venlafaxine besylate | 609345-58-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: venlafaxine besylate
• 英文别名: benzenesulfonic acid;1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexan-1-ol
• CAS: 609345-58-6
• 化学式: C₆H₆O₃S*C₁₇H₂₇NO₂
• 分子量: 435.585
• InChiKey: PTEFWGKCGCNHDM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.97
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  95.4
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  1-[2-氨基-1-(4-甲氧基苯基)乙基]环己醇 、 苯磺酸 在 聚合甲醛 、 甲酸 作用下， 以 水 为溶剂， 生成 venlafaxine besylate
  参考文献：
  名称：

  Venlafaxine besylate

  摘要：

  Venlafaxine besylate化合物相对于Venlafaxine hydrochloride具有一定优势，并且在制备药物组合物和治疗可用Venlafaxine的疾病和病情方面非常有用。Venlafaxine besylate可以轻松制备成为延长释放剂型，包括水凝胶片剂和其他基质片剂组合物。首选的片剂制备工艺包括热熔造粒。

  公开号：

  US20030195249A1

文献信息

• Low water-soluble venlafaxine salts
  申请人：SYNTHON BV

  公开号：US20030190353A1

  公开（公告）日：2003-10-09

  Low water soluble salts of venlafaxine, especially venlafaxine maleate, are provided. Such salts can provide a variety of dosage forms including hydrogel-based extended release dosage forms.

  提供了文拉法辛的低水溶性盐，尤其是文拉法辛酸盐。这些盐可以提供多种剂型，包括基于水凝胶的缓释剂型。
• [EN] VENLAFAXINE BASE<br/>[FR] BASE DE VENLAFAXINE
  申请人：SYNTHON BV

  公开号：WO2003082806A1

  公开（公告）日：2003-10-09

  The invention relates to a crystalline racemic venlafaxine base wherein said venlafaxine is in particle form having an average particle size within the range of 0.5 to 200 microns or a bulk density of at least 0.4 mg/ml, or a particular XRD pattern, to a process for making solid racemic venlafaxine base, which comprises precipitating racemic venlafaxine base from a solution of venlafaxine to form crystalline racemic venlafaxine base; wherein said precipitation is carried out in accordance with at least one of the following conditions: (i) said solution contains a combination of solvents comprising at least one organic polar solvent and at least one contrasolvent selected from water, an aliphatic hydrocarbon and an alicyclic hydrocarbon; or (ii) a seeding crystal of venlafaxine base is present.

  本发明涉及一种晶体外消旋文拉法辛碱基，其中所述文拉法辛以粒子形式存在，其平均粒径在0.5至200微米范围内或其堆积密度至少为0.4毫克/毫升，或具有特定的XRD图案，以制备固体外消旋文拉法辛碱基的方法，包括从文拉法辛溶液中沉淀外消旋文拉法辛碱基以形成晶体外消旋文拉法辛碱基；其中所述沉淀是根据以下至少一种条件进行的：（i）所述溶液含有至少一种有机极性溶剂和至少一种对比溶剂，所述对比溶剂选自水，脂肪烃和萜烃；或（ii）存在文拉法辛碱基的种晶。
• Venlafaxine base
  申请人：——

  公开号：US20030191347A1

  公开（公告）日：2003-10-09

  Venlafaxine base is obtained in pharmaceutically useful form. Two crystal forms of venlafaxine base are identified and a process of precipitating solid venlafaxine base is provided.

  Venlafaxine基质以药用形式获得。识别了Venlafaxine基质的两种晶体形式，并提供了一种沉淀固体Venlafaxine基质的过程。
• Venlafaxine-containing film-coated modified-release tablets
  申请人：Biovail Laboratories International S.r.l.

  公开号：EP2074993A1

  公开（公告）日：2009-07-01

  The present invention relates to a modified release composition of at least one form of venlafaxine, which is an enhanced absorption delayed controlled release composition. The composition comprises a core comprising at least one form of venlafaxine, less than 10% of a gelling agent and a pharmaceutically acceptable excipient. The composition further comprises a modified release coating which substantially surrounds the core which provides a delayed controlled release of the at least one form of venlafaxine.

  本发明涉及至少一种文拉法辛的改进释放组合物，它是一种增强吸收的延迟控释组合物。该组合物包括至少一种文拉法辛、少于 10%的胶凝剂和药学上可接受的赋形剂组成的核心。该组合物还包括一层改良释放涂层，该涂层基本上包围着核心，可延迟控制释放至少一种文拉法辛。
• Modified-release compositions of at least one form of venlafaxine
  申请人：Seth Pawan

  公开号：US20050244498A1

  公开（公告）日：2005-11-03

  The present invention relates to a modified release composition of at least one form of venlafaxine, which is an enhanced absorption delayed controlled release composition for oral administration suitable for once daily dosing. The composition comprises a core comprising at least one form of venlafaxine selected from the group consisting of venlafaxine, an active metabolite of venlafaxine, a pharmaceutically acceptable salt of venlafaxine, a pharmaceutically acceptable salt of an active metabolite of venlafaxine, and combinations thereof, and a pharmaceutically acceptable excipient. The composition further comprises a modified release coating which substantially surrounds the core. The compositions of the invention provide enhanced absorption delayed controlled release of the at least one form of venlafaxine such that the combined geometric mean ratio of the composition of the invention to the reference product for the AUC 0-t or the C max for venlafaxine and its active metabolite O-desmethylvenlafaxine is greater than 2 after first administration of the composition under fed or fasting conditions.

  本发明涉及至少一种文拉法辛的改进释放组合物，它是一种用于口服给药的增强吸收延迟控释组合物，适合每日给药一次。该组合物包含一个核心，该核心包含至少一种文拉法辛，该文拉法辛选自文拉法辛、文拉法辛的活性代谢物、文拉法辛的药学上可接受的盐、文拉法辛的活性代谢物的药学上可接受的盐及其组合，以及药学上可接受的赋形剂。本发明的组合物还包括一层改良释放涂层，该涂层基本上包围了核心。本发明的组合物能增强至少一种形式的文拉法辛的吸收延迟控释，从而使本发明组合物与参比产品的 AUC 0-t 或 最大值 大于 2。