gestodene valerate

• 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: gestodene valerate
• 英文别名: Gestodene valerate；[(8R,9S,10R,13S,14S,17R)-13-ethyl-17-ethynyl-3-oxo-1,2,6,7,8,9,10,11,12,14-decahydrocyclopenta[a]phenanthren-17-yl] pentanoate
• 化学式: C₂₆H₃₄O₃
• 分子量: 394.554
• InChiKey: NLEJLSSVKUJVJF-UKNJCJGYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  29
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.69
• 拓扑面积：
  43.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  戊酸酐 、 孕二烯酮 在 4-吡咯烷基吡啶 作用下， 以 吡啶 、 水 为溶剂， 生成 gestodene valerate
  参考文献：
  名称：

  Agent for transdermal administration that contains gestodene esters

  摘要：

  描述了一种用于经皮给药的药剂，其特点在于其含有1到20个碳原子的戈司通酮酯，可选择地与一个或两个雌激素结合。

  公开号：

  US05858394A1

文献信息

• Transdermal delivery system of hormones without penetration enhancers
  申请人：SCHERING AKTIENGESELLSCHAFT

  公开号：EP1541137A2

  公开（公告）日：2005-06-15

  The present invention relates to a patch comprising a drug-containing layer with low content of hormones, such as gestodene, and optionally an estrogen (e.g. ethinyl estradiol). Upon administering the patch to a woman, plasma levels of at least 1.0 ng/ml of Gestodene is achieved at steady state conditions without the need of incorporating penetration enhancers or permeation enhancers in the drug-containing layer. Satisfactorily plasma levels of the hormones is also achieved throughout a period of at least 1 week, making the patch applicable for being used in female contraception with the concept of administering the patch ones weekly.

  本发明涉及一种贴片，该贴片由含低含量激素（如孕烯）和可选雌激素（如炔雌醇）的药物层组成。妇女使用该贴片后，在稳态条件下，孕烯的血浆浓度至少可达到 1.0 纳克/毫升，而无需在含药层中加入渗透促进剂或渗透增强剂。在至少一周的时间里，激素的血浆浓度也能达到令人满意的水平，因此这种贴片可用于女性避孕，每周使用一次。
• Transdermal delivery of hormones without the need of penetration enhancers
  申请人：Langguth Thomas

  公开号：US20050142175A1

  公开（公告）日：2005-06-30

  The present invention relates to a patch comprising a drug-containing layer with low content of hormones, such as gestodene, and optionally an estrogen (e.g. ethinyl estradiol). Upon administering the patch to a woman, plasma levels of at least 1.0 ng/ml of Gestodene is achieved at steady state conditions without the need of incorporating penetration enhancers or permeation enhancers in the drug-containing layer. Satisfactorily plasma levels of the hormones is also achieved throughout a period of at least 1 week, making the patch applicable for being used in female contraception with the concept of administering the patch ones weekly.

  本发明涉及一种贴片，该贴片由含低含量激素（如孕烯）和可选雌激素（如炔雌醇）的药物层组成。妇女使用该贴片后，在稳态条件下，孕烯的血浆浓度至少可达到 1.0 纳克/毫升，而无需在含药层中加入渗透促进剂或渗透增强剂。在至少一周的时间里，激素的血浆浓度也能达到令人满意的水平，因此这种贴片可用于女性避孕，每周使用一次。
• Transdermal Delivery of Hormones without the Need of Penetration Enhancers
  申请人：Bayer Intellectual Property GmbH

  公开号：US20140109916A1

  公开（公告）日：2014-04-24

  The present invention relates to a patch comprising a drug-containing layer with low content of hormones, such as gestodene, and optionally an estrogen (e.g. ethinyl estradiol). Upon administering the patch to a woman, plasma levels of at least 1.0 ng/ml of Gestodene is achieved at steady state conditions without the need of incorporating penetration enhancers or permeation enhancers in the drug-containing layer. Satisfactorily plasma levels of the hormones is also achieved throughout a period of at least 1 week, making the patch applicable for being used in female contraception with the concept of administering the patch ones weekly.
• US5858394A
  申请人：——

  公开号：US5858394A

  公开（公告）日：1999-01-12
• US8668925B2
  申请人：——

  公开号：US8668925B2

  公开（公告）日：2014-03-11