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发明授权
US09186355B2 Rifaximin crystalline forms and methods of preparation thereof 有权
利福昔明晶体形式及其制备方法

Rifaximin crystalline forms and methods of preparation thereof
摘要：
The present invention is directed to methods for preparation of a composition comprising mixed crystalline polymorphs rifaximin α and rifaximin β. For example, practice of a method of the invention can provide the composition comprising mixed crystalline polymorphs rifaximin α and rifaximin β wherein the rifaximin β is present in about 3-12% (w/w) or is present in about 5-8% (w/w). The composition comprising mixed crystalline polymorphs rifaximin α and rifaximin β is prepared by dissolving raw rifaximin in a water-soluble organic solvent, for example ethanol, at reflux, then adding water to achieve a final mixed solvent of about 7:3 (v/v) solvent to water ratio, then cooling to 35-40° C. until crystallization commences, then further cooling with stirring to 0° C., then recovery of the crystallized material, and drying to a water content of between 2.5% and 5.0%, to provide the composition comprising mixed crystalline polymorphs rifaximin α and rifaximin β. The composition is suitable for medicinal use, such as in treatment of infections of the gastrointestinal tract.
摘要（中）：

本发明涉及制备包含混合结晶多晶型物利福昔明α和利福昔明组合物的组合物的方法。 例如，实施本发明的方法可以提供包含混合结晶多晶型物rifaximinα和利福昔明的组合物; 其中所述利福昔明和 以约3-12％（w / w）存在或以约5-8％（w / w）存在。 所述组合物包含混合结晶多晶型物利福昔明α和利福昔明＆bgr; 通过将生的利福昔明溶解在水溶性有机溶剂（例如乙醇）中回流制备，然后加入水以达到约7:3（v / v）溶剂与水的比例的最终混合溶剂，然后冷却至35- 40℃，直到结晶开始，然后在搅拌下进一步冷却至0℃，然后回收结晶物质，并干燥至2.5％至5.0％之间的水含量，以提供包含混合结晶多晶型物利福昔明α 和利福昔明 该组合物适用于医药用途，例如治疗胃肠道感染。

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