Methyloctatropine bromide | 80-50-2

• 物质功能分类: 天然产物 - 生物碱
• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 托烷生物碱
• 英文名称: Methyloctatropine bromide
• 英文别名: (8,8-dimethyl-8-azoniabicyclo[3.2.1]octan-3-yl) 2-propylpentanoate;bromide
• CAS: 80-50-2
• 化学式: C17H32BrNO2
• 分子量: 362.3
• InChiKey: QSFKGMJOKUZAJM-UHFFFAOYSA-M

物化性质

• 熔点：
  329°
• 溶解度：
  可溶于氯仿（少许）、甲醇（少许）
• 颜色/状态：
  CRYSTALS FROM ACETONE
• 气味：
  PROBABLY ODORLESS
• 味道：
  BITTER TASTE
• 稳定性/保质期：

  STABLE IN LIGHT, HEAT, & AIR.

计算性质

• 辛醇/水分配系数(LogP)：
  0.52
• 重原子数：
  21
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.94
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  3

ADMET

代谢

肝脏的，通过酶促水解。

Hepatic, by enzymatic hydrolysis.

来源:DrugBank

毒理性

• 相互作用

食物减少了大鼠对溴化甲基阿尼索特平的吸收速率，且有证据表明存在可饱和过程，影响这种化合物的肠道吸收。

RATE OF ABSORPTION OF ANISOTROPINE METHYL BROMIDE IS REDUCED BY FOOD IN RAT, & THERE IS EVIDENCE OF SATURABLE PROCESS, INFLUENCING INTESTINAL ABSORPTION OF THIS CMPD.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

...抗胆碱能药物，如阿尼索特罗平...预计会与地高辛发生相互作用.../可能导致血清地高辛水平升高/。 /阿尼索特罗平/

...ANTICHOLINERGIC AGENTS, SUCH AS ANISOTROPINE...WOULD BE EXPECTED TO INTERACT WITH DIGOXIN.../MAY CAUSE INCR SERUM DIGOXIN LEVELS/. /ANISOTROPINE/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

地西泮与甲溴辛托品相互作用，在减少隔离兔空肠的自发和刺激胃肠动力以及在兔结肠和狗胃袋的体内方面表现积极。

DIAZEPAM & OCTATROPINE METHYLBROMIDE INTERACTED POS IN REDUCING SPONTANEOUS & STIMULATED GI MOTILITY IN ISOLATED RABBIT JEJUNUM & IN VIVO IN RABBIT COLON & DOG GASTRIC POUCH.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

抗胆碱药通过尿液排泄可能会因为尿液碱化而延迟，使用尿液碱化剂如：含钙和/或镁的抗酸剂、碳酸酐酶抑制剂、柠檬酸盐、碳酸氢钠，可能会增强抗胆碱药的治疗效果和/或副作用。/抗胆碱药、解痉药/

Urinary excretion of anticholinergics may be delayed by the alkalinization of the urine, /with the use of urinary alkalizers such as: calcium- and/or magnesium-containing antacids, carbonic anhydrase inhibitors, citrates, sodium bicarbonate/ thus potentiating the anticholinergics' therapeutic and/or side effects. /Anticholinergics, antispasmodics/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

...部分副作用在高剂量后出现是由于神经节阻滞。...毒性剂量...产生...抗胆碱能中毒的典型症状，并伴有神经节阻滞的附加效果，罕见情况下还会出现神经肌肉阻滞，但通常不会显著涉及中枢神经系统。/季铵化合物/

...SOME OF SIDE EFFECTS SEEN AFTER HIGH DOSES ARE DUE TO GANGLIONIC BLOCKADE. ... TOXIC DOSES...PRODUCE...USUAL MANIFESTATIONS OF ANTIMUSCARINIC POISONING WITH ADDNL EFFECTS OF GANGLIONIC & RARELY, NEUROMUSCULAR BLOCK, BUT USUALLY WITHOUT SIGNIFICANT CNS INVOLVEMENT. /QUATERNARY AMMONIUM CMPD/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

• 吸收

胃肠吸收差且不规则。口服剂量的总吸收率约为10%至25%。

Gastrointestinal absorption is poor and irregular. Total absorption after an oral dose is about 10 to 25%.

来源:DrugBank

吸收、分配和排泄

口服给药后吸收差且不稳定...穿透结膜的能力也很差，以至于...这类化合物在眼科学中价值有限。中枢作用通常不足，因为这些药物不易通过血脑屏障。...关于命运和排泄所知甚少.../季铵化合物/

...POORLY & UNRELIABLY ABSORBED AFTER ORAL ADMIN... PENETRATION OF CONJUNCTIVA IS ALSO POOR, SO THAT...CMPD ARE OF LITTLE VALUE IN OPHTHALMOLOGY. CENTRAL EFFECTS ARE GENERALLY LACKING, BECAUSE THESE AGENTS DO NOT READILY PASS BLOOD-BRAIN BARRIER. ...LITTLE...KNOWN OF FATE & EXCRETION... /QUATERNARY AMMONIUM CMPD/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

全身autoradiography的小鼠SC、口服或IP剂量的抗痉挛药、[(14)C]anisotropine methbromide表明，腹膜外剂量主要分布在排泄器官(肾、肝、唾液腺和肠)。

WHOLE-BODY AUTORADIOGRAPHY OF MICE GIVEN SC, ORAL, OR IP DOSES OF ANTISPASMODIC, [(14)C]ANISOTROPINE METHBROMIDE SHOWED THAT PARENTERAL DOSES WERE DISTRIBUTED MAINLY IN EXCRETORY ORGANS (KIDNEYS, LIVER, SALIVARY GLANDS, & INTESTINES).

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

一些14C标记的阿尼索托品甲溴盐在给予小鼠后存在于胃粘膜、胰腺、输卵管、子宫和输精管中。这种阳离子不太可能轻易通过生物膜扩散，似乎不会轻易穿过血脑屏障、胎盘屏障或胃肠道上皮。

SOME (14)C /ANISOTROPINE METHBROMIDE/ WAS...PRESENT IN STOMACH MUCOSA, PANCREAS, OVIDUCTS, UTERUS, & SPERMATIC DUCTS /AFTER ADMIN TO MICE/. CATION WOULD NOT BE EXPECTED TO DIFFUSE EASILY ACROSS BIOLOGICAL MEMBRANES...DID NOT APPEAR READILY TO CROSS BLOOD-BRAIN OR PLACENTAL BARRIERS, OR GASTROINTESTINAL EPITHELIUM.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险品标志：
  Xn,N
• 安全说明：
  S36,S60,S61
• 危险类别码：
  R20/21/22
• WGK Germany：
  3
• 危险品运输编号：
  UN 3077 9/PG 3

文献信息

• Ceramic structures for controlled release of biologically active substances
  申请人：Moerck E. Rudi

  公开号：US20060210634A1

  公开（公告）日：2006-09-21

  The present invention provides compositions for controlled drug delivery, dosage forms, and processes for producing dosage forms. In a composition aspect of the present invention, a composition including a drug and a ceramic structure is provided. The ceramic structure has either a hollow portion wherein the drug is included in the hollow portion or is a collection of smaller particles bound together.

  本发明提供了用于控制药物释放的组成物、剂型和制造剂型的过程。在本发明的组成方面，提供了一种包括药物和陶瓷结构的组合物。陶瓷结构具有空心部分，药物包含在空心部分中，或者是由许多小颗粒组成的结合体。
• CAPSULE
  申请人：NIPPON SHINYAKU COMPANY, LIMITED

  公开号：EP0580861A1

  公开（公告）日：1994-02-02

  A prolonged-action capsule excellent in adhesion, stability, etc., in the digestive tract. The capsule comprises a polymer excellent in initial adhesion and another polymer excellent in shape retention, both of which are dispersed in a liquid substance, and a physiologically active substance dispersed or dissolved in a liquid substance, and contains water in an amount of 2 % or less as a whole.

  一种在消化道中具有良好粘附性和稳定性的长效胶囊。该胶囊由一种初始粘附性极佳的聚合物和另一种形状保持性极佳的聚合物组成，这两种聚合物都分散在一种液体物质中，还包括一种分散或溶解在液体物质中的生理活性物质，其整体含水量不超过 2%。
• FAST SOLUBLE TABLET
  申请人：NIPPON SHINYAKU COMPANY, LIMITED

  公开号：EP0627218A1

  公开（公告）日：1994-12-07

  A tablet which dissolves rapidly in the oral cavity and can be prepared in a simple manner without resort to any special preparation technique. The tablet comprises a sugar alcohol or the like as the principal ingredient and is prepared by the wet granulation method wherein a kneaded mixture of the sugar alcohol or the like with a drug is compression molded before drying. This tablet can be prepared merely by modifying partly the conventional tableting method and has a sufficient physicochemical stability.

  一种片剂，可在口腔中快速溶解，制备方法简单，无需采用任何特殊制备技术。这种片剂的主要成分是糖醇或类似物，制备方法是湿法制粒，将糖醇或类似物与药物的揉捏混合物在干燥前压制成型。这种片剂只需部分改变传统的压片方法即可制备，并具有足够的理化稳定性。
• CRYSTALLINE CONDITION DISLOCATING METHOD
  申请人：NIPPON SHINYAKU COMPANY, LIMITED

  公开号：EP0665009A1

  公开（公告）日：1995-08-02

  An object of this invention is to provide a method of dislocating the crystalline condition of crystalline medicine simply, speedily and homogeneously, and, moreover, in large quantities at once. This invention is directed to a method using an extruder when crystalline medicine in a certain crystalline condition (△ is dislocated to another crystalline condition (○), i.e., when the dislocation of crystalline condition (△->○) is carried out.

  本发明的目的是提供一种简单、快速和均匀地将结晶药物的结晶状态变位的方法，而且是一次性大量变位。本发明针对的是一种使用挤压机将某种结晶状态（△）的结晶药物变位到另一种结晶状态（○）的方法，即结晶状态（△->○）变位的方法。
• METHOD OF MANUFACTURING WAX MATRICES
  申请人：NIPPON SHINYAKU COMPANY, LIMITED

  公开号：EP0665010A1

  公开（公告）日：1995-08-02

  A method capable of manufacturing wax matrices efficiently in large quantities at once characterized in that a multiscrew extruder is used to achieve the object.

  一种能够一次性大量高效制造蜡基质的方法，其特征在于使用多螺杆挤压机来实现该目标。