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Updated: Jan 20, 2026
11:42
Iterative Optimization of DNA Duplexes for Crystallization of SeqA-DNA Complexes
Published on: November 1, 2012
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Complex methodology for rational design of Apremilast-benzoic acid co-crystallization process
Jan Jirát1, Daniel Ondo2, Martin Babor3
1Department of Chemical Engineering, University of Chemistry and Technology, Technická 3, 166 28 Prague 6 - Dejvice, Czech Republic.
International Journal of Pharmaceutics
|August 30, 2019
Summary
A new Apremilast co-crystal with benzoic acid enhances drug solubility and stability. This study details a scalable co-crystallization process, improving pharmaceutical development.
Area of Science:
- Pharmaceutical Science
- Materials Science
- Chemical Engineering
Background:
- Apremilast is a poorly soluble active pharmaceutical ingredient.
- Improving Apremilast's dissolution and stability is crucial for effective drug development.
- Co-crystallization offers a promising strategy to enhance drug properties.
Purpose of the Study:
- To design and develop a novel co-crystal of Apremilast with benzoic acid.
- To establish an efficient and scalable co-crystallization process.
- To improve the physicochemical properties of Apremilast.
Main Methods:
- Co-crystal design and synthesis using benzoic acid.
- Solvent selection and ternary phase diagram construction.
- Thermodynamic modeling of solid-liquid equilibria.
- Scale-up of the co-crystallization process to 100 mL.
Main Results:
- A novel Apremilast-benzoic acid co-crystal was successfully designed.
- The co-crystal demonstrated significantly improved dissolution and stability.
- An efficient co-crystallization process, including solvent selection and phase diagram analysis, was developed.
- The process was successfully scaled up, proving its feasibility for larger production.
Conclusions:
- The developed Apremilast co-crystal offers enhanced properties for pharmaceutical applications.
- The integrated methodology for co-crystallization process development is efficient and scalable.
- This work provides a viable route for producing larger quantities of the improved Apremilast solid form for further drug development.
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