5R,9R,13R,14S-oxycodone ibuprofenate | 701907-98-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 菲及其衍生物
• 英文名称: 5R,9R,13R,14S-oxycodone ibuprofenate
• 英文别名: Combonox；(4R,4aS,7aR,12bS)-4a-hydroxy-9-methoxy-3-methyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one;2-[4-(2-methylpropyl)phenyl]propanoic acid
• CAS: 701907-98-4
• 化学式: C₁₃H₁₈O₂*C₁₈H₂₁NO₄
• 分子量: 521.654
• InChiKey: BYQMUJKLALSITI-RKXJKUSZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.12
• 重原子数：
  38
• 可旋转键数：
  5
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  96.3
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  布洛芬 、 盐酸羟可待酮 在 氢氧化钾 作用下， 以 乙醇 、 水 为溶剂， 反应 1.0h， 生成 5R,9R,13R,14S-oxycodone ibuprofenate
  参考文献：
  名称：

  Narcotic-NSAID ion pairs

  摘要：

  本发明提供了一种公式为[narcotic]+[A]−的离子对化合物，其中[narcotic]+代表至少一个麻醉剂或其一个或多个立体化学异构体的至少一个阳离子，而[A]−代表至少一个非甾体抗炎药（NSAID）或其一个或多个立体化学异构体的至少一个阴离子。离子对化合物的一个例子是丙氧芬双氯芬酸。这些离子对化合物或其药物组合物在治疗表明需要镇痛剂、抗炎剂或两者都需要的方法中是有用的。在规定的使用条件下，离子对化合物在低pH环境中表现出较差或完全不溶性，但在胃中这类环境中却具有极佳的化学稳定性。离子对化合物在较高pH值的环境中，如小肠，能够快速溶解和离解，以释放组成的麻醉剂和非甾体抗炎药。

  公开号：

  US20050203115A1

文献信息

• Method of treating acute pain with a unitary dosage form comprising ibuprofen and oxycodone
  申请人：Newman Kenneth

  公开号：US20050059690A1

  公开（公告）日：2005-03-17

  The present invention is a method of achieving fast onset of pain relief for acute pain in a patient in need thereof comprising orally administering a unitary formulation (or oral dosage form) containing an effective analgesic amount of (a) oxycodone or a pharmaceutically acceptable salt thereof and (b) ibuprofen or a pharmaceutically acceptable salt thereof. Preferably, the unitary formulation contains (a) oxycodone or a pharmaceutically acceptable salt thereof and (b) ibuprofen or a pharmaceutically acceptable salt thereof at a weight ratio of from about 1:20 to about 1:100 and more preferably about 1:40 to about 1:80, based on the weights of molar equivalents of oxycodone hydrochloride and ibuprofen, respectively. Preferably, an amount of oxycodone and ibuprofen effective to provide partial or complete pain relief within 30 minutes is administered. More preferably, the amount is sufficient to provide partial or complete pain relief within 25 minutes. It has been discovered that administration of an oral dosage form containing both oxycodone and ibuprofen provides earlier onset of pain relief than administration of either active ingredient alone. Moreover, the earlier onset of pain relief may be attributable at least in part to administration of a single dosage form containing both active ingredients as opposed to administering oxycodone and ibuprofen in separate oral dosage forms (i.e., administration of a first dosage form containing oxycodone and a second dosage form containing ibuprofen). The method of the present invention is particularly useful for treating acute postoperative pain, including, but not limited to, moderate and/or severe acute postoperative pain (such as that resulting from dental surgery).

  本发明涉及一种用于急性疼痛患者快速缓解疼痛的方法，包括口服给予含有有效镇痛量的单一制剂（或口服剂型），所述单一制剂含有（a）盐酸氧考酚啡或其药学上可接受的盐和（b）布洛芬或其药学上可接受的盐。优选，所述单一制剂含有（a）盐酸氧考酚啡或其药学上可接受的盐和（b）布洛芬或其药学上可接受的盐，其重量比为大约1:20至大约1:100，更优选为大约1:40至大约1:80，基于氧考酚啡盐酸和布洛芬的摩尔当量重量。优选地，给予足够的氧考酚啡和布洛芬，以在30分钟内提供部分或完全缓解疼痛的效果。更优选地，该量足以在25分钟内提供部分或完全缓解疼痛的效果。已经发现，口服含有氧考酚啡和布洛芬的口服剂型比单独给予任何一种有效成分更早地缓解疼痛。此外，早期缓解疼痛的原因可能至少部分归因于单一剂量形式中同时给予两种有效成分，而不是分别给予氧考酚啡和布洛芬的口服剂型（即给予含有氧考酚啡的第一剂量形式和含有布洛芬的第二剂量形式）。本发明的方法特别适用于治疗急性术后疼痛，包括但不限于中度和/或严重的急性术后疼痛（如口腔手术引起的疼痛）。
• Method of treating acute pain with a unitary dosage form comprising ibuprofin and oxycodone
  申请人：Forest Laboratories, Inc.

  公开号：US20040186122A1

  公开（公告）日：2004-09-23

  The present invention is a method of achieving fast onset of pain relief for acute pain in a patient in need thereof comprising orally administering a unitary formulation (or oral dosage form) containing an effective analgesic amount of (a) oxycodone or a pharmaceutically acceptable salt thereof and (b) ibuprofen or a pharmaceutically acceptable salt thereof. Preferably, the unitary formulation contains (a) oxycodone or a pharmaceutically acceptable salt thereof and (b) ibuprofen or a pharmaceutically acceptable salt thereof at a weight ratio of from about 1:20 to about 1:100 and more preferably about 1:40 to about 1:80, based on the weights of molar equivalents of oxycodone hydrochloride and ibuprofen, respectively. Preferably, an amount of oxycodone and ibuprofen effective to provide partial or complete pain relief within 30 minutes is administered. More preferably, the amount is sufficient to provide partial or complete pain relief within 25 minutes. It has been discovered that administration of an oral dosage form containing both oxycodone and ibuprofen provides earlier onset of pain relief than administration of either active ingredient alone. Moreover, the earlier onset of pain relief may be attributable at least in part to administration of a single dosage form containing both active ingredients as opposed to administering oxycodone and ibuprofen in separate oral dosage forms (i.e., administration of a first dosage form containing oxycodone and a second dosage form containing ibuprofen). The method of the present invention is particularly useful for treating acute postoperative pain, including, but not limited to, moderate and/or severe acute postoperative pain (such as that resulting from dental surgery).

  本发明涉及一种治疗急性疼痛的快速缓解方法，包括口服给予含有效镇痛剂量的单一配方（或口服剂型），该配方包含（a）盐酸氧考酚啡或其药学上可接受的盐和（b）布洛芬或其药学上可接受的盐。优选，该单一配方包含（a）盐酸氧考酚啡或其药学上可接受的盐和（b）布洛芬或其药学上可接受的盐，其重量比为约1:20至约1:100，更优选为约1:40至约1:80，基于氧考酚啡盐酸和布洛芬的摩尔当量重量。优选地，给予足量的氧考酚啡和布洛芬，以在30分钟内提供部分或完全的疼痛缓解。更优选地，给予足量的氧考酚啡和布洛芬，以在25分钟内提供部分或完全的疼痛缓解。 发现口服剂型同时含有氧考酚啡和布洛芬，可比单独给予任一活性成分更快地缓解疼痛。此外，较早的疼痛缓解可能至少部分归因于单一剂量形式同时给予两种活性成分，而非分别给予氧考酚啡和布洛芬的口服剂型（即，给予包含氧考酚啡的第一剂量形式和包含布洛芬的第二剂量形式）。本发明的方法特别适用于治疗急性术后疼痛，包括但不限于中度和/或严重的急性术后疼痛（例如牙科手术引起的疼痛）。
• System and method of forming multilayer confectionery
  申请人：Jani Bharat

  公开号：US10973238B2

  公开（公告）日：2021-04-13

  A method and an apparatus for making a multilayer confectionery product provided. The method and apparatus include at least two sets of forming drums that form and laminate confectionery sheets.

  提供了一种制作多层糖果产品的方法和设备。该方法和设备包括至少两组成型滚筒，用于成型和层压糖果片。
• TAMPER-RESISTANT FIXED DOSE COMBINATION PROVIDING FAST RELEASE OF TWO DRUGS FROM PARTICLES AND A POWDER
  申请人：Grünenthal GmbH

  公开号：EP3285746A1

  公开（公告）日：2018-02-28
• SYSTEM AND METHOD OF FORMING MULTILAYER CONFECTIONERY
  申请人：Jani Bharat

  公开号：US20140004224A1

  公开（公告）日：2014-01-02

  A method and an apparatus for making a multilayer confectionery product provided. The method and apparatus include at least two sets of forming drums that form and laminate confectionery sheets.