title: Further improvement of orally disintegrating tablets using micronized ethylcellulose.
abstract: The aim of this study is to design a new orally disintegrating tablet (ODT) containing micronized ethylcellulose (MEC). The new ODT was prepared by physical mixing of rapidly disintegrating granules (RDGs) with MEC. To obtain RDGs, mannitol was spray-coated with a suspension of corn starch and crospovidone (9:1, w/w ratio) using a fluidized-bed granulator (suspension spray-coating method). The new ODTs were evaluated for their hardness, friability, thickness, internal structure (X-ray-CT scanning), in vivo disintegration time, and water absorption rate. Since MEC increases tablet hardness by increasing the contact frequency between the granules, the new ODTs could obtain high hardness (>50 N) and low friability (<0.5 %) with relatively low compression force. In addition, fine capillary channels formed in ODTs facilitated the wicking action and enabled rapid disintegration in vivo (<30 s). On the other hand, since MEC has low hygroscopicity, the tablet hardness of ODTs containing MEC remained high for 1 month in high-humidity conditions. In conclusion, the new ODTs containing MEC developed in this study possessed superior properties for clinical use and are expected to be applied for a wide range of functionally released drugs for bitter taste masking, sustained release, and controlled release (pH-dependent film coating, matrix, and microcapsule).
authors.affiliation: Towa Pharmaceutical Co., Ltd., 26-7 Ichiban-Cho, Kadoma, Osaka 571-0033, Japan. y-okuda@towayakuhin.co.jp
authors.forename: Yutaka
authors.initials: Y
authors.lastname: Okuda
authors.forename: Yosuke
authors.initials: Y
authors.lastname: Irisawa
authors.forename: Kazuto
authors.initials: K
authors.lastname: Okimoto
authors.forename: Takashi
authors.initials: T
authors.lastname: Osawa
authors.forename: Shinji
authors.initials: S
authors.lastname: Yamashita
mesh_terms: D000042:Absorption; D000284:Administration, Oral; D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry*; D006244:Hardness; D006245:Hardness Tests; D006813:Humidity; D007700:Kinetics; D008353:Mannitol / Q000737:chemistry; D008956:Models, Chemical; D011205:Povidone / Q000737:chemistry; D012995:Solubility; D013213:Starch / Q000737:chemistry; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods; D014057:Tomography, X-Ray Computed; D014867:Water / Q000737:chemistry; D017155:Wettability
chemical_list: D005079:Excipients; D013607:Tablets; D014867:Water; D008353:Mannitol; C013517:ethyl cellulose; D002482:Cellulose; D013213:Starch; D011205:Povidone