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Composition based on ziprasidone, method of treating psychoses and process for preparing big crystals of ziprasidone

机译:基于齐拉西酮的组合物,治疗精神病的方法和齐拉西酮大晶体的制备方法

摘要

In the present invention, there is disclosed a pharmaceutical composition comprising crystalline ziprasidone free base or crystalline ziprasidone hydrochloride particles having a mean particle size equal to or less than about 85 microns and a pharmaceutically acceptable diluent or carrier. There is also disclosed a process for preparing large crystals of ziprasidone hydrochloride monohydrate, comprising the steps of: 1) dissolving ziprasidone free base in a solvent comprising tetrahydrofuran and water, in a volume ratio of about 22 to 35 unit volumes of tetrahydrofuran to about 1.5 to 8 volumes of water; 2) heating the solution resulting from step (1); 3) adding hydrogen chloride to the solution resulting from step (2); and 4) cooling the solution resulting from step (3).
机译:在本发明中,公开了一种药物组合物,其包含平均粒径等于或小于约85微米的结晶齐拉西酮游离碱或结晶齐拉西酮盐酸盐颗粒和药学上可接受的稀释剂或载体。还公开了制备齐拉西酮盐酸盐一水合物大晶体的方法,该方法包括以下步骤:1)将齐拉西酮游离碱以约22至35单位体积的四氢呋喃对约1.5的体积比溶于包含四氢呋喃和水的溶剂中。到8体积的水; 2)加热步骤(1)得到的溶液; 3)向步骤(2)得到的溶液中加入氯化氢; 4)冷却步骤(3)得到的溶液。

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