[11-hydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-yl] butanoate | 13609-67-1

• 物质功能分类: 原料药 - 激素及调节内分泌功能类药 - 肾上腺皮质激素类药
• 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: [11-hydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-yl] butanoate
• CAS: 13609-67-1
• 化学式: C₂₅H₃₆O₆
• 分子量: 432.5
• InChiKey: BMCQMVFGOVHVNG-UHFFFAOYSA-N

物化性质

• 熔点：
  210.0 to 214.0 °C
• 沸点：
  466.2°C (rough estimate)
• 密度：
  1.0914 (rough estimate)
• 溶解度：
  可溶于氯仿（少许）、甲醇（少许）

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  31
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  101
• 氢给体数：
  2
• 氢受体数：
  6

安全信息

• WGK Germany：
  2
• 海关编码：
  2937210000
• 危险品运输编号：
  NONH for all modes of transport
• RTECS号：
  GM9002000
• 储存条件：
  室温

制备方法与用途

产品描述

丁酸氢化可的松是一种甾体皮质激素，能够抑制发炎及过敏皮肤的反应，同时亦能抑制与细胞加速再生有关联的反应。因此它常用于缓解多种症状，如红斑、水肿、皮肤增厚、皮肤表面粗糙的减退，以及减轻瘙痒、灼热感和疼痛等问题。

适应症

丁酸氢化可的松适用于治疗各型湿疹、过敏性皮炎、特应性皮炎、神经性皮炎、日光性皮炎、放射性皮炎、扁平苔藓、婴儿苔藓、进行性掌跖角化症、银屑病、非特异性肛门、外阴及阴囊瘙痒症等。

药代动力学

丁酸氢化可的松经皮肤迅速吸收，在皮肤内迅速显示高浓度，随后向血液转运后被酯酶水解为氢化可的松。它在消化道、肝、肾及膀胱中分布较多，并主要通过粪便排泄。

副作用

长期连续使用丁酸氢化可的松偶见药物性寻常痤疮样疹、酒渣样皮炎、口周皮炎，面颊及口周等处潮红、丘疹、脓疱、皮肤萎缩、毛细血管扩张、鱼鳞病样皮肤变化、紫癜、多毛、色素脱失等。

生物活性

丁酸氢化可的松是一种有效的局部用皮质甾类药物，可用于治疗一系列炎症性皮肤病，并作为激素类药使用。

文献信息

• Pharmaceutical compositions and methods of use of 4-pregenen-11β-17-21-triol-3,20-dione derivatives
  申请人：ALLERGAN, INC.

  公开号：US10188667B2

  公开（公告）日：2019-01-29

  The present invention relates to pharmaceutical compositions comprising 4-pregenen-11β-17-21-triol-3,20-dione derivatives, and their use as pharmaceuticals as modulators of the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR). The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat ocular conditions associated with the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR).

  本发明涉及包含 4-孕甾-11β-17-21-三醇-3,20-二酮衍生物的药物组合物，以及它们作为糖皮质激素受体（GR）和/或矿质皮质激素受体（MR）调节剂的药物用途。本发明具体涉及使用这些化合物及其药物组合物治疗与糖皮质激素受体（GR）和/或矿质类固醇受体（MR）相关的眼部疾病。
• PHARAMCEUTICAL COMPOSITIONS AND METHODS OF USE 4-PREGENEN-11BETA-17-21-TRIOL-3,20-DIONE DERIVATIVES
  申请人：Allergan, Inc.

  公开号：US20130123226A1

  公开（公告）日：2013-05-16

  The present invention relates to pharmaceutical compositions comprising 4-pregenen-11β-17-21-triol-3,20-dione derivatives, and their use as pharmaceuticals as modulators of the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR). The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat ocular conditions associated with the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR).
• PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF 4-PREGENEN-11BETA-17-21-TRIOL-3,20-DIONE DERIVATIVES
  申请人：ALLERGAN, INC.

  公开号：US20150005519A1

  公开（公告）日：2015-01-01

  The present invention relates to pharmaceutical compositions comprising 4-pregenen-11β-17-21-triol-3,20-dione derivatives, and their use as pharmaceuticals as modulators of the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR). The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat ocular conditions associated with the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR).
• SELF-EMULSIFYING DRUG DELIVERY (SEDDS) FOR OPHTHALMIC DRUG DELIVERY
  申请人：Allergan, Inc.

  公开号：US20180036233A1

  公开（公告）日：2018-02-08

  Provided herein are topical ophthalmic preparations which comprise a non-aqueous, self-emulsifying system which can spontaneously give rise to either nanosized emulsions upon contact with an aqueous phase. Also provided herein are methods for the preparation of the same and their use in formulating and delivering poorly water soluble drugs.
• US8865691B2
  申请人：——

  公开号：US8865691B2

  公开（公告）日：2014-10-21