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    • 4. 发明申请
    • A CONTROLLED-RELEASE PARTIAL GLYCINE AGONIST COMPOSITION FOR USE WITH LEVODOPA IN PARKINSON'S DISEASE AND METHOD OF USE
    • 一种控制释放部分GLYCINE AGONIST组合物,用于帕金森病中的雷帕多和其使用方法
    • WO2009059242A1
    • 2009-05-07
    • PCT/US2008082139
    • 2008-10-31
    • LAZARUS THERAPEUTICS INCFIORENTINI ROBERTO
    • FIORENTINI ROBERTO
    • A01N43/58
    • A61K31/00A61K31/196A61K31/198A61K31/4015A61K31/42A61K2300/00
    • A pharmaceutical composition comprises partial glycine agonist in a controlled release formulation for once a day administration to subjects with Parkinson's disease. The composition includes a controlled release material comprising a partial glycine agonist, a sustained release component, and at least one pharmaceutically acceptable excipient, wherein the composition upon initial administration of one dose provides a mean plasma concentration of the partial glycine agonist of ai least 10 µg/mL and not more than 30 µg/mL within one hour of administration and continues to provide a mean plasma concentration of the partial glycine agonist of not more than 30 µg/mL for 12 - 16 hours. The partial glycine agonist is administered in a dose effective to enhance the efficacy of the levodopa or to reduce the frequency or severity of side effects of the levodopa. A method for treating Parkinson's disease in a subject comprises administering levodopa to the patient at least once per dav and administering to the patient a once daily composition including a partial glycine agonist, formulated to provide a release profile wherein sufficient partial glycine agonist is delivered to the brain of the subject to enhance efficiency or reduce the side effects of each levodopa dose for up to 16 hours after administration of the partial glycine agonist.
    • 药物组合物包含控制释放制剂中的部分甘氨酸激动剂,每天给予帕金森氏病患者一天。 该组合物包括控释材料,其包含部分甘氨酸激动剂,持续释放组分和至少一种药学上可接受的赋形剂,其中初始给药一剂时的组合物提供至少10μg的部分甘氨酸激动剂的平均血浆浓度 / mL,给药1小时内不超过30μg/ mL,并持续提供不大于30μg/ mL的部分甘氨酸激动剂的平均血浆浓度12 - 16小时。 部分甘氨酸激动剂以有效提高左旋多巴功效或降低左旋多巴副作用的频率或严重程度的剂量给药。 在受试者中治疗帕金森病的方法包括向患者施用至少一次左旋多巴,并向患者施用每日一次的包含部分甘氨酸激动剂的组合物,其被配制成提供释放曲线,其中将足够的部分甘氨酸激动剂递送至 脑部,以提高效率或减少每次左旋多巴剂量在给予部分甘氨酸激动剂后长达16小时的副作用。