Crystalline vs. ionic liquid salt forms of active pharmaceutical ingredients: a position paper.
Why not consider liquid salt forms of active pharmaceutical ingredients (APIs) as an alternative versatile tool in the pharmaceutical industry? Recent developments have shown that known APIs can be readily converted into ionic liquids and that these novel phases often possess different properties (e.g., improved solubilities and dissolution rates), which may have a direct impact on the pharmacokinetics and pharmacodynamics of the drug. They may also offer the potential of novel and more efficient delivery modes, as well as patent protection for each of the new forms of the drug. Since these pharmaceutically active ionic liquids represent a thermodynamically stable phase, they avoid the troublesome issues surrounding polymorphism and "polymorphic transformation." In some cases, an active cation and an active anion can be combined to produce a liquid possessing dual functionality. Here we examine and challenge the current industry reliance on crystalline APIs by discussing the breadth and potential impact of liquid salts as a possible approach to phase control.
Stoimenovski
Jelena
J
Monash University, Clayton, Victoria, 3800, Australia.
MacFarlane
Douglas R
DR
Bica
Katharina
K
Rogers
Robin D
RD
D003460:Crystallization; D052578:Ionic Liquids / Q000737:chemistry*; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D012492:Salts / Q000737:chemistry*; D012995:Solubility
D052578:Ionic Liquids; D004364:Pharmaceutical Preparations; D012492:Salts