Chapter 9
Pharmaceutical Multicomponent
Crystals: Structure, Design,
and Properties
Okky Dwichandra Putra and Hidehiro Uekusa
Abstract Multicomponent crystals, which include cocrystals and salts, have been
of great interest to the pharmaceutical field owing to their ability to be used as an
alternative solid form of drugs with better physicochemical properties compared to
their corresponding parent drugs and as a potential source for patents and research
opportunities. Although multicomponent crystal formation was originally seen to
only improve the solubility and dissolution rate profiles of drug molecules, it has
also shown potential applications in overcoming other problems, such as hygroscopicity, poor tabletability, instability, and bitter taste. This chapter highlights some
multicomponent crystal applications that tackle common unfavorable physicochemical properties of drugs in the pharmaceutical field. The multicomponent crystal
design has been covered with regard to the relation between the crystal structure and
physicochemical properties. The study cases presented in this chapter emphasize
the structural aspect of multicomponent crystals to provide a molecular-level understanding of the physicochemical property changes accompanying multicomponent
crystal formation.
Keywords Multicomponent crystals · Cocrystal · Salt · Physicochemical
properties · Crystal structure · Design
O. D. Putra · H. Uekusa (B)
Department of Chemistry, Tokyo Institute of Technology, Ookayama 2-12-1, Meguro-ku, Tokyo,
Japan
e-mail: uekusa@chem.titech.ac.jp
O. D. Putra
e-mail: dwichandraputra@yahoo.com
© Springer Nature Singapore Pte Ltd. 2020
M. Sakamoto and H. Uekusa (eds.), Advances in Organic Crystal Chemistry,
https://doi.org/10.1007/978-981-15-5085-0_9
153
Pharmaceutical Multicomponent
Crystals: Structure, Design,
and Properties
Okky Dwichandra Putra and Hidehiro Uekusa
Abstract Multicomponent crystals, which include cocrystals and salts, have been
of great interest to the pharmaceutical field owing to their ability to be used as an
alternative solid form of drugs with better physicochemical properties compared to
their corresponding parent drugs and as a potential source for patents and research
opportunities. Although multicomponent crystal formation was originally seen to
only improve the solubility and dissolution rate profiles of drug molecules, it has
also shown potential applications in overcoming other problems, such as hygroscopicity, poor tabletability, instability, and bitter taste. This chapter highlights some
multicomponent crystal applications that tackle common unfavorable physicochemical properties of drugs in the pharmaceutical field. The multicomponent crystal
design has been covered with regard to the relation between the crystal structure and
physicochemical properties. The study cases presented in this chapter emphasize
the structural aspect of multicomponent crystals to provide a molecular-level understanding of the physicochemical property changes accompanying multicomponent
crystal formation.
Keywords Multicomponent crystals · Cocrystal · Salt · Physicochemical
properties · Crystal structure · Design
O. D. Putra · H. Uekusa (B)
Department of Chemistry, Tokyo Institute of Technology, Ookayama 2-12-1, Meguro-ku, Tokyo,
Japan
e-mail: uekusa@chem.titech.ac.jp
O. D. Putra
e-mail: dwichandraputra@yahoo.com
© Springer Nature Singapore Pte Ltd. 2020
M. Sakamoto and H. Uekusa (eds.), Advances in Organic Crystal Chemistry,
https://doi.org/10.1007/978-981-15-5085-0_9
153