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AR043547A1 - Formas polimorficas de rifaximina, procesos para su produccion y uso de las mismas en preparaciones medicinales - Google Patents

Formas polimorficas de rifaximina, procesos para su produccion y uso de las mismas en preparaciones medicinales

Info

Publication number
AR043547A1
AR043547A1 ARP040100781A ARP040100781A AR043547A1 AR 043547 A1 AR043547 A1 AR 043547A1 AR P040100781 A ARP040100781 A AR P040100781A AR P040100781 A ARP040100781 A AR P040100781A AR 043547 A1 AR043547 A1 AR 043547A1
Authority
AR
Argentina
Prior art keywords
rifaximin
water
temperature
crude
ethyl alcohol
Prior art date
Application number
ARP040100781A
Other languages
English (en)
Original Assignee
Alfa Wassermann Spa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33187382&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR043547(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Alfa Wassermann Spa filed Critical Alfa Wassermann Spa
Publication of AR043547A1 publication Critical patent/AR043547A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic 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
    • HELECTRICITY
    • H05ELECTRIC TECHNIQUES NOT OTHERWISE PROVIDED FOR
    • H05BELECTRIC HEATING; ELECTRIC LIGHT SOURCES NOT OTHERWISE PROVIDED FOR; CIRCUIT ARRANGEMENTS FOR ELECTRIC LIGHT SOURCES, IN GENERAL
    • H05B6/00Heating by electric, magnetic or electromagnetic fields
    • H05B6/02Induction heating
    • H05B6/10Induction heating apparatus, other than furnaces, for specific applications
    • H05B6/12Cooking devices
    • H05B6/1209Cooking devices induction cooking plates or the like and devices to be used in combination with them
    • H05B6/1236Cooking 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • A61P31/06Antibacterial agents for tuberculosis
    • HELECTRICITY
    • H05ELECTRIC TECHNIQUES NOT OTHERWISE PROVIDED FOR
    • H05BELECTRIC HEATING; ELECTRIC LIGHT SOURCES NOT OTHERWISE PROVIDED FOR; CIRCUIT ARRANGEMENTS FOR ELECTRIC LIGHT SOURCES, IN GENERAL
    • H05B6/00Heating by electric, magnetic or electromagnetic fields
    • H05B6/02Induction heating
    • H05B6/10Induction heating apparatus, other than furnaces, for specific applications
    • H05B6/12Cooking devices
    • H05B6/1209Cooking devices induction cooking plates or the like and devices to be used in combination with them
    • H05B6/1245Cooking devices induction cooking plates or the like and devices to be used in combination with them with special coil arrangements
    • H05B6/1263Cooking 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)
  • 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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Physics & Mathematics (AREA)
  • Electromagnetism (AREA)
  • Engineering & Computer Science (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

Formas cristalinas polimórficas del antibiótico rifaximina (INN) denominadas rifaximina a y rifaximina b y una forma pobremente cristalina denominada rifaximina g. Estas formas son de utilidad en la producción de preparaciones medicinales para uso por vía oral y tópica y se pueden obtener por medio de un proceso de cristalización llevado a cabo por disolución en caliente de la rifaximina cruda en alcohol etílico y por cristalización del producto mediante la adición de agua a una temperatura determinada y por un período de tiempo determinado. La cristalización es seguida de un secado llevado a cabo bajo condiciones controladas hasta alcanzar un contenido de agua específico en el producto final. Reivindicación 1: Una rifaximina alfa purificada, un polimorfo del antibiótico rifaximina, caracterizada porque dicha rifaximina alfa presenta un contenido de agua menor que un 4,5% y produce un difractograma de polvo por rayos X que presenta picos en valores de ángulos de difracción 2theta de 6,6s, 7,4s; 7,9s; 8,8s; 10,5s; 11,1s; 11,8s; 12,9s; 17,6s; 18,5s; 19,7s; 21,0s; 21,4s; 22,1s. Reivindicación 6: Un proceso para la producción de las rifaximinas alfa, beta y gamma, caracterizado porque comprende: hacer reaccionar un equivalente molar de rifaximina O con un exceso de 2-amino-4-metilpiridina en una mezcla de solventes compuesta de agua y alcohol etílico en una relación volumétrica que comprende entre 1:1 y 2:1, por un período de tiempo entre 2 y 8 horas, a una temperatura entre 40sC y 60sC, tratar la masa de reacción a temperatura ambiente con una solución de ácido ascórbico en una mezcla de agua, alcohol etílico y ácido clorhídrico acuoso concentrado, ajustar el pH de la masa de reacción en pH 2,0 con una solución acuosa concentrada de ácido clorhídrico, filtrar la suspensión, lavar todo sólido resultante con la mezcla de solventes de agua/alcohol etílico para obtener una rifaximina cruda, purificar la rifaximina cruda por disolución de la misma en alcohol etílico a una temperatura que comprende entre 45sC y 65sC, hacer precipitar la rifaximina cruda por adición de agua y por disminución de la temperatura de la suspensión a un valor entre 0sC y 50sC bajo agitación por un período de tiempo entre 4 y 36 horas, filtrar la suspensión, lavar el sólido resultante con agua, y secarlo bajo vacío o bajo condiciones de presión normal, con o sin un agente de secado, a una temperatura entre temperatura ambiente y 105sC, por un período de tiempo entre 2 y 72 horas.
ARP040100781A 2003-11-07 2004-03-11 Formas polimorficas de rifaximina, procesos para su produccion y uso de las mismas en preparaciones medicinales AR043547A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IT002144A ITMI20032144A1 (it) 2003-11-07 2003-11-07 Forme polimorfe di rifaximina, processi per ottenerle e

Publications (1)

Publication Number Publication Date
AR043547A1 true AR043547A1 (es) 2005-08-03

Family

ID=33187382

Family Applications (3)

Application Number Title Priority Date Filing Date
ARP040100781A AR043547A1 (es) 2003-11-07 2004-03-11 Formas polimorficas de rifaximina, procesos para su produccion y uso de las mismas en preparaciones medicinales
ARP110102194A AR081992A2 (es) 2003-11-07 2011-06-23 FORMA POLIMORFICA g DE RIFAXIMINA, PROCESOS PARA SU PRODUCCION Y SUS COMPOSICIONES FARMACEUTICAS
ARP110102193A AR081991A2 (es) 2003-11-07 2011-06-23 FORMA POLIMORFICA b DE RIFAXIMINA, PROCESOS PARA SU PRODUCCION Y SUS COMPOSICIONES FARMACEUTICAS

Family Applications After (2)

Application Number Title Priority Date Filing Date
ARP110102194A AR081992A2 (es) 2003-11-07 2011-06-23 FORMA POLIMORFICA g DE RIFAXIMINA, PROCESOS PARA SU PRODUCCION Y SUS COMPOSICIONES FARMACEUTICAS
ARP110102193A AR081991A2 (es) 2003-11-07 2011-06-23 FORMA POLIMORFICA b DE RIFAXIMINA, PROCESOS PARA SU PRODUCCION Y SUS COMPOSICIONES FARMACEUTICAS

Country Status (37)

Country Link
US (5) US7045620B2 (es)
EP (6) EP1676847B1 (es)
JP (5) JP2005139161A (es)
KR (4) KR20050043589A (es)
CN (4) CN1613858A (es)
AR (3) AR043547A1 (es)
AT (3) ATE421965T1 (es)
AU (2) AU2004200964A1 (es)
BR (2) BRPI0402382A (es)
CA (2) CA2460384A1 (es)
CL (1) CL2004000498A1 (es)
CO (1) CO5560083A1 (es)
CY (3) CY1108017T1 (es)
DE (4) DE602004019296D1 (es)
DK (3) DK1676847T3 (es)
ES (3) ES2320161T3 (es)
HR (2) HRP20040265A2 (es)
IL (2) IL160798A0 (es)
IT (1) ITMI20032144A1 (es)
JO (1) JO2470B1 (es)
MA (1) MA27069A1 (es)
MD (1) MD3653G8 (es)
ME (1) ME00424B (es)
MX (2) MXPA04002353A (es)
NO (1) NO334950B1 (es)
NZ (1) NZ531622A (es)
PL (3) PL1557421T3 (es)
PT (3) PT1557421E (es)
RS (4) RS54568B1 (es)
RU (1) RU2270200C2 (es)
SI (3) SI1676847T1 (es)
TN (2) TNSN04044A1 (es)
TW (1) TWI285107B (es)
UA (1) UA86384C2 (es)
WO (1) WO2005044823A2 (es)
YU (1) YU24804A (es)
ZA (1) ZA200401948B (es)

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