butorphanol tartrate | 58786-99-5

• 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: butorphanol tartrate
• 英文别名: butorphanol hydrogen tartrate；17-(cyclobutylmethyl)morphinan-3,14-diyl (S-(R*,R*))-2,3-dihydroxysuccinate；Torbugesic；(1S,9R,10S)-17-(cyclobutylmethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-triene-4,10-diol;2,3-dihydroxybutanedioic acid
• CAS: 58786-99-5
• 化学式: C₄H₆O₆*C₂₁H₂₉NO₂
• 分子量: 477.555
• InChiKey: GMTYREVWZXJPLF-SXWPHCFWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.24
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.68
• 拓扑面积：
  159
• 氢给体数：
  6
• 氢受体数：
  9

ADMET

毒理性

• 肝毒性

丁溴东莨菪碱治疗期间尚未见与血清酶水平升高或特异质、临床明显的肝脏损伤有关联。它通常仅用于短期治疗急性疼痛，而且对于长期使用的经验有限。 关于丁溴东莨菪碱的安全性和潜在肝毒性的参考资料，请参见“阿片类药物”概述部分。 药物类别：阿片类药物

Therapy with butorphanol has not been linked to serum enzyme elevations during therapy or to instances of idiosyncratic, clinically apparent liver injury. It is generally given for short periods of time for acute pain only and experience with prolonged use is limited. References on the safety and potential hepatotoxicity of butorphanol are given in the Overview section of the Opioids. Drug Class: Opioids

来源:LiverTox

安全信息

• 储存条件：
  库房应保持通风、低温和干燥，并与食品原料类分开存放。

反应信息

• 作为反应物：
  描述：

  butorphanol tartrate 、 sorbitan Trioleate 生成 布托啡诺
  参考文献：
  名称：

  Butorphanol sustained release formulations

  摘要：

  本发明提供了受控的、持续释放的丁丙诺啡制剂。这些制剂可以是丁丙诺啡游离基的水悬浮液或丁丙诺啡盐的油悬浮液。本发明还提供了使用这些制剂提供长期镇痛的方法。

  公开号：

  US06197344B1

文献信息

• [EN] AN IMPROVED PROCESS FOR THE PREPARATION OF BUTORPHANOL TARTRATE<br/>[FR] PROCÉDÉ DE PRÉPARATION AMÉLIORÉ DE TARTRATE DE BUTORPHANOL
  申请人：HIKAL LTD

  公开号：WO2017168444A1

  公开（公告）日：2017-10-05

  The present invention relates to an improved process for the preparation of Butorphanol tartrate of formula (I),

  这项发明涉及一种改进的制备盐酸布托啡诺的方法，其化学式为(I)。
• IONTOPHORESIS DEVICE
  申请人：HISAMITSU PHARMACEUTICAL CO. INC.

  公开号：EP0705619A1

  公开（公告）日：1996-04-10

  To avoid a reduction of the conductivity in iontophoresis due to the electrical decomposition and the changes in chemical properties of the electrodes themselves, covering by an electrical insulator, and to prevent a drop in the transport rate due to ions freed from the electrode. Provision is made of an electrode structure provided integrally with a reversible electrode and an auxiliary electrode for regeneration of the same and a regeneration current conducting means for conducting a current for regeneration of the reversible electrode when the therapeutic current is off, or the invention is comprised of a reversible electrode and an ion exchange membrane difficult for ions freed from that electrode to penetrate.

  为了避免在离子透入疗法中由于电极本身的电分解和化学性质的变化而导致电导率下降，需要用电绝缘体覆盖，并防止由于离子从电极中释放出来而导致传输速率下降。本发明提供了一种电极结构，该电极结构中集成有一个可逆电极和一个用于再生的辅助电极，以及一个再生电流传导装置，用于在治疗电流关闭时传导电流，使可逆电极再生，或者本发明由一个可逆电极和一个离子交换膜组成，从该电极释放的离子难以渗透。
• Drug administration composition for iontophoresis
  申请人：HISAMITSU PHARMACEUTICAL CO. INC.

  公开号：EP0813879A2

  公开（公告）日：1997-12-29

  A drug administration composition which is adapted for use in iontophoresis comprises a drug to be ionized and a humectant. The humectant is made, for example, of an amide with or without a co-humectant such as an amino acid or its derivative. The composition is effective in suppressing evaporation of moisture from a drug solution, keeping the electric conductivity over a long time, and transdermal administration of a drug through iontophoresis.

  一种适用于离子透入疗法的给药组合物由离子化药物和保湿剂组成。保湿剂例如由酰胺和或不含辅助保湿剂（如氨基酸或其衍生物）组成。该组合物可有效抑制药物溶液中水分的蒸发，长时间保持导电性，并通过离子透入疗法透皮给药。
• A device structure for iontophoresis
  申请人：HISAMITSU PHARMACEUTICAL CO. INC.

  公开号：EP0813887A2

  公开（公告）日：1997-12-29

  An iontophoretic device structure of the dissolution-on-use type is provided, wherein an ionized drug is transdermally or transmucosally administered into a living body. The device structure comprises (a) a non-polarizable electrode, (b) a hydrophilic, polymeric gel layer dispersing an ion exchange resin which is able to specifically inhibit the movement of ions dissolved out from the electrode being in use, and (c) a drug layer retaining a drug in a dry condition in a drug retaining membrane, wherein when said device is in use, said drug layer is brought into contact with said hydrophilic, polymeric gel layer so that said drug in the dry condition is dissolved. A humectant may be contained in the hydrophilic, polymeric gel layer and/or the drug layer.

  本发明提供了一种使用即溶型离子渗透装置结构，可将离子化药物经皮或经粘膜注入活体。该装置结构包括：(a) 一个不可极化的电极；(b) 一个亲水性聚合物凝胶层，该凝胶层分散有一种离子交换树脂，该树脂能够特异性地抑制从使用中的电极溶出的离子的移动；(c) 一个药物层，该药物层将处于干燥状态的药物保留在药物保留膜中，当使用所述装置时，所述药物层与所述亲水性聚合物凝胶层接触，从而使处于干燥状态的所述药物溶解。亲水性聚合物凝胶层和/或药物层中可能含有保湿剂。
• ADHESIVE PREPARATIONS
  申请人：HISAMITSU PHARMACEUTICAL CO. INC.

  公开号：EP1074251A1

  公开（公告）日：2001-02-07

  Adhesive preparations with improved percutaneous absorption of physiologically active substances, in particular, matrix adhesive preparations containing a base drug salt and an organic acid salt having an mean diameter of from 0.1 to 100 µm are provided.

  提供了可改善生理活性物质经皮吸收的粘合剂制剂，特别是含有平均直径为 0.1 至 100 微米的碱基药物盐和有机酸盐的基质粘合剂制剂。