These studies allow to gather knowledge on the nature of the solid states of a given compound.
Investigations on properties on such solid state allow to the right solid phase.
Reliable solid state studies are essential prerequisite for robust crystallization process, pharmaceutical development, elaboration of IP, patents and regulatory files.
We perform numerous experiments (1000+) on small-scale samples of a few mg, controlled by XRPD to highlight new solid states.
We carry out specific screenings for polymorphs/hydrates/solvates, salts and co-crystals.
Data are collected, interpreted and presented in a full-detailed report.
Co-crystals are studied when salt formation is not an option. The co-crystal generally exhibits lower stability than the free form and therefore higher aqueous solubility.
Specific experimental protocols promoting the formation and crystallization of co-crystals are carried out. As for the salts, the preferred co-crystallizers are small molecules that are pharmaceutically acceptable, inexpensive and capable of forming intermolecular bonds. Since incongruent solubility is a typical feature of co-crystal experiments, investigations and characterizations are performed accordingly.
Salt formation is a widely used means to improve crystallinity and/or water solubility. Salt screenings involve salt formation with counterions and crystallization in solvents. Salts improve API solubility, crystallinity and expand the solid phase portfolio.
Specific experimental protocols favoring the formation of salts and crystallization are carried out. Preferred counterions are small molecules that are pharmaceutically acceptable, inexpensive and exhibit appropriate pKa value(s).
What is it ?
Polymorphism is the ability of a molecule to crystallize in several solid forms. Polymorphism control is a mandatory prerequisite for safe and successful pharmaceutical development.
The aim is to create a maximum of opportunities for the compound to present its possible polymorphic forms, hydrates/solvates, amorphous solid. This study consists of numerous crystallization tests under various conditions for the identification of new phases (e.g. maturation, evaporation, cooling, anti-solvent, exposure to steam and more). Polymorphism control thus avoids late development problems due to the appearance of new phases. This also secures the intellectual property (IP) of the customer.