DIFFERENTIAL SCANNING CALORIMETRY ANALYSIS,EQUILIBRIUM SOLUTION AND LIPID-WATER PARTITION COEFFICIENT OF O-19,A PROMISING PRODRUG CANDIDATE OF O-DESMETHYLVENLAFAXINE
Compound O-19 is a promising prodrug candidate of O-desmethylvenlafaxine(ODV)with excellent oral bioavailability and improved brain uptake.In present investigation,with the aim to gain the information on druggability of O-19,the DSC analysis and physicochemical properties including solubility(S),lipid/water partition coefficient(Log P)coupled with solid state stability evaluation were performed and compared with ODV.Results indicated that O-19 showed unique double peaks associated with the crystal transition during differential scanning calorimeter(DSC)processing as well as excellent stable properties during storage in room temperature.Its solubility and Log P exhibited similar trends towards ODV and mainly influenced by the countered pH environment.Herein,this work would be helpful for the further development of O-19 as a novel antidepressant drug.
Compound O-19 DSC analysis solubility Log P
Zihao Zhang Guiyong Wang Zhongyu Zhang Yang Zhang
School of Chemistry and Pharmaceutical Engineering,Jilin Institute of Chemical Technology,Jilin 132022,China
国际会议
吉林
英文
222-225
2018-06-23(万方平台首次上网日期,不代表论文的发表时间)