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    • 1. 发明申请
    • THERAPEUTIC COMPOSITIONS COMPRISING A POLYPEPTIDE
    • 包含多肽的治疗组合物
    • WO1995003823A1
    • 1995-02-09
    • PCT/US1994008560
    • 1994-07-29
    • ALZA CORPORATION
    • ALZA CORPORATIONYANG, HeechungNGUYEN, Vu, AnhDONG, Liang, C.WONG, Patrick, S.-L.
    • A61K38/27
    • A61K38/27A61K9/1617A61K38/28A61K47/12A61K47/44
    • The present invention is directed to a pharmaceutical formulation of a therapeutic polypeptide together with a permeation-enhancing mixture of sodium salicylate and an oil to provide enhanced absorption of the polypeptide through the wall of the gastrointestinal tract, and particularly of the colon, after oral administration, the amount of oil being from about 10 wt % to about 30 wt %, preferably from about 15 wt % to about 25 wt %, of the total formulation and the amount of sodium salicylate being from about 70 wt % to about 90 wt %, preferably from about 75 wt % to about 85 wt %, of the total formulation. The polypeptide may be non-lyophilized. The pharmaceutical formulation is characterized as a solid, which provides a convenient and improved format for handling and storage and for the preparation of oral dosage forms (such as pills, capsules and delivery vessels) containing a homogeneous mixture of ingredients.
    • 本发明涉及治疗性多肽的药物制剂以及水杨酸钠和油的渗透增强混合物,以在口服给药之后通过胃肠道的壁,特别是结肠壁增强吸收多肽 ,油的量为总制剂的约10重量%至约30重量%,优选约15重量%至约25重量%,水杨酸钠的量为约70重量%至约90重量% ,优选约75重量%至约85重量%。 多肽可以是非冻干的。 药物制剂的特征在于固体,其提供用于处理和储存的方便和改进的形式,以及用于制备含有均匀成分混合物的口服剂型(例如丸剂,胶囊和递送容器)。