沙芬酰胺在不同溶剂中的溶解度测定及热力学关联研究

Solubility Determination and Thermodynamic Correlation Study of Safinamide in Six Solvents

溶解度数据是设计和优化结晶过程的重要依据。沙芬酰胺(SAF)是一种新型的单胺氧化酶(MAO-B)抑制剂,在临床上主要用于治疗帕金森病。利用重量法测定了沙芬酰胺在6种纯溶剂(包括甲醇、乙醇、异丙醇、丙酮、乙腈和乙酸乙酯)中的溶解度,测定温度范围为293.15~328.15K,测试压力为常压。沙芬酰胺在6种溶剂中的摩尔溶解度均随温度的升高而增大。在一定温度下,溶解度的由大到小依次为丙酮、甲醇、乙醇、乙酸乙酯、异丙醇、乙腈。用修正的Apelblat方程模型对摩尔溶解度和温度进行数学关联。结果表明:Apelblat方程与沙芬酰胺的摩尔溶解度具有较好的相关性。

Solubility data are an important basis for the design and optimization of crystallization processes.Safinamide(SAF)is a novel monoamine oxidase(MAO-B)inhibitor that is used clinically primarily for the treatment of Parkinson's disease.The solubility of SAF in 6 pure solvents including methanol,ethanol,isopropanol,acetone,acetonitrile and ethyl acetate was measured at temperatures from 293.15 K to 328.15 K under atmospheric pressure by a gravimetric method.The molar solubility of SAF in all six solvents was increased with the increase of temperature.At a given temperature,the solubility order from big to small was as follows:acetone,methanol,ethanol,ethyl acetate,isopropanol,acetonitrile.A modified Apelblat equation model was used to mathematically correlate molar solubility and temperature.The results showed that the Apelblat equation correlated well with the molar solubility of SAF.