美沙吡林富马酸盐 | 33032-12-1

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 美沙吡林富马酸盐
• 中文别名: 富马酸噻吡二胺富马酸噻吩甲吡胺；富马酸美沙吡林
• 英文名称: (E)-but-2-enedioic acid;N,N-dimethyl-N'-pyridin-2-yl-N'-(thiophen-2-ylmethyl)ethane-1,2-diamine
• CAS: 33032-12-1
• 化学式: C18H23N3O4S
• 分子量: 377.5
• InChiKey: GYIUBPDECOMZDC-WLHGVMLRSA-N

物化性质

• 熔点：
  135-136°

计算性质

• 辛醇/水分配系数(LogP)：
  2.42
• 重原子数：
  26
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  122
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• Composition for reducing menstrual pain
  申请人：WHITBY RESEARCH, Inc.

  公开号：EP0081823A1

  公开（公告）日：1983-06-22

  A composition for treating dysmenorrhea in a human female having dysmenorrhea comprising an effective, menstrual pain reducing amount of dextromethorphan, preferably as the hydrobromide.

  一种用于治疗女性痛经的组合物，其中含有有效的、可减轻经痛的右美沙芬，最好是氢溴酸盐。
• Medicated compositions containing sucralfate and processes for their production
  申请人：WARNER-LAMBERT COMPANY

  公开号：EP0403048A2

  公开（公告）日：1990-12-19

  There are disclosed novel medicated compositions useful in treating a wide variety of disorders. The novel compositions comprise sucralfate and a therapeutically effective amount of a medicament. In a preferred embodiment, the medicament is selected from the group consisting of antacids, antiulcer medicaments, gastro-unstable medicaments, and medicaments which are normally administered in divided doses two or more times daily. Such medicated compositions are useful in treating various disorders by providing a mucous membrane adherent protective gel in the stomach having the medicament entrapped therein. The novel medicated compositions may be utilized in a wide variety of pharmaceutical products. This invention also relates to methods by which these medicated compositions and pharmaceutical products may be prepared.

  本文公开了可用于治疗多种疾病的新型药物组合物。这些新型组合物包括琥珀酸盐和治疗有效量的药物。在一个优选的实施方案中，药物选自抗酸剂、抗溃疡药物、胃肠道不稳定药物和通常每天分两次或多次给药的药物组成的组。这种药物组合物通过在胃中提供一种粘膜附着保护凝胶（其中夹带药物）来治疗各种疾病。这种新型药物组合物可用于多种医药产品中。本发明还涉及制备这些药物组合物和药品的方法。
• Chewable spray dried spheroidal microcapsules and wax coated microcapsules and methods for preparing same
  申请人：WARNER-LAMBERT COMPANY

  公开号：EP0421581A1

  公开（公告）日：1991-04-10

  The present invention pertains to a spray dried spheroidal microcapsule under about 150 microns in diameter which comprises (a) a medicament present in an amount from about 1% to about 90%, by weight of the microcapsule composition, (b) a film forming polymer present in an amount from about 8% to about 90%, by weight of the microcapsule composition, (c) a plasticizing agent in an amount from about 5% to about 30%, by weight of the film forming polymer. In another embodiment, the invention is directed at a spheroidal coated microcapsule under about 850 microns in diameter which comprises at least one spray dried spheroidal microcapsule core under about 150 microns in diameter and a coating layer over the core, wherein the coating layer comprises in percentages by weight of the coating layer composition (a) an edible material having a melting point from about 25o C. to about 100o C. selected from the group consisting of (i) fatty acids having an iodine value from about 1 to about 10, (ii) natural waxes, (iii) synthetic waxes, and (iv) mixtures thereof, present in an amount from about 80% to about 99.5%, and (b) a surface active agent present in an amount from about 0.5% to about 20%.

  本发明涉及一种直径小于约 150 微米的喷雾干燥球形微胶囊，它包括：(a) 一种药物，其含量为微胶囊组合物重量的约 1%至约 90%；(b) 一种成膜聚合物，其含量为微胶囊组合物重量的约 8%至约 90%；(c) 一种增塑剂，其含量为成膜聚合物重量的约 5%至约 30%。在另一个实施方案中，本发明涉及一种直径小于约 850 微米的球形包衣微胶囊，该微胶囊包括至少一个直径小于约 150 微米的喷雾干燥球形微胶囊芯和覆盖在芯上的包衣层，其中包衣层包括以重量百分比计的包衣层组合物 (a) 一种可食用材料，其熔点在约 25o C. 至约 100o C. 之间。(b) 一种表面活性剂，含量约为 0.5%至约 20%。
• Chewable spray dried spheroidal microcapsules and polymer coated microcapsules and method for preparing same
  申请人：WARNER-LAMBERT COMPANY

  公开号：EP0421582A1

  公开（公告）日：1991-04-10

  The present invention pertains to a spray dried spheroidal microcapsule under about 150 microns in diameter which comprises (a) a medicament present in an amount from about 1% to about 90%, by veight of the microcapsule composition, (b) a film forming polymer present in an amount from about 8% to about 90%, by weight of the microcapsule composition, and (c) a plasticizing agent present in an amount from about 5% to about 30%, by weight of the film forming polymer. In another embodiment, the invention is directed at a spheroidal coated microcapsule under about 850 microns in diameter which comprises at least one spray dried spheroidal microcapsule core under about 150 microns in diameter and a coating layer over the core, wherein the coating layer comprises (a) a film forming polymer, and (b) a plasticizing agent present in an amount from about 5% to about 30%, by weight of the film forming polymer.

  本发明涉及一种直径小于约 150 微米的喷雾干燥球形微胶囊，它包括：(a) 一种药物，其含量为微胶囊组合物重量的约 1%至约 90%；(b) 一种成膜聚合物，其含量为微胶囊组合物重量的约 8%至约 90%；(c) 一种增塑剂，其含量为成膜聚合物重量的约 5%至约 30%。在另一个实施方案中，本发明涉及一种直径小于约 850 微米的球形包衣微胶囊，它包括至少一个直径小于约 150 微米的喷雾干燥球形微胶囊芯和覆盖在芯上的包衣层，其中包衣层包括(a)成膜聚合物，和(b)增塑剂，按成膜聚合物的重量计，其含量从约 5%到约 30%。
• Chewable spheroidal coated microcapsules and methods for preparing same
  申请人：WARNER-LAMBERT COMPANY

  公开号：EP0477135A1

  公开（公告）日：1992-03-25

  The present invention pertains to a chewable spheroidal coated microcapsule under about 850 microns in diameter which comprises at least one spray congealed spheroidal microcapsule core under about 200 microns in diameter, a first wax spray coating layer over the core, and a second oil coating layer over the first coated core, wherein the coated microcapsule comprises (A) a microcapsule core comprising, in percentages by weight of the microcapsule core (a) a medicament present in an amount from about 1% to about 40%, (b) an edible material having a melting point from about 25°C. to about 100°C. selected from the group consisting of (i) fatty acids having an iodine value from about 1 to about 10, (ii) natural waxes, (iii) synthetic waxes, and (iv) mixtures thereof, present in an amount from about 9.5% to about 98.5%, (c) an emulsifying agent present in an amount from about 0.5% to about 20%, (B) a first wax spray coating layer over the microcapsule core comprising, in percentages by weight of the first coating layer (a) an edible material having a melting point from about 25°C. to about 100°C. selected from the group consisting of (i) fatty acids having an iodine value from about 1 to about 10, (ii) natural waxes, (iii) synthetic waxes, and (iv) mixtures thereof, present in an amount from about 60% to about 99.5%, (b) an emulsifying agent present in an amount from about 0.5% to about 20%, and (C) a second oil coating layer over the first coated microcapsule core comprising an edible vegetable oil having a melting point in the range from about 25°C. to about 90°C.

  本发明涉及一种直径小于约850微米的可咀嚼球形包衣微胶囊，它包括至少一个直径小于约200微米的喷雾凝固球形微胶囊芯，在该芯上有第一喷蜡包衣层，以及在第一包衣芯上有第二喷油包衣层、其中包衣微胶囊包括 (A) 微胶囊芯，以微胶囊芯的重量百分比计 (a) 药物，其含量从约1%到约40%； (b) 可食用材料，其熔点从约25°C.至约 100°C.的可食用材料，选自以下组别：(i) 碘值在约 1 至约 10 之间的脂肪酸；(ii) 天然蜡；(iii) 合成蜡；(iv) 它们的混合物，含量在约 9.(B) 微胶囊芯上的第一喷蜡涂层，以第一涂层的重量百分比计包括 (a) 一种可食用材料，其熔点为约 25°C 至约 100°C。(b) 一种乳化剂，含量约为 0.5%至约 20%；以及 (C) 覆盖在第一涂层微胶囊芯上的第二油涂层层，包括熔点在约 25°C 至约 90°C 范围内的可食用植物油。