Azithromycin dihydrochloride | 90581-31-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: Azithromycin dihydrochloride
• 英文别名: (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-11-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-3,4,10-trihydroxy-13-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,6,8,10,12,14-heptamethyl-1-oxa-6-azacyclopentadecan-15-one;dihydrochloride
• CAS: 90581-31-0
• 化学式: C38H74Cl2N2O12
• 分子量: 821.9
• InChiKey: WUTMHODASJRZBL-KUJJYQHYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.74
• 重原子数：
  54
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.97
• 拓扑面积：
  180
• 氢给体数：
  7
• 氢受体数：
  14

文献信息

• [EN] ADDITION SALTS OF AZITHROMYCIN AND CITRIC ACID AND PROCESS FOR PREPARING THEM<br/>[FR] SELS D'ADDITION D'AZITHROMYCINE ET D'ACIDE CITRIQUE ET LEUR PROCEDE DE PREPARATION
  申请人：SINT QUIMICA SA

  公开号：WO2004106355A1

  公开（公告）日：2004-12-09

  Said addition salts have a molar ratio between azithromycin and citric acid such as to provide a pH comprised between 4.0 and 8.0 in a 10 % aqueous solution. The process for preparing said salts comprises: a) dissolving azithromycin in a solvent or mixture of solvents; b) adding citric acid; and c) isolating the product obtained by crystallisation. The addition salts of azithromycin and citric acid are stable and soluble in aqueous medium, being useful antibacterial and antiprotozoan agents.

  所述加合物盐具有阿奇霉素和柠檬酸之间的摩尔比，以便在10％水溶液中提供pH值介于4.0和8.0之间。制备所述盐的过程包括：a）在溶剂或溶剂混合物中溶解阿奇霉素；b）加入柠檬酸；和c）通过结晶分离所得的产物。阿奇霉素和柠檬酸的加合物盐在水介质中稳定且可溶，是有用的抗菌和抗原虫剂。
• Crystalline Azithromycin L-Malate Monohydrate and Pharmaceutical Composition Containing Same
  申请人：Kwon Bo Sung

  公开号：US20090318375A1

  公开（公告）日：2009-12-24

  This invention provides a crystalline azithromycin L-malate monohydrate for treating various microbial infections, which has high thermostability, solubility and non-hygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.

  该发明提供了一种晶体阿奇霉素L-苹果酸一水合物，用于治疗各种微生物感染，具有高热稳定性、溶解度和不吸湿性，以及一种制备该晶体的方法和含有该晶体的药物组合物。
• Addition salts of azithromycin and citric acid and process for preparing them
  申请人：Cosme Gomez Antonio

  公开号：US20070021359A1

  公开（公告）日：2007-01-25

  Said addition salts have a molar ratio between azithromycin and citric acid such as to provide a pH comprised between 4.0 and 8.0 in a 10% aqueous solution. The process for preparing said salts comprises: a) dissolving azithromycin in a solvent or mixture of solvents; b) adding citric acid; and c) isolating the product obtained by crystallisation. The addition salts of azithromycin and citric acid are stable and soluble in aqueous medium, being useful antibacterial and antiprotozoan agents.

  所述加合盐的摩尔比例在阿奇霉素和柠檬酸之间，以便在10％水溶液中提供pH值介于4.0和8.0之间。制备所述盐的过程包括：a）将阿奇霉素溶解在溶剂或溶剂混合物中；b）添加柠檬酸；以及c）通过结晶分离所得的产物。阿奇霉素和柠檬酸的加合盐在水介质中稳定且易溶，是有用的抗菌和抗原虫剂。
• Azalide antibiotics for the topical treatment or prevention of ocular infections
  申请人：INSITE VISION INCORPORATED

  公开号：EP1588702A1

  公开（公告）日：2005-10-26

  The topical application of an azalide antibiotic such as azithromycin and an additional medicament to the eye is useful in treating or preventing ocular infections. In one embodiment, the azalide antibiotic is supplied to the eye in a depot for sustained release. A more convenient dosing regimen can also be provided by the use of an appropriate depot.

  在眼部局部使用阿扎啶类抗生素（如阿奇霉素）和其他药物有助于治疗或预防眼部感染。在一个实施方案中，氮杂环类抗生素是以持续释放的药库形式供应给眼部的。使用适当的药剂库也可以提供更方便的给药方案。
• Topical treatment or prevention of ocular infections
  申请人：INSITE VISION INCORPORATED

  公开号：US20040266702A1

  公开（公告）日：2004-12-30

  The topical application of an azalide antibiotic such as azithromycin to the eye is useful in treating or preventing ocular infections. In one embodiment, the azalide antibiotic is supplied to the eye in a depot for sustained release. A more convenient dosing regimen can also be provided by the use of an appropriate depot. Furthermore, a composition containing a combination of medicaments is also provided.

  在眼部局部使用阿扎啶类抗生素（如阿奇霉素）有助于治疗或预防眼部感染。在一个实施方案中，氮杂环类抗生素以持续释放的药剂形式供应眼部。使用适当的药剂库也可以提供更方便的给药方案。此外，还提供了一种含有多种药物组合的组合物。