溶性药物的预期经皮吸收。
• 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。
• 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。