WO2016161989A3 - 一种硫酸氢氯吡格雷i晶型球形结晶的制备方法 - Google Patents
一种硫酸氢氯吡格雷i晶型球形结晶的制备方法 Download PDFInfo
- Publication number
- WO2016161989A3 WO2016161989A3 PCT/CN2016/090135 CN2016090135W WO2016161989A3 WO 2016161989 A3 WO2016161989 A3 WO 2016161989A3 CN 2016090135 W CN2016090135 W CN 2016090135W WO 2016161989 A3 WO2016161989 A3 WO 2016161989A3
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- WIPO (PCT)
- Prior art keywords
- spherical crystals
- clopidogrel bisulphate
- crystalline form
- present
- crystals
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- 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)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
本发明克服了单一溶剂难以制备球形结晶的技术困难,采用单一溶剂2-丁醇,通过控制加入硫酸氢氯吡格雷I晶型晶种的量及粒径,使得硫酸氢氯吡格雷以特定粉体形态范围的球形结晶稳定从溶液体系中析出,所得硫酸氢氯吡格雷球形结晶具有特定粉体性质,在溶剂残留、堆密度和流动性等方面均处于较优状态,有利于粉末直压制剂工艺的实现。本发明还进一步公开了一种包含采用本发明工艺制备得到硫酸氢氯吡格雷I晶型球形结晶的药物组合物。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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CN201510432264.9 | 2015-07-21 | ||
CN201510432264.9A CN105061459B (zh) | 2015-07-21 | 2015-07-21 | 一种硫酸氢氯吡格雷i晶型球形结晶的制备方法 |
Publications (2)
Publication Number | Publication Date |
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WO2016161989A2 WO2016161989A2 (zh) | 2016-10-13 |
WO2016161989A3 true WO2016161989A3 (zh) | 2016-12-01 |
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Application Number | Title | Priority Date | Filing Date |
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PCT/CN2016/090135 WO2016161989A2 (zh) | 2015-07-21 | 2016-07-15 | 一种硫酸氢氯吡格雷i晶型球形结晶的制备方法 |
Country Status (2)
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CN (1) | CN105061459B (zh) |
WO (1) | WO2016161989A2 (zh) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105061459B (zh) * | 2015-07-21 | 2016-08-24 | 深圳信立泰药业股份有限公司 | 一种硫酸氢氯吡格雷i晶型球形结晶的制备方法 |
CN110606854A (zh) * | 2018-06-14 | 2019-12-24 | 华东理工大学 | 一种i晶型硫酸氢氯吡格雷的可控制备方法 |
CN109096302A (zh) * | 2018-07-27 | 2018-12-28 | 天津大学 | 球形硫酸氢氯吡格雷ii晶型及制备方法 |
CN109438467B (zh) * | 2018-11-14 | 2021-03-26 | 四川青木制药有限公司 | 一种硫酸氢氯吡格雷ⅱ型球形结晶的制备方法 |
CN111499655B (zh) * | 2019-01-31 | 2023-01-06 | 华东理工大学 | 一种制备球形晶体的三液乳化溶剂扩散法 |
CN113121559B (zh) * | 2019-12-31 | 2023-08-29 | 惠州信立泰药业有限公司 | 一种高堆密度的ii型硫酸氢氯吡格雷球形结晶及制备方法 |
CN111662304B (zh) * | 2020-06-08 | 2022-03-29 | 天津大学 | 一种快速制备硫酸氢氯吡格雷i晶型球形晶体的方法 |
CN114369100B (zh) * | 2021-12-15 | 2023-06-20 | 浙江车头制药股份有限公司 | 一种硫酸氢氯吡格雷球形晶型i的制备方法 |
CN114560895A (zh) * | 2022-01-05 | 2022-05-31 | 苏州赜文医药科技有限公司 | 一种三磷酸腺苷二钠的球形晶体的制备方法及应用 |
Citations (7)
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---|---|---|---|---|
US20050059696A1 (en) * | 2003-05-08 | 2005-03-17 | Dr. Reddy's Laboratories Limited | Process for the recovery of S -(+)-methyl- (2-chlorophenyl)- (6,7-dihydro- 4H-thieno [3,2-c] pyrid-5-yl) acetate hydrogen sulfate (clopidogrel bisulfate) from its (R) and mixture of (R) and (S)- isomers |
CN101962387A (zh) * | 2010-09-13 | 2011-02-02 | 四川制药制剂有限公司 | 一种新结晶形态的氯吡格雷硫酸氢盐及其制备方法 |
WO2011052940A2 (ko) * | 2009-10-29 | 2011-05-05 | 동아제약주식회사 | 클로피도그랠 황산수소염 ⅰ형 제조방법 |
CN103717207A (zh) * | 2011-07-12 | 2014-04-09 | 三进制药株式会社 | 氯吡格雷硫酸氢盐球形粒子及包含此物质的药品合成物及其制造方法 |
CN104817571A (zh) * | 2014-12-31 | 2015-08-05 | 天津大学 | 一种制备球形硫酸氢氯吡格雷i晶型的方法 |
CN105012298A (zh) * | 2015-07-17 | 2015-11-04 | 深圳信立泰药业股份有限公司 | 一种含有球形硫酸氢氯吡格雷i晶型的药物组合物及其制备方法 |
CN105061459A (zh) * | 2015-07-21 | 2015-11-18 | 深圳信立泰药业股份有限公司 | 一种硫酸氢氯吡格雷i晶型球形结晶的制备方法 |
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2015
- 2015-07-21 CN CN201510432264.9A patent/CN105061459B/zh not_active Expired - Fee Related
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2016
- 2016-07-15 WO PCT/CN2016/090135 patent/WO2016161989A2/zh active Application Filing
Patent Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20050059696A1 (en) * | 2003-05-08 | 2005-03-17 | Dr. Reddy's Laboratories Limited | Process for the recovery of S -(+)-methyl- (2-chlorophenyl)- (6,7-dihydro- 4H-thieno [3,2-c] pyrid-5-yl) acetate hydrogen sulfate (clopidogrel bisulfate) from its (R) and mixture of (R) and (S)- isomers |
WO2011052940A2 (ko) * | 2009-10-29 | 2011-05-05 | 동아제약주식회사 | 클로피도그랠 황산수소염 ⅰ형 제조방법 |
CN101962387A (zh) * | 2010-09-13 | 2011-02-02 | 四川制药制剂有限公司 | 一种新结晶形态的氯吡格雷硫酸氢盐及其制备方法 |
CN103717207A (zh) * | 2011-07-12 | 2014-04-09 | 三进制药株式会社 | 氯吡格雷硫酸氢盐球形粒子及包含此物质的药品合成物及其制造方法 |
CN104817571A (zh) * | 2014-12-31 | 2015-08-05 | 天津大学 | 一种制备球形硫酸氢氯吡格雷i晶型的方法 |
CN105012298A (zh) * | 2015-07-17 | 2015-11-04 | 深圳信立泰药业股份有限公司 | 一种含有球形硫酸氢氯吡格雷i晶型的药物组合物及其制备方法 |
CN105061459A (zh) * | 2015-07-21 | 2015-11-18 | 深圳信立泰药业股份有限公司 | 一种硫酸氢氯吡格雷i晶型球形结晶的制备方法 |
Also Published As
Publication number | Publication date |
---|---|
CN105061459A (zh) | 2015-11-18 |
CN105061459B (zh) | 2016-08-24 |
WO2016161989A2 (zh) | 2016-10-13 |
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