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    • 5. 发明申请
    • PROCESS OF PREPARING ZIPRASIDONE MESYLATE
    • 制备ZIPRASIDONE MESYLATE的方法
    • WO2006086787A1
    • 2006-08-17
    • PCT/US2006/005188
    • 2006-02-13
    • TEVA PHARMACEUTICAL INDUSTRIES LTD.TEVA PHARMACEUTICALS USA, INC.MAINFELD, AlexGOLD, AmirMENDELOVICI, Marioara
    • MAINFELD, AlexGOLD, AmirMENDELOVICI, Marioara
    • C07D417/12
    • C07D417/14C07D417/12
    • In one embodiment, the present invention provides a process of preparing amorphou ziprasidone mesylate comprising the step of spray-drying a solution of ziprasidone mesylat in a solvent selected from a group consisting of: C 1 -C 5 alcohols, C 2 -C 8 ethers, glacial acetic acid and mixtures thereof with water, using an outlet temperature of above about 90°C Preferably the inlet temperature is above the outlet temperature. In another embodiment, the present invention provides a process of preparing ziprasidone mesylate crystal form characterized by X-ray powder diffraction peaks at 11.7, 17.3, 23.5, 24.2, and 25.2 degrees two-theta, ± 0.2 degrees two-theta (herein defined as Form I) comprising the step of spray-drying a solution of ziprasidone mesylate in a solvent selected from a group consisting of: glacial acetic acid and mixtures thereof with C 2 -C 8 ethers using an outlet temperature of above about 70°C, and collecting the obtained Form I. Preferably the inlet temperature is above the outlet temperature. In another embodiment, the present invention provides a process of preparing ziprasidone mesylate crystal form characterized by X-ray powder diffraction peaks at 17.1. 18.7, 23.8, and 24.4 degrees two-theta, ±0.2 degrees two-theta (herein defined as Form VIII) comprising the step of spray-drying a solution of ziprasidone mesylate in C 1 -C 5 alcohols and mixtures thereof with water using an outlet temperature of from about above 45°C to about 70°C. Preferably the inlet temperature is above the outlet temperature.
    • 在一个实施方案中,本发明提供了一种制备甲氧基缩甲硅烷基缩水甘油酯的方法,包括以下步骤:将齐拉西酮甲磺酸盐溶液在选自以下的溶剂中喷雾干燥的步骤:C 1 -C 3 > 5个醇,C 2 -C 8 - 醚,冰乙酸及其与水的混合物,使用出口温度高于约90℃。优选地, 入口温度高于出口温度。 在另一个实施方案中,本发明提供了制备齐拉西酮甲磺酸盐晶体形式的方法,其特征在于在11.7,17.3,23.5,24.2和25.2度2θ,±0.2度2θ(本文定义为 形式I)包括将齐拉西酮甲磺酸酯溶液在选自以下的溶剂中喷雾干燥的步骤:冰醋酸及其与C 2 -C 8的混合物 >使用出口温度高于约70℃的醚,并收集所获得的形式I.优选地,入口温度高于出口温度。 在另一个实施方案中,本发明提供了制备在17.1℃下以X射线粉末衍射峰为特征的齐拉西酮甲磺酸盐晶体形式的方法。 18.7,28.8和24.4度2θ,±0.2度2θ(本文定义为形式VIII),包括将齐拉西酮甲磺酸酯溶液在C 1 -C 3 > 5℃的醇及其与水的混合物,其出口温度为约45℃至约70℃。 优选地,入口温度高于出口温度。