柠檬酸异米尼尔

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 柠檬酸异米尼尔
• 英文名称: 2-(carboxymethyl)-2,4-dihydroxy-4-oxobutanoate;(4-cyano-5-methyl-4-phenylhexan-2-yl)-dimethylazanium
• 化学式: C22H32N2O7
• 分子量: 436.5
• InChiKey: ZXASMEUEMIIBDZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  31
• 可旋转键数：
  10
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  159
• 氢给体数：
  4
• 氢受体数：
  9

文献信息

• COMPOSITION FOR HOT MELT EXTRUSION AND METHOD FOR PRODUCING HOT MELT EXTRUDATE BY USING SAME
  申请人：SHIN-ETSU CHEMICAL CO., LTD.

  公开号：US20160095928A1

  公开（公告）日：2016-04-07

  Provided is a composition for hot melt extrusion including a drug and hypromellose acetate succinate (HPMCAS) having a hydroxypropoxy molar substitution of 0.40 or more and a mole ratio of an acetyl group to a succinyl group of less than 1.6. Further, provided is a method for producing a hot melt extrudate including the step of hot melt-extruding a composition for hot melt extrusion including a drug and hypromellose acetate succinate having a molar hydroxypropoxy substitution of 0.40 or more and a mole ratio of an acetyl group to a succinyl group of less than 1.6, at a hot melt temperature of not lower than a melting temperature of the hypromellose acetate succinate or of not lower than a temperature at which both the hypromellose acetate succinate and the drug are melted.

  提供了一种用于热熔挤出的组合物，其中包括一种药物和羟丙基甲基纤维素醋酸琥珀酸酯（HPMCAS），其羟丙氧基摩尔取代度为0.40或更高，乙酰基与琥珀酰基的摩尔比小于1.6。此外，提供了一种制备热熔挤出物的方法，其中包括热熔挤出一种组合物，该组合物包括一种药物和羟丙基甲基纤维素醋酸琥珀酸酯，其羟丙氧基摩尔取代度为0.40或更高，乙酰基与琥珀酰基的摩尔比小于1.6，在不低于羟丙基甲基纤维素醋酸琥珀酸酯熔点或两者均熔化的温度下进行热熔挤出。
• SOLUTION FOR SPRAY DRYING COMPRISING HYPROMELLOSE ACETATE SUCCINATE AND METHOD FOR PRODUCING SOLID DISPERSION
  申请人：Shin-Etsu Chemical Co., Ltd.

  公开号：US20160136283A1

  公开（公告）日：2016-05-19

  There are provided a solution for spray drying having a high transmittance and markedly reduced generation of undissolved matter; and a method for producing a solid dispersion by using the solution for spray drying so that clogging with the undissolved matter is reduced and dissolution is improved. More specifically, there is provided a solution for spray drying comprising hypromellose acetate succinate (HPMCAS) having a hydroxypropoxy molar substitution of 0.40 or more, a solvent, and a drug. There is also provided a method for producing a solid dispersion comprising the step of removing the solvent from the spray drying solution.

  提供了一种具有高透过率和明显减少未溶物生成的喷雾干燥解决方案；以及通过使用该喷雾干燥解决方案制备固体分散物的方法，从而减少未溶物的堵塞并提高溶解度。更具体地，提供了一种喷雾干燥解决方案，包括羟丙甲纤维素醋酸琥珀酸酯（HPMCAS），其羟丙氧基摩尔取代度为0.40或更高，一种溶剂和一种药物。还提供了一种制备固体分散物的方法，其中包括从喷雾干燥溶液中去除溶剂的步骤。
• 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。
• CAPSULE
  申请人：NIPPON SHINYAKU COMPANY, LIMITED

  公开号：EP0580861A1

  公开（公告）日：1994-02-02

  A prolonged-action capsule excellent in adhesion, stability, etc., in the digestive tract. The capsule comprises a polymer excellent in initial adhesion and another polymer excellent in shape retention, both of which are dispersed in a liquid substance, and a physiologically active substance dispersed or dissolved in a liquid substance, and contains water in an amount of 2 % or less as a whole.

  一种在消化道中具有良好粘附性和稳定性的长效胶囊。该胶囊由一种初始粘附性极佳的聚合物和另一种形状保持性极佳的聚合物组成，这两种聚合物都分散在一种液体物质中，还包括一种分散或溶解在液体物质中的生理活性物质，其整体含水量不超过 2%。
• FAST SOLUBLE TABLET
  申请人：NIPPON SHINYAKU COMPANY, LIMITED

  公开号：EP0627218A1

  公开（公告）日：1994-12-07

  A tablet which dissolves rapidly in the oral cavity and can be prepared in a simple manner without resort to any special preparation technique. The tablet comprises a sugar alcohol or the like as the principal ingredient and is prepared by the wet granulation method wherein a kneaded mixture of the sugar alcohol or the like with a drug is compression molded before drying. This tablet can be prepared merely by modifying partly the conventional tableting method and has a sufficient physicochemical stability.

  一种片剂，可在口腔中快速溶解，制备方法简单，无需采用任何特殊制备技术。这种片剂的主要成分是糖醇或类似物，制备方法是湿法制粒，将糖醇或类似物与药物的揉捏混合物在干燥前压制成型。这种片剂只需部分改变传统的压片方法即可制备，并具有足够的理化稳定性。