(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;ethanol

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (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;ethanol
• 化学式: C40H78N2O13
• 分子量: 795.1
• InChiKey: HVDVAJFACWNIJY-WVVFQGGUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  55
• 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：
  200
• 氢给体数：
  6
• 氢受体数：
  15

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。
• ETHANOLATE OF AZITHROMYCIN, PROCESS FOR MANUFACTURE, AND PHARMACEUTICAL COMPOSITIONS THEREOF
  申请人：——

  公开号：US20020007049A1

  公开（公告）日：2002-01-17

  A novel, non-hygroscopic form of azithromycin is disclosed, as well as a method for preparing it by the gradual crystallization of azithromycin from ethanol by the addition of a minimal amount of water to effect crystal formation. Pharmaceutical compositions containing this novel form of azithromycin are also disclosed.

  本发明揭示了一种新型的非吸湿性阿奇霉素形式，以及一种通过将少量水加入乙醇中逐渐结晶阿奇霉素的方法来制备它的方法。还揭示了含有这种新型阿奇霉素形式的药物组合物。
• 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。
• Crystalline azithromycin, process for manufacture and pharmaceutical compositions thereof
  申请人：Teva Pharmaceutical Industries Limited

  公开号：EP1484062A1

  公开（公告）日：2004-12-08

  Crystalline azithromycin is disclosed, as well as a method for preparing it by the gradual crystallization from ethanol by the addition of a minimal amount of water to effect crystal formation. Pharmaceutical compositions containing this form of azithromycin are also disclosed.

  本发明公开了结晶阿奇霉素，以及通过加入极少量的水从乙醇中逐渐结晶以形成晶体的制备方法。还公开了含有这种形式的阿奇霉素的药物组合物。
• Azithromycin multiparticulate dosage forms by liquid-based processes
  申请人：Appel E. Leah

  公开号：US20050123616A1

  公开（公告）日：2005-06-09

  Liquid-based processes are disclosed for forming azithromycin multiparticulates having minimal amounts of azithromycin esters.

  本发明公开了用于形成阿奇霉素多微粒的液基工艺，这些多微粒具有极少量的阿奇霉素酯。