文献类型：期刊文献

英文题名：Influence of Temperature, Solvents, and Excipients on Crystal Transformation of Agomelatine

作者：Liu, Yan[1];Gao, Huiru[1];Xu, Hao[1];Ren, Fuzheng[1];Ren, Guobin[1]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Lab Pharmaceut Crystal Engn & Technol, Shanghai 20037, Peoples R China

年份：2016

卷号：20

期号：9

起止页码：1559

外文期刊名：ORGANIC PROCESS RESEARCH & DEVELOPMENT

收录：;EI(收录号：20163802827226);WOS:【SCI-EXPANDED(收录号:WOS:000383640100001)】；

基金：The authors would like to thank the supports from the Shanghai Committee of Science and Technology (Grant 14DZ1930802) and National Natural Science Foundation of China (No. 21576080)

语种：英文

外文关键词：Temperature

摘要：Agomelatine is a new and novel non-SSRI potential treatment option for major depressive disorders, discovered and developed by Servier Laboratories with first marketing approval in 2009. In this work, the solution-mediated crystal form I to II transformation process was studied. The influence factors, such as system temperature, crystallization solvents, and some pharmaceutical excipients, were investigated. DSC, XRPD, SEM, react IR, and in situ FBRM were used to monitor the transformation process. Compared with crystal form I of agomelatine, form II was the thermodynamic stable one, therefore, the transformation was a spontaneous process. By increasing the system temperature and/or the volume ratio of IPA in the solvent mixture, the transformation process would be accelerated. Lactose hydrate and HPMC would slightly inhibit the transformation, while PVP K30 would accelerate transformation process by increasing the solubility.