Estimating the Solubility, Solution Thermodynamics, and Molecular Interaction of Aliskiren Hemifumarate in Alkylimidazolium Based Ionic Liquids

Molecules

Muzaffar Iqbal¹  Raisuddin Ali²  Mohammad Muqtader³  MohammedF. Aldawsari³  SaadM. Alshahrani³  BjadK. Almutairy³  Abdullah Alshetaili³  Md.Khalid Anwer³  Ahmed Alalaiwe³  Faiyaz Shakeel⁴ 

[1] Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia;Department of Pharmaceutics and Central Lab, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia;Department of Pharmaceutics, College of Pharmacy Prince Sattam Bin Abdulaziz University, Al-Alkharj, 11942, Saudi Arabia;Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia;

关键词: ionic liquids;    solubility;    thermodynamics;    molecular interaction;    entropy;   

DOI  :  10.3390/molecules24152807

来源: DOAJ

【 摘 要 】

Estimating the solubility and solution thermodynamics parameters of aliskiren hemifumarate (AHF) in three different room temperature ionic liquids (RTILs), Transcutol-HP (THP) and water are interesting as there is no solubility data available in the literature. In the current study, the solubility and solution thermodynamics of AHF in three different RTILs, THP and water at the temperature range from 298.2 to 318.2 K under air pressure 0.1 MP were evaluated. The solid phase evaluation by Differential Scanning Calorimetry (DSC) and Powder X-ray Diffraction (PXRD) indicated no conversion of AHF into polymorph. The mole fraction solubility of AHF was found to be highest in 1-hexyl-3-methylimidazolium hexafluorophosphate (HMMHFP) ionic liquid (7.46 × 10⁻²) at 318.2 K. The obtained solubility values of AHF was regressed by the Apelblat and van’t Hoff models with overall root mean square deviations (RMSD) of 0.62% and 1.42%, respectively. The ideal solubility of AHF was higher compared to experimental solubility values at different temperatures. The lowest activity coefficient was found in HMMHFP, which confirmed highest molecular interaction between AHF−HMMHFP. The estimated thermodynamic parameters confirmed endothermic and entropy driven dissolution of AHF in different RTILs, THP, and water.

【 授权许可】

Unknown