1,13-dimethyl-10-(2-phenylethyl)-10-azatricyclo[7.3.1.02,7]trideca-2(7),3,5-trien-4-ol;hydron;bromide

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 6,7-苯并吗啡烷
• 英文名称: 1,13-dimethyl-10-(2-phenylethyl)-10-azatricyclo[7.3.1.02,7]trideca-2(7),3,5-trien-4-ol;hydron;bromide
• 化学式: C22H28BrNO
• 分子量: 402.4
• InChiKey: MNMGNPZLUMHSKK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.74
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  23.5
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• Analgesics for nasal administration
  申请人：Birch John Phillip

  公开号：US20050142072A1

  公开（公告）日：2005-06-30

  An analgesic and a delivery agent are combined in a pharmaceutical composition such that, on introduction into the nasal cavity of a patient to be treated, the analgesic may be delivered to the bloodstream to produce within 30 minutes a therapeutic plasma concentration, C ther , of 0.2 ng/ml or greater which is maintained for a duration T maint of at least 2 hours. The analgesic may be an opioid analgesic or a non-steroidal anti-inflammatory drug.

  一种镇痛剂和传递剂被组合在一种制药组合物中，以便在引入到需要治疗的患者的鼻腔中时，镇痛剂可以被传递到血液中，在30分钟内产生治疗性血浆浓度Cther，达到0.2ng/ml或更高，并且维持至少2小时的持续时间Tmaint。镇痛剂可以是阿片类镇痛剂或非甾体抗炎药。
• Analgesics
  申请人：Birch John Phillip

  公开号：US20070231269A1

  公开（公告）日：2007-10-04

  An analgesic and a delivery agent are combined in a pharmaceutical composition such that, on introduction into the nasal cavity of a patient to be treated, the analgesic may be delivered to the bloodstream to produce within 30 minutes a therapeutic plasma concentration, C ther , of 0.2 ng/ml or greater which is maintained for a duration T maint of at least 2 hours. The analgesic may be an opioid analgesic or a non-steroidal anti-inflammatory drug.

  一种镇痛剂和输送剂被结合在一种制药组合物中，这样，在将其引入要治疗的患者的鼻腔时，镇痛剂可以被输送到血液中，在30分钟内产生治疗性血浆浓度Cther，至少为0.2 ng/ml，并且该浓度可维持至少2小时的持续时间Tmaint。该镇痛剂可以是阿片类镇痛剂或非甾体抗炎药。
• Oral pharmaceutical composition
  申请人：Euroceltique S.A.

  公开号：EP0205282A2

  公开（公告）日：1986-12-17

  A sustained release, oral pharmaceutical composition in solid unit dosage form, for application to the mucosa of the oral or nasal cavity, comprises compressed, mucosa adhesive cellulose, coated granules, the granules comprising a drug, a higher aliphatic alcohol and a hydrated water soluble hydroxyalkyl cellulose. Preferably the composition is in the form of a buccal tablet, especially a kidney shaped buccal tablet. Preferred materials are morphine as the drug, hydroxypropyl cellulose as the mucosa adhesive cellulose, cetostearyl alcohol as the aliphatic alcohol and hydroxyethyl cellulose as the water soluble cellulose. The composition has enhanced adherent properties (to the mucosa) and prolongs the bioavailability of the drug.

  一种用于口腔或鼻腔粘膜的固体单位剂型缓释口服药物组合物，由压缩的粘膜粘附性纤维素包衣颗粒组成，颗粒由药物、高级脂肪醇和水合水溶性羟烷基纤维素组成。 组合物最好是口腔片剂，特别是肾形口腔片剂。优选的材料有作为药物的吗啡、作为粘膜粘合纤维素的羟丙基纤维素、作为脂肪醇的鲸蜡硬脂醇和作为水溶性纤维素的羟乙基纤维素。 该组合物具有更强的粘附性（粘膜），并能延长药物的生物利用度。
• Drug delivery device, its preparation and use
  申请人：Smith & Nephew plc

  公开号：EP0250125A2

  公开（公告）日：1987-12-23

  A device suitable for the topical administration of a pharmacologically active agent to an animal is described. The device comprises an active agent impermeable barrier layer, a reservoir containing the active agent which is in contact with the inner surface of the barrier layer and a removable protector layer in contact with the other surface of the reservoir. The reservoir comprises a fibrous mat into which the pharmacologically active agent is incorporated either by dissolving in the polymer forming the mat or by impregnation of a preformed mat. Alternative forms of the reservoir comprise a fibre mat coated on a skin contacting surface with a pressure sensitive adhesive and a fibre mat contained within a gel matrix. The device may be used to deliver nitroglycerin, oxybutynin or phenazocine transdermally.

  本文描述了一种适用于对动物局部施用药理活性剂的装置。该装置包括一个不透活性剂的阻隔层、一个与阻隔层内表面接触的含有活性剂的储液器和一个与储液器另一表面接触的可移动保护层。储液器由纤维毡组成，药理活性剂通过溶解在形成纤维毡的聚合物中或通过浸渍预制纤维毡的方式加入到纤维毡中。储液器的另一种形式包括在与皮肤接触的表面涂上压敏粘合剂的纤维毡和包含在凝胶基质中的纤维毡。该装置可用于透皮给药硝酸甘油、奥昔布宁或苯那佐辛。
• Pharmaceutical formulations for dry powder inhalers
  申请人：Vectura Limited

  公开号：EP1829533A2

  公开（公告）日：2007-09-05

  A powder for use in a dry powder inhaler comprises: i) a fraction of fine particle size constituted by a mixture of physiologically acceptable excipient and an additive; ii) a fraction of coarse particles; and iii) at least one active ingredient. The powder is suitable for efficacious delivery of active ingredients into the low respiratory tract of patients suffering from pulmonary diseases such as asthma. In particular, the invention provides a formulation to be administered as dry powder for inhalation which is freely flowable, can be produced in a simple way, is physically and chemically stable and capable of delivering accurate doses and/or high fine particle fraction of low strength active ingredients by using a high- or medium resistance device.

  一种用于干粉吸入器的粉末包括：i) 由生理上可接受的赋形剂和添加剂的混合物构成的细颗粒部分；ii) 粗颗粒部分；iii) 至少一种活性成分。这种粉末适用于向哮喘等肺部疾病患者的低呼吸道有效输送活性成分。特别是，本发明提供了一种可作为吸入用干粉给药的制剂，该制剂可自由流动，生产工艺简单，物理和化学性质稳定，能够通过使用高阻力或中等阻力装置输送精确剂量和/或高细颗粒部分的低强度活性成分。