Polymorphic control and Ionic liquids
It is known that more than 95% of drugs are marketed as solids and more than 50% of them are salts. Up to now pharmaceutical industry has relied predominantly on solids, primarily crystalline forms, for the delivery of the active pharmaceutical ingredient (API), for reasons of purity, thermal stability, manufacturing and ease of handling. However, solids are often strongly affected by polymorphic conversions, which impact the bioavailability and thus the drug efficacy, imposing great financial and patenting issues. Having this in mind, it is extremely important to control this solid state phenomenon, or even avoid it, recurring to new alternatives. In past several years, ionic liquids (ILs) have been implemented as green solvents for the synthesis and crystallization of organic/inorganic compounds. In this sense we are focus on controlling polymorphism using this type of solvent alternative. For that we are developing and exploring two different approaches: i) control polymorphism by using ILs as possible green and challenging alternative crystallization media; ii) avoid polymorphism by combining biocompatible compounds with APIs, giving rise to the third generation of ILs, called API-ILs. |
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