4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide acetylsalicylic acid (1:1) | 1174325-88-2

• 分子结构分类: 有机化合物
• 英文名称: 4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide acetylsalicylic acid (1:1)
• 英文别名: meloxicam acetylsalicylic acid (1:1)；meloxicam:acetylsalicylic acid；2-acetyloxybenzoic acid;4-hydroxy-2-methyl-N-(5-methyl-1,3-thiazol-2-yl)-1,1-dioxo-1lambda6,2-benzothiazine-3-carboxamide；2-acetyloxybenzoic acid;4-hydroxy-2-methyl-N-(5-methyl-1,3-thiazol-2-yl)-1,1-dioxo-1λ6,2-benzothiazine-3-carboxamide
• CAS: 1174325-88-2
• 化学式: C₉H₈O₄*C₁₄H₁₃N₃O₄S₂
• 分子量: 531.567
• InChiKey: UNKNFLRPNFEZPB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.26
• 重原子数：
  36
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  200
• 氢给体数：
  3
• 氢受体数：
  11

反应信息

• 作为产物：
  描述：

  美洛昔康 、 阿司匹林 以 氯仿 为溶剂， 反应 1.0h， 生成 4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide acetylsalicylic acid (1:1)
  参考文献：
  名称：

  无溶剂声化学法可作为制备药物共晶的途径†

  摘要：

  我们描述了从固体试剂开始的无溶剂声化学法合成药物相关共晶体的方法。使用标准的超声波清洗浴，在20–60分钟内发生了定量转化，从而产生了扑热息痛和阿司匹林的共结晶以及一系列共形成物。除了该方法的实用性之外，这项工作提出了有关不存在液相的声空化的有趣的机械问题。

  DOI：

  10.1039/c9cc00013e

文献信息

• In vivo studies of crystalline forms of meloxicam
  申请人：Hanna Mazen

  公开号：US20090203680A1

  公开（公告）日：2009-08-13

  The invention is directed to novel crystalline forms of meloxicam. These novel crystalline forms of meloxicam have improved bioavailability, an enhanced rate of dissolution and shorter time to C max in blood, as compared to pure meloxicam.

  本发明涉及美洛昔康的新晶体形式。这些新晶体形式的美洛昔康具有比纯美洛昔康更好的生物利用度，更快的溶解速度和更短的达到血浆Cmax的时间。
• [EN] MELOXICAM CO-CRYSTALS<br/>[FR] CO-CRISTAUX DE MÉLOXICAM
  申请人：MYLAN LABORATORIES LTD

  公开号：WO2020095316A1

  公开（公告）日：2020-05-14

  Co-crystals of meloxicam co-formers can be prepared by co-crystallization from a polar solvent, such as aqueous dimethyl sulfoxide; or by slurry processes, such as with ethyl acetate. Such co-crystals have improved purities and are physically stable under storage for several months.

  美洛昔康辅基的共晶可以通过在极性溶剂中共结晶制备，例如水溶性二甲基亚砜；或者通过浆状过程，例如乙酸乙酯。这种共晶具有提高的纯度，并且在存储数月后仍然具有物理稳定性。
• MELOXICAM CO-CRYSTAL COMPOSITIONS
  申请人：Mylan Specialty L.P.

  公开号：US20220184095A1

  公开（公告）日：2022-06-16

  The solubility and bioavailability properties of meloxicam can be improved by preparing compositions of meloxicam co-crystals and reducing the particle size of (e.g., “nanosizing”) co-crystals. Such compositions with improved dissolution pharmacokinetic properties can be prepared by granulation and blending the co-crystals with extragranular excipients to provide oral solid dosage forms. As a result of the improved properties of the meloxicam oral dosage forms, the compositions may be useful for the treatment of pain, including acute pain.
• [EN] MELOXICAM CO-CRYSTAL COMPOSITIONS<br/>[FR] COMPOSITIONS DE CO-CRISTAUX DE MÉLOXICAM
  申请人：MYLAN SPECIALTY L P

  公开号：WO2020219406A1

  公开（公告）日：2020-10-29

  The solubility and bioavailability properties of meloxicam can be improved by preparing compositions of meloxicam co-crystals and reducing the particle size of (e.g., "nanosizing") co-crystals. Such compositions with improved dissolution pharmacokinetic properties can be prepared by granulation and blending the co-crystals with extragranular excipients to provide oral solid dosage forms. As a result of the improved properties of the meloxicam oral dosage forms, the compositions may be useful for the treatment of pain, including acute pain.
• [EN] ORAL SOLID MELOXICAM FORMULATIONS FOR THE TREATMENT OF ACUTE PAIN<br/>[FR] FORMULATIONS SOLIDES PAR VOIE ORALE DE MÉLOXICAM PERMETTANT LE TRAITEMENT DE LA DOULEUR AIGUË
  申请人：MYLAN SPECIALTY L P

  公开号：WO2021216545A1

  公开（公告）日：2021-10-28

  Oral solid pharmaceutical compositions containing meloxicam co-crystals described herein allow for the use of meloxicam for the treatment of acute pain. In particular, the improved dissolution and bioavailability of the meloxicam co-crystal compositions provide more rapid uptake of meloxicam in vivo as evidenced by increase blood plasma concentrations in a decreased amount of time following administration. A correlation between improved plasma concentrations and in vivo analgesic action are provided for the first time.