柳酸安替比林 | 520-07-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 柳酸安替比林
• 中文别名: 柳比林；非那酮水杨酸盐
• 英文名称: Antipyrine salicylate
• 英文别名: 1,5-dimethyl-2-phenylpyrazol-3-one;2-hydroxybenzoic acid
• CAS: 520-07-0
• 化学式: C18H18N2O4
• 分子量: 326.3
• InChiKey: WQAQKERCWPUIMH-UHFFFAOYSA-N

物化性质

• 熔点：
  91-92°

计算性质

• 辛醇/水分配系数(LogP)：
  2.57
• 重原子数：
  24
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  81.1
• 氢给体数：
  2
• 氢受体数：
  5

安全信息

• 海关编码：
  2933199090

制备方法与用途

类别：有毒物品

毒性分级：中毒

急性毒性：

• 小鼠 LD50: 1200 毫克/公斤
• 豚鼠 LD50: 1600 毫克/公斤

可燃性危险特性：可燃；燃烧时会产生有毒氮氧化物烟雾

储运特性：库房通风、低温干燥

灭火剂：干粉、泡沫、沙土、二氧化碳、雾状水

文献信息

• Technology for the Preparation of Microparticles
  申请人：Malakhov Michael

  公开号：US20090098207A1

  公开（公告）日：2009-04-16

  Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

  微球是通过将溶液中的大分子或小分子与抗溶剂和对离子接触，并冷却溶液而制备的。这些微球可用于制备具有明确定义尺寸的药物、营养保健品、化妆品等产品。
• Celecoxib prodrug
  申请人：——

  公开号：US20040092566A1

  公开（公告）日：2004-05-13

  N-[[4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-sulfonyl]propanamide and pharmaceutically acceptable salts thereof are useful prodrugs of the selective COX-2 inhibitory drug celecoxib, which can be administered to a subject by any suitable route.

  N-[[4-[[5-(4-甲基苯基)-3-(三氟甲基)-1H-吡唑-1-基]苯基]-磺酰]丙酰胺及其药用盐是选择性COX-2抑制药物美洛昔布的有效前药，可通过任何合适的途径给予受试者。
• [EN] PHARMACEUTICAL COMPOSITIONS WITH IMPROVED DISSOLUTION<br/>[FR] COMPOSITIONS PHARMACEUTIQUES A DISSOLUTION AMELIOREE
  申请人：TRANSFORM PHARMACEUTICALS INC

  公开号：WO2004000284A1

  公开（公告）日：2003-12-31

  The invention relates to methods of screening mixtures containing a pharmaceutical compound an excipient to identify properties of the pharmaceutical compound/excipient combination that retard solid-state nucleation. The invention further relates to increasing the solubility, dissolution and bioavailability of a drug with low solubility in gastric fluids conditions by combining the drug with a recrystallization/precipitation retardant and an optional enhancer.

  本发明涉及筛选包含药物化合物和赋形剂的混合物的方法，以识别延缓固态成核的药物化合物/赋形剂组合的特性。该发明还涉及通过将药物与再结晶/沉淀抑制剂和可选增效剂结合，来增加低溶解度药物在胃液条件下的溶解度、溶出性和生物利用度。
• Odorless formulation for treating mucosal discontinuities
  申请人：——

  公开号：US20040132810A1

  公开（公告）日：2004-07-08

  The present invention includes a method for making a formulation for treating mucosal discontinuities, comprising: providing phenolic compounds and treating the purified phenolic compounds with sulfuric acid to make sulfonic acids and sulfonate salts. The present invention also includes formulations prepared by the method.

  本发明涉及一种用于制备治疗黏膜不连续的配方的方法，包括：提供酚类化合物，并用硫酸处理纯化的酚类化合物以制备磺酸和磺酸盐。本发明还包括通过该方法制备的配方。
• Crystalline parecoxib sodium
  申请人：——

  公开号：US20030232871A1

  公开（公告）日：2003-12-18

  Parecoxib sodium is provided in a crystalline form that is substantially anhydrous and substantially nonsolvated. Various such anhydrous, nonsolvated crystal forms have been identified, including Forms A, B and E as described herein. Also provided is a parecoxib sodium drug substance wherein at least about 90% of the parecoxib sodium is in one or more anhydrous, nonsolvated crystal forms. Such a drug substance is a storage-stable intermediate that can be further processed, for example by dissolution or slurrying in an aqueous medium together with one or more parenterally acceptable excipients, followed by lyophilization of the resulting solution or slurry to provide a reconstitutable injectable composition suitable for therapeutic use.

  Parecoxib钠以晶体形式提供，该晶体形式基本上是无水和基本上是非溶剂化的。已经确定了各种这样的无水，非溶剂化的晶体形式，包括本文中描述的A、B和E形式。还提供了一种Parecoxib钠药物物质，其中至少约90％的Parecoxib钠以一种或多种无水，非溶剂化的晶体形式存在。这种药物物质是一种存储稳定的中间体，可以进一步加工，例如通过在水性介质中与一个或多个肠外可接受的赋形剂一起溶解或混悬，然后冻干所得的溶液或混悬物，以提供适用于治疗用的可重组注射剂组成。