普瑞巴林晶型Ⅰ在纯溶剂及丙酮-水混合溶剂中的溶解度测定与关联Measurement and Correlation of Pregabalin Form Ⅰ Solubility in Pure Solvents and Acetone-Water Mixtures
于玉振,张晓慧,李鹏坤,王荣荣,李战军,刘宇恒,李雯
摘要(Abstract):
通过平衡法测定了283.15~328.15 K温度下普瑞巴林晶型I在水、甲醇、乙醇、丙酮、四氢呋喃、N,N-二甲基甲酰胺、乙酸乙酯及丙酮-水混合溶剂中的溶解度,实验结果表明:普瑞巴林晶型I在所测定的所有纯溶剂及丙酮-水混合溶剂中的溶解度均随温度的升高而增大;在丙酮-水混合溶剂中,溶解度随着丙酮的摩尔分数的增加而降低,在丙酮的摩尔分数达到0.83附近时溶解度最小,接近0。采用修订的Apelblat经验方程和(CNIBS)/Redlich-Kister方程对溶解度数据进行关联,结果令人满意。所得实验数据和拟合模型为普瑞巴林在工业结晶及药物多晶型等方面的研究提供了重要的依据。
关键词(KeyWords): 普瑞巴林;溶解度;测定;关联;模型
基金项目(Foundation): 河南省科技厅产学研合作项目(152107000043);; 河南省教育厅科学技术研究重点项目(914A5300007)
作者(Author): 于玉振,张晓慧,李鹏坤,王荣荣,李战军,刘宇恒,李雯
参考文献(References):
- [1]Living with Fibromyalgia,drugs approved to manage pain:Federal Drug Administration(FDA)[S].Washington,DC:FDA,2008.
- [2]Lee C H,Liou H H.Pregabalin activates ROMK1 channels via c AMP-dependent protein kinase and protein kinase C[J].European Journal of Pharmacology,2014,740(5):35-44.
- [3]Lindsley C W.2013 Trends and statistics for prescription medications in the United States:CNS highest ranked and record number of prescriptions dispensed[J].Acs Chemical Neuroscience,2015,6(3):356-357.
- [4]Lindsley C W.The top prescription drugs of 2012 globally:biologics dominate,but small molecule CNS drugs hold on to top spots[J].Acs Chemical Neuroscience,2013,4(6):905-907.
- [5]Cogoni G,Souza B D,Croker D M,et al.Solubility of(s)-3-(aminomethyl)-5-methylhexanoicacid in pure and binary solvent mixtures[J].Journal of Chemical and Engineering Data,2016,61(1):587-593.
- [6]SUN Peng(孙鹏),LIU Jun-guo(刘俊果),YANG Yu-huai(杨玉淮),et al.Determination and correlation of solubilities of avermectins in different systems of alcohol-water(阿维素在不同醇-水溶剂体系中溶解度的测定与关联)[J].Journal of Chemical Engineering of Chinese Universities(高校化学工程学报),2010,24(5):735-738.
- [7]Mudalip S K A,Bakar M R A,Jamal P,et al.Solubility and dissolution thermodynamic data of mefenamic acid crystals in different classes of organic solvents[J].Journal of Chemical and Engineering Data,2013,58(12):3447-3452.
- [8]SUN Xian-xiang(孙贤祥),CHEN Yu-ting(陈玉婷),XIA Tian-xi(夏天喜).Measurement and prediction of solubility of s-timolol-d-tartrate salt in organic solvents(S-噻吗洛尔-D-酒石酸非对映体盐在有机溶剂中的溶解度测定和预测)[J].Journal of Chemical Engineering of Chinese Universities(高校化学工程学报),2012,26(1):7-12.
- [9]YUE Jin-cai(岳金彩),ZHU Nan-nan(朱南南),LIU Xian-hong(刘先红),et al.Measurement and correlation of the solubility of4-tert-butylphenol in Na Cl solution(对叔丁基苯酚在盐水中溶解度的测定及关联)[J].Chemical Industry and Engineering(化学工业与工程),2014,31(1):33-37.
- [10]Shen Y M,Liu Z F,Li T,et al.Determination and correlation of solubility of tylosintartratein alcohol mixtures[J].Journal of Chemical Thermodynamics,2015,80:128-134.
- [11]Zhang Y,Liu J J,Zhang L,et al.Solubility of 2,5-di-tert-butylhydroquinone and process design for its purification using crystallization[J].Journal of Chemical and Engineering Data,2015,60(7):1968-1974.
- [12]WANG Wei(汪伟),ZHANG Yan(张彦),WANG Ya-yun(王亚运),et al.Measurement and correlation of the solubility of aluminium ethoxide(三乙醇铝溶解度的测定及关联)[J].Journal of Chemical Engineering of Chinese Universities(高校化学工程学报),2015,29(6):1293-1295.
- [13]YANG Jiu-li(杨久利),SHA Zuo-liang(沙作良),YANG Li-bin(杨立斌),et al.Measurement and correlation of glycine solubility in acetone-water mixture(甘氨酸在丙酮-水混合溶剂中溶解度的测定与关联)[J].Journal of Chemical Engineering of Chinese Universities(高校化学工程学报),2015,29(2):471-475.