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Liquid formulations of compounds active at sulfonylurea receptors

机译:对磺酰脲受体有活性的化合物的液体制剂

摘要

The invention provides liquid formulations of compounds that act at sulfonylurea receptors that are suitable for intravenous and intra-arterial infusion. Compounds active at a sulfonylurea receptor include glibenclamide, tolbutamide, repaglinide, nateglinide, meglitinide, midaglizole, LY397364, LY389382, glyclazide, and glimepiride. Liquid formulations may be concentrated solutions suitable for storage; may be diluted (e.g., dilution of 1:1 or 1:1.2) suitable for bolus injections, and may be further diluted (e.g., dilution of 1:10 or 1:20 or more) for intravenous and intra-arterial infusion over an extended period of time. For example, a liquid formulation may include at least about 0.05 mg/ml glibenclamide in a water-based solution including 40% polyethylene glycol 300, 10% Ethanol, 50% water, at about pH 9. The solution may include a buffer, and is suitable for storage in refrigerator or at room temperature. This solution may be diluted 1:1, or more (e.g., 1:20) without precipitation of the glibenclamide.
机译:本发明提供了对磺酰脲受体起作用的化合物的液体制剂,其适合于静脉内和动脉内输注。对磺酰脲受体有活性的化合物包括格列本脲,甲苯磺丁酰胺,瑞格列奈,那格列奈,美格列奈,咪达唑,LY397364,LY389382,甘氨特和格列美脲。液体制剂可以是适合于储存的浓缩溶液。可以稀释(例如1:1或1:1.2的稀释度)以适合推注,也可以进一步稀释(例如1:10或1:20或更高的稀释度)进行静脉和动脉内输注延长时间。例如,液体制剂可以在包含pH约为9的40%聚乙二醇300、10%乙醇,50%水的水基溶液中包含至少约0.05mg / ml的格列本脲。该溶液可以包含缓冲剂,和适合存放在冰箱或室温下。该溶液可以1∶1或更高(例如1∶20)稀释而不使格列本脲沉淀。

著录项

  • 公开/公告号US10688111B2

    专利类型

  • 公开/公告日2020-06-23

    原文格式PDF

  • 申请/专利权人 BIOGEN CHESAPEAKE LLC;

    申请/专利号US201615094461

  • 申请日2016-04-08

  • 分类号A61K31/64;A61K47/18;A61K9/08;A61K47/26;A61K47/10;A61K9;

  • 国家 US

  • 入库时间 2022-08-21 11:31:27

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