布洛芬精氨酸 | 57469-82-6

• 物质功能分类: 生物化工 - 氨基酸及其衍生物 - 精氨酸类衍生物
• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 苯丙酸
• 中文名称: 布洛芬精氨酸
• 英文名称: ibuprofen L-arginine salt
• 英文别名: ibuprofen arginine；ibuprofen L-arginate；Ibuprofen arginate；L-arginine salt of 2-(4-isobutyl-phenyl)-propionic acid；Spedifen；[(4S)-4-amino-4-carboxybutyl]-(diaminomethylidene)azanium;2-[4-(2-methylpropyl)phenyl]propanoate
• CAS: 57469-82-6
• 化学式: C₆H₁₄N₄O₂*C₁₃H₁₈O₂
• 分子量: 380.487
• InChiKey: GCCOJNYCFNSJII-VWMHFEHESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.73
• 重原子数：
  27
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  165
• 氢给体数：
  5
• 氢受体数：
  6

安全信息

• 海关编码：
  2925290090
• 储存条件：
  存储条件：2-8°C，密封保存，并确保干燥。

文献信息

• Aryl (Ethanoic) Propanoic Acid Ascorbyl Ester, Preparation Method Thereof And Medicament Containing The Same
  申请人：Tang Luhong

  公开号：US20120115897A1

  公开（公告）日：2012-05-10

  The present invention designs and synthesizes the ascorbyl ester derivatives of the aryl (ethanoic) propanoic acid non-steroidal anti-inflammatory medicaments, such as ibuprofen, ketoprofen and naproxen, and addition salt of the derivatives with pharmaceutical acid or pharmaceutical alkaline. The non-steroidal anti-inflammatory medicament which takes the ibuprofen as the representative is a common antipyretic analgesic medicament. The invention has remarkable antipyretic and analgesic effects and good safety except for anti-inflammatory effect, thus being not only suitable for adults, but also suitable for the elderly people, infants and children. The aryl (ethanoic) propanoic acid ascorbyl ester can be converted into ascorbyl ester derivatives and the addition salts of the derivatives with pharmaceutical acid or pharmaceutical alkaline, which can improve the water solubility thereof, facilitate intravenously administration, reduce the onset time, improve the bioavailability, reduce the stimulation effect to gastrointestinal tract, and enhance the penetrating capacity to hemato encephalic barrier, and can be used as a novel medicament to be applied for antiphlogistic, antipyresis, analgesia, treatment of arthritis, dysmenorrheal, multiple sclerosis, pneumonia cystic fibrosis and patent ductus arteriosus of premature infants, and prevention and treatment of cerebral apoplexy, hypoxic-ischemic brain damage, senile dementia and certain cancers.

  本发明设计并合成了芳基（乙酸）丙酸非甾体抗炎药物，例如布洛芬、酮洛芬和萘普生的抗坏血酸酯衍生物，以及这些衍生物与药用酸或药用碱的加成盐。以布洛芬为代表的非甾体抗炎药是一种常见的解热镇痛药。本发明除了具有抗炎效果外，还具有显著的解热和镇痛效果，安全性良好，因此不仅适用于成人，也适用于老年人、婴幼儿。芳基（乙酸）丙酸抗坏血酸酯可转化为抗坏血酸酯衍生物以及这些衍生物与药用酸或药用碱的加成盐，这可以提高其水溶性，便于静脉给药，减少起效时间，提高生物利用度，减少对胃肠道的刺激作用，增强穿透血脑屏障的能力，并可作为新型药物应用于消炎、解热、镇痛、治疗关节炎、痛经、多发性硬化症、肺炎、囊性纤维化和早产儿动脉导管未闭，以及预防和治疗脑卒中、缺氧缺血性脑损伤、老年痴呆症和某些癌症。
• Rapidly solubilizing ibuprofen granulate
  申请人：Losan Pharma GmbH

  公开号：EP1800667A1

  公开（公告）日：2007-06-27

  A process for producing a rapidly solubilizing ibuprofen granulate, the process comprising providing a mixture comprising solid ibuprofen and at least 0.8 mole per mole ibuprofen of one or more basic compounds, which basic compounds comprise from 0.5 to 1.2 mole per mole ibuprofen, but not more, of a base selected from the group consisting of sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, sodium glycinate, potassium glycinate, tribasic sodium and potassium phosphates and mixtures of said bases, and reacting the ibuprofen and said one or more basic compounds in the presence of not more free water than the quantity exceeding the amount of water required for forming solid hydrates in said granulate by more than 1 mole per mole of ibuprofen. The obtainable granulate and the pharmaceutical compositions and dosage forms that may be produced therefrom are distinguished by their high solubility and rapid disintegration and dissolution in aqueous media, by their good flow properties and compressibility, by rapidly achieving onset of analgesic effect, etc.

  一种制备快速溶解布洛芬颗粒的方法，该方法包括提供一种混合物，该混合物包括固态布洛芬和至少0.8摩尔/摩尔布洛芬的一种或多种碱性化合物，其中所述碱性化合物包括每摩尔布洛芬0.5至1.2摩尔，但不超过该数量的一种选自羟氧化钠、羟氧化钾、碳酸钠、碳酸钾、甘氨酸钠、甘氨酸钾、三碱性磷酸钠和钾及其混合物的碱。在不超过所述颗粒中所需水分数量超过每摩尔布洛芬1摩尔的自由水存在下，将布洛芬和所述一种或多种碱性化合物在反应中。可获得的颗粒以及可以从中制备的药物组成物和剂型具有高溶解度和快速在水性介质中分解和溶解，具有良好的流动性和可压缩性，快速达到镇痛效果等特点。
• Ibuprofen-Effervescent Preparation Having a High Dissolution Rate and Method for the Production thereof
  申请人：Gruber Peter

  公开号：US20100172981A1

  公开（公告）日：2010-07-08

  Effervescent ibuprofen formulations, which contain (a) an active ingredient-containing granule which contains a water-soluble ibuprofen salt and a basic excipient, and (b) an effervescent granule which contains an acid component and a carbon dioxide-forming component, and a process for their preparation.

  泡腾型布洛芬配方，包含（a）含有水溶性布洛芬盐和碱性辅料的活性成分颗粒，以及（b）含有酸性成分和产生二氧化碳的成分的泡腾颗粒，以及其制备过程。
• Non-effervescent ibuprofen compositions
  申请人：Roche Consumer Health (Worldwide) Ltd

  公开号：EP0418043A1

  公开（公告）日：1991-03-20

  The unpleasant taste of water-soluble ibuprofen salts in aqueous solution is masked by incorporating in the solution a taste-masking amount of an alkali metal bicarbonate, alkali metal monohydrogen phosphate or alkali metal tribasic citrate. Preferably, the taste-masking compound is an alkali metal bicarbonate, especially sodium bicarbonate.

  在水溶液中加入一定量的碱金属碳酸氢盐、碱金属磷酸一氢盐或碱金属柠檬酸三盐，可掩盖水溶性布洛芬盐的难闻味道。掩味化合物最好是碱金属碳酸氢盐，特别是碳酸氢钠。
• Antiprotozoal methods, compositions and feedstuffs
  申请人：UNIVERSITEIT GENT

  公开号：EP1234508A1

  公开（公告）日：2002-08-28

  Methods and compositions for the prophylactic treatment of coccidiosis and other protozoal infections are described. Preferably, these are administered in the drinking water of the animals, e.g. in the drinking water of poultry to provide a mass prophylactic treatment. These formulations include L-arginine and may also include a modulator of the NO biosynthesis pathway, e.g. and NSAID such as Ibuprofen. These formulations have also been found to improve egg production in hens.

  本文介绍了预防性治疗球虫病和其他原生动物感染的方法和组合物。最好是在动物的饮用水中，例如在家禽的饮用水中施用，以提供大规模的预防性治疗。 这些制剂包括 L-精氨酸，还可能包括 NO 生物合成途径的调节剂，例如非甾体抗炎药，如布洛芬。 研究还发现，这些制剂可提高母鸡的产蛋量。