PROBLEM TO BE SOLVED: To provide a method for manufacturing granules that mask a physiologically active substance having bitterness and have improved oral administration of a patient by a simple method having high safety.SOLUTION: Microparticles (fine particles) that guarantee light stability and mask bitterness are produced by feeding additive powder particles to a jet fluidized bed granulator, spraying a liquid in which donepezil hydrochloride is dispersed, suspended or partially dissolved in an aqueous solution of polymer binder to the particles while keeping a fluidized state to prepare nuclear particles (granules), spraying a liquid in which insoluble additive particles dispersed or suspended in an aqueous solution of a polymer binder is wet ground to the surfaces of the nuclear particles to form a barrier layer and then coating the particles with a membrane agent for elution control. Further the obtained microparticles are mixed with another additive, regranulated and then tableted to produce high-quality tablets quickly disintegrable in oral cavity, which guarantee light stability and have superior oral administration.COPYRIGHT: (C)2012,JPO&INPIT【課題】苦味を有する生理活性物質をマスキングし患者の服用性を改善した造粒物を、簡便かつ安全性の高い方法での製造する方法を提供する。【解決手段】添加剤粉末粒子を噴流流動層造粒装置に仕込み、流動状態を保ちながら、塩酸ドネペジルを高分子結合剤水溶液に分散・懸濁・一部溶解した液をスプレー添加することで核粒子(造粒物)を調製した後、高分子結合剤水溶液に分散・懸濁した不溶性添加剤粒子を湿式粉砕した液を前記の核粒子の表面にスプレー添加してバリア層を形成し、ついで、溶出制御のための膜剤を被覆することで、光安定性を担保し苦味マスクされた微小粒子(細粒)を製造する。さらに、得られた微小粒子を、他の添加剤と配合、再造粒した後打錠することにより、光安定性を担保し服用性に優れた高品質の口腔内速崩壊錠を製造することができる。【選択図】なし
