Recent advances in the identification and prediction of polymorphs

Area of Science:

• Pharmaceutical Science
• Materials Science
• Chemical Engineering

Background:

• Polymorphism, the ability of a solid material to exist in multiple crystalline forms, is a critical factor in drug development.
• Uncontrolled polymorphic transitions during pharmaceutical processing can lead to inconsistent product quality and efficacy.

Purpose of the Study:

• To highlight the importance of understanding polymorphism for controlling crystallization processes.
• To emphasize the role of small-scale studies and structural data in achieving desired polymorph selection.

Main Methods:

• Leveraging detailed structural data of polymorphs.
• Strategic design of substrates and additives.
• Careful design of initial small-scale crystallization studies.

Main Results:

• Significant advances in controlling polymorph outcomes during crystallization.
• Demonstrated ability to selectively obtain desired polymorphs or suppress undesired ones.
• Potential to avoid problematic phase changes during scale-up and manufacturing.

Conclusions:

• Increased understanding of polymorphism enables precise control over crystallization.
• Initial small-scale studies are crucial for designing robust manufacturing processes.
• Tailored processing conditions ensure the desired polymorphic form is maintained throughout drug production.