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    • 49. 发明申请
    • AQUEOUS SUSPENSIONS OF SUBMICRON 9-HYDROXYRISPERIDONE FATTY ACID ESTERS
    • 现代的亚微米的9-羟基利培酮ORDER的脂肪酸酯水悬浮液
    • WO99025354A2
    • 1999-05-27
    • PCT/EP1998/007321
    • 1998-11-10
    • C07D471/04A61K9/08A61K9/14A61K31/505A61K31/506A61K31/517A61K31/519A61P25/00A61P25/18A61P25/22A61P25/24A61P25/28
    • A61K9/0019A61K9/145A61K9/146Y10S977/775Y10S977/915Y10S977/926
    • The present invention is concerned with a pharmaceutical composition suitable as a depot formulation for administration via intramuscular or subcutaneous injection, comprising: (1) as an active ingredient a therapeutically effective amount of a 9-hydroxy-risperidone fatty acid ester or a salt, or a stereoisomer or a stereoisomeric mixture thereof in submicron form and (2) a pharmaceuticall acceptable carrier; wherein the pharmaceutically acceptable carrier is water and the active ingredient is suspended therein: and with a process of preparing such a composition. The invention further concerns such a pharmaceutical composition for use as a medicament in the treatment of psychosis, schizophrenia, schizoaffective disorders, non-schizophrenic psychoses, behavioural disturbances associated with neurodegenerative disorders, e.g. in dementia, behavioural disturbances in mental retardation and autism, Tourette's syndrome, bipolar mania, depression, anxiety.
    • 本发明涉及作为通过肌内注射或皮下注射,包括贮库制剂用于给药的药物组合物:(1)作为活性成分的治疗有效量的脂肪酸酯9-羟基利培酮, 或该酯的盐,立体异构体或立体异构体混合物,其形式为亚微米颗粒; 和(2)药学上可接受的赋形剂,其是水并且其中活性成分是悬浮的。 还提供了制备这种组合物的方法,本发明还涉及用作精神病,精神分裂症,分裂情感性障碍,非精神分裂性精神病,行为障碍与神经退行性疾病相关的疾病的药物的药物组合物 如老年痴呆症,智力迟钝和孤独症,图雷特氏综合征,双相躁狂,抑郁,焦虑行为障碍。