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 AI
1, Meng-han LIU
1, 2, Lu-feng WANG
3, Jing-jing GAO
1, Guang YANG
1, Hong-gang ZHOU
1, Cheng YANG
1, 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=
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
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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:aixioayu@nankai.edu.cn。
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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:aixioayu@nankai.edu.cn。
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