丙利酸钾 | 49848-01-3

• 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
• 中文名称: 丙利酸钾
• 英文名称: Prorenoate
• 英文别名: 3-[(1R,2R,4R,10R,11S,14S,15R,18S)-15-hydroxy-10,14-dimethyl-7-oxo-15-pentacyclo[9.7.0.02,4.05,10.014,18]octadec-5-enyl]propanoic acid
• CAS: 49848-01-3
• 化学式: C₂₃H₃₂O₄
• 分子量: 372.5
• InChiKey: OHZWNMVYJJTNKU-VAFIVCJBSA-N

物化性质

• 沸点：
  560.4±50.0 °C(Predicted)
• 密度：
  1.24±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  27
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  74.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  坎利酮 、 地西淄酮 、 Mexrenoic acid 、 丙利酸钾 、 螺内酯 、 (4Α,5Α,17Β)-4,5-环氧-3,17-二羟基-4,17-二甲基雄甾-2-烯-2-氰 、 美螺利酮 、 Oxprenoate 、 螺利酮 、 (7a,17b)-7-(乙酰基硫代)-4',5'-二氢-螺[雄甾-4-烯-17,2'(3'H)-呋喃]-3-酮 、 α-prorenone 、 依普利酮 生成 坎利酸
  参考文献：
  名称：

  Pharmaceutical preparation comprising an active dispersed on a matrix

  摘要：

  本发明涉及制药技术领域，描述了一种新型的有利的活性成分制备方法。该新型制备方法适用于生产大量的药物剂型。在新型制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油三酯和脂肪酸酯等一种或多种赋形剂组成的基质中。

  公开号：

  US20070122474A1

文献信息

• Compositions comprising drospirenone moleculary dispersed
  申请人：Bayer Schering Pharma Aktiengesellschaft

  公开号：EP1980242A1

  公开（公告）日：2008-10-15

  The present invention relates to liquid pharmaceutical compositions comprising steroidal drugs, such as drospirenone, in molecularly dispersed form. The compositions are adapted for oral administration and preferably to be absorbed from the gastro-intestinal tract. Such compositions are found to have high bioavailability, good chemical stability, and fast in-vitro dissolution release and can be produced under conditions, which do not require costly equipment or safety guards.

  本发明涉及由甾体药物（如屈螺酮）以分子分散形式组成的液体药物组合物。这些组合物适合口服，最好能从胃肠道吸收。这种组合物具有生物利用度高、化学稳定性好、体外溶解释放快等特点，而且可以在不需要昂贵设备或安全防护装置的条件下生产。
• Stabilised supersaturated solid solutions of steroidal drugs
  申请人：Bayer Schering Pharma Aktiengesellschaft

  公开号：EP2087883A1

  公开（公告）日：2009-08-12

  The present invention relates to a powdery composition comprising a steroidal molecule; and a pharmaceutically acceptable carrier having a specific surface area of 200-1000 m2/g; wherein the steroidal molecule is dissolved in a solvent absorbed onto the surface of the pharmaceutically acceptable carrier and wherein the steroidal molecule is present in the solvent in a supersaturated concentration.

  本发明涉及一种粉末状组合物，该组合物包含类固醇分子；以及比表面积为 200-1000 m2/g 的药学上可接受的载体；其中，类固醇分子溶解在溶剂中，被吸收到药学上可接受的载体表面，并且类固醇分子以过饱和浓度存在于溶剂中。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• Molecular dispersions of drospirenone
  申请人：Funke Adrian

  公开号：US20050220825A1

  公开（公告）日：2005-10-06

  Described are pharmaceutical compositions comprising at least one steroidal drug such as a progestin (e.g. drospirenone, progesterone, eplerenone, etonogestrel) and/or an estrogen (estradiol and esters thereof) in molecularly dispersed form. The composition comprises a steroidal drug, preferably drospirenone, which is present in the composition in a non-particulate form. Preferably, the drug is present in a dissolved state in the excipient. The molecularly dispersed drug will be released very fast as dissolution takes place instantly when the dosage unit has disintegrated. Also described are methods for preparing the pharmaceutical compositions and methods of using the compositions.

  所述药物组合物包含至少一种类固醇药物，如分子分散形式的孕激素（如屈螺酮、黄体酮、依普利酮、依托孕烯）和/或雌激素（雌二醇及其酯类）。 组合物包含一种甾体药物，最好是屈螺酮，它以非颗粒形式存在于组合物中。 药物最好以溶解状态存在于赋形剂中。 分子分散的药物会很快释放出来，因为当剂量单位崩解时，溶解会立即发生。 此外，还介绍了药物组合物的制备方法和组合物的使用方法。
• Stabilised supersaturated solids of lipophilic drugs
  申请人：Funke Adrian

  公开号：US20050207990A1

  公开（公告）日：2005-09-22

  Methods for improving solubility and bioavailability of lipophilic compounds are described. Particularly, described are stabilized superstaturated solid solutions, particularly in power form, of lipophilic drugs, such as steroidal molecules.

  本文介绍了提高亲脂化合物溶解度和生物利用度的方法。特别是描述了亲脂性药物（如类固醇分子）的稳定过饱和固体溶液，尤其是动力形式的溶液。