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    • 6. 发明申请
    • OPTIMISED PREPARATIONS OF HIGHLY ADAPTABLE AGGREGATES
    • 优选的高度适应性聚合物的制备
    • WO2012126966A2
    • 2012-09-27
    • PCT/EP2012/055040
    • 2012-03-21
    • CEVC, Gregor
    • CEVC, Gregor
    • A61K9/127
    • A61K9/127A61K9/0014A61K9/1272
    • The present invention describes improved compositions comprising aggregates having a higher adaptability, or deformability, owing to the inclusion of certain hydrophilic additives, including suitable organic ionic compounds. The disclosed compositions demonstrate superior adaptability and stability over otherwise similar compositions lacking the disclosed additives. The invention furthermore provides methods for manufacturing said aggregate preparations, wherein the resulting preparations are useful for applications such as receiving an aggregate payload with active ingredients, for biological agent delivery, and for a non¬ invasive targeted treatment of localised body regions at or below the application site of said aggregates.
    • 本发明描述了由于包括某些亲水性添加剂(包括合适的有机离子化合物)而包含具有较高适应性或可变形性的聚集体的改进的组合物。 所公开的组合物相对于缺乏所公开的添加剂的相似组合物表现出优异的适应性和稳定性。 本发明还提供了用于制造所述聚集制剂的方法,其中所得制剂可用于例如接收具有活性成分的聚集体有效载荷,用于生物试剂递送的应用,以及用于非侵入性靶向治疗局部或下方 所述聚集体的应用场所。
    • 7. 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。
    • 9. 发明公开
    • OPTIMISED PREPARATIONS OF HIGHLY ADAPTABLE AGGREGATES
    • 最佳ZUBEREITUNGEN VON HOCHADAPTIBBENEN AGGREGATEN
    • EP2688554A2
    • 2014-01-29
    • EP12710719.1
    • 2012-03-21
    • Cevc, Gregor
    • Cevc, Gregor
    • A61K9/127
    • A61K9/127A61K9/0014A61K9/1272
    • The present invention describes improved compositions comprising aggregates having a higher adaptability, or deformability, owing to the inclusion of certain hydrophilic additives, including suitable organic ionic compounds. The disclosed compositions demonstrate superior adaptability and stability over otherwise similar compositions lacking the disclosed additives. The invention furthermore provides methods for manufacturing said aggregate preparations, wherein the resulting preparations are useful for applications such as receiving an aggregate payload with active ingredients, for biological agent delivery, and for a noninvasive targeted treatment of localised body regions at or below the application site of said aggregates.
    • 本发明描述了由于包括某些亲水性添加剂(包括合适的有机离子化合物)而包含具有较高适应性或可变形性的聚集体的改进的组合物。 所公开的组合物相对于缺乏所公开的添加剂的相似组合物表现出优异的适应性和稳定性。 本发明还提供了用于制造所述聚集制剂的方法,其中所得制剂可用于例如接收具有活性成分的聚集体有效载荷,用于生物试剂递送的应用,以及用于在施用部位处或下方的非侵入性靶向治疗局部体区 的所述聚集体。
    • 10. 发明公开
    • Präparat zur Wirkstoffapplikation in Kleinsttröpfchenform
    • Kleinsttröpfchenform的Präparatzur Wirkstoffapplikation。
    • EP0475160A1
    • 1992-03-18
    • EP91114163.8
    • 1991-08-23
    • Cevc, Gregor, Prof. Dr.
    • Cevc, Gregor, Prof. Dr.
    • A61K9/127
    • A61K9/127A61K9/0019A61K9/1272
    • Die Erfindung betrifft ein Präparat zur Applikation von Wirkstoffen in Form kleinster, insbesondere mit einer membranartigen Hülle aus einer oder wenigen Lagen amphiphiler Moleküle bzw. mit einer amphiphilen Trägersubstanz versehenen Flüssigkeitströpfchen, insbesondere zum Transport des Wirkstoffes in und durch natürliche Barrieren und Konstriktionen wie Häute und dergleichen. Das Präparat weist einen Gehalt einer randaktiven Substanz auf, der bis zu 99 Mol.-% des Gehaltes dieser Substanz entspricht, durch den der Solubilisierungspunkt der Tröpfchen erreicht wird. Das Präparat eignet sich zur nichtinvasiven Verabreichung von Antidiabetica, insbesondere von Insulin. Die Erfindung betrifft außerdem ein Verfahren zur Herstellung solcher Präparate.
    • 本发明涉及一种以微小液滴形式给药的制剂,特别是提供了一种或多种两亲性分子或两亲性载体物质的膜状覆盖物,特别是用于运输 药物通过天然屏障和收缩膜如膜等。 该制剂含有相当于该物质含量达99mol%的边界活性物质,通过该物质达到液滴的溶解点。 该制剂适用于非侵入性给予抗糖尿病药,特别是胰岛素。 本发明还涉及制备这种制剂的方法。