Xu Haojie, Kang Lingling, Qin Jinmei, Lin Jiayu, Xue Min, Meng Zihui
School of Chemistry and Chemical Engineering, Beijing Institute of Technology, Beijing 102488, China.
Shandong Xinhua Pharmaceutical Company Limited, Zibo 255005, Shandong, China.
ACS Omega. 2020 Mar 13;5(11):6141-6145. doi: 10.1021/acsomega.0c00156. eCollection 2020 Mar 24.
A precise determination method of azilsartan solubility between 293.15 and 333.15 K in several ordinary solvents and some of their aqueous mixtures was established by high-performance liquid chromatography. In all tested solvents, its solubility shows exponential growth with the increase in temperature. This trend is especially pronounced in methanol and ethanol. The order of solubility of azilsartan can be expressed as ethanol > tetrahydrofuran > ethanol/water (8/2, v/v) > methanol > methanol/water (8/2, v/v) > -propanol > isopropanol > ethanol/Water (5/5, v/v) > acetonitrile. The solubility data of azilsartan were well correlated by the λ model. Moreover, the thermodynamic data including the dissolving enthalpy, entropy, and Gibbs free energy of azilsartan in each solvent were calculated which is crucial to its preparation technology study.
采用高效液相色谱法建立了阿齐沙坦在293.15至333.15 K之间于几种常见溶剂及其部分水混合溶剂中的精确测定方法。在所有测试溶剂中，其溶解度随温度升高呈指数增长。这种趋势在甲醇和乙醇中尤为明显。阿齐沙坦的溶解度顺序可表示为：乙醇＞四氢呋喃＞乙醇/水（8/2，v/v）＞甲醇＞甲醇/水（8/2，v/v）＞正丙醇＞异丙醇＞乙醇/水（5/5，v/v）＞乙腈。阿齐沙坦的溶解度数据与λ模型具有良好的相关性。此外，还计算了阿齐沙坦在每种溶剂中的溶解焓、熵和吉布斯自由能等热力学数据，这些数据对其制剂工艺研究至关重要。
