Morphine 3-phosphate | 51065-90-8

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 吗啡烷
• 英文名称: Morphine 3-phosphate
• 英文别名: [(4R,4aR,7S,7aR,12bS)-7-hydroxy-3-methyl-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-9-yl] dihydrogen phosphate
• CAS: 51065-90-8
• 化学式: C₁₇H₂₀NO₆P
• 分子量: 365.3
• InChiKey: PBRNFPZMSRCMQS-KOFBORESSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.8
• 重原子数：
  25
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  99.5
• 氢给体数：
  3
• 氢受体数：
  7

文献信息

• Osmotic extented-release dosage form
  申请人：ALZA CORPORATION

  公开号：EP1384471A1

  公开（公告）日：2004-01-28

  A membrane system for use in an extended release dosage form comprises an internal compartment (15) defined by the membrane system, an interior wall (16) surrounding the internal compartment, wherein the fluid permeability of the interior wall is responsive to osmolarity of an osmotic core (18) comprised in the internal compartment, and a fluid-permeable exterior wall (12) surrounding the interior wall.

  一种用于缓释剂型的膜系统，包括由膜系统限定的内室（15）、围绕内室的内壁（16），其中内壁的液体渗透性与内室中渗透核（18）的渗透压有关，以及围绕内壁的液体可渗透外壁（12）。
• Osmotic extended-release dosage form
  申请人：ALZA CORPORATION

  公开号：EP1600154A1

  公开（公告）日：2005-11-30

  A dosage form comprising a composition comprising a drug surrounded by an interior and an exterior wall with an exit for administering the drug to a patient; and a method of using the dosage form are disclosed for an indicated therapy.

  本发明公开了一种剂型，该剂型包括由药物组成的组合物，组合物由内壁和外壁包围，外壁设有出口，用于向患者施用药物；还公开了使用该剂型进行指定治疗的方法。
• MEDICINAL COMPOSITION FOR TRANSDERMAL ABSORPTION, MEDICINAL COMPOSITION STORING UNIT AND TRANSDERMAL ABSORPTION PREPARATION USING THE SAME
  申请人：Teika Pharmaceutical Co., Ltd.

  公开号：EP2123274A1

  公开（公告）日：2009-11-25

  An object of the invention is to provide a transdermal absorption preparation capable of sustaining the blood morphine concentration at an effective level over at least 48 hours, etc. This transdermal absorption preparation comprises a medicinal composition for transdermal absorption in which an active ingredient selected from morphine and salts thereof is blended in such an amount as corresponding to the saturation solubility or more in an active ingredient-holding vehicle having fluidity at a temperature around the human skin surface temperature and at least a portion of the active ingredient is held in a crystalline form, characterized in that, in the case where a preparation obtained from the above-described medicinal composition for transdermal absorption is applied to the uninjured skin of the back of a white rabbit having been shaven with electrical clippers for 72 hours, the available amount of the active ingredient per single dose of the preparation is from 10 mg to 400 mg in terms of morphine base, and the plasma concentrations of the active ingredient 24 hours and 48 hours after the application of the preparation under the above-described conditions are each at least 40 ng/mL in terms of morphine base, and so on.

  本发明的目的是提供一种透皮吸收制剂，能够在至少 48 小时内将血液中的吗啡浓度维持在有效水平等。这种透皮吸收制剂包括一种用于透皮吸收的药物组合物，其中的活性成分选自吗啡及其盐类，其用量相当于在人体皮肤表面温度附近具有流动性的活性成分保持载体中的饱和溶解度或更高，并且至少有一部分活性成分以结晶形式保持，其特征在于、将上述药物组合物制得的透皮吸收制剂涂抹在用电剪剃过毛的白兔背部未受伤的皮肤上 72 小时的情况、以吗啡碱计，每次单剂量制剂中有效成分的可用量为 10 毫克至 400 毫克；以吗啡碱计，在上述条件下使用制剂 24 小时和 48 小时后，有效成分的血浆浓度均至少为 40 纳克/毫升，等等。
• Complexes of phosphate derivatives
  申请人：——

  公开号：US20040052754A1

  公开（公告）日：2004-03-18

  There is provided a composition comprising the reaction product of: (a) one or more phosphate derivatives of one or more hydroxylated actives; and (b) one or more complexing agents selected from the group consisting of amphoteric surfactants, cationic surfactants, amino acids having nitrogen functional groups and proteins rich in these amino acids.

  提供了一种组合物，该组合物包含以下物质的反应产物 (a) 一种或多种羟化活性物质的一种或多种磷酸盐衍生物；和 (b) 一种或多种络合剂，选自由两性表面活性剂、阳离子表面活性剂、具有氮官能团的氨基酸和富含这些氨基酸的蛋白质组成的组。
• Transdermal transport of compounds
  申请人：West Michael Simon

  公开号：US20050089495A1

  公开（公告）日：2005-04-28

  There is provided a topical formulation comprising an effective skin-penetrating amount of one or more phosphate derivatives of one or more pharmaceutical hydroxy compounds and an acceptable carrier.

  本文提供了一种局部制剂，它包含有效皮肤渗透量的一种或多种药用羟基化合物的磷酸酯衍生物和可接受的载体。