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High-throughput crystallization: polymorphs, salts, co-crystals and solvates of pharmaceutical solids
Sherry L Morissette1, Orn Almarsson, Matthew L Peterson
1TransForm Pharmaceuticals, Inc., 29 Hartwell Avenue, Lexington, MA 02421, USA. morissette@transformpharma.com
Advanced Drug Delivery Reviews
|February 14, 2004
Summary
High-throughput (HT) crystallization accelerates pharmaceutical development by exploring diverse solid forms like polymorphs, salts, and co-crystals. This technology impacts stability, bioavailability, and regulatory processes.
Area of Science:
- Pharmaceutical Science
- Materials Science
Background:
- High-throughput (HT) screening and combinatorial synthesis are established in drug discovery but less so in development.
- Emerging strategies focus on accelerating pharmaceutical development and characterizing solid form diversity.
Purpose of the Study:
- To review the opportunities and challenges of HT crystallization technologies in pharmaceutical research and development.
- To highlight the importance of solid form diversity, including polymorphs, salts, hydrates, and solvates.
Main Methods:
- Review of emerging high-throughput crystallization technologies.
- Analysis of the impact of solid form diversity on pharmaceutical development.
Main Results:
- HT crystallization enables rapid exploration of diverse pharmaceutical solid forms.
- Solid form diversity significantly influences drug stability, bioavailability, and intellectual property.
Conclusions:
- HT crystallization technologies offer significant advantages for pharmaceutical development.
- Addressing challenges in HT crystallization is crucial for optimizing drug substance characterization and control.