Nabiximols | 56575-23-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: Nabiximols
• 英文别名: (6aR,10aR)-6,6,9-trimethyl-3-pentyl-6a,7,8,10a-tetrahydrobenzo[c]chromen-1-ol;2-[(1R,6R)-3-methyl-6-prop-1-en-2-ylcyclohex-2-en-1-yl]-5-pentylbenzene-1,3-diol
• CAS: 56575-23-6
• 化学式: C42H60O4
• 分子量: 628.9
• InChiKey: SSNHGLKFJISNTR-DYSNNVSPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  11.58
• 重原子数：
  46
• 可旋转键数：
  10
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  69.9
• 氢给体数：
  3
• 氢受体数：
  4

ADMET

代谢

THC和CBD在肝脏中被多种细胞色素P450同工酶代谢，包括CYP2C9、CYP2C19、CYP2D6和CYP3A4。它们可以在脂肪组织中储存长达四周，然后以亚治疗水平缓慢释放回血液中，并通过肾脏和胆道系统进行代谢。

THC and CBD are metabolized in the liver by a number of cytochrome P450 isoenzymes, including CYP2C9, CYP2C19, CYP2D6 and CYP3A4. They may be stored for as long as four weeks in the fatty tissues from which they are slowly released at sub-therapeutic levels back into the blood stream and metabolized via the renal and biliary systems.

来源:DrugBank

吸收、分配和排泄

• 吸收

个体受试者的血浆浓度数据和药代动力学参数显示出很高的受试者间变异性。在单次颊部给药后，CBD和THC的最大血浆浓度通常在两到四个小时内出现。与吸入吸烟的大麻相比，通过颊部给药时，血液中THC和其他大麻素的水平较低。由于吸收较慢，快速重新分布到脂肪组织，并且部分THC在首次通过肝脏代谢为11-OH-THC，一种具有精神活性的代谢物，因此血液中的浓度低于吸入相同剂量时的浓度。

Individual subject plasma concentration data and pharmacokinetic parameters show a high degree of inter-subject variability. Following a single buccal administration, maximum plasma concentrations of both CBD and THC typically occur within two to four hours. When administered buccally, blood levels of THC and other cannabinoids are lower compared with inhalation of smoked cannabis. The resultant concentrations in the blood are lower than those obtained by inhaling the same dose because absorption is slower, redistribution into fatty tissues is rapid and additionally some of the THC undergoes hepatic first-pass metabolism to 11-OH-THC, a psycho-active metabolite.

来源:DrugBank

吸收、分配和排泄

• 消除途径

纳比西莫斯通过尿液和粪便排出。

Nabiximols is excreted in the urine and faeces.

来源:DrugBank

吸收、分配和排泄

• 分布容积

大麻素在全身分布；它们高度溶于脂肪，并在脂肪组织中积累。大麻素从脂肪组织中的释放负责其延长的终末消除半衰期。

Cannabinoids are distributed throughout the body; they are highly lipid soluble and accumulate in fatty tissue. The release of cannabinoids from fatty tissue is responsible for the prolonged terminal elimination half-life.

来源:DrugBank

文献信息

• METHOD FOR PRODUCING A PHARMACEUTICAL COMPOSITION OF POLYMERIC NANOPARTICLES FOR TREATING NEUROPATHIC PAIN CAUSED BY PERIPHERAL NERVE COMPRESSION
  申请人：UNIVERSIDAD DE SEVILLA

  公开号：US20180042860A1

  公开（公告）日：2018-02-15

  The object of the present invention is the method for obtaining a pharmaceutical composition of polymeric nanoparticles for the treatment of neuropathic pain caused by peripheral nerve compression, related to the pharmaceutical industry and nanotechnology. The invention particularly relates to a novel system for orally administering the cannabinoid drug CB13 based on polymeric nanoparticles capable of alleviating pain for nine days following a single oral administration of an aqueous suspension of nanoparticles.
• CANNABIS BASED THERAPEUTIC AND METHOD OF USE
  申请人：SPIRTOS Nicola Michael

  公开号：US20210023044A1

  公开（公告）日：2021-01-28

  The present disclosure relates to cannabinoid-based therapeutics, and their use in treating pain, e.g., chronic pain. The present disclosure also relates to cannabinoid-based therapeutics, and their use in treating opioid addiction.