Preparations of Agglomerated Crystals of Polymorphic Mixtures and a New Complex of Indomethacin—Epirizole by the Spherical Crystallization Technique

Particle Design of Drugs via Spherical Crystallization: A Review from Fundamental Aspects to Technology Development

“…Kawashima et al, therefore, developed a spherical co-agglomeration technique based on the SC method and successfully obtained complex agglomerates consisting of indomethacin and epirizole. 20 Spherical co-agglomeration enables co-crystallization and co-agglomeration of drugs, or the crystallization of one drug and simultaneous agglomeration with another drug or excipient, which has potential applications in drug combination, enhancing dissolution rate, and sustained/controlled release. A variety of complex agglomerates such as ibuprofen−rivaroxaban, 21 gemfibrozil− nimodipine, 22 and sustained-release nitrendipine microspheres 23,24 were prepared by spherical co-agglomeration.…”

“…The conventional SC technologies are not suitable for producing agglomerates that combine two or more drugs or for low-dose drugs. Kawashima et al, therefore, developed a spherical co-agglomeration technique based on the SC method and successfully obtained complex agglomerates consisting of indomethacin and epirizole . Spherical co-agglomeration enables co-crystallization and co-agglomeration of drugs, or the crystallization of one drug and simultaneous agglomeration with another drug or excipient, which has potential applications in drug combination, enhancing dissolution rate, and sustained/controlled release.…”

Advances in Crystallization Processes

“…Currently, this technique is used more frequently for the solid dispersion preparation of water-insoluble drugs in order to improve their solubility, dissolution rate and simplify the manufacturing process (Cui et al, 2003, Tapas et al 2009. Spherical crystallization has been developed by Yoshiaki Kawashima and co-workers as a novel particulate design technique to improve processibility such as mixing, filling, tableting characteristics and dissolution rate of pharmaceuticals (Kawashima et al, 1974(Kawashima et al, , 1981(Kawashima et al, , 1983(Kawashima et al, , 1984(Kawashima et al, , 1985(Kawashima et al, , 1989(Kawashima et al, , 1991(Kawashima et al, , 1994(Kawashima et al, , 2002(Kawashima et al, , 2003. The resultant crystals can be designated as spherical agglomerates (Kulkarni and Nagavi, 2002).…”

Preparation of Carvedilol Spherical Crystals Having Solid Dispersion Structure by the Emulsion Solvent Diffusion Method and Evaluation of Its in vitro Characteristics

“…Currently, this technique is used more frequently for the solid dispersion preparation of water-insoluble drugs in order to improve their solubility, dissolution rate and simplify the manufacturing process (Cui et al, 2003, Tapas et al 2009, 2010. Spherical crystallization has been developed by Yoshiaki Kawashima and co-workers as a novel particulate design technique to improve processibility such as mixing, filling, tableting characteristics and dissolution rate of pharmaceuticals (Kawashima et al, 1974(Kawashima et al, , 1976(Kawashima et al, , 1981(Kawashima et al, , 1982(Kawashima et al, , 1983(Kawashima et al, , 1984(Kawashima et al, , 1985(Kawashima et al, , 1989(Kawashima et al, , 1991(Kawashima et al, , 1994(Kawashima et al, , 1995(Kawashima et al, , 2002(Kawashima et al, , 2003. The resultant crystals can be designated as spherical agglomerates (Kulkarni and Nagavi, 2002).…”