Solid Form Screenings
Finding the right polymorph, salt, cocrystal, solvate or amorphous form for your compound through solid form screening
To ensure optimal physical properties, bioavailability, and a strong intellectual property (IP) strategy, it’s essential to identify and select the best solid form of your drug substance, being it a polymorph, a salt, a cocrystal, a solvate or an amorphous form. At Enantia, we provide the solid form screening programs adapted to each stage of yout development.
From an initial solid form screening to quickly identify a suitable and stable crystalline form for early-stage candidates, to a comprehensive screening at later development stages for derisking strategies, intellectual property protection and life cycle management.
The solid forms from our screenings are then characterized, and the selected ones are progressed into crystallization process development programs to ensure an efficient and robust preparation method for clinical and manufacturing production stages.
Our screenings
Polymorph Screening
Any molecule with an ordered crystal lattice structure can exhibit polymorphism, meaning it can exist in different crystalline forms known as polymorphs. Each of these forms may have distinct chemical and physical properties, which can emerge under specific conditions.
At Enantia we conduct polymorph screenings combining multiple techniques and conditions to understand the polymorphic landscape of your compound, and determine the relative stability of different polymorphs so to quickly identify the most stable one.
Depending on the stage and needs of your project, you can choose from an Initial polymorphism screening to quickly identify the most stable polymorph of your candidate with a minimum investment, as well as a more Comprehensive polymorphism study to find other metastable forms not known to date, to minimize risks in drug development and for IP purposes.
Cocrystal screening
Since 2006, Enantia has been at the forefront of the cocrystal field, being Seglentis® one of the cocrystals discovered at Enantia and approved by the FDA.
Our cocrystal screening methodology has been refined over the years to obtain one of the highest ratios of success in the market, and is complemented with our services in characterization and development of scalable preparation procedures for the selected cocrystal forms.
Cocrystals are multi-component systems that can be used to improve the physicochemical properties of small molecules and as part of claims in solid state and formulation patents.
They offer a game-changing advantage over traditional salts as they can be formed even with non-ionizable molecules, and furthermore, their crystal structure reduces the risk of polymorphic changes, minimizing unexpected downstream processing issues.
As a result of the increasing relevance of these solid forms over the last decades, both the FDA and the EMA recognize cocrystals as accepted solid forms of a drug substance (see the cocrystal guidelines from the FDA and the EMA).
Salt screening
Salt formation is a proven strategy to increase solubility, stability and reduice the hygroscopicity of drug substances. At Enantia, we provide tailored salt screening and selection services to identify and develop the most suitable salt forms, either as pharmaceutically acceptable salts, as well as to be used in purification and resolution strategies.
Our process evaluates a wide range of counterions under various conditions, focusing on critical properties like solubility, crystallinity, thermal stability, and hygroscopicity.
Amorphous form development
A growing number of new chemical entities (NCEs) face challenges due to poor aqueous solubility, leading to low bioavailability. For such molecules, amorphous forms can be the optimal solution.
Enantia has the capability to develop amorphous forms and amorphous dispersions using our Buchi B-290 Mini Spray Dryer. This versatile instrument supports both aqueous and organic solvents and enables the preparation of pure amorphous forms and spray-dried dispersions (SDD) in polymers.
We also provide comprehensive support for amorphous material development, including stability assessment across various formulations and production methods. Our experts also develop assays to accurately determine whether there is any crystalline transformation during manufacturing, storage and formulation.