title: A novel approach to a fine particle coating using porous spherical silica as core particles.
abstract: Abstract The applicability of porous spherical silica (PSS) was evaluated as core particles for pharmaceutical products by comparing it with commercial core particles such as mannitol (NP-108), sucrose and microcrystalline cellulose spheres. We investigated the physical properties of core particles, such as particle size distribution, flow properties, crushing strength, plastic limit, drying rate, hygroscopic property and aggregation degree. It was found that PSS was a core particle of small particle size, low friability, high water adsorption capacity, rapid drying rate and lower occurrence of particle aggregation, although wettability is a factor to be carefully considered. The aggregation and taste-masking ability using PSS and NP-108 as core particles were evaluated at a fluidized-bed coating process. The functional coating under the excess spray rate shows different aggregation trends and dissolution profiles between PSS and NP-108; thereby, exhibiting the formation of uniform coating under the excess spray rate in the case of PSS. This expands the range of the acceptable spray feed rates to coat fine particles, and indicates the possibility of decreasing the coating time. The results obtained in this study suggested that the core particle, which has a property like that of PSS, was useful in overcoming such disadvantages as large particle size, which feels gritty in oral cavity; particle aggregation; and the long coating time of the particle coating process. These results will enable the practical fine particle coating method by increasing the range of optimum coating conditions and decreasing the coating time in fluidized bed technology.
authors.affiliation: Global Formulation Research, Japan, Pharmaceutical Science and Technology Core Function Unit, Eisai Product Creation Systems, Eisai Co. Ltd. , 1, Kawashimatakehaya-machi, Kakamigahara, Gifu , Japan .
authors.forename: Makoto
authors.initials: M
authors.lastname: Ishida
authors.forename: Jumpei
authors.initials: J
authors.lastname: Uchiyama
authors.forename: Keiko
authors.initials: K
authors.lastname: Isaji
authors.forename: Yuta
authors.initials: Y
authors.lastname: Suzuki
authors.forename: Yasuyuki
authors.initials: Y
authors.lastname: Ikematsu
authors.forename: Shigeru
authors.initials: S
authors.lastname: Aoki
mesh_terms: D000327:Adsorption; D002482:Cellulose / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D008353:Mannitol / Q000737:chemistry; D010316:Particle Size; D016062:Porosity; D012822:Silicon Dioxide / Q000737:chemistry*; D012995:Solubility; D013395:Sucrose / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods*; D014867:Water / Q000737:chemistry
chemical_list: D014867:Water; D008353:Mannitol; D013395:Sucrose; D012822:Silicon Dioxide; D002482:Cellulose; C109691:microcrystalline cellulose
keywords: Aggregation; Hausner ratio; fluidized bed; granule; hygroscopic; manufacturability; median diameter; plastic limit