KR930006022A - 페넴의 결정화법 - Google Patents
페넴의 결정화법 Download PDFInfo
- Publication number
- KR930006022A KR930006022A KR1019920017057A KR920017057A KR930006022A KR 930006022 A KR930006022 A KR 930006022A KR 1019920017057 A KR1019920017057 A KR 1019920017057A KR 920017057 A KR920017057 A KR 920017057A KR 930006022 A KR930006022 A KR 930006022A
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- KR
- South Korea
- Prior art keywords
- crystallization method
- aqueous solution
- temperature
- solution
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D477/00—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
- C07D477/10—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with 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
- C07D477/12—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with 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 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6
- C07D477/16—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with 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 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6 with hetero atoms or carbon atoms 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 3
- C07D477/20—Sulfur atoms
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Communicable Diseases (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
본 발명은 (1R, 5S, 6S)-2-[(6, 7-디히드로-5H-피라졸로[1, 2-a]-[1, 2, 4]-트리아졸륨-6-일)]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트(이하, L-627로 약칭함)의 수용액을 용액의 공융온도 내지 0℃ 미만의 온도범위로 유지함을 특징으로 하는 L-627의 결정화법에 관한 것이다. 상기 방법은 결정화로 수반되는 L-627의 손실을 줄이고, 바이알 제제 제조시 공정수를 줄이며, 이들 공정을 멸균 및 분진-미함유 조건하에 용이하게 유지할수 있고, 약제를 정량적으로 정확하게 분산시킬수 있으며, 사용시 결정을 용매에 신속히 용해하는 이점을 제공한다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (23)
- (1R, 5S, 6S)-2-[(6, 7-디히드로-5H-피라졸로[1, 2-a]-[1, 2, 4]-트리아졸륨-6-일)]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트 화합물의 수용액을 용액의 공융온도 내지 0℃ 미만의 온도범위로 유지함을 특징으로 하는, 상기 화합물의 결정화법.
- 제1항에 있어서, 수용액을 동결한 후 용액의 공융온도 내지 0℃ 미만의 온도범위로 유지하는 결정화법.
- 제1항에 있어서, 공유온도가 -10∼-2℃인 결정화법.
- 제1항에 있어서, 수용액을 용액의 공융온도 내지 0℃ 미만의 온도범위로 유지하는 결정화법.
- 제2항 또는 제4항에 있어서, 동결공정이 -40∼-10℃에서 0.5∼48시간 동안 수행되는 결정화법.
- 제1항에 있어서, 온도가 -6∼-1℃인 결정화법.
- 제6항에 있어서, 온도가 -4∼-2℃인 결정화법.
- 제1항에 있어서, 수용액을 용액의 공융온도 내지 0℃ 미만의 온도범위로 유지하는 시간이 0.5∼48시간인 결정화법.
- 제8항에 있어서, 시간이 5∼30시간인 결정화법.
- 제8항에 있어서, 시간이 10∼20시간인 결정화법.
- 제1항에 있어서, 수용액이 알칼리 금속 할라이드를 함유하는 결정화법.
- 제11항에 있어서, 알칼리 금속 할라이드를 함유하는 결정화법.
- 제11항에 있어서, 알칼리 금속 할라이드의 수용액 중의 농도가 0.1∼10%(w/w)인 결정화법.
- 제1항에 있어서, 수용액에 유기용매가 추가되는 결정화법.
- 제14항에 있어서, 유기용매의 C1-6알콜 C3-7또는 케톤인 결정화법.
- 제14항에 있어서, C1-6알콜이 에탄올인 결정화법.
- 제14항에 있어서, 유기용매의 수용액 중의 농도가 1-10%(v/v)인 결정화법.
- 제1항에 있어서, (1R, 5S, 6S)-2-[(6, 7-디히드로-5H-피라졸로[1, 2-a]-[1, 2, 4]-트리아졸륨-6-일)]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트 화합물의 수용액 중의 농도가 0.5∼10%(w/w)인 결정화법.
- 제18항에 있어서, 농도가 1.5∼2.5%(w/w)인 결정화법.
- 제1항에 있어서, 수용액을 동결한 후 용액의 공융온도 내지 0℃ 미만의 온도범위로 유지한 후 동결하는 일련의 공정을 1∼15회 반복하는 결정화법.
- (1R, 5S, 6S)-2-[(6, 7-디히드로-5H-피라졸로[1, 2-a]-[1, 2, 4]-트리아졸륨-6-일)]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트 화합물을 제1항에 따른 방법에 따라 바이알에서 결정화하고, 결정을 감압하에 건조시키고, 바이알을 밀폐함을 특징으로 하는, 상기 화합물의 함유하는 바이알의 제조방법.
- 제21항에 따른 방법으로 제조된 바이알.
- 제1항에 있어서, (1R, 5S, 6S)-2-[(6, 7-디히드로-5H-피라졸로[1, 2-a]-[1, 2, 4]-트리아졸륨-6-일)]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트의 결정의 융점을 초과하지 않는 온도에서 건조공정을 수행한 다음, 결정내의 함수량을 6∼8%(w/w)로 감소시킨후, 환경온도를 25∼50℃로 유지하고 5㎜Hg이하의 감압하에 4∼40시간동안 상기 화합물의 결정내의 수분이 약2%(w/w)이하로 될 때까지건조공정을 수행하는 결정화법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP24164891 | 1991-09-20 | ||
JP91-241648 | 1991-09-20 |
Publications (1)
Publication Number | Publication Date |
---|---|
KR930006022A true KR930006022A (ko) | 1993-04-20 |
Family
ID=17077445
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019920017057A KR930006022A (ko) | 1991-09-20 | 1992-09-18 | 페넴의 결정화법 |
Country Status (9)
Country | Link |
---|---|
US (2) | US5286856A (ko) |
EP (1) | EP0533149A1 (ko) |
JP (1) | JP2767171B2 (ko) |
KR (1) | KR930006022A (ko) |
FI (1) | FI924210A (ko) |
IL (1) | IL103218A0 (ko) |
NO (2) | NO923619L (ko) |
TW (1) | TW264475B (ko) |
ZA (1) | ZA927164B (ko) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101013535B1 (ko) * | 2004-10-21 | 2011-02-14 | 주식회사 만도 | 자동차의 파워 스티어링 장치용 실린더 튜브와 피드튜브의 조립 구조물 |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW264475B (ko) * | 1991-09-20 | 1995-12-01 | Takeda Pharm Industry Co Ltd | |
US6111098A (en) * | 1994-05-02 | 2000-08-29 | Shionogi & Co., Ltd. | Crystal of pyrrolidylthiocarbapenem derivative, lyophilized preparation containing said crystal, and process for producing the same |
AU749234B2 (en) * | 1998-03-02 | 2002-06-20 | Merck Sharp & Dohme Corp. | Process for synthesizing carbapenem antibiotics |
DE10300620B4 (de) * | 2002-05-18 | 2017-04-13 | Carl Zeiss Meditec Ag | Trägervorrichtung für ein medizinisch-optisches Gerät |
MX2009003160A (es) | 2006-09-25 | 2009-04-06 | Ptc Therapeutics Inc | Formas cristalinas del acido 3-[5-(2-fluorofenil)-[1,2,4]oxadiazol -3-il]-benzoico. |
WO2009047604A1 (en) * | 2007-10-08 | 2009-04-16 | Orchid Chemicals & Pharmaceuticals Limited | Process for the preparation of carbapenem antibiotic |
DE102008043318A1 (de) | 2008-10-30 | 2010-05-12 | Mvg Metallverarbeitungsgesellschaft Mbh | Anhängekupplung |
WO2013132422A1 (en) * | 2012-03-05 | 2013-09-12 | Orchid Chemicals & Pharmaceuticals Ltd | An improved process for the preparation of carbapenem antibiotic |
AR091222A1 (es) | 2012-05-30 | 2015-01-21 | Meiji Seika Pharma Co Ltd | INHIBIDOR DE b-LACTAMASA Y PROCESO PARA PREPARARLO |
WO2014097221A1 (en) | 2012-12-21 | 2014-06-26 | Ranbaxy Laboratories Limited | Process for the purification of biapenem |
BR112016006246B8 (pt) | 2013-09-24 | 2021-10-05 | Meiji Seika Pharma Co Ltd | Processos de produção de derivados de diazabiciclo-octano e compostos intermediários dos mesmos |
EP3613740A1 (en) | 2013-10-08 | 2020-02-26 | Meiji Seika Pharma Co., Ltd. | Preparation of a diazabicyclooctane derivative |
JP6779787B2 (ja) | 2014-12-05 | 2020-11-04 | Meiji Seikaファルマ株式会社 | ジアザビシクロオクタン誘導体の結晶及び安定な凍結乾燥製剤の製造法 |
CN114349772B (zh) * | 2020-10-13 | 2022-11-25 | 珠海联邦制药股份有限公司 | 一种比阿培南粗品的精制方法 |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4029655A (en) * | 1975-04-11 | 1977-06-14 | Eli Lilly And Company | Method of preparing stable sterile crystalline cephalosporins for parenteral administration |
IL53427A0 (en) * | 1976-11-24 | 1978-01-31 | Lilly Co Eli | Method of preparing a rapidly dissolving powder of sterile crystalline cefozolin sodium for parenteral administration |
JPS6024080B2 (ja) * | 1977-06-01 | 1985-06-11 | 武田薬品工業株式会社 | 結晶の製造法 |
GB1589317A (en) * | 1977-11-24 | 1981-05-13 | Lilly Co Eli | Freeze drying cephalothin sodium |
JPS56120615A (en) * | 1980-02-27 | 1981-09-22 | Nippon Chemiphar Co Ltd | Preparation of lyophilized powder of cephalothin |
US4713451A (en) * | 1984-04-09 | 1987-12-15 | Merck & Co., Inc. | Crystalline dimethyliminothienamycin |
IE60588B1 (en) * | 1986-07-30 | 1994-07-27 | Sumitomo Pharma | Carbapenem compound in crystalline form, and its production and use |
US4866171A (en) * | 1987-04-11 | 1989-09-12 | Lederle (Japan), Ltd. | (1R,5S,6S)-2-[(6,7-dihydro-5H-pyrazolo[1,2-a][1,2,4]triazolium-6-yl)]thio-6-[R-1-hydroxyethyl]-1-methyl-carbapenum-3-carboxylate |
JPS6425779A (en) * | 1987-04-11 | 1989-01-27 | Lederle Japan Ltd | (1r,5s,6s)-2-substituted-thio-6-((r)-1-hydroxyethyl)-1-methyl -carbapenem-3-carboxylic acid derivative |
DK168047B1 (da) * | 1987-12-07 | 1994-01-24 | Lederle Japan Ltd | (1r,5s,6s)-2-substitueret thio-6-oe(r)-1-hydroxyethylaa-1-methyl-carbapenem-3-carboxylsyrederivater, fremgangsmaade til remstilling deraf, midler og praeparater indeholdende den krystallinske forbindelse samt dens anvendelse. |
US5082661A (en) * | 1990-09-26 | 1992-01-21 | Elizabeth Arden Co., Division Of Conopco, Inc. | Odorless cosmetic compositions in gelatin capsules |
GB9021061D0 (en) * | 1990-09-27 | 1990-11-07 | Unilever Plc | Encapsulating method and products containing encapsulated material |
TW264475B (ko) * | 1991-09-20 | 1995-12-01 | Takeda Pharm Industry Co Ltd | |
JPH08505877A (ja) * | 1993-01-29 | 1996-06-25 | アグロン・ファーマシュウティカルズ・インコーポレーテッド | 抗増殖剤としての縮合複素環式グルタミン酸誘導体 |
-
1992
- 1992-09-16 TW TW081107287A patent/TW264475B/zh active
- 1992-09-17 NO NO92923619A patent/NO923619L/no unknown
- 1992-09-17 EP EP92115869A patent/EP0533149A1/en not_active Withdrawn
- 1992-09-18 US US07/946,614 patent/US5286856A/en not_active Expired - Fee Related
- 1992-09-18 ZA ZA927164A patent/ZA927164B/xx unknown
- 1992-09-18 KR KR1019920017057A patent/KR930006022A/ko not_active Application Discontinuation
- 1992-09-18 IL IL103218A patent/IL103218A0/xx unknown
- 1992-09-18 FI FI924210A patent/FI924210A/fi not_active Application Discontinuation
- 1992-09-18 JP JP4249767A patent/JP2767171B2/ja not_active Expired - Lifetime
-
1993
- 1993-11-30 US US08/159,252 patent/US5424069A/en not_active Expired - Fee Related
-
1997
- 1997-03-21 NO NO971332A patent/NO971332D0/no unknown
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101013535B1 (ko) * | 2004-10-21 | 2011-02-14 | 주식회사 만도 | 자동차의 파워 스티어링 장치용 실린더 튜브와 피드튜브의 조립 구조물 |
Also Published As
Publication number | Publication date |
---|---|
ZA927164B (en) | 1994-03-18 |
AU645442B2 (en) | 1994-01-13 |
TW264475B (ko) | 1995-12-01 |
JP2767171B2 (ja) | 1998-06-18 |
EP0533149A1 (en) | 1993-03-24 |
FI924210A0 (fi) | 1992-09-18 |
NO923619L (no) | 1993-03-22 |
FI924210A (fi) | 1993-03-21 |
NO971332L (no) | 1993-03-22 |
AU2459792A (en) | 1993-03-25 |
NO971332D0 (no) | 1997-03-21 |
US5286856A (en) | 1994-02-15 |
NO923619D0 (no) | 1992-09-17 |
IL103218A0 (en) | 1993-02-21 |
US5424069A (en) | 1995-06-13 |
JPH05271241A (ja) | 1993-10-19 |
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