奥拉帕利多晶型及晶型转化研究  

Polymorphs and crystal forms transformation of olaparib

作　　者：张娇 黄欣[2] 胡瑞馨 李宏名 ZHANG Jiao;HUANG Xin;HU Ruixin;LI Hongming(Sichun Kelun Pharmaceutical Co.Ltd.,Chengdu 611138,China;Tianjin University,Tianjin 300072,China;College of Horticulture,Sichuan Agricultural University,Chengdu 611130,China;Sinopharm Chuankang Pharmaceutical Co.Ltd.,Chengdu 611730,China)

机构地区：[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

出　　处：《化学工业与工程》2023年第1期120-126,共7页Chemical Industry and Engineering

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。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.

关 键 词：奥拉帕利 异质同晶溶剂化物 晶型转化 

分 类 号：O799[理学—晶体学]