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    • 5. 发明申请
    • AGGREGATE WITH INCREASED DEFORMABILITY, COMPRISING AT LEAST THREE AMPHIPATS, FOR IMPROVED TRANSPORT THROUGH SEMI-PERMEABLE BARRIERS AND FOR THE NON-INVASIVE DRUG APPLICATION IN VIVO, ESPECIALLY THROUGH THE SKIN
    • 累积增加的可变性,包括至少三种药物,通过半渗透性障碍物进行改进的运输,以及通过皮肤特别是非侵入性药物应用
    • WO2004032900A1
    • 2004-04-22
    • PCT/EP2003/011202
    • 2003-10-09
    • IDEA AGCEVC, GregorVIERL, Ulrich
    • CEVC, GregorVIERL, Ulrich
    • A61K9/127
    • A61K9/127A61K9/0014A61K9/1272A61K31/192A61K31/196A61K31/405A61K31/5415
    • The application describes combinations of at least three amphipatic substances forming aggregate suspensions in a polar liquid. Judicious choice of system components, which differ at least 2-times to 10-times in solubility, ensures said aggregates to have extended, unusually adaptable surfaces. This is probably due to simultaneous action on said aggregates of at least two more soluble substances amongst said three system components, at least one of which is an active ingredient and preferably a drug; the third component, alternatively, can take the role of a drug. The application further deals with the use of said combinations in pharmaceutical preparations capable of transporting drugs into the body of warm blood creatures. This is made possible by the drug loading capability of said aggregates with the highly flexible and deformable coating, which renders the resulting drug carriers highly adaptable. The application finally reveals suitable methods and favourable conditions for carrier manufacturing and application. The application also describes novel formulations of nonsteroidal anti-inflammatory drugs (NSAIDs) based on complex aggregates with at least three amphipatic components suspended in a suitable, e.g. pharmaceutically acceptable, polar liquid medium.
    • 本申请描述了在极性液体中形成聚集体悬浮液的至少三种两亲物质的组合。 系统组件的可靠选择,其溶解度至少是2倍至10倍,确保所述聚集体具有延伸的,异常适应性的表面。 这可能是由于所述三种体系组分中至少两种可溶性物质对所述聚集体的同时作用,其中至少一种是活性成分,优选药物; 替代地,第三组分可以起到药物的作用。 本申请进一步涉及能够将药物输送到温血生物体内的药物制剂中所述组合的用途。 这可以通过所述聚集体与高度柔性和可变形的涂层的药物加载能力而实现,这使得所得到的药物载体高度适应。 该应用终于揭示了载体制造和应用的合适方法和有利条件。 本申请还描述了基于复合聚集体的非甾体抗炎药(NSAID)的新型制剂,其中至少三种两亲成分悬浮在合适的例如, 药学上可接受的极性液体培养基。