Claims for Patent: 10,703,763

Summary for Patent: 10,703,763

Title:	Polymorphous forms of rifaximin, processes for their production and use thereof in the medicinal preparations
Abstract:	Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin .delta. and rifaximin .epsilon. 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.
Inventor(s):	Viscomi; Giuseppe Claudio (Sasso Marconi, IT), Campana; Manuela (Bologna, IT), Confortini; Donatella (Calderara, IT), Barbanti; Maria (Bologna, IT), Braga; Dario (Bologna, IT)
Assignee:	ALFASIGMA S.P.A. (Bologna, IT)
Application Number:	16/291,900
Patent Claims:	1. A method of treating bacterial activity in the gastrointestinal tract of a subject, the method comprising: orally administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of rifaximin .delta. together with a pharmaceutically acceptable excipient selected from the group consisting of diluting, binding, lubricating, disintegrating, colouring, flavouring and sweetening agents, wherein rifaximin .delta. has a powder X-ray diffractogram showing peaks at values of the diffraction angles 2.theta. of about 5.7.degree..+-.0.2, 6.7.degree..+-.0.2, 7.1.degree..+-.0.2, 8.0.degree..+-.0.2, 8.7.degree..+-.0.2, 10.4.degree..+-.0.2, 10.8.degree..+-.0.2, 11.3.degree..+-.0.2, 12.1.degree..+-.0.2, 17.0.degree..+-.0.2, 17.3.degree..+-.0.2, 17.5.degree..+-.0.2, 18.5.degree..+-.0.2, 18.8.degree..+-.0.2, 19.1.degree..+-.0.2, 21.0.degree..+-.0.2, 21.5.degree..+-.0.2. 2. The method of claim 1, wherein the pharmaceutical composition is in a formulation selected from the group consisting of coated or uncoated tablet, hard or soft gelatin capsule, sugar-coated pill, lozenge, wafer sheet, pellet, and powder in sealed packet. 3. A method of treating bacterial activity in the gastrointestinal tract of a subject, the method comprising: topically administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of rifaximin .delta., wherein rifaximin .delta. has a powder X-ray diffractogram showing peaks at values of the diffraction angles 2.theta. of about 5.7.degree..+-.0.2, 6.7.degree..+-.0.2, 7.1.degree..+-.0.2, 8.0.degree..+-.0.2, 8.7.degree..+-.0.2, 10.4.degree..+-.0.2, 10.8.degree..+-.0.2, 11.3.degree..+-.0.2, 12.1.degree..+-.0.2, 17.0.degree..+-.0.2, 17.3.degree..+-.0.2, 17.5.degree..+-.0.2, 18.5.degree..+-.0.2, 18.8.degree..+-.0.2, 19.1.degree..+-.0.2, 21.0.degree..+-.0.2, 21.5.degree..+-.0.2. 4. The method of claim 3, wherein the pharmaceutical composition is in a formulation selected from the group consisting of ointment, pomade, cream, gel and lotion. 5. The method of claim 1, wherein rifaximin .delta. has a water content between 3.0% and 4.5%. 6. A method of treating bacterial activity in the gastrointestinal tract of a subject, the method comprising: orally administering to the subject by oral route a pharmaceutical composition comprising a therapeutically effective amount of rifaximin .epsilon. together with a pharmaceutically acceptable excipient selected from the group consisting of diluting, binding, lubricating, disintegrating, colouring, flavouring and sweetening agents, wherein rifaximin .epsilon. has a powder X-ray diffractogram showing peaks at values of the diffraction angles 2.theta. of 7.0.degree..+-.0.2, 7.3.degree..+-.0.2, 8.2.degree..+-.0.2, 8.7.degree..+-.0.2, 10.3.degree..+-.0.2, 11.1.degree..+-.0.2, 11.7.degree..+-.0.2, 12.4.degree..+-.0.2, 14.5.degree..+-.0.2, 16.3.degree..+-.0.2, 17.2.degree..+-.0.2, 18.0.degree..+-.0.2, 19.4.degree..+-.0.2. 7. The method of claim 6, wherein the pharmaceutical composition is in a formulation selected from the group consisting of coated or uncoated tablet, hard or soft gelatin capsule, sugar-coated pill, lozenge, wafer sheet, pellet, and powder in sealed packet. 8. A method of treating bacterial activity in the gastrointestinal tract of a subject, the method comprising: topically administering to the subject by oral route a pharmaceutical composition comprising a therapeutically effective amount of rifaximin .epsilon., wherein rifaximin .epsilon. has a powder X-ray diffractogram showing peaks at values of the diffraction angles 2.theta. of 7.0.degree..+-.0.2, 7.3.degree..+-.0.2, 8.2.degree..+-.0.2, 8.7.degree..+-.0.2, 10.3.degree..+-.0.2, 11.1.degree..+-.0.2, 11.7.degree..+-.0.2, 12.4.degree..+-.0.2, 14.5.degree..+-.0.2, 16.3.degree..+-.0.2, 17.2.degree..+-.0.2, 18.0.degree..+-.0.2, 19.4.degree..+-.0.2. 9. The method of claim 8, wherein the pharmaceutical composition is in a formulation selected from the group consisting of ointment, pomade, cream, gel and lotion.