Oxycodone phosphate | 1211844-14-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 菲及其衍生物
• 英文名称: Oxycodone phosphate
• 英文别名: (4R,4aS,7aR,12bS)-4a-hydroxy-9-methoxy-3-methyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one;phosphoric acid
• CAS: 1211844-14-2
• 化学式: C18H24NO8P
• 分子量: 413.4
• InChiKey: TZKVACZYAHJHRA-RKXJKUSZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.12
• 重原子数：
  28
• 可旋转键数：
  1
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  137
• 氢给体数：
  4
• 氢受体数：
  9

文献信息

• [EN] A METHOD FOR PREPARING OXYCODONE<br/>[FR] PROCÉDÉ DE PRÉPARATION D'OXYCODONE
  申请人：JOHNSON MATTHEY PLC

  公开号：WO2014022733A1

  公开（公告）日：2014-02-06

  The present invention provides a process for preparing an oxycodone acid adduct, said process comprising hydrogenating an aqueous solution of 14-hydroxycodeinone and an acid to form a solution of the oxycodone acid adduct, wherein the hydrogenation is carried out at one or more temperatures greater than ambient temperature in the presence of a hydrogenation catalyst and hydrogen gas, wherein the solution of oxycodone acid adduct comprises 6α-oxycodol in an amount ≤ about 0.800 area % as determined by HPLC.

  本发明提供了一种制备盐酸氧考酮加合物的方法，该方法包括将14-羟基可待因的水溶液和酸氢化以形成盐酸氧考酮加合物的溶液，其中氢化是在存在氢化催化剂和氢气的条件下，在大于环境温度的一个或多个温度下进行的，其中盐酸氧考酮加合物的溶液包含≤约0.800面积％的6α-氧考酚，如HPLC所确定的。
• PROCESS
  申请人：JOHNSON MATTHEY PUBLIC LIMITED COMPANY

  公开号：US20140045876A1

  公开（公告）日：2014-02-13

  The present invention provides a process for preparing an oxycodone acid adduct, said process comprising hydrogenating an aqueous solution of 14-hydroxycodeinone and an acid to form a solution of the oxycodone acid adduct, wherein the hydrogenation is carried out at one or more temperatures greater than ambient temperature in the presence of a hydrogenation catalyst and hydrogen gas, wherein the solution of oxycodone acid adduct comprises 6α-oxycodol in an amount ≦about 0.800 area % as determined by HPLC.

  本发明提供了一种制备盐酸氧考酮加合物的方法，该方法包括在氢化催化剂和氢气存在下，在一个或多个高于环境温度的温度下，将14-羟基可待因和酸的水溶液氢化成盐酸氧考酮加合物的溶液，其中所述的氢化反应在高于环境温度的一个或多个温度下进行，所述的盐酸氧考酮加合物的溶液中包含6α-氧考酮的含量≦约0.800面积% ，由HPLC测定。
• Dosage forms and compositions for osmotic delivery of variable dosages of oxycodone
  申请人：——

  公开号：US20030224051A1

  公开（公告）日：2003-12-04

  Dosage forms, compositions and methods for the controlled release of oxycodone over a prolonged period of time are described. The present invention discloses a novel means for delivering varying doses of oxycodone using a drug composition having only oxycodone, a polymer carrier and varying amounts of salt to provide a particular viscosity of the hydrated drug core for delivery of the drug at the desired release rate. The present invention functions by modulating the viscosity of the hydrated drug layer in operation by the addition or reduction of salts in the drug composition. The system is independent of solubility enhancers or pH modifiers. The sustained release dosage forms provide therapeutically effective average steady-state plasma oxycodone concentrations when administered once per day.

  本发明描述了长时间控制释放羟考酮的剂型、组合物和方法。本发明公开了一种新颖的方法，可使用仅含有羟考酮、聚合物载体和不同量盐的药物组合物来递送不同剂量的羟考酮，以提供水合药物核心的特定粘度，从而以所需的释放速率递送药物。本发明通过在药物组合物中添加或减少盐来调节水合药物层的粘度。该系统与溶解度增强剂或 pH 值调节剂无关。这种缓释剂型每天给药一次，可提供治疗有效的平均稳态血浆羟考酮浓度。
• Methods and dosage forms for controlled delivery of oxycodone
  申请人：——

  公开号：US20040010000A1

  公开（公告）日：2004-01-15

  Dosage forms and methods for the controlled release of oxycodone over a prolonged period of time are described. The sustained release dosage forms provide therapeutically effective average steady-state plasma oxycodone concentrations when administered once per day. This once-a-day dosing regimen results in only one peak plasma oxycodone concentration occurrence in each 24 hour period that occurs at a later time after administration and exhibits a lesser magnitude than the peak plasma oxycodone concentration that occurs following administration of oxycodone in an immediate-release dosage form and other prior art extended release dosage forms.

  本文介绍了长时间控制释放羟考酮的剂型和方法。这种缓释剂型每天给药一次，可提供治疗有效的平均稳态血浆羟考酮浓度。这种每天一次的给药方案导致在每 24 小时内仅出现一次血浆羟考酮浓度峰值，该峰值出现在给药后的较晚时间，其幅度小于在速释剂型和其他现有技术的缓释剂型中给药后出现的血浆羟考酮浓度峰值。
• Once-a-day, oral, controlled-release, oxycodone dosage forms
  申请人：Hwang Stephen

  公开号：US20050106249A1

  公开（公告）日：2005-05-19

  Oxycodone formulations are provided which produce substantially flat in vivo steady state plasma profiles. Tolerance levels associated with such profiles and tolerance levels associated with biphasic profiles are shown not to be statistically different. The substantially flat in vivo steady state plasma profiles are produced by dosage forms having substantially zero order in vitro release profiles. Such release profiles produce low single dose in vivo C max levels which can reduce the probability of adverse side effects.

  所提供的羟考酮制剂可产生基本平坦的体内稳态血浆曲线。与这种曲线相关的耐受水平和与双相曲线相关的耐受水平在统计学上没有差异。体内稳态血浆曲线基本平坦是由体外释放曲线基本为零阶的剂型产生的。这种释放曲线可产生较低的单剂量体内 C 最大值 水平，从而降低了不良副作用的发生概率。