title: Preparation of Controlled-Release Fine Particles Using a Dry Coating Method.
abstract: Wet coating methods use organic solvents to prepare layered particles that provide controlled-release medications. However, this approach has disadvantages in that it can cause particle agglomeration, reduce pharmaceutical stability, and leave residual organic solvents. We used a dry coating method to overcome these issues. Fine particles (less than 50 μm in diameter) of controlled-release theophylline were created using theophylline (TP; model drug), polyethylene glycol 20,000 (PEG; drug fixative), hydrogenated castor oil (HCO; controlled-release material), hydrogenated rapeseed oil (HRSO; controlled-release material), and cornstarch (CS; core particle). An ultrahigh-speed mixer was employed to mix TP and CS for 5 min at 28,000 rpm. Subsequent addition of PEG produced single-core particles with a drug reservoir coating. Addition of HCO and HRSO to these particles produced a controlled-release layer on their surface, resulting in less than 10% TP dissolution after 8 h. We successfully demonstrated that this dry coating method could be used to coat 16-μm CS particles with a drug reservoir layer and a controlled-release layer, producing multi-layer coated single-core particles that were less than 50 μm in diameter. These can be used to prepare controlled-release tablets, capsules, and orally disintegrating tablets.
authors.affiliation: Department of Pharmaceutical Technology, College of Pharmaceutical Sciences, Matsuyama University, 4-2 Bunkyo-cho, Matsuyama, Ehime, 790-8578, Japan. snakamur@cc.matsuyama-u.ac.jp.
authors.forename: Shohei
authors.initials: S
authors.lastname: Nakamura
authors.affiliation: Department of Pharmaceutical Technology, College of Pharmaceutical Sciences, Matsuyama University, 4-2 Bunkyo-cho, Matsuyama, Ehime, 790-8578, Japan.
authors.forename: Takatoshi
authors.initials: T
authors.lastname: Sakamoto
authors.affiliation: Department of Pharmaceutical Technology, College of Pharmaceutical Sciences, Matsuyama University, 4-2 Bunkyo-cho, Matsuyama, Ehime, 790-8578, Japan.
authors.forename: Tomonori
authors.initials: T
authors.lastname: Ito
authors.affiliation: Tokyo Printing Ink Manufacturing Company Limited, 1-397 Yoshino-cho, Kita-ku, Saitama, Saitama, 331-0811, Japan.
authors.forename: Kazuhiro
authors.initials: K
authors.lastname: Kabasawa
authors.affiliation: Department of Pharmaceutical Technology, College of Pharmaceutical Sciences, Matsuyama University, 4-2 Bunkyo-cho, Matsuyama, Ehime, 790-8578, Japan.
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Yuasa
mesh_terms: D002214:Capsules / Q000737:chemistry; D002368:Castor Oil / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry; D005229:Fatty Acids, Monounsaturated / Q000737:chemistry; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D000074262:Rapeseed Oil; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D013213:Starch / Q000737:chemistry; D013607:Tablets / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods; D013806:Theophylline / Q000737:chemistry
chemical_list: D002214:Capsules; D003692:Delayed-Action Preparations; D005079:Excipients; D005229:Fatty Acids, Monounsaturated; D000074262:Rapeseed Oil; D012997:Solvents; D013607:Tablets; D011092:Polyethylene Glycols; D002368:Castor Oil; D013213:Starch; D013806:Theophylline
keywords: controlled-release fine particles; drug reservoir coating; dry coating; multi-layer coating; theophylline