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    • 5. 发明申请
    • TRANSNASAL ANTICONVULSIVE PHARMACEUTICAL COMPOSITION COMPRISING POORLY SOLUBLE ANTICONVULSANT
    • 包含不良溶解性物质的跨药物药物组合物
    • WO2009139589A2
    • 2009-11-19
    • PCT/KR2009002567
    • 2009-05-14
    • SK HOLDINGS CO LTDBAEK MYOUNG-KIJO JAE-HOONCHANG HYE-JIN
    • BAEK MYOUNG-KIJO JAE-HOONCHANG HYE-JIN
    • A61K9/08
    • A61K31/5513A61K9/0043A61K47/26A61K47/44
    • There is provided a transnasal anticonvulsive pharmaceutical composition including a poorly soluble anticonvulsant. The anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray- administered, comprises diethylene glycol monoethyl ether and fatty acid ester, wherein the fatty acid ester is selected from the group consisting of caprylocaproyl polyoxylglyceride, isopropyl palmitate, oleoyl polyoxylglyceride, sorbitan monolaurate 20, methyl laurate, ethyl laurate, and polysorbate 20. Also, the anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether, fatty acid ester, methylpyrrolidone, water and alcohol. Therefore, the transnasal anticonvulsive pharmaceutical composition may be useful to highly enhance the bioavailability of the poorly soluble anticonvulsant. Also, the transnasal anticonvulsive pharmaceutical composition may be useful to allow the poorly soluble anticonvulsant to show the improved viscosity and/or enhanced solubility in order to effectively deliver the poorly soluble anticonvulsant at a therapeutic dose.
    • 提供了包含难溶性抗惊厥药的经鼻抗惊厥药物组合物。 包含作为经鼻喷雾给药的作为活性成分的难溶性抗惊厥药的抗惊厥药物组合物包含二甘醇单乙醚和脂肪酸酯,其中脂肪酸酯选自辛酰己酰基聚氧乙烯甘油酯,棕榈酸异丙酯,油酰基 聚氧乙烯甘油酯,脱水山梨糖醇单月桂酸酯20,月桂酸甲酯,月桂酸乙酯和聚山梨酸酯20.此外,通过经鼻喷雾给药的包含作为活性成分的难溶性抗惊厥药的抗惊厥药物组合物包括二甘醇单乙醚,脂肪酸酯,甲基吡咯烷酮 ,水和酒精。 因此,经鼻抗惊厥药物组合物可用于高度增强难溶性抗惊厥药的生物利用度。 此外,经鼻抗惊厥药物组合物可用于使难溶性抗惊厥药显示出改善的粘度和/或增加的溶解性,以有效递送治疗剂量下的难溶性抗惊厥药。