EA200000742A1 - Кристаллографически стабильные аморфные цефалоспориновые композиции и способ их получения - Google Patents

Кристаллографически стабильные аморфные цефалоспориновые композиции и способ их получения

Info

Publication number
EA200000742A1
EA200000742A1 EA200000742A EA200000742A EA200000742A1 EA 200000742 A1 EA200000742 A1 EA 200000742A1 EA 200000742 A EA200000742 A EA 200000742A EA 200000742 A EA200000742 A EA 200000742A EA 200000742 A1 EA200000742 A1 EA 200000742A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compositions
product
cefalosporin
production
stable amorphous
Prior art date
Application number
EA200000742A
Other languages
English (en)
Other versions
EA002881B1 (ru
Inventor
Масахиро Онодера
Масамити Сукегава
Кийоси Ясуи
Тацуо Ватанабе
Тойоми Сато
Ясуси Мураи
Кацухару Иинума
Original Assignee
Мейдзи Сейка Кайся Лтд.
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
Application filed by Мейдзи Сейка Кайся Лтд. filed Critical Мейдзи Сейка Кайся Лтд.
Publication of EA200000742A1 publication Critical patent/EA200000742A1/ru
Publication of EA002881B1 publication Critical patent/EA002881B1/ru

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • A61K31/546—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • 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
    • C07D501/00—Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14—Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16—Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/20—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/24—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Inorganic Chemistry (AREA)
  • Cephalosporin Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Настоящее изобретение раскрывает способы получения желтых порошкообразных композиций для перорального введения, состоящих, по существу, из частиц из гомогенной смеси аморфного вещества Цефдиторен пивоксила с водорастворимой высокомолекулярной добавкой. Данные композиции могут быть получены путем растворения кристаллического вещества Цефдиторен пивоксила и водорастворимой высокомолекулярной добавки в водном растворе кислоты, затем нейтрализации полученного раствора для соосаждения продукта и сушки осажденного таким образом продукта с последующим выделением продукта в виде вышеуказанных частиц.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200000742A 1998-01-07 1999-01-07 Кристаллографически стабильные аморфные цефалоспориновые композиции и способ их получения EA002881B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP192098 1998-01-07
PCT/JP1999/000020 WO1999034832A1 (fr) 1998-01-07 1999-01-07 Compositions de cephalosporine amorphes, stables du point de vue cristallographique et procede de preparation de ces compositions

Publications (2)

Publication Number Publication Date
EA200000742A1 true EA200000742A1 (ru) 2001-02-26
EA002881B1 EA002881B1 (ru) 2002-10-31

Family

ID=11515039

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200000742A EA002881B1 (ru) 1998-01-07 1999-01-07 Кристаллографически стабильные аморфные цефалоспориновые композиции и способ их получения

Country Status (23)

Country Link
US (2) US6342493B1 (ru)
EP (1) EP1051978B1 (ru)
JP (1) JP3413406B2 (ru)
KR (1) KR100435315B1 (ru)
CN (1) CN1151845C (ru)
AU (1) AU736555B2 (ru)
BR (1) BRPI9907084B8 (ru)
CA (1) CA2316841C (ru)
CZ (1) CZ302082B6 (ru)
EA (1) EA002881B1 (ru)
ES (1) ES2393972T3 (ru)
HK (1) HK1035148A1 (ru)
HU (1) HU230295B1 (ru)
ID (1) ID25469A (ru)
IL (2) IL137004A0 (ru)
NZ (1) NZ505871A (ru)
PL (1) PL194097B1 (ru)
PT (1) PT1051978E (ru)
SK (1) SK286631B6 (ru)
TR (1) TR200001903T2 (ru)
TW (1) TW587946B (ru)
UA (1) UA70311C2 (ru)
WO (1) WO1999034832A1 (ru)

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PL194097B1 (pl) * 1998-01-07 2007-04-30 Meiji Seika Kaisha Kompozycja zawierająca krystalograficznie trwałą amorficzną cefalosporynę i sposób jej wytwarzania
JP4803935B2 (ja) 1999-10-08 2011-10-26 アフィニアム・ファーマシューティカルズ・インコーポレイテッド Ｆａｂｉ阻害剤
DE60230934D1 (de) 2001-04-06 2009-03-05 Affinium Pharm Inc Fab-i-inhibitoren
EP1389462B1 (en) 2001-04-26 2012-06-06 Meiji Seika Pharma Co., Ltd. Amorphous cefditoren pivoxil composition and process for producing the same
WO2004030673A1 (ja) 2002-10-02 2004-04-15 Meiji Seika Kaisha, Ltd. 経口吸収性が改善された抗菌性医薬組成物
ES2518316T3 (es) 2002-12-06 2014-11-05 Debiopharm International Sa Compuestos heterocíclicos, métodos de fabricación de los mismos y su uso en terapia
WO2004082586A2 (en) * 2003-03-17 2004-09-30 Affinium Pharmaceuticals, Inc. Phamaceutical compositions comprising inhibitors of fab i and further antibiotics
EP1650266A1 (en) * 2003-06-20 2006-04-26 Meiji Seika Kaisha Ltd. Product of coprecipitation of sparingly soluble substance and water-soluble polymer and process for producing the same
ATE539738T1 (de) * 2003-10-08 2012-01-15 Meiji Seika Pharma Co Ltd Nichtkristalline antibakterielle zusammensetzung mit cefditoren-pivoxil
WO2005044824A2 (en) * 2003-11-07 2005-05-19 Ranbaxy Laboratories Limited Processes for the preparation of highly pure 3-(2-substituted vinyl) cephalosporin
JP2005162696A (ja) * 2003-12-04 2005-06-23 Nichiko Pharmaceutical Co Ltd 溶出性に優れたセフジトレンピボキシル製剤
WO2005082330A2 (en) * 2004-02-19 2005-09-09 Ranbaxy Laboratories Limited Co-precipitated amorphous cefditoren pivoxil and dosage forms comprising the same
PT1828167E (pt) 2004-06-04 2014-10-08 Debiopharm Int Sa Derivados de acrilamida como agentes antibióticos
US20080069879A1 (en) * 2006-05-02 2008-03-20 Ravishekhar Bhiwgade Stable solid dosage form containing amorphous cefditoren pivoxil and process for preparation thereof
WO2008009122A1 (en) 2006-07-20 2008-01-24 Affinium Pharmaceuticals, Inc. Acrylamide derivatives as fab i inhibitors
WO2008057058A1 (en) * 2006-11-10 2008-05-15 Nobel Ilac Sanayii Ve Ticaret As Oral pharmaceutical compositions
EP3255045A1 (en) 2007-02-16 2017-12-13 Debiopharm International SA Salts, prodrugs and polymorphs of fab i inhibitors
CN101560216B (zh) * 2009-05-27 2011-06-15 上海交通大学 头孢妥仑酯的制备方法
WO2012010938A2 (en) * 2010-07-23 2012-01-26 Lupin Limited Pharmaceutical compositions of cefditoren pivoxil
ES2554630T3 (es) 2010-09-30 2015-12-22 Toyama Chemical Co., Ltd. Sal sódica de 6-fluoro-3-hidroxi-2-pirazinocarboxamida
ES2561878T3 (es) 2010-09-30 2016-03-01 Toyama Chemical Co., Ltd. Sal de meglumina de 6-fluoro-3-hidroxi-2-pirazinacarboxamida
LT2861608T (lt) 2012-06-19 2019-07-10 Debiopharm International Sa (e)-n-metil-n-((3-metilbenzofuran-2-il)metil)-3-(7-okso-5,6,7,8-tetrahidro-1,8-nafthidrin-3-il)akrilamido provaisto dariniai
US9951009B2 (en) * 2013-08-29 2018-04-24 Cadila Healthcare Limited Polymorphic form of pyrrole derivative and intermediate thereof
EP3244879A1 (en) 2015-01-16 2017-11-22 Ögün, Yusuf Toktamis Cefditoren pivoxil compositions with improved stability and production methods thereof
HUE052140T2 (hu) 2016-02-26 2021-04-28 Debiopharm Int Sa Diabéteszes lábfertõzések kezelésére szolgáló gyógyszer
CN109053768A (zh) * 2018-08-07 2018-12-21 中国医药集团总公司四川抗菌素工业研究所 一种无定型头孢妥仑酯的制备方法
CN110251467A (zh) * 2019-06-26 2019-09-20 北京济美堂医药研究有限公司 一种无定形态头孢妥仑匹酯组合物的制备方法
CN112190539B (zh) * 2020-11-10 2021-11-02 深圳立健药业有限公司 一种头孢妥仑匹酯组合物及其应用

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Also Published As

Publication number Publication date
WO1999034832A8 (fr) 1999-10-28
JP3413406B2 (ja) 2003-06-03
HUP0101272A3 (en) 2002-07-29
TW587946B (en) 2004-05-21
IL137004A (en) 2008-11-03
BRPI9907084B8 (pt) 2021-05-25
EP1051978A1 (en) 2000-11-15
CZ20002542A3 (cs) 2000-12-13
EP1051978A4 (en) 2007-05-02
WO1999034832A1 (fr) 1999-07-15
ES2393972T8 (es) 2013-02-25
NZ505871A (en) 2002-10-25
HK1035148A1 (en) 2001-11-16
SK286631B6 (sk) 2009-02-05
CA2316841A1 (en) 1999-07-15
BR9907084A (pt) 2000-10-17
KR20010033961A (ko) 2001-04-25
SK10262000A3 (sk) 2001-01-18
PT1051978E (pt) 2012-11-20
HUP0101272A2 (hu) 2001-12-28
CN1151845C (zh) 2004-06-02
PL341589A1 (en) 2001-04-23
KR100435315B1 (ko) 2004-06-10
AU736555B2 (en) 2001-08-02
ES2393972T3 (es) 2013-01-03
CZ302082B6 (cs) 2010-09-29
HU230295B1 (hu) 2015-12-28
US6486149B2 (en) 2002-11-26
AU1784599A (en) 1999-07-26
BRPI9907084B1 (pt) 2017-04-25
US6342493B1 (en) 2002-01-29
EP1051978B1 (en) 2012-08-22
US20020037322A1 (en) 2002-03-28
PL194097B1 (pl) 2007-04-30
CA2316841C (en) 2007-11-20
EA002881B1 (ru) 2002-10-31
ID25469A (id) 2000-10-05
CN1290177A (zh) 2001-04-04
TR200001903T2 (tr) 2000-11-21
UA70311C2 (ru) 2004-10-15
IL137004A0 (en) 2001-06-14

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