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化学工业与工程 2023, Vol. 40 Issue (1) :120-126    DOI: 10.13353/j.issn.1004.9533.20220365
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奥拉帕利多晶型及晶型转化研究
张娇1, 黄欣2, 胡瑞馨3, 李宏名4
1. 四川科伦药物研究院有限公司, 成都 611138;
2. 天津大学化工学院, 天津 300072;
3. 四川农业大学园艺学院, 成都 611130;
4. 国药集团川抗制药有限公司, 成都 611730
Polymorphs and crystal forms transformation of olaparib
ZHANG Jiao1, HUANG Xin2, HU Ruixin3, LI Hongming4
1. Sichun Kelun Pharmaceutical Co. Ltd., Chengdu 611138, China;
2. Tianjin University, Tianjin 300072, China;
3. College of Horticulture, Sichuan Agricultural University, Chengdu 611130, China;
4. Sinopharm Chuankang Pharmaceutical Co. Ltd., Chengdu 611730, China

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摘要 奥拉帕利是全球首个上市的聚腺苷二磷酸-核糖聚合酶抑制剂。研究了奥拉帕利形成异质同晶溶剂化物的现象的机理,并进一步通过四氢呋喃溶剂化物单晶解析了奥拉帕利异质同晶溶剂化物的类型为独立位点型;研究了奥拉帕尼无水晶型A/L热力学稳定关系,分析了溶剂介导下稳定晶型向介稳晶型异常转变的可能原因;同时考察了温度和水体积比对无水晶型A与水合物晶型H相变过程的影响。
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张娇
黄欣
胡瑞馨
李宏名
关键词奥拉帕利   异质同晶溶剂化物   晶型转化     
Abstract: Olaparib is the first marketed poly-ADP-ribose polymerase inhibitor in the worldwide. In this paper, isostructural solvates phenomenon of olaparib were studied, it is found that isostructural solvates were determined to be isolated structure by single crystal of tetrahydrofuran solvate. Then, the thermodynamic stability relationship of anhydrous polymorph A and L was studied, and the possible reasons for the abnormal transformation from stable form to metastable form in organic solvents were analyzed. Furthermore, the effects of temperature and water ratio on the phase transition processes of Form A and hydrate Form H were investigated.
Keywordsolaparib   isostructural solvates   crystal form transformation     
Received 2022-07-25;
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Corresponding Authors: 李宏名,副研究员,E-mail:hongming.li@163.com。     Email: hongming.li@163.com
About author: 张娇(1990-),女,硕士,工程师,现从事药物晶型方面的研究。
引用本文:   
张娇, 黄欣, 胡瑞馨, 李宏名.奥拉帕利多晶型及晶型转化研究[J].  化学工业与工程, 2023,40(1): 120-126
ZHANG Jiao, HUANG Xin, HU Ruixin, LI Hongming.Polymorphs and crystal forms transformation of olaparib[J].  Chemcial Industry and Engineering, 2023,40(1): 120-126
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