环戊丙羟勃龙 | 1254-35-9

• 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: 环戊丙羟勃龙
• 中文别名: 氧宝龙戊丙酯；羟勃龙环戊丙酸酯
• 英文名称: Oxabolone cipionate
• 英文别名: [(8R,9S,10R,13S,14S,17S)-4-hydroxy-13-methyl-3-oxo-2,6,7,8,9,10,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl] 3-cyclopentylpropanoate
• CAS: 1254-35-9
• 化学式: C₂₆H₃₈O₄
• 分子量: 414.6
• InChiKey: KHKDIUPVDIEHAH-KXLSUQFWSA-N

物化性质

• 熔点：
  158-160°
• 比旋光度：
  D20 +30° (c = 1 in chloroform)

计算性质

• 辛醇/水分配系数(LogP)：
  5.7
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.846
• 拓扑面积：
  63.6
• 氢给体数：
  1
• 氢受体数：
  4

ADMET

代谢

前药奥沙波龙环戊酸酯转化为奥沙波龙。奥沙波龙然后代谢成4-羟基雌-4-烯-3,17-二酮（M2），这是通过氧化17-羟基团形成的最丰富的代谢物。4-羟基雌烷-3,17-二酮（M1）是通过还原A环双键以及氧化17-羟基团形成的。存在三种异构体化合物作为另一种代谢物，即3α,4-二羟基-5α-雌烷-17-酮，3α,4-二羟基-5β-雌烷-17-酮和3β,4-二羟基-5α-雌烷-17-酮。

The prodrug oxabolone cipionate is converted to oxabolone. Oxabolone is then metabolized into 4-Hydroxyestr-4-en-3,17-dione (M2) which is the most abundant metabolite via oxidation of the 17-hydroxyl group. 4-Hydroxyestran-3,17-dione (M1) is formed by reduction of the A ring double bond along with the oxidation of the 17-hydroxyl group. Three isomeric compounds exist as another metabolite, as the 3α,4-dihydroxy-5α-estran-17-one, 3α,4-dihydroxy-5β-estran-17-one, and 3β,4-dihydroxy-5α-estran-17-one.

来源:DrugBank

吸收、分配和排泄

• 消除途径

代谢物和奥沙波龙的未改变形式可以在尿液中检测到。

The metabolites and unchanged form of oxabolone can be detected in the urine.

来源:DrugBank

吸收、分配和排泄

• 清除

静脉注射氧代波龙癸酸盐后第一天的消除速度较慢，并在给药第五天达到快速排泄阶段，此时尿液中达到最高水平。

The elimination on the first day following intravenous injection of oxabolone cipionate is slow and reaches a rapid excretion phase with the maximum urinary level in the fifth day of administration.

来源:DrugBank

文献信息

• Stabilized aqueous suspensions for parenteral use
  申请人：PHARMACIA & UP JOHN S.p.A.

  公开号：US20030130245A1

  公开（公告）日：2003-07-10

  A pharmaceutical aqueous suspension formulation for parenteral administration having substantially stabilized pH, comprising a biologically active compound and a pH controlling effective concentration of L-Methionine. Preferably, the biologically active compound is a steroidal compound, for instance exemestane, medroxyprogesterone acetate and estradiol cypionate or a combination of medroxyprogesterone acetate and estradiol cypionate.

  一种用于肠外给药的水悬浮剂制剂，具有基本稳定的 pH 值，包含一种生物活性化合物和一种 pH 值控制有效浓度的 L-蛋氨酸。生物活性化合物最好是类固醇化合物，例如依西美坦、醋酸甲羟孕酮和环戊丙酸雌二醇或醋酸甲羟孕酮和环戊丙酸雌二醇的组合。
• Stabilized injectable suspension of a steroidal drug
  申请人：——

  公开号：US20030114430A1

  公开（公告）日：2003-06-19

  A parenterally deliverable composition is provided, comprising an aqueous medium having dispersed therein, in solid particulate form, a steroidal drug in a therapeutically effective amount. The aqueous medium comprises one or more wetting and/or suspending agents in an amount effective to provide controlled flocculation of the drug, at least one of the wetting and/or suspending agents being susceptible to oxidative degradation. The composition further comprises, as a component thereof or as an adjunct thereto, means for protecting the oxidative degradation susceptible agent from oxidative degradation.

  本发明提供了一种肠外给药组合物，它包括一种水性介质，其中分散有治疗有效量的固体颗粒状甾体药物。该水介质包含一种或多种润湿剂和/或悬浮剂，其有效量可控制药物的絮凝，润湿剂和/或悬浮剂中至少有一种易氧化降解。该组合物还包括保护易氧化降解剂不被氧化降解的装置，作为其组分或附属物。
• Stabilized steroidal suspension
  申请人：——

  公开号：US20030165568A1

  公开（公告）日：2003-09-04

  A pharmaceutical aqueous suspension formulation for parenteral administration having substantially stabilized pH, comprising a biologically active compound and a pH controlling effective concentration of a polyvinylpyrrolidone compound. Preferably the biologically active compound is a steroidal compound, for instance, exemestane, medroxyprogesterone acetate or estradiol cypionate or a combination of medroxyprogesterone acetate and estradiol cypionate.

  一种用于肠外给药的水悬浮液制剂，具有基本稳定的 pH 值，包含一种生物活性化合物和一种 pH 值控制有效浓度的聚乙烯吡咯烷酮化合物。生物活性化合物最好是类固醇化合物，例如依西美坦、醋酸甲羟孕酮或环丙酸雌二醇或醋酸甲羟孕酮和环丙酸雌二醇的组合。
• Ester and ether derivatives of 4-hydroxy-19-nortestosterone and a method for the regulation of athletic function in humans
  申请人：Nutri Sport Pharmacal, Inc.

  公开号：US20030199486A1

  公开（公告）日：2003-10-23

  This invention relates to a method of administering an effective extended release amount of at least one of the ester or ether derivatives of 4-hydroxy-19-nortestosterone for the regulation of athletic function in humans as a dietary supplement.

  本发明涉及一种作为膳食补充剂给药有效缓释量的至少一种 4-羟基-19-去甲睾酮的酯或醚衍生物的方法，用于调节人体的运动功能。
• STABILIZED STEROIDAL SUSPENSION
  申请人：PHARMACIA & UPJOHN S.p.A.

  公开号：EP1282401A2

  公开（公告）日：2003-02-12