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    EXENDINS TO LOWER CHOLESTEROL AND TRIGLYCERIDES
    4.
    发明申请
    EXENDINS TO LOWER CHOLESTEROL AND TRIGLYCERIDES 审中-公开
    降低胆固醇和胆固醇

    公开(公告)号：US20110263496A1

    公开(公告)日：2011-10-27

    申请号：US12992060

    申请日：2009-05-20

    申请人： Mark Fineman ,  Leigh MacConell ,  Kristin Taylor

    发明人： Mark Fineman ,  Leigh MacConell ,  Kristin Taylor

    IPC分类号： A61K38/26 ,  A61P9/10 ,  A61P3/06

    CPC分类号： A61K38/179 ,  A61K9/5031 ,  A61K38/2278 ,  A61K38/26 ,  A61K47/34

    摘要： Provided herein are pharmaceutical formulations containing exendins, exendin agonists, or exendin analog agonists that are administered at therapeutic plasma concentration levels over a sustained period of time to lower total cholesterol levels; to lower LDL-cholesterol levels; to lower triglyceride levels; to treat dyslipidemia; to treat and slow the progression of atherosclerosis; and to treat, prevent, and reduce the risk of heart attacks and strokes in patients. In the pharmaceutical formulations and methods of the invention, the exendin may be exendin-4, an exendin-4 agonist, or an exendin-4 analog agonist. The pharmaceutical formulations may be polymer-based pharmaceutical formulations that may be administered once weekly. An exemplary pharmaceutical formulation comprises 5% (w/w) of exenatide, about 2% (w/w) of sucrose, and about 93% (w/w) of a poly(lactide-co-glycolide) polymer, wherein the poly(lactide-co-glycolide) polymer is in the form of microshperes encapsulating the exenatide.

    摘要翻译： 本文提供含有以持续时间段以治疗血浆浓度水平施用以降低总胆固醇水平的毒蜥吐宁，毒蜥外泌肽激动剂或毒蜥外泌肽类似物激动剂的药物制剂; 降低低密度脂蛋白胆固醇水平; 降低甘油三酯水平; 治疗血脂异常 治疗和减缓动脉粥样硬化的进展; 并治疗，预防和减少患者心脏病发作和中风的风险。 在本发明的药物制剂和方法中，毒蜥外泌肽可以是毒蜥外泌肽-4，毒蜥外泌肽-4激动剂或毒蜥外泌肽-4类似物激动剂。 药物制剂可以是可以每周一次施用的基于聚合物的药物制剂。 示例性药物制剂包含5％（w / w）的艾塞那肽，约2％（w / w）的蔗糖和约93％（w / w）的聚（丙交酯 - 共 - 乙交酯）聚合物，其中聚 （丙交酯 - 共 - 乙交酯）聚合物是包封艾塞那肽的微胶囊形式。