chloromethyl (8S,9S,10R,11S,13S,14S,17S)-17-((ethoxycarbonyl)oxy)-11-hydroxy-10,13-dimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylate | 82034-46-6

• 物质功能分类: 生物化工 - 抑制剂 - 内分泌及激素(Endocrinology & Hormones)
• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: chloromethyl (8S,9S,10R,11S,13S,14S,17S)-17-((ethoxycarbonyl)oxy)-11-hydroxy-10,13-dimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylate
• 英文别名: chloromethyl (8S,9S,10R,11S,13S,14S,17S)-17-ethoxycarbonyloxy-11-hydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthrene-17-carboxylate
• CAS: 82034-46-6
• 化学式: C₂₄H₃₁ClO₇
• 分子量: 466.9
• InChiKey: DMKSVUSAATWOCU-ICASLIHPSA-N

物化性质

• 熔点：
  220.5-223.5
• 沸点：
  600.1±55.0 °C(Predicted)
• 密度：
  1.31±0.1 g/cm3(Predicted)
• 溶解度：
  DMSO：可溶5mg/mL，澄清（加热）

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  99.1
• 氢给体数：
  1
• 氢受体数：
  7

安全信息

• WGK Germany：
  3
• 危险品运输编号：
  NONH for all modes of transport
• 海关编码：
  2937229000

制备方法与用途

氯替泼诺是一种用于眼科疾病的局部类固醇药物,主要用于治疗对皮质类固醇敏感的眼部疾病。其主要特点和注意事项包括:

1. 主要适应症是对皮质类固醇敏感性眼病,如角膜炎、结膜炎等。

2. 使用前需摇匀药液,每日4次滴入结膜囊中。

3. 滴用频率可适当增加至每小时一次,但不宜过早停药。

4. 对于术后炎症的治疗,应在手术后24小时内开始使用,持续2周左右。

5. 需在医生指导下定期检查眼内压等指标。

6. 可能会出现一系列不良反应,如视力异常、结膜炎等。如果症状无改善应及时就医。

7. 使用过程中应注意不要污染滴管,避免佩戴隐形眼镜。

8. 长期使用需警惕潜在的严重副作用,如青光眼、后囊下白内障形成等。

9. 有病毒性眼部感染病史者应谨慎使用。

10. 存放于儿童接触不到的地方。

总之,氯替泼诺是一种有效的局部类固醇药物,但需在医生指导下规范使用,并注意观察不良反应。

文献信息

• Use of loteprednol etabonate for the treatment of dry eye
  申请人：BAUSCH & LOMB INCORPORATED

  公开号：EP2127655A1

  公开（公告）日：2009-12-02

  Disclosed in embodiments herein is a method of treating chronic dry eye in a patient in need thereof, the method comprising topically administering to the patient Loteprednol etabonate in an ophthalmolically acceptable carrier.

  本文实施例中公开了一种治疗有需要的患者慢性干眼症的方法，该方法包括向患者局部施用眼科可接受载体中的洛泼尼醇酯。
• USE OF LOTEPREDNOL ETABONATE FOR THE TREATMENT OF DRY EYE
  申请人：BAUSCH & LOMB INCORPORATED

  公开号：EP1744759A2

  公开（公告）日：2007-01-24
• Use of Loteprednol etabonate for the treatment of dry eye
  申请人：Meyering J. Robert

  公开号：US20050182039A1

  公开（公告）日：2005-08-18

  Disclosed in embodiments herein is a method of treating dry eye in a patient in need thereof, the method comprising topically administering to the patient Loteprednol etabonate in an ophthalmolically acceptable carrier.
• Compositions, formulations and kit with anti-sense oligonucleotide and anti-inflammatory steroid and/or obiquinone for treatment of respiratory and lung disesase
  申请人：Nyce W. Jonathan

  公开号：US20070021360A1

  公开（公告）日：2007-01-25

  A pharmaceutical composition and formulations comprise preventative, prophylactic or therapeutic amounts of an oligo(s) anti-sense to a specific gene(s) or its corresponding mRNA(s), and a glucocorticoid and/or non-glucocorticoid steroid or a ubiquinone or their salts. The agents, composition and formulations are used for treatment of ailments associated with impaired respiration, bronchoconstriction, lung allergy(ies) or inflammation, and abnormal levels of adenosine, adenosine receptors, sensitivity to adenosine, lung surfactant and ubiquinone, such as pulmonary fibrosis, vasoconstriction, inflammation, allergies, allergic rhinitis, asthma, impeded respiration, lung pain, cystic fibrosis, bronchoconstriction, COPD, RDS, ARDS, cancer, and others. The present treatment is effectively administered by itself for conditions without known therapies, as a substitute for therapies exhibiting undesirable side effects, or in combination with other treatments, e.g. before, during and after other respiratory system therapies, radiation, chemotherapy, antibody therapy and surgery, among others. Each of the agents of this invention may be administered directly into the respiratory system so that they gain direct access to the lungs, or by other effective routes of administration. A kit comprises a delivery device, the agents and instructions for its use.
• Ophthalmic composition for dry eye therapy
  申请人：Xia Erning

  公开号：US20070110812A1

  公开（公告）日：2007-05-17

  Disclosed in embodiments are gel formulations which are not subject to the settling out phenomena that may be observed with Loteprednol etabonate suspensions.