Polymorphic forms of rifaximin, processes for their...

C - Chemistry – Metallurgy – 07 – D

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C07D 498/22 (2006.01) A61K 31/437 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2538546

Crystalline polymorphic forms of rifaximin (INN), referred to as rifaximin .alpha. and rifaximin .beta., and a poorly crystalline form referred to as rifaximin .gamma., useful in the production of medicaments containing rifaximin for the oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and causing the crystallization of the product by addition of water at a fixed temperature and for a fixed period of time, followed by drying under controlled conditions until reaching a precise water content in the end product, are the object of the invention.

L'invention concerne des formes polymorphes cristallines de rifaximine (INN) appelées rifaximine .alpha. et rifaximine .beta., et une forme faiblement cristalline appelée rifaximine .gamma., qui servent à produire des médicaments contenant de la rifaximine, lesquels sont destinés à être administrés par voie orale et topique. Lesdites formes sont obtenues au moyen d'un procédé de cristallisation qui consiste : à dissoudre à chaud la rifaximine brute dans de l'alcool éthylique ; à engendrer la cristallisation du produit par addition d'eau, à une température fixe, sur un laps de temps fixe ; à effectuer un processus de séchage dans des conditions déterminées jusqu'à ce que le produit final présente une teneur en eau définie.?¿

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