US 2015/0175627 A1 · POLYMORPHIC FORMS ALPHA, BETA AND GAMMA OF RIFAXIMIN

Abstract

Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.

Claims39

Dependent claims

-3. (canceled)

A polymorph rifaximin preparation having at least one X-ray powder diffraction pattern peak at about:

7.4°±0.2, 7.9°±0.2, and 6.6°±0.2;
or
7.4°±0.2, 8.8°±0.2, and 6.6°±0.2;
or
7.4°±0.2, 10.5°±0.2, and 6.6°±0.2;
or
7.4°±0.2, 11.1°±0.2, and 6.6°±0.2;
or
7.4°±0.2, 6.6°±0.2, and 12.9°±0.2;
or
7.4°±0.2, 11.8°±0.2, and 17.6°±0.2;
or
7.4°±0.2, 11.8°±0.2, and 19.7°±0.2;
or
7.4°±0.2, 11.8°±0.2, and 21.4°±0.2;
or
7.4°±0.2, 11.8°±0.2, and 22.1°±0.2, or
7.4°±0.2, 11.1°±0.2, and 12.9°±0.2;
or
7.4°±0.2, 11.1°±0.2, and 19.7°±0.2;
or
7.4°±0.2, 12.9°±0.2, and 19.7°±0.2;
or
11.1°±0.2, 11.8°±0.2, and 19.7°±0.2;
or
11.1°±0.2, 19.7°±0.2, and 21.4°±0.2;
or
11.1°±0.2, 19.7°±0.2, and 22.1°±0.2, or
11.8°±0.2, 12.9°±0.2, and 19.7°±0.2;
or
11.8°±0.2, 19.7°±0.2, and 22.1°±0.2, 2θ,
at least one X-ray powder diffraction pattern peak at about
5.4°±0.2, 6.4°±0.2, and 7.0°±0.2, or
5.4°±0.2, 6.4°±0.2, and 7.8°±0.2;
or
5.4°±0.2, 6.4°±0.2, and 9.0°±0.2;
or
5.4°±0.2, 6.4°±0.2, and 10.4°±0.2;
or
5.4°±0.2, 6.4°±0.2, and 13.1°±0.2, or
5.4°±0.2, 7.0°±0.2, and 14.4°±0.2;
or
5.4°±0.2 10.4°±0.2, and 18.3°±0.2;
or
5.4°±0.2 10.4°±0.2, and 20.9°±0.2;
or
5.4°±0.2 10.4°±0.2, and 17.1°±0.2, or
6.4°±0.2 7.0°±0.2, and 10.4°±0.2;
or
6.4°±0.2 7.8°±0.2, and 10.4°±0.2;
or
6.4°±0.2 9.0°±0.2, and 10.4°±0.2;
or
6.4°±0.2 10.4°±0.2, and 14.4°±0.2;
or
10.4°±0.2 13.1°±0.2, and 14.4°±0.2;
or
10.4°±0.2 17.1°±0.2, and 17.9°±0.2;
or
10.4°±0.2 17.9°±0.2, and 18.3°±0.2;
or
10.4°±0.2 17.9°±0.2, and 20.9°±0.2;
or
10.4°±0.2 18.3°±0.2, and 20.9°±0.2;
or
14.4°±0.2 17.1°±0.2, and 18.3°±0.2;
or
17.1°±0.2 18.3°±0.2, and 20.9°±0.2;
or
14.4°±0.2 17.1°±0.2, and 20.9°±0.2, 2θ,
Or at least one X-ray powder diffraction pattern peaks at about:
5.0°±0.2, 7.1 and 8.4°±0.2, 2θ;
and
a halo peak.

71 more elements

Dependencies are inferred from the claim text.

Polymorphic forms alpha, beta and gamma of rifaximin

Life of this patent

Polymorphic forms alpha, beta and gamma of rifaximin

Life of this patent

Abstract

Claims39