Formulations for cell-schedule dependent anticancer agents
    1.
    发明申请
    Formulations for cell-schedule dependent anticancer agents 审中-公开
    细胞计划依赖抗癌剂的制剂

    公开(公告)号:US20060121085A1

    公开(公告)日:2006-06-08

    申请号:US11222668

    申请日:2005-09-09

    IPC分类号: A61K31/7072 A61F2/00 A61K9/14

    摘要: The present invention provides a flowable composition suitable for use as a controlled release implant. The composition includes: (a) a biodegradable, biocompatible thermoplastic polymer that is at least substantially insoluble in aqueous medium, water or body fluid; (b) a cell-cycle dependent biological agent, a schedule-dependent biological agent, a metabolite thereof, a pharmaceutically acceptable salt thereof, or a prodrug thereof; and (c) a biocompatible organic liquid, at standard temperature and pressure, in which the thermoplastic polymer is soluble. The present invention also provides a method of treating cancer in a mammal. The present invention also provides a method of blocking, impeding, or otherwise interfering with cell cycle progression at the G1-phase, G1/S interphase, S-phase, G2/M interface or M-phase of the cell cycle in a mammal. The methods includes administering to a mammal an effective amount of a flowable composition of the present invention.

    摘要翻译: 本发明提供适合用作控释剂的可流动组合物。 组合物包括:(a)可生物降解的生物相容性热塑性聚合物,其至少基本上不溶于水性介质,水或体液; (b)细胞周期依赖性生物制剂,计划依赖性生物制剂,其代谢物,其药学上可接受的盐或其前药; 和(c)在标准温度和压力下的热塑性聚合物可溶的生物相容性有机液体。 本发明还提供了一种治疗哺乳动物癌症的方法。 本发明还提供在哺乳动物的细胞周期的G1期,G1 / S间期,S期,G2 / M界面或M期,阻断,阻碍或以其他方式干扰细胞周期进程的方法。 所述方法包括向哺乳动物施用有效量的本发明的可流动组合物。

    Stabilized Polymeric Delivery System
    2.
    发明申请
    Stabilized Polymeric Delivery System 有权
    稳定的聚合物输送系统

    公开(公告)号:US20080299168A1

    公开(公告)日:2008-12-04

    申请号:US11667433

    申请日:2005-11-10

    IPC分类号: A61K9/00 A61K31/765 A61P43/00

    摘要: The invention relates to a delivery system for the sustained and controlled delivery of a group of bioactive agents. More particularly, the invention relates to a delivery system and a method for delivery of a bioactive agent containing a nucleophilic functional group by means of a biodegradable, sustained-release implant. The implant may be a preformed implant, microparticles or an in situ formed implant. The implant includes a biodegradable thermoplastic polymer, the bioactive agent having a nucleophilic group substituent and a stabilizing associate as well as other optional components. The combination of the stabilizing associate with the bioactive agent prevents and/or minimizes and/or lessens degradation of the thermoplastic polymer by the bioactive agent.

    摘要翻译: 本发明涉及用于持续和控制地递送一组生物活性剂的递送系统。 更具体地,本发明涉及通过可生物降解的持续释放植入物递送含有亲核官能团的生物活性剂的递送系统和方法。 植入物可以是预先形成的植入物,微粒或原位形成的植入物。 植入物包括可生物降解的热塑性聚合物,生物活性剂具有亲核基团取代基和稳定缔合物以及其它任选的组分。 稳定缔合物与生物活性剂的组合防止和/或最小化和/或减少生物活性剂对热塑性聚合物的降解。

    Stabilized polymeric delivery system comprising a water-insoluble polymer and an organic liquid
    3.
    发明授权
    Stabilized polymeric delivery system comprising a water-insoluble polymer and an organic liquid 有权
    包含水不溶性聚合物和有机液体的稳定的聚合物递送系统

    公开(公告)号:US08173148B2

    公开(公告)日:2012-05-08

    申请号:US11667433

    申请日:2005-11-10

    IPC分类号: A61F13/00 A61K9/70 A61K38/00

    摘要: The invention relates to a delivery system for the sustained and controlled delivery of a group of bioactive agents. More particularly, the invention relates to a delivery system and a method for delivery of a bioactive agent containing a nucleophilic functional group by means of a biodegradable, sustained-release implant. The implant may be a preformed implant, microparticles or an in situ formed implant. The implant includes a biodegradable thermoplastic polymer, the bioactive agent having a nucleophilic group substituent and a stabilizing associate as well as other optional components. The combination of the stabilizing associate with the bioactive agent prevents and/or minimizes and/or lessens degradation of the thermoplastic polymer by the bioactive agent.

    摘要翻译: 本发明涉及用于持续和控制地递送一组生物活性剂的递送系统。 更具体地,本发明涉及通过可生物降解的持续释放植入物递送含有亲核官能团的生物活性剂的递送系统和方法。 植入物可以是预先形成的植入物,微粒或原位形成的植入物。 植入物包括可生物降解的热塑性聚合物,生物活性剂具有亲核基团取代基和稳定缔合物以及其它任选的组分。 稳定缔合物与生物活性剂的组合防止和/或最小化和/或减少生物活性剂对热塑性聚合物的降解。

    Sustained delivery formulations of rapamycin compounds
    4.
    发明授权
    Sustained delivery formulations of rapamycin compounds 有权
    雷帕霉素化合物的持续递送配方

    公开(公告)号:US08313763B2

    公开(公告)日:2012-11-20

    申请号:US11706569

    申请日:2007-02-15

    IPC分类号: A61F2/00

    摘要: The present invention relates to a rapamycin sustained release delivery system for treatment of diseases responsive to rapamycin. The sustained release delivery system of the invention includes a flowable composition containing rapamycin or a rapamycin derivative, which is capable of providing an implant containing the rapamycin or derivative thereof. The flowable composition may be injected into tissue whereupon it coagulates to become the solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, an organic liquid and rapamycin or a rapamycin derivative.

    摘要翻译: 本发明涉及一种雷帕霉素持续释放递送系统,用于治疗对雷帕霉素有响应的疾病。 本发明的持续释放递送系统包括含有雷帕霉素或雷帕霉素衍生物的可流动组合物,其能够提供含有雷帕霉素或其衍生物的植入物。 可流动组合物可以注射到组织中,随后凝结成为固体或凝胶,整体式植入物。 可流动组合物包括可生物降解的热塑性聚合物,有机液体和雷帕霉素或雷帕霉素衍生物。

    DEHYDRATED HYDROGEL INCLUSION COMPLEX OF A BIOACTIVE AGENT WITH FLOWABLE DRUG DELIVERY SYSTEM
    5.
    发明申请
    DEHYDRATED HYDROGEL INCLUSION COMPLEX OF A BIOACTIVE AGENT WITH FLOWABLE DRUG DELIVERY SYSTEM 有权
    生物活性剂与流动性药物递送系统的脱水氢化物复合物

    公开(公告)号:US20110171305A1

    公开(公告)日:2011-07-14

    申请号:US12995956

    申请日:2009-06-03

    摘要: The invention provides a controlled release biodegradable polymer formulation adapted for administering bioactive agents such as therapeutic proteins to a patient through implantation of a bolus that forms a depot within the patient's body tissues. The formulation includes a dehydrated inclusion complex of the bioactive agent within a hydrogel, wherein the hydrogel can comprise a polymerized polyalkyleneglycolyl diacrylate, and, optionally, polyalkyleneglycolyl monoacrylates, including methacrylates. Alternatively, the hydrogel can comprise hyaluronic acid, chitosan, agarose, polyvinylacetate, polyvinylpyrrolide, or polyvinylalcohol nanoparticles. The bioactive agent can be a macromolecular material, such as a protein. A method of forming the inventive formulation is also provided, as well as a method for using the formulation in the treatment of a malcondition in a patient in need thereof.

    摘要翻译: 本发明提供了一种控制释放的可生物降解的聚合物制剂,其适于通过植入在患者体内组织内形成贮库的大丸剂向患者施用生物活性剂如治疗性蛋白质。 该制剂包括生物活性剂在水凝胶内的脱水包合络合物,其中所述水凝胶可以包含聚合的聚亚烷基二醇二丙烯酸酯,和任选的聚亚烷基二醇酰基单丙烯酸酯,包括甲基丙烯酸酯。 或者,水凝胶可以包含透明质酸,壳聚糖,琼脂糖,聚乙酸乙烯酯,聚乙烯吡咯烷酮或聚乙烯醇纳米颗粒。 生物活性剂可以是大分子物质,如蛋白质。 还提供了形成本发明制剂的方法,以及用于在有需要的患者中治疗无效的制剂的方法。

    SUSTAINED DELIVERY FORMULATIONS OF RAPAMYCIN COMPOUNDS
    7.
    发明申请
    SUSTAINED DELIVERY FORMULATIONS OF RAPAMYCIN COMPOUNDS 审中-公开
    RAPAMYCIN化合物的持续递送配方

    公开(公告)号:US20140094484A1

    公开(公告)日:2014-04-03

    申请号:US13633572

    申请日:2012-10-02

    摘要: The present invention relates to a rapamycin sustained release delivery system for treatment of diseases responsive to rapamycin. The sustained release delivery system of the invention includes a flowable composition containing rapamycin or a rapamycin derivative, which is capable of providing an implant containing the rapamycin or derivative thereof. The flowable composition may be injected into tissue whereupon it coagulates to become the solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, an organic liquid and rapamycin or a rapamycin derivative.

    摘要翻译: 本发明涉及一种雷帕霉素持续释放递送系统,用于治疗对雷帕霉素有响应的疾病。 本发明的持续释放递送系统包括含有雷帕霉素或雷帕霉素衍生物的可流动组合物,其能够提供含有雷帕霉素或其衍生物的植入物。 可流动组合物可以注射到组织中,随后凝结成为固体或凝胶,整体式植入物。 可流动组合物包括可生物降解的热塑性聚合物,有机液体和雷帕霉素或雷帕霉素衍生物。