MD3653G8 - Forme polimorfe de rifaximină, procedee de obţinere a lor şi utilizarea acestora în calitate de antibiotic - Google Patents
Forme polimorfe de rifaximină, procedee de obţinere a lor şi utilizarea acestora în calitate de antibioticInfo
- Publication number
- MD3653G8 MD3653G8 MDA20060080A MD20060080A MD3653G8 MD 3653 G8 MD3653 G8 MD 3653G8 MD A20060080 A MDA20060080 A MD A20060080A MD 20060080 A MD20060080 A MD 20060080A MD 3653 G8 MD3653 G8 MD 3653G8
- Authority
- MD
- Moldova
- Prior art keywords
- rifaximin
- water content
- produces
- powder
- values
- Prior art date
Links
- NZCRJKRKKOLAOJ-XRCRFVBUSA-N rifaximin Chemical compound OC1=C(C(O)=C2C)C3=C4N=C5C=C(C)C=CN5C4=C1NC(=O)\C(C)=C/C=C/[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@H](C)[C@@H](OC)\C=C\O[C@@]1(C)OC2=C3C1=O NZCRJKRKKOLAOJ-XRCRFVBUSA-N 0.000 title abstract 8
- 229960003040 rifaximin Drugs 0.000 title abstract 8
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000003242 anti bacterial agent Substances 0.000 title 1
- 229940088710 antibiotic agent Drugs 0.000 title 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 5
- 239000000843 powder Substances 0.000 abstract 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 2
- 230000003115 biocidal effect Effects 0.000 abstract 1
- 239000007795 chemical reaction product Substances 0.000 abstract 1
- 238000002425 crystallisation Methods 0.000 abstract 1
- 230000008025 crystallization Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000001035 drying Methods 0.000 abstract 1
- 235000019441 ethanol Nutrition 0.000 abstract 1
- 238000010438 heat treatment Methods 0.000 abstract 1
- 239000000047 product Substances 0.000 abstract 1
- 230000000699 topical effect Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
-
- H—ELECTRICITY
- H05—ELECTRIC TECHNIQUES NOT OTHERWISE PROVIDED FOR
- H05B—ELECTRIC HEATING; ELECTRIC LIGHT SOURCES NOT OTHERWISE PROVIDED FOR; CIRCUIT ARRANGEMENTS FOR ELECTRIC LIGHT SOURCES, IN GENERAL
- H05B6/00—Heating by electric, magnetic or electromagnetic fields
- H05B6/02—Induction heating
- H05B6/10—Induction heating apparatus, other than furnaces, for specific applications
- H05B6/12—Cooking devices
- H05B6/1209—Cooking devices induction cooking plates or the like and devices to be used in combination with them
- H05B6/1236—Cooking devices induction cooking plates or the like and devices to be used in combination with them adapted to induce current in a coil to supply power to a device and electrical heating devices powered in this way
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A61P31/06—Antibacterial agents for tuberculosis
-
- H—ELECTRICITY
- H05—ELECTRIC TECHNIQUES NOT OTHERWISE PROVIDED FOR
- H05B—ELECTRIC HEATING; ELECTRIC LIGHT SOURCES NOT OTHERWISE PROVIDED FOR; CIRCUIT ARRANGEMENTS FOR ELECTRIC LIGHT SOURCES, IN GENERAL
- H05B6/00—Heating by electric, magnetic or electromagnetic fields
- H05B6/02—Induction heating
- H05B6/10—Induction heating apparatus, other than furnaces, for specific applications
- H05B6/12—Cooking devices
- H05B6/1209—Cooking devices induction cooking plates or the like and devices to be used in combination with them
- H05B6/1245—Cooking devices induction cooking plates or the like and devices to be used in combination with them with special coil arrangements
- H05B6/1263—Cooking devices induction cooking plates or the like and devices to be used in combination with them with special coil arrangements using coil cooling arrangements
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Electromagnetism (AREA)
- Physics & Mathematics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
Abstract
Invenţia se referă la forme polimorfe de rifaximină, şi anume la formele α, β, γ.Forma polimorfă α de rifaximină are un conţinut de apă mai mic de 4,5% şi o difractogramă a pulberii cu raze X manifestând vârfuri la valorile unghiurilor de difracţie 2θ 6,6°; 7,4°; 7,9°; 8,8°; 10,5°; 11,1°; 11,8°; 12,9°; 17,6°; 18,5°; 19,7°; 21,0°; 21,4°; 22,1°.Forma polimorfă β de rifaximină are un conţinut de apă mai mare de 4,5% şi o difractogramă a pulberii cu raze X manifestând vârfuri la valorile unghiurilor de difracţie 2θ 5,4°; 6,4°; 7,0°; 7,8°; 9,0°; 10,4°; 13,1°; 14,4°; 17,1°; 17,9°; 18,3°; 20,9°.Forma polimorfă γ de rifaximină are un conţinut de apă între 1,0% şi 2,0% şi o difractogramă a pulberii cu raze X manifestând, în general, un profil amorf şi câteva vârfuri semnificative la valorile unghiurilor de difracţie 2θ 5,0°; 7,1°; 8,4°.Invenţia se referă de asemenea la procedee de obţinere a lor, la care prin încălzire se diluează rifaximină brută în alcool etilic şi se iniţiază cristalizarea produsului prin adăugarea apei la o temperatură anumită, pe parcursul unui anumit interval de timp, după care se realizează uscarea sub control, până când produsul finit ajunge la un anumit conţinut de apă.Formele polimorfe obţinute de rifaximină se utilizează în calitate de preparate medicamentoase cu acţiune antibiotică pentru administrare orală şi locală.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT002144A ITMI20032144A1 (it) | 2003-11-07 | 2003-11-07 | Forme polimorfe di rifaximina, processi per ottenerle e |
| PCT/EP2004/012490 WO2005044823A2 (en) | 2003-11-07 | 2004-11-04 | Polymorphous forms of rifaximin as antibiotics |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| MD20060080A MD20060080A (ro) | 2006-11-30 |
| MD3653F2 MD3653F2 (ro) | 2008-07-31 |
| MD3653G8 true MD3653G8 (ro) | 2016-08-31 |
Family
ID=33187382
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MDA20060080A MD3653G8 (ro) | 2003-11-07 | 2004-11-04 | Forme polimorfe de rifaximină, procedee de obţinere a lor şi utilizarea acestora în calitate de antibiotic |
Country Status (37)
| Country | Link |
|---|---|
| US (5) | US7045620B2 (ro) |
| EP (6) | EP1676848B1 (ro) |
| JP (5) | JP2005139161A (ro) |
| KR (4) | KR20050043589A (ro) |
| CN (4) | CN1613858A (ro) |
| AR (3) | AR043547A1 (ro) |
| AT (3) | ATE361927T1 (ro) |
| AU (2) | AU2004200964A1 (ro) |
| BR (2) | BRPI0402382A (ro) |
| CA (2) | CA2460384A1 (ro) |
| CL (1) | CL2004000498A1 (ro) |
| CO (1) | CO5560083A1 (ro) |
| CY (3) | CY1108017T1 (ro) |
| DE (4) | DE602004006367C5 (ro) |
| DK (3) | DK1557421T3 (ro) |
| ES (3) | ES2320160T4 (ro) |
| HR (2) | HRP20040265A2 (ro) |
| IL (2) | IL160798A0 (ro) |
| IT (1) | ITMI20032144A1 (ro) |
| JO (1) | JO2470B1 (ro) |
| MA (1) | MA27069A1 (ro) |
| MD (1) | MD3653G8 (ro) |
| ME (1) | ME00424B (ro) |
| MX (2) | MXPA04002353A (ro) |
| NO (1) | NO334950B1 (ro) |
| NZ (1) | NZ531622A (ro) |
| PL (3) | PL1676847T3 (ro) |
| PT (3) | PT1676847E (ro) |
| RS (4) | RS54571B1 (ro) |
| RU (1) | RU2270200C2 (ro) |
| SI (3) | SI1676847T1 (ro) |
| TN (2) | TNSN04044A1 (ro) |
| TW (1) | TWI285107B (ro) |
| UA (1) | UA86384C2 (ro) |
| WO (1) | WO2005044823A2 (ro) |
| YU (1) | YU24804A (ro) |
| ZA (1) | ZA200401948B (ro) |
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|---|---|---|---|---|
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| US7048906B2 (en) * | 1995-05-17 | 2006-05-23 | Cedars-Sinai Medical Center | Methods of diagnosing and treating small intestinal bacterial overgrowth (SIBO) and SIBO-related conditions |
| ITMI20032144A1 (it) * | 2003-11-07 | 2005-05-08 | Alfa Wassermann Spa | Forme polimorfe di rifaximina, processi per ottenerle e |
| US20080262024A1 (en) * | 2003-11-07 | 2008-10-23 | Giuseppe Claudio Viscomi | Rifaximin compositions and method of use |
| US7902206B2 (en) * | 2003-11-07 | 2011-03-08 | Alfa Wassermann, S.P.A. | Polymorphic forms α, β and γ of rifaximin |
| US7923553B2 (en) * | 2003-11-07 | 2011-04-12 | Alfa Wassermann, S.P.A. | Processes for the production of polymorphic forms of rifaximin |
| US7906542B2 (en) * | 2004-11-04 | 2011-03-15 | Alfa Wassermann, S.P.A. | Pharmaceutical compositions comprising polymorphic forms α, β, and γ of rifaximin |
| PT1698630E (pt) | 2005-03-03 | 2014-09-15 | Alfa Wassermann Spa | Novas formas polimorfas de rifaximina, processos para a sua produção e a sua utilização nas preparações medicinais |
| ITBO20050123A1 (it) * | 2005-03-07 | 2005-06-06 | Alfa Wassermann Spa | Formulazioni farmaceutiche gastroresistenti contenenti rifaximina |
| ES2538478T3 (es) | 2006-08-02 | 2015-06-22 | Salix Pharmaceuticals, Inc. | Métodos para el tratamiento de enteritis por radiación |
| ITMI20061692A1 (it) | 2006-09-05 | 2008-03-06 | Alfa Wassermann Spa | Uso di polioli per ottenere forme polimorfe stabili di rifaximina |
| KR101480732B1 (ko) * | 2006-09-22 | 2015-01-21 | 씨아이피엘에이 엘티디. | 리팍시민 |
| US20080161337A1 (en) * | 2007-01-03 | 2008-07-03 | Leonard Weinstock | Use of Rifaximin for the Treatment of Chronic Prostatitis |
| US20080159987A1 (en) * | 2007-01-03 | 2008-07-03 | Leonard Weinstock | Use of Rifaximin for the Treatment of Restless Legs Syndrome |
| ITMI20071241A1 (it) * | 2007-06-20 | 2008-12-21 | Solmag S P A | Processo per la preparazione di rifaximina amorfa e rifaximina amorfa cosi' ottenuta |
| US8383151B2 (en) * | 2007-07-06 | 2013-02-26 | Lupin Limited | Pharmaceutical compositions of rifaximin |
| AU2016203925B2 (en) * | 2007-07-06 | 2016-10-20 | Lupin Limited | Pharmaceutical compositions of rifaximin |
| EP3714878B1 (en) * | 2007-07-06 | 2022-01-19 | Lupin Limited | Pharmaceutical compositions of rifaximin |
| US7709634B2 (en) * | 2007-09-20 | 2010-05-04 | Apotex Pharmachem Inc. | Amorphous form of rifaximin and processes for its preparation |
| SG10201607926VA (en) | 2008-02-25 | 2016-11-29 | Salix Pharmaceuticals Ltd | Forms of rifaximin and uses thereof |
| US8486956B2 (en) * | 2008-02-25 | 2013-07-16 | Salix Pharmaceuticals, Ltd | Forms of rifaximin and uses thereof |
| US11779571B2 (en) * | 2008-02-26 | 2023-10-10 | Salix Pharmaceuticals, Inc. | Methods for treating irritable bowel syndrome (IBS) |
| ES2727728T3 (es) | 2008-02-26 | 2019-10-18 | Salix Pharmaceuticals Ltd | Métodos para el tratamiento del síndrome del intestino irritable |
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| ES2986825T3 (es) * | 2011-11-02 | 2024-11-12 | Salix Pharmaceuticals Inc | Rifaximina para la repetición de tratamiento del síndrome del intestino irritable con predominio de diarrea |
| JP2013184902A (ja) * | 2012-03-06 | 2013-09-19 | Aska Pharmaceutical Co Ltd | リファキシミン含有結晶 |
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| ITBO20120368A1 (it) | 2012-07-06 | 2014-01-07 | Alfa Wassermann Spa | Composizioni comprendenti rifaximina e amminoacidi, cristalli di rifaximina derivanti da tali composizioni e loro uso. |
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| EA201591267A1 (ru) | 2013-03-15 | 2016-03-31 | Альфа Вассерманн С.П.А. | Рифаксимин для применения в лечении вагинальных инфекций |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0161534B1 (en) * | 1984-05-15 | 1989-09-20 | ALFA FARMACEUTICI S.p.A. | New process for the synthesis of pyrido-imidazo-refamycins |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0161534B1 (en) * | 1984-05-15 | 1989-09-20 | ALFA FARMACEUTICI S.p.A. | New process for the synthesis of pyrido-imidazo-refamycins |
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Owner name: ALFASIGMA S.P.A., IT VIALE SARCA N.223, MILANO (MI Free format text: PREVIOUS NAME OF PROPRIETOR: ALFA WASSERMANN S.P.A., IT VIA ENRICO FERMI, 1, I-65020 ALANNO (PE), ITALIA |