title: Fine granules showing sustained drug release prepared by high-shear melt granulation using triglycerin full behenate and milled microcrystalline cellulose.
abstract: This study aimed to prepare fine granules with a diameter less than 200μm and sustained drug release properties by melt granulation. Triglycerin full behenate (TR-FB) was examined as a new meltable binder (MB) by comparison of its properties with those of glycerin monostearate (GM), widely used as MB. The effect of milling microcrystalline cellulose (MCC), an excipient for melt granulation, on the granule properties was also investigated. TR-FB was more stable during heating and storage than GM, and produced smaller granules with narrower particle size distribution, larger yield in the 106-200μm range, uniform roundness and better sustained drug release profile than those prepared with GM. Granules prepared with milled MCC had almost the same physicochemical properties as those produced with intact MCC. However, milled MCC produced granules with a more rigid structure and smaller void space than intact MCC. Consequently, the granules produced with milled MCC showed better sustained drug release behavior than those prepared with intact MCC. We successfully prepared fine granules with sustained drug release properties and diameter of less than 200μm using TR-FB and milled MCC.
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
authors.forename: Hajime
authors.initials: H
authors.lastname: Aoki
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
authors.forename: Yasunori
authors.initials: Y
authors.lastname: Iwao
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
authors.forename: Takeaki
authors.initials: T
authors.lastname: Uchimoto
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
authors.forename: Shuji
authors.initials: S
authors.lastname: Noguchi
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
authors.forename: Ryusuke
authors.initials: R
authors.lastname: Kajihara
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
authors.forename: Kana
authors.initials: K
authors.lastname: Takahashi
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
authors.forename: Masayuki
authors.initials: M
authors.lastname: Ishida
authors.affiliation: Japan Synchrotron Radiation Research Institute, 1-1-1 Kouto, Sayo-gun, Hyogo 679-5198, Japan.
authors.forename: Yasuko
authors.initials: Y
authors.lastname: Terada
authors.affiliation: Japan Synchrotron Radiation Research Institute, 1-1-1 Kouto, Sayo-gun, Hyogo 679-5198, Japan.
authors.forename: Yoshio
authors.initials: Y
authors.lastname: Suzuki
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan. Electronic address: s-itai@u-shizuoka-ken.ac.jp.
authors.forename: Shigeru
authors.initials: S
authors.lastname: Itai
mesh_terms: D000082:Acetaminophen / Q000737:chemistry; D001964:Bromhexine / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D002482:Cellulose / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods*; D065546:Drug Liberation; D005227:Fatty Acids / Q000737:chemistry*; D010316:Particle Size; D033362:Powder Diffraction; D014961:X-Ray Diffraction
chemical_list: D003692:Delayed-Action Preparations; D005227:Fatty Acids; D000082:Acetaminophen; D002482:Cellulose; C109691:microcrystalline cellulose; D001964:Bromhexine
keywords: Computed tomography; High-shear melt granulation; Internal structure; Milling process; Synchrotron X-ray radiation; Triglycerin full behenate