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    NSAID FORMULATIONS, BASED ON HIGHLY ADAPTABLE AGGREGATES, FOR IMPROVED TRANSPORT THROUGH BARRIERS AND TOPICAL DRUG DELIVERY
    1.
    发明申请
    NSAID FORMULATIONS, BASED ON HIGHLY ADAPTABLE AGGREGATES, FOR IMPROVED TRANSPORT THROUGH BARRIERS AND TOPICAL DRUG DELIVERY 审中-公开
    基于高适应性聚合物的NSAID配方，通过障碍物和局部药物递送进行改进的运输

    公开(公告)号：US20090060989A1

    公开(公告)日：2009-03-05

    申请号：US12244703

    申请日：2008-10-02

    申请人： Gregor Cevc ,  Ulrich Vierl

    发明人： Gregor Cevc ,  Ulrich Vierl

    IPC分类号： A61K9/127 ,  A61K31/192 ,  A61K31/196 ,  A61P29/00 ,  A61K31/405

    CPC分类号： A61K9/127 ,  A61K9/1272 ,  A61K31/192 ,  A61K31/196 ,  A61K31/405 ,  A61K31/5415 ,  A61K47/10 ,  A61K47/12 ,  A61K47/16 ,  A61K47/20 ,  A61K47/26 ,  A61K47/34 ,  Y10S514/886

    摘要： The invention 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. A suitably ionised NSAID is one of the two, amongst said three, components that tends to destabilise lipid membranes, the other system component with such activity being typically a surfactant. In contrast, the remaining amongst said at least three amphipatic components typically forms a stable lipid membrane on it's own. An essential characteristics of the resulting, relatively large, aggregates is an improved ability to penetrate pores, in a semi-permeable barrier, at least 30%, and often much smaller than the average diameter of the complex aggregate. This enables said aggregates to mediate NSAID transport through semi-permeable barriers including mammalian skin. As a result of the skin penetration by NSAID loaded large aggregates, the drug delivered transcutaneously with such carriers gets deeper into the tissue than the corresponding NSAID 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 thus allows therapy of deep tissues under the drug administration site, which is medically highly desirable.

    摘要翻译： 本发明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血浆中。 药学上可接受的极性液体培养基。 合适的电离的NSAID是趋向于使脂质膜不稳定的所述三种组分中的两种之一，具有这种活性的其它体系组分通常是表面活性剂。 相比之下，所述至少三种两亲成分中的剩余部分通常在其自身上形成稳定的脂质膜。 所得到的相对大的聚集体的基本特征是在半渗透性屏障中渗透孔的改进能力，至少30％，并且通常远小于复合物聚集体的平均直径。 这使得所述聚集体能够通过包括哺乳动物皮肤的半渗透屏障介导NSAID转运。 由于通过NSAID装载的大聚集体的皮肤渗透，与这种载体经皮递送的药物比来自皮肤表面上的溶液的相应NSAID更深入组织中。 这被认为是由于合适的大载体绕过皮肤上表皮 - 真皮连接处的毛细血管的局部水槽的特殊能力。 载体介导的局部施用的NSAID的递送因此允许治疗药物施用部位下的深层组织，其在医学上是非常需要的。

    AGGREGATES 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
    2.
    发明申请
    AGGREGATES 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 审中-公开
    累积增加的可变性，包括至少三种AMPHIPATS，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

    公开(公告)号：US20120177698A1

    公开(公告)日：2012-07-12

    申请号：US13315236

    申请日：2011-12-08

    申请人： Gregor Cevc ,  Ulrich Vierl

    发明人： Gregor Cevc ,  Ulrich Vierl

    IPC分类号： A61K9/00

    CPC分类号： A61K9/127 ,  A61K9/1272 ,  A61K31/192 ,  A61K31/196 ,  A61K31/405 ,  A61K31/5415 ,  A61K47/10 ,  A61K47/12 ,  A61K47/16 ,  A61K47/20 ,  A61K47/26 ,  A61K47/34 ,  Y10S514/886

    摘要： The invention describes combinations of at least three amphipatic substances forming aggregate suspensions in a polar liquid. Judicious choice of system components 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 disclosure 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 disclosure also provides methods and favourable conditions for carrier manufacturing and application.

    摘要翻译： 本发明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可确保所述聚合体具有扩展的，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; 替代的第三个组分可以起到药物的作用。 本公开进一步涉及在能够将药物输送到温血生物体内的药物制剂中使用所述组合。 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。 本公开还提供了载体制造和应用的方法和有利条件。

    NSAID formulations, based on highly adaptable aggregates, for improved transport through barriers and topical drug delivery
    3.
    发明授权
    NSAID formulations, based on highly adaptable aggregates, for improved transport through barriers and topical drug delivery 有权
    NSAID制剂基于高适应性聚集体，用于改善通过屏障和局部药物递送的运输

    公开(公告)号：US07473432B2

    公开(公告)日：2009-01-06

    申请号：US10357617

    申请日：2003-02-04

    申请人： Gregor Cevc ,  Ulrich Vierl

    发明人： Gregor Cevc ,  Ulrich Vierl

    IPC分类号： A61K9/127

    CPC分类号： A61K9/127 ,  A61K9/1272 ,  A61K31/192 ,  A61K31/196 ,  A61K31/405 ,  A61K31/5415 ,  A61K47/10 ,  A61K47/12 ,  A61K47/16 ,  A61K47/20 ,  A61K47/26 ,  A61K47/34 ,  Y10S514/886

    摘要： The invention 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. A suitably ionised NSAID is one of the two, amongst said three, components that tends to destabilise lipid membranes, the other system component with such activity being typically a surfactant. In contrast, the remaining amongst said at least three amphipatic components typically forms a stable lipid membrane on it's own. An essential characteristics of the resulting, relatively large, aggregates is an improved ability to penetrate pores, in a semi-permeable barrier, at least 30%, and often much smaller than the average diameter of the complex aggregate. This enables said aggregates to mediate NSAID transport through semi-permeable barriers including mammalian skin. As a result of the skin penetration by NSAID loaded large aggregates, the drug delivered transcutaneously with such carriers gets deeper into the tissue than the corresponding NSAID 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 thus allows therapy of deep tissues under the drug administration site, which is medically highly desirable.

    摘要翻译： 本发明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血浆中。 药学上可接受的极性液体培养基。 合适的电离的NSAID是趋向于使脂质膜不稳定的所述三种组分中的两种之一，具有这种活性的其它体系组分通常是表面活性剂。 相比之下，所述至少三种两亲成分中的剩余部分通常在其自身上形成稳定的脂质膜。 所得到的相对大的聚集体的基本特征是在半渗透性屏障中渗透孔的改进能力，至少30％，并且通常远小于复合物聚集体的平均直径。 这使得所述聚集体能够通过包括哺乳动物皮肤的半渗透屏障介导NSAID转运。 由于通过NSAID装载的大聚集体的皮肤渗透，与这种载体经皮递送的药物比来自皮肤表面上的溶液的相应NSAID更深入组织中。 这被认为是由于合适的大载体绕过皮肤上表皮 - 真皮连接处的毛细血管的局部水槽的特殊能力。 载体介导的局部施用的NSAID的递送因此允许治疗药物施用部位下的深层组织，其在医学上是非常需要的。

    NSAID FORMULATIONS, BASED ON HIGHLY ADAPTABLE AGGREGATES, FOR IMPROVED TRANSPORT THROUGH BARRIERS AND TOPICAL DRUG DELIVERY
    5.
    发明申请
    NSAID FORMULATIONS, BASED ON HIGHLY ADAPTABLE AGGREGATES, FOR IMPROVED TRANSPORT THROUGH BARRIERS AND TOPICAL DRUG DELIVERY 审中-公开

    公开(公告)号：US20090060990A1

    公开(公告)日：2009-03-05

    申请号：US12250980

    申请日：2008-10-14

    申请人： Gregor Cevc ,  Ulrich Vierl

    发明人： Gregor Cevc ,  Ulrich Vierl

    IPC分类号： A61K9/127 ,  A61P29/00

    CPC分类号： A61K9/127 ,  A61K9/1272 ,  A61K31/192 ,  A61K31/196 ,  A61K31/405 ,  A61K31/5415 ,  A61K47/10 ,  A61K47/12 ,  A61K47/16 ,  A61K47/20 ,  A61K47/26 ,  A61K47/34 ,  Y10S514/886

    摘要： The invention 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. A suitably ionised NSAID is one of the two, amongst said three, components that tends to destabilise lipid membranes, the other system component with such activity being typically a surfactant. In contrast, the remaining amongst said at least three amphipatic components typically forms a stable lipid membrane on it's own. An essential characteristics of the resulting, relatively large, aggregates is an improved ability to penetrate pores, in a semi-permeable barrier, at least 30%, and often much smaller than the average diameter of the complex aggregate. This enables said aggregates to mediate NSAID transport through semi-permeable barriers including mammalian skin. As a result of the skin penetration by NSAID loaded large aggregates, the drug delivered transcutaneously with such carriers gets deeper into the tissue than the corresponding NSAID 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 thus allows therapy of deep tissues under the drug administration site, which is medically highly desirable.

    NSAID FORMULATIONS, BASED ON HIGHLY ADAPTABLE AGGREGATES, FOR IMPROVED TRANSPORT THROUGH BARRIERS AND TOPICAL DRUG DELIVERY
    6.
    发明申请
    NSAID FORMULATIONS, BASED ON HIGHLY ADAPTABLE AGGREGATES, FOR IMPROVED TRANSPORT THROUGH BARRIERS AND TOPICAL DRUG DELIVERY 审中-公开
    基于高适应性聚合物的NSAID配方，通过障碍物和局部药物递送进行改进的运输

    公开(公告)号：US20090042989A1

    公开(公告)日：2009-02-12

    申请号：US12250823

    申请日：2008-10-14

    申请人： Gregor Cevc ,  Ulrich Vierl

    发明人： Gregor Cevc ,  Ulrich Vierl

    IPC分类号： A61K31/196 ,  A61K31/192

    CPC分类号： A61K9/127 ,  A61K9/1272 ,  A61K31/192 ,  A61K31/196 ,  A61K31/405 ,  A61K31/5415 ,  A61K47/10 ,  A61K47/12 ,  A61K47/16 ,  A61K47/20 ,  A61K47/26 ,  A61K47/34 ,  Y10S514/886

    摘要： The invention 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. A suitably ionised NSAID is one of the two, amongst said three, components that tends to destabilise lipid membranes, the other system component with such activity being typically a surfactant. In contrast, the remaining amongst said at least three amphipatic components typically forms a stable lipid membrane on it's own. An essential characteristics of the resulting, relatively large, aggregates is an improved ability to penetrate pores, in a semi-permeable barrier, at least 30%, and often much smaller than the average diameter of the complex aggregate. This enables said aggregates to mediate NSAID transport through semi-permeable barriers including mammalian skin. As a result of the skin penetration by NSAID loaded large aggregates, the drug delivered transcutaneously with such carriers gets deeper into the tissue than the corresponding NSAID 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 thus allows therapy of deep tissues under the drug administration site, which is medically highly desirable.

    摘要翻译： 本发明描述了基于复合聚集体的非甾体抗炎药（NSAIDS）的新制剂，其中至少有三个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。 合适的电离的NSAID是趋向于使脂质膜不稳定的所述三种组分中的两种之一，具有这种活性的其它体系组分通常是表面活性剂。 相比之下，所述至少三种两亲成分中的剩余部分通常在其自身上形成稳定的脂质膜。 所得到的相对大的聚集体的基本特征是在半渗透性屏障中渗透孔的改进能力，至少30％，并且通常远小于复合物聚集体的平均直径。 这使得所述聚集体能够通过包括哺乳动物皮肤的半渗透屏障介导NSAID转运。 由于通过NSAID装载的大聚集体的皮肤渗透，与这种载体经皮递送的药物比来自皮肤表面上的溶液的相应NSAID更深入组织中。 这被认为是由于合适的大载体绕过皮肤上表皮 - 真皮连接处的毛细血管的局部水槽的特殊能力。 载体介导的局部施用的NSAID的递送因此允许治疗药物施用部位下的深层组织，其在医学上是非常需要的。

    AGGREGATES 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
    9.
    发明申请
    AGGREGATES 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 审中-公开
    累积增加的可变性，包括至少三种AMPHIPATS，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

    公开(公告)号：US20090155235A1

    公开(公告)日：2009-06-18

    申请号：US12356381

    申请日：2009-01-20

    申请人： Gregor Cevc ,  Ulrich Vierl

    发明人： Gregor Cevc ,  Ulrich Vierl

    IPC分类号： A61K31/122 ,  A61K31/192 ,  A61K31/196 ,  A61K31/485 ,  G01N33/48

    CPC分类号： A61K9/127 ,  A61K9/1272 ,  A61K31/192 ,  A61K31/196 ,  A61K31/405 ,  A61K31/5415 ,  A61K47/10 ,  A61K47/12 ,  A61K47/16 ,  A61K47/20 ,  A61K47/26 ,  A61K47/34 ,  Y10S514/886

    摘要： The invention 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 patent 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 patent finally reveals suitable methods and favourable conditions for carrier manufacturing and application.

    摘要翻译： 本发明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; 替代的第三个组分可以起到药物的作用。 该专利还涉及在能够将药物输送到温血生物体内的药物制剂中使用所述组合。 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。 该专利终于揭示了载体制造和应用的合适方法和有利条件。