CN107011289A - 沃替西汀β晶型的制备方法 - Google Patents

沃替西汀β晶型的制备方法 Download PDF

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Publication number
CN107011289A
CN107011289A CN201710141511.9A CN201710141511A CN107011289A CN 107011289 A CN107011289 A CN 107011289A CN 201710141511 A CN201710141511 A CN 201710141511A CN 107011289 A CN107011289 A CN 107011289A
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Prior art keywords
vortioxetine
beta crystal
preparation
solvent
crystal
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CN201710141511.9A
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Inventor
赵林
赵云萍
赵国磊
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Wanquan Pharmaceutical (xiamen) Co Ltd Wante
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Wanquan Pharmaceutical (xiamen) Co Ltd Wante
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Priority to CN201710141511.9A priority Critical patent/CN107011289A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明属于医药技术、晶型药物领域，涉及了一种抗抑郁药物沃替西汀乳酸盐的制备及研究，丰富了其晶型的研究，能够使医药研发工作者在沃替西汀晶型研究过程具有全面的了解和掌控。

Description

沃替西汀β晶型的制备方法
技术领域
本发明属于医药技术、晶型药物领域，具体涉及抗抑郁药物沃替西汀乳酸盐晶型的研究。
背景技术
沃替西汀(vortioxetine)，化学名1-[2-（2,4-二甲基苯基硫基）苯基]哌嗪乳酸盐，适用于重度抑郁症的治疗，2013年9月美国食品药品监督管理局(FDA)批准其上市，商品名为Latuda，其分子式如下：
药物多晶型的研究是新药研发、工艺设计以及药物剂型设计过程中非常重要的组成部分。充分了解某一药物多晶型的现象及各种晶型的性质，对于药物研发工作者根据生物利用度及稳定性在设计原料药及制剂的制备工艺时具有极大的帮助。同时也保证了药物的质量，为患者的安全用药提供了有力的保障。
发明内容
本发明公开了一种抗抑郁药物沃替西汀(化学式如下)的β晶型及其制备方法：
本发明还涉及了沃替西汀β晶型的制备方法：将样品置于适宜的溶剂的中，加热回流，冷却析晶后的到产物，具体为先以乙酸乙酯为溶剂成乳酸盐，得到的乳酸盐在甲醇、乙醇、丙酮、乙酸丁酯为溶剂的体系中加热回流，进而冷却析晶，得到沃替西汀β晶型，其中，溶剂：原料药=5：1-50：1。
本发明的有益效果在于公开了一种抗抑郁药物沃替西汀β晶型。沃替西汀作为一种具有多晶型的药物，本发明丰富了其晶型的研究，能够使医药研发工作者在沃替西汀晶型研究过程具有全面的了解和掌控。
具体实施实例
以下结合实例对本发明进行更详细的描述，但不作为对本发明的限制。
实施例1
向单口瓶(100 mL)中加入乙酸乙酯(AR，50 mL)和沃替西汀乳酸盐(5g)，加热使其回流，回流一小时，降温，冷却析晶；析晶2h后抽滤，滤饼干燥16h，即得到沃替西汀β晶型。
实施例2
向三口瓶（100 ml）中加入甲醇（AR，50m）和沃替西汀（5g），加热到50℃，维持该温度1h，趁热抽滤，将滤液转移至单口瓶中，加入乳酸，搅拌2h后，抽滤，滤饼干燥16h，即得到沃替西汀β晶型。

Claims (3)

1.一种抗抑郁药物沃替西汀β晶型，其制备方法为在甲醇为溶剂的体系中打浆，得到晶体为类白色晶体。
2.根据权利要求1所述的沃替西汀β晶型制备过程，先以乙酸乙酯为溶剂成乳酸盐，得到的乳酸盐在甲醇、乙醇、丙酮、乙酸丁酯为溶剂的体系中加热回流，进而冷却析晶，得到沃替西汀β晶型。
3.根据权利要求1所述的沃替西汀β晶型制备过程，溶剂：原料药=5：1-50：1。
CN201710141511.9A 2017-03-10 2017-03-10 沃替西汀β晶型的制备方法 Pending CN107011289A (zh)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106518807A (zh) * 2016-09-17 2017-03-22 北京万全德众医药生物技术有限公司 乳酸沃替西汀晶型的制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102405048A (zh) * 2009-04-24 2012-04-04 H.隆德贝克有限公司 1-[2-(2,4-二甲基苯硫基)苯基]哌嗪盐的液体制剂
CN103936694A (zh) * 2014-04-23 2014-07-23 中国药科大学 一种抗抑郁药沃替西汀的制备方法
CN105111167A (zh) * 2015-08-06 2015-12-02 华南理工大学 一种沃替西汀半盐酸盐及其制备方法和药物组合物
CN104736526B (zh) * 2013-09-12 2016-04-20 杭州普晒医药科技有限公司 沃替西汀盐及其晶体、它们的制备方法、药物组合物和用途

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102405048A (zh) * 2009-04-24 2012-04-04 H.隆德贝克有限公司 1-[2-(2,4-二甲基苯硫基)苯基]哌嗪盐的液体制剂
CN104736526B (zh) * 2013-09-12 2016-04-20 杭州普晒医药科技有限公司 沃替西汀盐及其晶体、它们的制备方法、药物组合物和用途
CN103936694A (zh) * 2014-04-23 2014-07-23 中国药科大学 一种抗抑郁药沃替西汀的制备方法
CN105111167A (zh) * 2015-08-06 2015-12-02 华南理工大学 一种沃替西汀半盐酸盐及其制备方法和药物组合物

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106518807A (zh) * 2016-09-17 2017-03-22 北京万全德众医药生物技术有限公司 乳酸沃替西汀晶型的制备方法

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Application publication date: 20170804