title: Practical approach to prepare solid dispersion drug product using spherical silicate.
abstract: The purpose of this study is to establish a novel approach for preparing a solid dispersion drug product using spherical silicate by a Wurster-type fluidized bed granulator. The spherical silicate used in this study has porous structure and ideal particle size for loading by a Wurster-type fluidized bed granulator. As model drugs, ibuprofen (IBU), indomethacin (IMC), and phenytoin (PNT) were used and the proposed approach was applied to prepare amorphous drug. All drugs could be loaded on the spherical silicate in an amorphous state. On the other hand, spray drying of spherical silicate suspended in IBU solution was conducted to prepare amorphous product of IBU as a reference; however, complete amorphization was not achieved. Dissolution profiles of each drug after loading on spherical silicate by a Wurster-type fluidized bed granulator were evaluated, and dramatic improvement of dissolution was observed compared with those of crystalline drug. In the proposed approach, specific surface area and particle size of spherical silicate were determined as a key factors to contribute to high yield of amorphous product.
authors.affiliation: Pharmaceutical Science and Technologies, Eisai Co., Ltd., 1 Kawashimatakehaya-machi, Kakamigahara, Gifu 501-6195, Japan; Department of Pharmaceutical Engineering, School of Pharmacy, Aichi Gakuin University, 1-100 Kusumoto, Chikusaku, Nagoya, Aichi 464-8650, Japan.
authors.forename: Kentaro
authors.initials: K
authors.lastname: Nagane
authors.affiliation: Pharmaceutical Science and Technologies, Eisai Co., Ltd., 1 Kawashimatakehaya-machi, Kakamigahara, Gifu 501-6195, Japan.
authors.forename: Susumu
authors.initials: S
authors.lastname: Kimura
authors.affiliation: Pharmaceutical Science and Technologies, Eisai Co., Ltd., 1 Kawashimatakehaya-machi, Kakamigahara, Gifu 501-6195, Japan.
authors.forename: Koji
authors.initials: K
authors.lastname: Ukai
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmacy, Aichi Gakuin University, 1-100 Kusumoto, Chikusaku, Nagoya, Aichi 464-8650, Japan.
authors.forename: Noriko
authors.initials: N
authors.lastname: Ogawa
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmacy, Aichi Gakuin University, 1-100 Kusumoto, Chikusaku, Nagoya, Aichi 464-8650, Japan. Electronic address: hiromitu@dpc.agu.ac.jp.
authors.forename: Hiromitsu
authors.initials: H
authors.lastname: Yamamoto
mesh_terms: D003460:Crystallization; D007052:Ibuprofen / Q000737:chemistry*; D007213:Indomethacin / Q000737:chemistry*; D010316:Particle Size; D010672:Phenytoin / Q000737:chemistry*; D016062:Porosity; D017640:Silicates / Q000737:chemistry*; D012995:Solubility; D012996:Solutions / Q000737:chemistry; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D017640:Silicates; D012996:Solutions; D010672:Phenytoin; D007052:Ibuprofen; D007213:Indomethacin
keywords: Ibuprofen; Indomethacin; Microbead silicate; Phenytoin; Solid dispersion; Wurster-type fluidized bed granulator