Discover as soon as possible the most stable form at ambient conditions to guarantee robust process development of new drug substance and drug formulation. Otherwise, there will be a risk that during the crystallisation process scale-up, or upon storage, or in the formulation, the less stable form transforms to a more stable one.
Polymorphism – The ability of molecules to crystallise in different arrangements or conformations of the constituents in the crystal lattice. Different polymorphic forms of drug substances can have different solid-state properties such as solubility, dissolution rate, bioavailability, melting point, physical and chemical stability, mechanical and micromeritic properties. Therefore, investigation of the variety of possible polymorphic forms of potentially new drug candidates must be studied and one must be selected for further development.
If this transformation suddenly occurs during development, it will be necessary to perform the full analysis program again – and this can be costly!
Polymorph screening must be implemented during the preformulation process starting from drug discovery to:
- Perform screening and present the results to authorities to register the drug and have permission to conduct clinical trials.
- Found a polymorphic form that is appropriate for development.
- Study the solid-state properties of new forms.
- Demonstrate the drug administration authorities that the selected form is stable, can be reproduced in the synthesis process and does not change during shelf life, manufacturing process, and formulation shelf life.
- Have a deeper understanding of your drug solid-state properties.
- Evaluate and avoid risks due to unexpected polymorphic form appearance in later stages of development and manufacturing.
Originators and Generics, it is your vital interest to conduct polymorph, salt, cocrystal etc. screening:
- Originators, find the best possible strategy to protect your intellectual property and have additional patent time.
- Generic companies, use possible gaps to avoid patent infringement and be as early as possible on a market.
We assist you in selecting the optimal package that fits your requirements and budget.
Basic Package Designed to find polymorphic forms/crystalline structures of the sample. The tendency to form new crystalline structures, solvates and hydrates in standard processing solvents. An investigation under standard process conditions (e.g. drying, milling and compaction).
Quality and Risk Package This package is designed to find the most stable crystalline structure of the API, define the form for clinical development, including the analysis of relative stability and solubility of the identified forms.
Extended Package Based on results from previous screening: What would be relevant focus areas from here: Special group of solvents, limited temperature range, thermal analysis, etc.