UA89809C2 - Новые полиморфные формы рифаксимина, способ их получения и их применение в медицинских препаратах - Google Patents

Новые полиморфные формы рифаксимина, способ их получения и их применение в медицинских препаратах Download PDF

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Publication number
UA89809C2
UA89809C2 UAA200708880A UAA200708880A UA89809C2 UA 89809 C2 UA89809 C2 UA 89809C2 UA A200708880 A UAA200708880 A UA A200708880A UA A200708880 A UAA200708880 A UA A200708880A UA 89809 C2 UA89809 C2 UA 89809C2
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Ukraine
Prior art keywords
rifaximin
temperature
ethyl alcohol
water
drying
Prior art date
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UAA200708880A
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English (en)
Ukrainian (uk)
Inventor
Джузеппе Клаудіо Віскомі
Мануела Кампана
Донателла Конфортіні
Марія Міріам Барбанті
Даріо Браґа
Original Assignee
Альфа Вассерманн С.П.А.
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Application filed by Альфа Вассерманн С.П.А. filed Critical Альфа Вассерманн С.П.А.
Publication of UA89809C2 publication Critical patent/UA89809C2/ru

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D499/00—Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D499/21—Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with a nitrogen atom directly attached in position 6 and a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
    • C07D499/44—Compounds with an amino radical acylated by carboxylic acids, attached in position 6
    • C07D499/48—Compounds with an amino radical acylated by carboxylic acids, attached in position 6 with a carbon chain, substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, attached to the carboxamido radical
    • C07D499/58—Compounds with an amino radical acylated by carboxylic acids, attached in position 6 with a carbon chain, substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, attached to the carboxamido radical substituted in alpha-position to the carboxamido radical
    • C07D499/64—Compounds with an amino radical acylated by carboxylic acids, attached in position 6 with a carbon chain, substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, attached to the carboxamido radical substituted in alpha-position to the carboxamido radical by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Abstract

Объектом изобретения являются кристаллические полиморфные формы антибиотика рифаксимина (INN) под названиями рифаксимин EMBED Equation.3 и рифаксимин EMBED Equation.3 , которые полезны в изготовлении медицинских препаратов для перорального и местного применения и получены кристаллизацией, которую проводят горячим растворением необработанного рифаксимина в этиловом спирте и кристаллизацией продукта добавлением воды при определенной температуре на протяжении определенного времени, а потом проводят сушку в контролируемых условиях до достижения постоянного содержания воды в конечном продукте.
UAA200708880A 2005-03-03 2006-02-27 Новые полиморфные формы рифаксимина, способ их получения и их применение в медицинских препаратах UA89809C2 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP05004695.2A EP1698630B1 (en) 2005-03-03 2005-03-03 New polymorphous forms of rifaximin, processes for their production and use thereof in the medicinal preparations

Publications (1)

Publication Number Publication Date
UA89809C2 true UA89809C2 (ru) 2010-03-10

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UAA200708880A UA89809C2 (ru) 2005-03-03 2006-02-27 Новые полиморфные формы рифаксимина, способ их получения и их применение в медицинских препаратах

Country Status (28)

Country Link
US (9) US8193196B2 (ru)
EP (1) EP1698630B1 (ru)
JP (2) JP5737825B2 (ru)
KR (1) KR100885755B1 (ru)
CN (1) CN1900077B (ru)
AU (1) AU2006222312B8 (ru)
BR (1) BRPI0608073A8 (ru)
CA (1) CA2594789C (ru)
DK (1) DK1698630T3 (ru)
ES (1) ES2522895T3 (ru)
HK (1) HK1096396A1 (ru)
HR (1) HRP20070433B1 (ru)
IL (1) IL184694A0 (ru)
MA (1) MA29345B1 (ru)
MD (1) MD4081G2 (ru)
ME (1) ME00272B (ru)
MX (1) MX2007010742A (ru)
NO (1) NO342197B1 (ru)
NZ (1) NZ556737A (ru)
PL (1) PL1698630T3 (ru)
PT (1) PT1698630E (ru)
RS (1) RS54570B1 (ru)
RU (1) RU2397985C2 (ru)
SI (1) SI1698630T1 (ru)
TN (1) TNSN07292A1 (ru)
UA (1) UA89809C2 (ru)
WO (1) WO2006094662A1 (ru)
ZA (1) ZA200707397B (ru)

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