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    • 2. 发明申请
    • LIQUID FORMULATIONS OF COMPOUNDS ACTIVE AT SULFONYLUREA RECEPTORS
    • 化合物的液体配方在磺酰脲受体中有活性
    • WO2009097443A3
    • 2009-12-10
    • PCT/US2009032455
    • 2009-01-29
    • REMEDY PHARMACEUTICALS INCJACOBSON SVEN MARTINCLARKE GILLIANMATHARU RAJINDER
    • JACOBSON SVEN MARTINCLARKE GILLIANMATHARU RAJINDER
    • A61K9/08A61K31/64A61K47/10A61K47/34A61P3/10
    • A61K31/64A61K9/0019A61K9/08A61K47/10A61K47/18A61K47/26
    • 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.
    • 本发明提供了适用于静脉内和动脉内输注的磺酰脲受体的化合物的液体制剂。 在磺酰脲受体中活性的化合物包括格列本脲,甲苯磺丁脲,瑞格列奈,那格列奈,麦格列奈,米格列齐,LY397364,LY389382,氯格列齐和格列美脲。 液体制剂可以是适合储存的浓缩溶液; 可以稀释(例如,稀释1:1或1:1.2)适合于推注,并可进一步稀释(例如,稀释1:10或1:20或更高),用于静脉内和动脉内输注 延长一段时间 例如,液体制剂在包含40%聚乙二醇300,10%乙醇,50%水,约pH 9的水溶液中可包含至少约0.05mg / ml格列本脲。该溶液可包括缓冲液,和 适用于冰箱或室温储存。 该溶液可以以1:1或更多(例如1:20)稀释,而不会沉淀格列本脲。
    • 3. 发明申请
    • LIQUID FORMULATIONS OF COMPOUNDS ACTIVE AT SULFONYLUREA RECEPTORS
    • 在磺酰脲类受体上具有活性的化合物的液体制剂
    • WO2009097443A2
    • 2009-08-06
    • PCT/US2009/032455
    • 2009-01-29
    • REMEDY PHARMACEUTICALS, INC.JACOBSON, Sven, MartinCLARKE, GillianMATHARU, Rajinder
    • JACOBSON, Sven, MartinCLARKE, GillianMATHARU, Rajinder
    • A61K9/08A61K31/64A61K47/10A61K47/34A61P3/10
    • A61K31/64A61K9/0019A61K9/08A61K47/10A61K47/18A61K47/26
    • 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.
    • 本发明提供了作用于适用于静脉内和动脉内输注的磺酰脲类受体的化合物的液体制剂。 对磺酰脲受体具有活性的化合物包括格列本脲,甲苯磺丁脲,瑞格列奈,那格列奈,美格列奈,米格列唑,LY397364,LY389382,甘氨酰叠氮和格列美脲。 液体制剂可以是适合储存的浓缩溶液; 可以被稀释(例如,1:1或1:1.2的稀释)适合于快速浓注,并且可以进一步稀释(例如1:10或1:20或更多的稀释)用于静脉内和动脉内输注 延长一段时间。 例如,液体制剂可以包含至少约0.05mg / ml格列本脲,所​​述基于水的溶液包含在约pH 9的40%聚乙二醇300,10%乙醇,50%水。该溶液可以包含缓冲剂,并且 适合于在冰箱或室温下储存。 该溶液可以1:1或更多(例如1:20)稀释而不沉淀格列本脲。