NSAID formulations, based on highly adaptable aggr

专利名称：NSAID formulations, based on highly

adaptable aggregates, for improvedtransport through barriers and topical drugdelivery

发明人：Gregor Cevc,Ulrich Vierl申请号：US10357617申请日：20030204

公开号：US20040071767A1公开日：20040415

摘要：The invention describes novel formulations of nonsteroidal anti-inflammatorydrugs (NSAIDs) based on complex aggregates with at least three amphipatic componentssuspended in a suitable, e.g. pharmaceutically acceptable, polar liquid medium. A suitablyionised NSAID is one of the two, amongst said three, components that tends todestabilise lipid membranes, the other system component with such activity beingtypically a surfactant. In contrast, the remaining amongst said at least three amphipaticcomponents typically forms a stable lipid membrane on it's own. An essentialcharacteristics of the resulting, relatively large, aggregates is an improved ability topenetrate pores, in a semi-permeable barrier, at least 30%, and often much smaller thanthe average diameter of the complex aggregate. This enables said aggregates tomediate NSAID transport through semi-permeable barriers including mammalian skin. Asa result of the skin penetration by NSAID loaded large aggregates, the drug deliveredtranscutaneously with such carriers gets deeper into the tissue than the correspondingNSAID from a solution on the skin surface. This is believed to be due to the special ability

of suitable large carriers to bypass the local sink of blood capillaries at the epidermal-dermal junction in the skin. The carrier-mediated delivery of locally applied NSAIDs thusallows therapy of deep tissues under the drug administration site, which is medicallyhighly desirable.

申请人：CEVC GREGOR,VIERL ULRICH

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