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    • 3. 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)。
    • 4. 发明申请
    • OSMOTIC DEVICE FOR DELAYED DELIVERY OF AGENT
    • 用于延迟交付代理的OSMOTIC设备
    • WO1992013521A1
    • 1992-08-20
    • PCT/US1992000635
    • 1992-01-27
    • ALZA CORPORATION
    • ALZA CORPORATIONWONG, Patrick, S.-L.THEEUWES, FelixLARSEN, Steven, D.
    • A61K09/00
    • A61K9/0004A61K9/4808
    • The present invention is directed to a fluid-imbibing dispensing device (1) for the initially delayed delivery of an active agent (20) to a fluid environment of use and to a method of using the dispensing device. The dispenser comprises a housing (12) having a first wall section (14) and a second wall section (16) in slidably telescoping arrangement with each other, which housing (12) maintains its integrity in the environment of use; an internal compartment (18) surrounded and defined by the housing (12); at least one active agent formulation (20) in the compartment; and an expansion means (22) and a partition layer (24) in the compartment for separating apart the first and second wall sections (14, 16) of the housing (12) after exposure to the environment of use to expose the active agent formulations (20) to the environment of use.
    • 本发明涉及一种流体吸入分配装置(1),用于将活性剂(20)最初延迟递送到使用的流体环境和使用分配装置的方法。 分配器包括具有彼此可滑动地伸缩布置的第一壁部分(14)和第二壁部分(16)的壳体(12),该壳体(12)在使用环境中保持其完整性; 由所述壳体(12)包围和限定的内部隔室(18); 所述隔室中的至少一种活性剂制剂(20); 以及在隔室中的膨胀装置(22)和分隔层(24),用于在暴露于使用环境之后将壳体(12)的第一和第二壁部分(14,16)分开以暴露活性剂配方 (20)使用环境。
    • 6. 发明申请
    • DISPENSER CONTAINING HYDROPHOBIC AGENT
    • 含有疏水剂的分配器
    • WO1995006460A1
    • 1995-03-09
    • PCT/US1994009709
    • 1994-08-31
    • ALZA CORPORATION
    • ALZA CORPORATIONDONG, Liang, C.ESPINAL, Steven, D.WONG, Patrick, S.-L.GUITTARD, George, V.HAMEL, Lawrence, G.
    • A61K09/00
    • A61K9/0004A61K9/2013A61K9/2054
    • The present invention is directed to a formulation for the delivery of hydrophobic active agents to a fluid environment of use while avoiding aggregation of the hydrophobic agents in the environment, the formulation comprising a hydrophobic active agent in an amount of 50 wt% (percent by weight) or greater together with polyoxyethylene 40 stearate and a disintegrant. The present invention is also directed to an improvement in a fluid-activated delivery device (10) wherein the delivery device includes a housing (12) defining an internal compartment (14), an active agent formulation (15) in the compartment, exit means (13) in the housing (12) for delivering the active agent formulation (15) from the delivery device, a fluid-activated expandable driving member (16) in the compartment, optionally a partition layer between the active agent formulation (15) and the driving member (16), and optionally a lubricant subcoat (18); wherein the improvement comprises an active agent formulation (15) comprising a hydrophobic active agent in an amount of 50 wt% (percent by weight) or greater together with polyoxyethylene 40 stearate and a disintegrant.
    • 本发明涉及用于将疏水性活性剂递送至使用的流体环境的制剂,同时避免疏水剂在环境中的聚集,所述制剂包含50重量%(重量百分比)的疏水性活性剂 )或更大,与聚氧乙烯40硬脂酸酯和崩解剂一起。 本发明还涉及流体激活的输送装置(10)的改进,其中输送装置包括限定内部隔室(14)的壳体(12),隔室中的活性剂制剂(15),出口装置 (13),用于从所述输送装置输送活性剂制剂(15),所述隔室中的流体活化的可膨胀驱动构件(16),任选地在所述活性剂制剂(15)和 驱动构件(16)和任选的润滑剂底涂层(18); 其中所述改进包括活性剂制剂(15),其包含50重量%(重量百分比)以上的疏水性活性剂以及聚氧乙烯40硬脂酸酯和崩解剂。