Liposomal antineoplastic agent compositions
    11.
    发明授权
    Liposomal antineoplastic agent compositions 失效
    脂质体抗肿瘤剂组合物

    公开(公告)号:US5795589A

    公开(公告)日:1998-08-18

    申请号:US794988

    申请日:1997-02-05

    IPC分类号: A61K9/127 A61K9/133

    摘要: A method for encapsulation of antineoplastic agents in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes may be made by a process that loads the drug by an active mechanism using a transmembrane ion gradient, preferably a tranamembrane pH gradient. Using this technique, trapping efficiencies approach 100%, and liposomes may be loaded with drug immediately prior to use, eliminating stability problem related to drug retention in the liposomes. Drug:lipid ratios employed are about 3-80 fold higher than for traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. An assay method to determine free antineoplastic agents in a liposome preparation is also disclosed.

    摘要翻译: 提供了在脂质体中包封抗肿瘤剂的方法,优选具有高的药物:脂质比。 脂质体可以通过使用跨膜离子梯度,优选跨膜pH梯度的活性机制来加载药物的方法制备。 使用这种技术,捕获效率接近100%,脂质体可以在使用前立即加载药物,消除与脂质体中药物滞留有关的稳定性问题。 药物:使用的脂质比例比传统脂质体制剂高约3-80倍,并且药物从脂质体的释放速率降低。 还公开了一种在脂质体制剂中测定游离抗肿瘤剂的测定方法。

    High drug:lipid formulations of liposomal antineoplastic agents
    12.
    发明授权
    High drug:lipid formulations of liposomal antineoplastic agents 失效
    高药物:脂质体抗肿瘤剂的脂质制剂

    公开(公告)号:US5616341A

    公开(公告)日:1997-04-01

    申请号:US112875

    申请日:1993-08-26

    IPC分类号: A61K9/127 A61K9/133

    摘要: A method for encapsulation of antineoplastic agents in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes may be made by a process that loads the drug by an active mechanism using a transmembrane ion gradient, preferably a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%, and liposomes may be loaded with drug immediately prior to use, eliminating stability problems related to drug retention in the liposomes. Drug:lipid ratios employed are about 3-80 fold higher than for traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. An assay method to determine free antineoplastic agents in a liposome preparation is also disclosed.

    摘要翻译: 提供了在脂质体中包封抗肿瘤剂的方法,优选具有高的药物:脂质比。 脂质体可以通过使用跨膜离子梯度,优选跨膜pH梯度的活性机制加载药物的方法制备。 使用这种技术,捕获效率接近100%,脂质体可以在使用前立即加载药物,消除与脂质体中药物滞留有关的稳定性问题。 药物:使用的脂质比例比传统脂质体制剂高约3-80倍,并且药物从脂质体的释放速率降低。 还公开了一种在脂质体制剂中测定游离抗肿瘤剂的测定方法。

    Encapsulation of antineoplastic agents in liposomes
    13.
    发明授权
    Encapsulation of antineoplastic agents in liposomes 失效
    抗肿瘤剂在脂质体中的封装

    公开(公告)号:US5077056A

    公开(公告)日:1991-12-31

    申请号:US284751

    申请日:1988-12-12

    IPC分类号: A61K9/127

    摘要: Methods for encapsulating ionizable antineoplastic agents in liposomes using transmembrane potentials are provided. Trapping efficiencies approaching 100% and rapid loading are readily achieved. Dehydration protocols which allow liposomes to be conveniently used in the administration of antineoplastic agents in a clinical setting are also provided. In accordance with other aspects of the invention, transmembrane potentials are used to reduce the rate of release of ionizable drugs from liposomes.

    摘要翻译: 提供了使用跨膜电位将可电离抗肿瘤剂包封在脂质体中的方法。 捕获效率接近100%,快速加载容易实现。 还提供允许脂质体在临床环境中方便地用于施用抗肿瘤剂的脱水方案。 根据本发明的其他方面,使用跨膜电位来降低可离子化药物从脂质体释放的速率。

    Composition for targeting, storing and loading of liposomes
    16.
    发明授权
    Composition for targeting, storing and loading of liposomes 失效
    用于靶向,储存和加载脂质体的组合物

    公开(公告)号:US4885172A

    公开(公告)日:1989-12-05

    申请号:US941913

    申请日:1986-12-15

    IPC分类号: A61K9/127 A61K47/48

    摘要: The present invention describes a composition consisting of liposomes covalently or non-covalently coupled to the glycoprotein streptavidin. The streptavidin may additionally be coupled to biotinated proteins such as Immunoglobulin G or monoclonal antibodies.The liposomes of the invention may have a transmembrane potential across their membranes, and may be dehydrated. In addition, the composition may contain ionizable bioactive agents such as antineoplastic agents, and may be used in diagnostic assays.

    摘要翻译: 本发明描述由与糖蛋白链霉抗生物素蛋白共价或非共价偶联的脂质体组成的组合物。 链霉亲和素可以另外与生物素化蛋白例如免疫球蛋白G或单克隆抗体偶联。 本发明的脂质体可跨过其膜具有跨膜电位,并且可以脱水。 此外,组合物可以含有可离子化的生物活性剂,例如抗肿瘤剂,并且可以用于诊断测定。

    Methods for increasing the circulation half-life of protein-based
therapeutics
    19.
    发明授权
    Methods for increasing the circulation half-life of protein-based therapeutics 失效
    增加蛋白质治疗剂循环半衰期的方法

    公开(公告)号:US5780054A

    公开(公告)日:1998-07-14

    申请号:US588014

    申请日:1996-01-17

    IPC分类号: A61K9/127

    CPC分类号: A61K9/1271 Y10S436/829

    摘要: Methods of increasing the circulation half-life of protein-based therapeutics in a host, the methods comprising: (a) administering to the host an amount of a first liposome formulation comprising liposomes and an antineoplastic agent; and (b) administering to the host a second formulation comprising the protein-based therapeutic, wherein the amount of the first liposome formulation is sufficient to suppress an immune response to the protein-based therapeutic of the second formulation, thereby increasing the circulation half-life of the protein-based therapeutic.

    摘要翻译: 增加宿主中基于蛋白质的治疗剂的循环半衰期的方法,所述方法包括:(a)向宿主施用一定量的包含脂质体和抗肿瘤剂的第一脂质体制剂; 并且(b)向宿主施用包含基于蛋白质的治疗剂的第二制剂,其中第一脂质体制剂的量足以抑制对第二制剂的基于蛋白质的治疗的免疫应答,从而增加循环半衰期, 基于蛋白质的治疗的生命。