(2R,5R)-2-methylspiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane];hydrate;hydrochloride

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂螺癸烷衍生物
• 英文名称: (2R,5R)-2-methylspiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane];hydrate;hydrochloride
• 化学式: C10H20ClNO2S
• 分子量: 253.79
• InChiKey: JKJRNPOQQPBPOV-DCXXCVGISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.16
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  38.8
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• PROCESS FOR PRODUCTION OF QUINUCLIDINE COMPOUNDS
  申请人：Kitagawa Yutaka

  公开号：US20130060036A1

  公开（公告）日：2013-03-07

  Provided is a production method for a cis-QMF, which has a low environmental burden and is industrially advantageous. Specifically provided is a production method for a cis-type 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine hydrochloride, including: reacting a cis-trans isomer mixture of 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine with p-nitrobenzoic acid; resolving the resultant product to produce a cis-type 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine p-nitrobenzoate; and converting the p-nitrobenzoate into a hydrochloride.

  提供了一种生产cis-QMF的方法，该方法具有低环境负担且在工业上具有优势。具体提供了一种用于生产顺式2-烷基螺(1,3-噁硫杂环戊烷-5,3′)喹啉盐酸盐的方法，包括：将2-烷基螺(1,3-噁硫杂环戊烷-5,3′)喹啉的顺反异构体混合物与对硝基苯甲酸反应；将所得产物分离以产生顺式2-烷基螺(1,3-噁硫杂环戊烷-5,3′)喹啉对硝基苯甲酸酯；并将对硝基苯甲酸酯转化为盐酸盐。
• METHOD FOR PRODUCING PATCH, AND PATCH
  申请人：Hashimoto Eiji

  公开号：US20140037710A1

  公开（公告）日：2014-02-06

  A method for producing a patch including a support layer and an adhesive layer, comprising the step of forming the adhesive layer with use of an adhesive layer composition obtained by mixing an alkali metal diacetate, a drug, and a nonaqueous adhesive base such that the molar ratio between the drug and the alkali metal diacetate (the number of moles of the drug:the number of moles of the alkali metal diacetate) is from 1:0.5 to 1:15.

  一种生产贴片的方法，包括形成支撑层和粘合层，其中粘合层的制备步骤是使用粘合层组合物通过混合一种碱金属二乙酸盐、一种药物和一种非水粘合基材料形成，使得药物和碱金属二乙酸盐的摩尔比（药物的摩尔数：碱金属二乙酸盐的摩尔数）在1:0.5到1:15之间。
• PHARMACEUTICAL COMPOSITION
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP1862184A1

  公开（公告）日：2007-12-05

  The present invention provides an intraoral rapid-disintegrating pharmaceutical composition which exhibits excellent intraoral disintegrating property and high hardness, and which can be applied, in particular, to a pharmaceutically active ingredient which is unstable in water. The pharmaceutical composition, which contains lactose and powdered cellulose, exhibits high hardness without prolongation of its intraoral disintegration time. When a disintegrating agent is further incorporated into the pharmaceutical composition, the hardness of the composition is increased without prolongation of its intraoral disintegration time. When magnesium aluminometasilicate, and one or more species selected from among silicic acid and silicic acid salts other than magnesium aluminometasilicate are further incorporated into the pharmaceutical composition, the composition exhibits higher hardness without prolongation of its intraoral disintegration time. The pharmaceutical composition of the present invention can be produced by means of a generally employed industrial production process without using a special preparation technique.

  本发明提供了一种口腔内快速崩解药物组合物，它具有优异的口腔内崩解性能和高硬度，尤其适用于在水中不稳定的药物活性成分。该药物组合物含有乳糖和纤维素粉末，具有高硬度，且不会延长口腔内崩解时间。当在药物组合物中进一步加入崩解剂时，组合物的硬度会增加，而口腔内崩解时间不会延长。当铝硅酸镁和一种或多种从硅酸和硅酸盐（铝硅酸镁除外）中选出的物质被进一步加入药物组合物中时，组合物会显示出更高的硬度，而不会延长其口内崩解时间。本发明的药物组合物可通过一般采用的工业生产工艺生产，无需使用特殊的制备技术。
• SUSTAINED RELEASE PREPARATION AND PROCESS FOR PRODUCTION THEREOF
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP2191848A1

  公开（公告）日：2010-06-02

  The present invention provides a preparation which is a sustained-release preparation capable of providing a dissolution profile that permits once-daily administration even in the case of a highly water-soluble drug, and which can exhibit stable drug dissolution behavior and can be reduced in its size; and a method for producing the same. A preparation containing a highly water-soluble drug, a gel-forming polymer, and a low-melting lipophilic substance is usable as a sustained-release preparation that permits once-daily administration, and enables reduction in its size and simple production thereof, and thus, the objects have been achieved.

  本发明提供了一种制剂，它是一种即使在高水溶性药物的情况下也能提供允许每日给药一次的溶解曲线的缓释制剂，它能表现出稳定的药物溶解行为，并能减小其体积；以及生产这种制剂的方法。一种含有高水溶性药物、凝胶形成聚合物和低熔点亲脂物质的制剂可用作缓释制剂，允许每日给药一次，并能减小其体积和简单生产，从而实现了上述目的。
• DISINTEGRATING PARTICLE COMPOSITION AND ORALLY RAPIDLY DISINTEGRATING TABLET
  申请人：FUJI CHEMICAL INDUSTRY CO., LTD.

  公开号：EP2465539A1

  公开（公告）日：2012-06-20

  There has been a need for an orally rapidly disintegrating tablet which has a good texture and taste in the oral cavity, such a sufficient hardness as not giving any worry of being chipped or dusted during production or transportation and good disintegrating properties in the oral cavity and can sustain a sufficient hardness even under humid conditions after opening. Disclosed are a disintegrating particle composition which is prepared by dispersing, in the presence of water, mannitol, xylitol, an inorganic excipient, a disintegrating agent and carmellose and drying, and an orally rapidly disintegrating tablet which comprises said disintegrating particle composition, an active substance and a disintegrating agent. The disintegrating tablet has a good texture and taste, an appropriate hardness and good disintegrating properties and can sustain a sufficient hardness under humid conditions.

  人们需要一种口服快速崩解片剂，这种片剂在口腔中具有良好的质地和口感，有足够的硬度，不会担心在生产或运输过程中碎裂或沾上灰尘，在口腔中具有良好的崩解性能，即使在开封后潮湿的条件下也能保持足够的硬度。本发明公开了一种崩解颗粒组合物，其制备方法是在有水存在的情况下，将甘露醇、木糖醇、无机赋形剂、崩解剂和卡麦芽糖分散并干燥；还公开了一种口服快速崩解片剂，其包括所述崩解颗粒组合物、活性物质和崩解剂。该崩解片具有良好的质地和口感、适当的硬度和良好的崩解性能，并能在潮湿条件下保持足够的硬度。