POLYMORPHOUS FORMS OF RIFAXIMIN, PROCESSES FOR THEIR PRODUCTION AND USE THEREOF IN THE MEDICINAL PREPARATIONS
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Accused Products
Abstract
Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin δ and rifaximin ε useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization process 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.
0 Citations
27 Claims
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1-18. -18. (canceled)
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19. A method of treating bacterial activity in the gastrointestinal tract of a subject, the method comprising:
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orally administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of rifaximin δ
together with a pharmaceutically acceptable excipient selected from the group consisting of diluting, binding, lubricating, disintegrating, colouring, flavouring and sweetening agents,wherein rifaximin δ
has a powder X-ray diffractogram showing peaks at values of the diffraction angles 2θ
of about 5.7°
±
0.2, 6.7°
±
0.2, 7.1°
±
0.2, 8.0°
±
0.2, 8.7°
±
0.2, 10.4°
±
0.2, 10.8°
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0.2, 11.3°
±
0.2, 12.1°
±
0.2, 17.0°
±
0.2, 17.3°
±
0.2, 17.5°
±
0.2, 18.5°
±
0.2, 18.8°
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0.2, 19.1°
±
0.2, 21.0°
±
0.2, 21.5°
±
0.2. - View Dependent Claims (20, 23)
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21. A method of treating bacterial activity in the gastrointestinal tract of a subject, the method comprising:
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topically administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of rifaximin δ
,wherein rifaximin δ
has a powder X-ray diffractogram showing peaks at values of the diffraction angles 2θ
of about 5.7°
±
0.2, 6.7°
±
0.2, 7.1°
±
0.2, 8.0°
±
0.2, 8.7°
±
0.2, 10.4°
±
0.2, 10.8°
±
0.2, 11.3°
±
0.2, 12.1°
±
0.2, 17.0°
±
0.2, 17.3°
±
0.2, 17.5°
±
0.2, 18.5°
±
0.2, 18.80±
0.2, 19.1°
±
0.2, 21.0°
±
0.2, 21.5°
±
0.2. - View Dependent Claims (22)
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24. A method of treating bacterial activity in the gastrointestinal tract of a subject, the method comprising:
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orally administering to the subject by oral route a pharmaceutical composition comprising a therapeutically effective amount of rifaximin ε
together with a pharmaceutically acceptable excipient selected from the group consisting of diluting, binding, lubricating, disintegrating, colouring, flavouring and sweetening agents,wherein rifaximin ε
has a powder X-ray diffractogram showing peaks at values of the diffraction angles 2θ
of 7.0°
±
0.2, 7.3°
±
0.2, 8.2°
±
0.2, 8.7°
±
0.2, 10.3°
±
0.2, 11.1°
±
0.2, 11.7°
±
0.2, 12.4°
±
0.2, 14.5°
±
0.2, 16.3°
±
0.2, 17.2°
±
0.2, 18.0°
±
0.2, 19.4°
±
0.2. - View Dependent Claims (25)
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26. A method of treating bacterial activity in the gastrointestinal tract of a subject, the method comprising:
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topically administering to the subject by oral route a pharmaceutical composition comprising a therapeutically effective amount of rifaximin ε
,wherein rifaximin ε
has a powder X-ray diffractogram showing peaks at values of the diffraction angles 2θ
of 7.0°
±
0.2, 7.3°
±
0.2, 8.2°
±
0.2, 8.7°
±
0.2, 10.3°
±
0.2, 11.1°
±
0.2, 11.7°
±
0.2, 12.4°
±
0.2, 14.5°
±
0.2, 16.3°
±
0.2, 17.2°
±
0.2, 18.0°
±
0.2, 19.4°
±
0.2. - View Dependent Claims (27)
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Specification