Abstract:
The design and synthesis of pharmaceutical cocrystals have received great interest in the
recent years. Cocrystallization of drug substances offers a tremendous opportunity for the
development of new drug products with superior physical and pharmacological properties such as
solubility, stability, hydroscopicity, dissolution rates and bioavailability. This short review
summarizes this highly topical field, covering why the topic is of interest in pharmaceutical
formulation, the definitions and practical scope of cocrystals, cocrystal preparation and
characterization, a comparison of different (traditional and novel) methods for cocrystal formation
and the implications for regulatory control and intellectual property protection. Traditionally,
cocrystals can be prepared by solvent evaporation method, grinding, and slurry method, but every
method has its limitations for certain conditions. The current trend for cocrystal formation uses
sophisticated methods such as the hot melt extrusion method, spray-drying method, supercritical
fluid technology and the newest method: laser irradiation. The purpose of the development of a
new method is not only to overcome the limitation of traditional cocrystallization methods, but also
to generate simpler steps and a continuous process for the production of the cocrystal product. This
article provides a brief explanation of each method that can be used to generate pharmaceutical
cocrystals as well as evaluation of cocrystals. This article also covers how the developing field of
cocrystallization may impact the pharmaceutical intellectual property landscape.
