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    • 2. 发明申请
    • A SUSTAINED-RELEASE SOLID MEDICAMENT FORM AND A METHOD FOR THE PREPARATION THEREFOF
    • 持续释放固体药物形式及其制备方法
    • WO1989005634A1
    • 1989-06-29
    • PCT/JP1988000258
    • 1988-03-11
    • SHIN-ETSU CHEMICAL CO., LTD.SEKIGAWA, FujioKOKUBO, HiroyasuONDA, Yoshiro
    • SHIN-ETSU CHEMICAL CO., LTD.
    • A61K09/52
    • A61K9/5078A61K9/1676
    • Different from conventional sustained-release granular solid medicament form of which each granule has a structure formed of a core granule containing a pharmaceutically effective ingredient and a coating layer thereon for controlling the releasing rate of the effective ingredient, each granule of the inventive medicament form has a structure formed of a core granule mainly composed of an excipient and a coating layer thereon of a cellulose ether insoluble in hot water and the pharmaceutically effective ingredient is contained in the coating layer of the cellulose ether. The granules are prepared by coating core granules of an excipient with a coating liquid which is a hot aqueous dispersion of a powdery cellulose ether insoluble in hot water and contains the pharmaceutically effective ingredient dissolved or dispersed therein. If necessary, the granules are provided with an overcoating layer of a wax-like material to further improve the controllability of the releasing rate of the effective ingredient.
    • 与常规的缓释颗粒状固体药物形式不同,其中每个颗粒具有由含有药学有效成分的核心颗粒形成的结构和其上的涂层,用于控制有效成分的释放速率,本发明药物形式的每个颗粒具有 在纤维素醚的涂层中含有由主要由赋形剂构成的核心颗粒和其上不溶于热水的纤维素醚和其药学上有效成分的涂层形成的结构。 通过涂覆赋形剂的核心颗粒来制备颗粒,所述涂布液是不溶于热水的粉末状纤维素醚的热水分散体,并含有溶解或分散在其中的药学有效成分。 如果需要,颗粒设置有蜡状材料的外涂层,以进一步提高有效成分的释放速率的可控性。