title: Application of spherical silicate to prepare solid dispersion dosage forms with aqueous polymers.
abstract: The objective of this study is to prepare and characterize solid dispersions of nifedipine (NP) using porous spherical silicate micro beads (MB) that were approximately 100 μm in diameter with vinylpyrrolidone/vinyl acetate copolymer (PVP/VA) and a Wurster-type fluidized bed granulator. Compared with previously reported solid dispersion using only MB, the supersaturation of NP dissolved from the proposed system of MB and PVP/VA was maintained during dissolution tests. The proposed system produced a solid dispersion product coated on MB, and morphology was maintained after the coating process to prepare solid dispersion; therefore, the powder characteristics, such as flowability of the proposed solid dispersion product, was tremendously preferable to that of the conventional spray-dried solid dispersions of NP with PVP/VA, expecting to make the consequent manufacturing processes easy for development. Another advantage in the terms of manufacturing is its simple process to prepare solid dispersion by spraying the drug and polymer that were dissolved in an organic solvent onto a MB in a Wurster-type fluidized bed granulator, thus, simplifying the optimization and scale-up with ease.
authors.affiliation: Pharmaceutical Science and Technologies, Eisai Co., Ltd., 1 Kawashima takehaya-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 Kawashima takehaya-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 Kawashima takehaya-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: Chisato
authors.initials: C
authors.lastname: Takahashi
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; D065546:Drug Liberation; D008863:Microspheres; D009543:Nifedipine / Q000008:administration & dosage*; D010316:Particle Size; D011205:Povidone / Q000031:analogs & derivatives* / Q000737:chemistry; D011208:Powders / Q000737:chemistry; D017640:Silicates / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013678:Technology, Pharmaceutical / Q000379:methods*; D014867:Water / Q000737:chemistry
chemical_list: D011208:Powders; D017640:Silicates; C549547:vinylacetate-vinylpyrrolidone copolymer; D014867:Water; D011205:Povidone; D009543:Nifedipine
keywords: Nifedipine; Silicate sphere; Solid dispersion; Vinylpyrrolidone/vinyl acetate copolymer; Wurster-type fluidized bed granulator