Article(id=1322246413786923018, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1322246381633389353, articleNumber=null, orderNo=null, doi=null, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=null, receivedDateStr=null, revisedDate=null, revisedDateStr=null, acceptedDate=1610553600000, acceptedDateStr=2021-01-14, onlineDate=1793177711196, onlineDateStr=2026-10-28, pubDate=1623686400000, pubDateStr=2021-06-15, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1793177711196, onlineIssueDateStr=2026-10-28, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1793177711196, creator=13701087609, updateTime=1793177711196, updator=13701087609, issue=Issue{id=1322246381633389353, tenantId=1146029695717560320, journalId=1235980733773295621, year='2021', volume='30', issue='11', pageStart='961', pageEnd='1056', issueExtLink='null', onlineDate='null', pubDate='1623686400000', pubDateStr='2021-06-15', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1793177703531, creator='13701087609', updateTime=1793178125547, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext={EN=IssueExt(id=1322248152208486593, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1322246381633389353, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1322248152212680898, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1322246381633389353, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null, downloadFileDto=null}, startPage=1022, endPage=1030, ext={EN=ArticleExt(id=1322246413954695179, articleId=1322246413786923018, tenantId=1146029695717560320, journalId=1235980733773295621, language=EN, title=Polycrystalline study of compound CP0119, columnId=null, journalTitle=Chinese Journal of New Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=
Objective:

To systematically study the polymorphism of compound CP0119.

Methods:

Totally 100 conditions such as volatile crystallization, slurry crystallization, anti-solvent crystallization, cooling crystallization, diffusion crystallization and water vapor stress crystallization were used to select the crystal types. Different crystal types were characterized by X-ray powder diffraction analysis (XRPD), differential scanning thermal analysis (DSC), thermogravimetric analysis (TGA) and Fourier infrared spectroscopy (FT-IR). Dynamic water adsorption test (DVS) was used to determine the wettability of anhydrous crystal. The stability and translatability of the crystal samples were studied by stress testing. The most stable crystal in the corresponding solvent at room temperature was determined by crystal competition test and its stability was investigated.

Results:

In addition to the original crystal type (crystal type 1), 9 new crystal types were screened and prepared. Many kinds of methods could be used to identify the crystal samples in different material states. The competitive test showed that the crystal type 1 was the most stable crystal type, and the stability test showed that the crystal form and melting point crystal of type 1 were not changed when it was placed in long-term and accelerated conditions for 10 d.

Conclusion:

By systematically studying the polycrystalline form of compound CP0119, the preparation method, material composition, crystal form stability and crystal form transformation rule of the 9 crystal forms were clarified, which provided scientific basis for the subsequent preparation process and preparation research.

, authors=Xiao-yu AI1, Meng-han LIU1, 2, Lu-feng WANG3, Jing-jing GAO1, Guang YANG1, Hong-gang ZHOU1, Cheng YANG1, authorsList=Xiao-yu AI, Meng-han LIU, Lu-feng WANG, Jing-jing GAO, Guang YANG, Hong-gang ZHOU, Cheng YANG, authorCompany=null, correspAuthors=Guang YANG, Hong-gang ZHOU, Cheng YANG, authorNote=null, correspAuthorsNote=null, copyrightStatement=null, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=null, pdfFileSize=null, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=null, mapNumber=null, fund=null), CN=ArticleExt(id=1322246414168604684, articleId=1322246413786923018, tenantId=1146029695717560320, journalId=1235980733773295621, language=CN, title=化合物CP0119的多晶型研究, columnId=1236330556003242277, journalTitle=中国新药杂志, columnName=实验研究, runingTitle=null, highlight=null, articleAbstract=
目的:

系统研究化合物CP0119的多晶型现象。

方法:

采用挥发结晶、晶浆结晶、抗溶剂结晶、冷却结晶、扩散结晶和水汽应激结晶等100个条件对晶型进行筛选;采用X射线粉末衍射分析法(XRPD)、差示扫描量热法(DSC)、热重分析(TGA)和傅里叶红外光谱法(FT-IR)对不同晶型进行表征;动态水吸附实验(DVS)用于测定无水物晶型的引湿性;通过影响因素实验研究晶型样品的稳定性和转晶规律;通过晶型竞争实验确定室温下相应溶剂中的最稳晶型,并考察其稳定性。

结果:

除原研药晶型(晶型1)外,筛选并制备出9种新晶型;多种检测方法均可有效鉴别不同物质状态的晶型样品;竞争性实验表明,晶型1是最稳定的晶型,稳定性考察实验表明,晶型1在长期和加速条件下放置10 d,晶型和熔点不发生改变。

结论:

通过对化合物CP0119的多晶型进行系统性研究,阐明了其10种晶型的制备方法、物质组成、晶型稳定性及晶型转变规律,为之后的制备工艺和制剂研究提供了科学依据。

, authors=艾笑羽1, 刘曚晗1, 2, 王路锋3, 高晶晶1, 杨光1, 周红刚1, 杨诚1, authorsList=艾笑羽, 刘曚晗, 王路锋, 高晶晶, 杨光, 周红刚, 杨诚, authorCompany=null, correspAuthors=杨光, 周红刚, 杨诚, authorNote=

艾笑羽,女,博士,副教授,主要研究方向为新药研发。联系电话:(022)85358566,E-mail:。

, correspAuthorsNote=
杨诚,男,博士,教授,主要研究方向为新药研发。联系电话:(022)85358566,E-mail:。
周红刚,男,博士,副教授,主要研究方向为开发器官纤维化、肿瘤和炎症相关适应证等的创新药物。联系电话:(022)85358566,E-mail:。
杨光,男,博士,副研究员,主要研究方向为药物化学、有机合成和化学生物学。联系电话:(022)85358566,E-mail:。
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艾笑羽,女,博士,副教授,主要研究方向为新药研发。联系电话:(022)85358566,E-mail:。

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艾笑羽,女,博士,副教授,主要研究方向为新药研发。联系电话:(022)85358566,E-mail:。

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化合物CP0119的多晶型研究
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艾笑羽 1 , 刘曚晗 1, 2 , 王路锋 3 , 高晶晶 1 , 杨光 1 , 周红刚 1 , 杨诚 1
中国新药杂志 | 实验研究 2021,30(11): 1022-1030
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中国新药杂志 |实验研究 2021 , 30 (11) : 1022 -1030
化合物CP0119的多晶型研究
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艾笑羽1 , 刘曚晗1, 2, 王路锋3, 高晶晶1, 杨光1 , 周红刚1 , 杨诚1
作者信息
  • 1南开大学药学院,天津 300350
  • 2天津国际生物医药联合研究院,天津市分子药物研究重点实验室,天津 300450
  • 3中国医药研究开发中心有限公司,北京 102206
通讯作者:
杨诚,男,博士,教授,主要研究方向为新药研发。联系电话:(022)85358566,E-mail:。
周红刚,男,博士,副教授,主要研究方向为开发器官纤维化、肿瘤和炎症相关适应证等的创新药物。联系电话:(022)85358566,E-mail:。
杨光,男,博士,副研究员,主要研究方向为药物化学、有机合成和化学生物学。联系电话:(022)85358566,E-mail:。
作者简介:

艾笑羽,女,博士,副教授,主要研究方向为新药研发。联系电话:(022)85358566,E-mail:。

Polycrystalline study of compound CP0119
Xiao-yu AI1 , Meng-han LIU1, 2, Lu-feng WANG3, Jing-jing GAO1, Guang YANG1 , Hong-gang ZHOU1 , Cheng YANG1
Affiliations
  • 1College of Pharmacy, Nankai University, Tianjin 300350, China
  • 2Tianjin International Biomedical Research Institute, Tianjin Key Laboratory of Molecular Drug Research, Tianjin 300450, China
  • 3China Pharmaceutical Research and Development Center Co., Ltd., Beijing 102206, China
出版时间: 2021-06-15
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目的:

系统研究化合物CP0119的多晶型现象。

方法:

采用挥发结晶、晶浆结晶、抗溶剂结晶、冷却结晶、扩散结晶和水汽应激结晶等100个条件对晶型进行筛选;采用X射线粉末衍射分析法(XRPD)、差示扫描量热法(DSC)、热重分析(TGA)和傅里叶红外光谱法(FT-IR)对不同晶型进行表征;动态水吸附实验(DVS)用于测定无水物晶型的引湿性;通过影响因素实验研究晶型样品的稳定性和转晶规律;通过晶型竞争实验确定室温下相应溶剂中的最稳晶型,并考察其稳定性。

结果:

除原研药晶型(晶型1)外,筛选并制备出9种新晶型;多种检测方法均可有效鉴别不同物质状态的晶型样品;竞争性实验表明,晶型1是最稳定的晶型,稳定性考察实验表明,晶型1在长期和加速条件下放置10 d,晶型和熔点不发生改变。

结论:

通过对化合物CP0119的多晶型进行系统性研究,阐明了其10种晶型的制备方法、物质组成、晶型稳定性及晶型转变规律,为之后的制备工艺和制剂研究提供了科学依据。

化合物CP0119  /  多晶型  /  晶型鉴别  /  晶型转变  /  晶型稳定性
Objective:

To systematically study the polymorphism of compound CP0119.

Methods:

Totally 100 conditions such as volatile crystallization, slurry crystallization, anti-solvent crystallization, cooling crystallization, diffusion crystallization and water vapor stress crystallization were used to select the crystal types. Different crystal types were characterized by X-ray powder diffraction analysis (XRPD), differential scanning thermal analysis (DSC), thermogravimetric analysis (TGA) and Fourier infrared spectroscopy (FT-IR). Dynamic water adsorption test (DVS) was used to determine the wettability of anhydrous crystal. The stability and translatability of the crystal samples were studied by stress testing. The most stable crystal in the corresponding solvent at room temperature was determined by crystal competition test and its stability was investigated.

Results:

In addition to the original crystal type (crystal type 1), 9 new crystal types were screened and prepared. Many kinds of methods could be used to identify the crystal samples in different material states. The competitive test showed that the crystal type 1 was the most stable crystal type, and the stability test showed that the crystal form and melting point crystal of type 1 were not changed when it was placed in long-term and accelerated conditions for 10 d.

Conclusion:

By systematically studying the polycrystalline form of compound CP0119, the preparation method, material composition, crystal form stability and crystal form transformation rule of the 9 crystal forms were clarified, which provided scientific basis for the subsequent preparation process and preparation research.

CP0119  /  polycrystalline  /  crystalline differentiation  /  crystalline transformation  /  crystalline stability
艾笑羽, 刘曚晗, 王路锋, 高晶晶, 杨光, 周红刚, 杨诚. 化合物CP0119的多晶型研究. 中国新药杂志, 2021 , 30 (11) : 1022 -1030 .
Xiao-yu AI, Meng-han LIU, Lu-feng WANG, Jing-jing GAO, Guang YANG, Hong-gang ZHOU, Cheng YANG. Polycrystalline study of compound CP0119[J]. Chinese Journal of New Drugs, 2021 , 30 (11) : 1022 -1030 .

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2021年第30卷第11期
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  • 首发时间:2026-10-28
  • 出版时间:2021-06-15
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  • 录用日期:2021-01-14
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    1南开大学药学院,天津 300350
    2天津国际生物医药联合研究院,天津市分子药物研究重点实验室,天津 300450
    3中国医药研究开发中心有限公司,北京 102206

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杨诚,男,博士,教授,主要研究方向为新药研发。联系电话:(022)85358566,E-mail:。
周红刚,男,博士,副教授,主要研究方向为开发器官纤维化、肿瘤和炎症相关适应证等的创新药物。联系电话:(022)85358566,E-mail:。
杨光,男,博士,副研究员,主要研究方向为药物化学、有机合成和化学生物学。联系电话:(022)85358566,E-mail:。
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2种不同金属材料的力学参数
科
Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)
属
Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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