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WO2004058261A1 - Preparation aqueuse antibacterienne - Google Patents

Preparation aqueuse antibacterienne Download PDF

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Publication number
WO2004058261A1
WO2004058261A1 PCT/JP2003/016451 JP0316451W WO2004058261A1 WO 2004058261 A1 WO2004058261 A1 WO 2004058261A1 JP 0316451 W JP0316451 W JP 0316451W WO 2004058261 A1 WO2004058261 A1 WO 2004058261A1
Authority
WO
WIPO (PCT)
Prior art keywords
aqueous preparation
group
antibacterial
carboxylic acid
aqueous
Prior art date
Application number
PCT/JP2003/016451
Other languages
English (en)
Japanese (ja)
Inventor
Yoshimine Fujii
Toshiaki Tomitsuka
Original Assignee
Daiichi Pharmaceutical Co., Ltd.
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 Daiichi Pharmaceutical Co., Ltd. filed Critical Daiichi Pharmaceutical Co., Ltd.
Priority to AU2003289478A priority Critical patent/AU2003289478A1/en
Publication of WO2004058261A1 publication Critical patent/WO2004058261A1/fr

Links

Classifications

    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K9/08—Solutions
    • 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

Definitions

  • the present invention relates to a liquid preparation containing a quinolonecarboxylic acid-based antibacterial agent having improved stability, and a method for producing the same.
  • Quinolonecarboxylic acid derivatives are useful as pharmaceuticals because of their high antibacterial activity and safety, and various derivatives have been reported (JP-A-2-231475).
  • sitafloxacin names based on international common names (INN: International Nonproprietary Names) are used. Has a particularly strong antibacterial activity, but has the problem of reduced photostability in aqueous solutions.
  • INN International Nonproprietary Names
  • liquid formulation that solves this problem by coexisting sodium chloride in an aqueous solution of sitafloxacin. Have been.
  • the present invention provides an antibacterial aqueous preparation containing the quinolone carboxylic acid-based antibacterial agent, which improves the stability of the aqueous solution containing the antibacterial agent and is intended for parenteral use, and a method for producing the same.
  • the purpose is to: 6451 DISCLOSURE OF THE INVENTION
  • the present inventors have conducted intensive studies on an antibacterial aqueous preparation containing a quinolone carboxylic acid antibacterial agent and found that the addition of sugar alcohols to the quinolone carboxylic acid antibacterial agent significantly improved the stability. Heading, the present invention has been completed. Ie
  • the present invention provides the following components (A) and (B):
  • the present invention provides a method for producing an antibacterial aqueous preparation, which comprises a step of preparing an aqueous solution in which a quinolone carboxylic acid antibacterial agent and a sugar alcohol are dissolved, and a step of adjusting the pH of the aqueous solution. It is.
  • R 1 represents an amino group, a methylamino group, a hydroxyl group, a thiol group or a hydrogen atom, and is preferably a hydrogen atom.
  • R 2 is the following substituent
  • Z represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or an alkoxyalkyl group having 1 to 6 carbon atoms in which the alkyl group having 1 to 6 carbon atoms is substituted with the alkoxy group having 1 to 6 carbon atoms (
  • a methoxyalkyl group, a methoxyethyl group, an ethoxymethyl group, etc. a phenylalkyl group of an alkyl chain having 1 to 6 carbon atoms in which the alkyl group having 1 to 6 carbon atoms is substituted with a phenyl group (for example, a benzyl group) , Phenethyl group, etc.), phenyl group, acetomethyl group, bivaloyloxymethyl group, ethoxycalponyloxy group, choline group, dimethylaminoethyl group, 5-indanyl group, phthalidinyl group 5-substituted 1-2-ox
  • an acid, a base, an aqueous solution thereof, or a combination thereof can be generally used.
  • a base or its aqueous solution a dilute aqueous solution may be used, and an aqueous solution of about 1 mol 1 ZL can be used.
  • Solid or powdered sodium hydroxide may be used in addition to the aqueous solution.
  • the base is not limited to sodium hydroxide.
  • the acid is not limited to hydrochloric acid, and a solid or powdered material other than an aqueous solution, such as citric acid, may be used.
  • Active ingredient Compound a (free form) 225mg (200rag)
  • the antibacterial aqueous preparation containing the quinoline carboxylic acid antibacterial agent and the sugar alcohol of the present invention has high stability and is particularly useful for parenteral use.

Landscapes

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

Abstract

L'invention concerne une préparation aqueuse antibactérienne qui contient les ingrédients suivants (A) et (B) : (A) un antibactérien du type acide quinolonecarboxylique et (B) un alcool de sucre. Ladite préparation aqueuse antibactérienne présente une stabilité accrue.
PCT/JP2003/016451 2002-12-24 2003-12-22 Preparation aqueuse antibacterienne WO2004058261A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003289478A AU2003289478A1 (en) 2002-12-24 2003-12-22 Antibacterial water-based preparation

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2002-372505 2002-12-24
JP2002372505A JP2006151808A (ja) 2002-12-24 2002-12-24 抗菌性水性製剤

Publications (1)

Publication Number Publication Date
WO2004058261A1 true WO2004058261A1 (fr) 2004-07-15

Family

ID=32677231

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2003/016451 WO2004058261A1 (fr) 2002-12-24 2003-12-22 Preparation aqueuse antibacterienne

Country Status (4)

Country Link
JP (1) JP2006151808A (fr)
AU (1) AU2003289478A1 (fr)
TW (1) TW200507845A (fr)
WO (1) WO2004058261A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1757598A4 (fr) * 2004-05-13 2010-07-21 Daiichi Seiyaku Co Dérivé de pyrrolidine substituée
US12036219B2 (en) 2013-03-15 2024-07-16 Melinta Subsidiary Corp. Methods of treating infections in overweight and obese patients using antibiotics

Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0334087A1 (fr) * 1988-03-23 1989-09-27 Abbott Laboratories Agent antimicrobien pour trousse de diagnostic in-vitro
US4957922A (en) * 1985-10-24 1990-09-18 Bayer Aktiengesellschaft Infusion solutions of 1-cyclopropyl-6-fluoro-1,4-di-hydro-4-oxo-7-(1-piperazinyl)-quinoline-3-carboxylic acid
WO1993005816A1 (fr) * 1991-09-17 1993-04-01 Alcon Laboratories, Inc. Compositions contenant des antibiotiques quinolone et du sulfonate de polystyrol
EP0549857A1 (fr) * 1991-12-31 1993-07-07 Korea Research Institute Of Chemical Technology Dérivés d'acides quinolone-carboxyliques comme agent antibactérien
JPH07300472A (ja) * 1992-12-28 1995-11-14 Korea Res Inst Chem Technol 新規キノロンカルボン酸誘導体およびその製造方法
JP2000072674A (ja) * 1998-08-28 2000-03-07 Ota Seiyaku Kk ノスカピン経口医薬液剤
KR20000040012A (ko) * 1998-12-14 2000-07-05 손경식 퀴놀론계 항균화합물의 주사 또는 주입용 수용액 제제
EP1031569A1 (fr) * 1997-10-27 2000-08-30 Toyama Chemical Co., Ltd. Procedes servant a preparer des derives 7-isoindolinequinolonecarboxyliques et leurs intermediaires, sels d'acides 7-isoindolinequinolonecarboxyliques, leurs hydrates, compositions les contenant en tant qu'ingredients actifs
WO2001010408A2 (fr) * 1999-08-06 2001-02-15 Bayer Aktiengesellschaft Composition pharmaceutique aqueuse a base de moxifloxacine ou de ses sels
WO2001076603A1 (fr) * 2000-04-07 2001-10-18 Daiichi Pharmaceutical Co., Ltd. Compositions medicamenteuses contenant un derive de camptothecine et un agent de regulation de ph
WO2001080858A1 (fr) * 2000-04-24 2001-11-01 Daiichi Pharmaceutical Co., Ltd. Preparation liquide stable

Patent Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4957922A (en) * 1985-10-24 1990-09-18 Bayer Aktiengesellschaft Infusion solutions of 1-cyclopropyl-6-fluoro-1,4-di-hydro-4-oxo-7-(1-piperazinyl)-quinoline-3-carboxylic acid
EP0334087A1 (fr) * 1988-03-23 1989-09-27 Abbott Laboratories Agent antimicrobien pour trousse de diagnostic in-vitro
WO1993005816A1 (fr) * 1991-09-17 1993-04-01 Alcon Laboratories, Inc. Compositions contenant des antibiotiques quinolone et du sulfonate de polystyrol
EP0549857A1 (fr) * 1991-12-31 1993-07-07 Korea Research Institute Of Chemical Technology Dérivés d'acides quinolone-carboxyliques comme agent antibactérien
JPH07300472A (ja) * 1992-12-28 1995-11-14 Korea Res Inst Chem Technol 新規キノロンカルボン酸誘導体およびその製造方法
EP1031569A1 (fr) * 1997-10-27 2000-08-30 Toyama Chemical Co., Ltd. Procedes servant a preparer des derives 7-isoindolinequinolonecarboxyliques et leurs intermediaires, sels d'acides 7-isoindolinequinolonecarboxyliques, leurs hydrates, compositions les contenant en tant qu'ingredients actifs
JP2000072674A (ja) * 1998-08-28 2000-03-07 Ota Seiyaku Kk ノスカピン経口医薬液剤
KR20000040012A (ko) * 1998-12-14 2000-07-05 손경식 퀴놀론계 항균화합물의 주사 또는 주입용 수용액 제제
WO2001010408A2 (fr) * 1999-08-06 2001-02-15 Bayer Aktiengesellschaft Composition pharmaceutique aqueuse a base de moxifloxacine ou de ses sels
WO2001076603A1 (fr) * 2000-04-07 2001-10-18 Daiichi Pharmaceutical Co., Ltd. Compositions medicamenteuses contenant un derive de camptothecine et un agent de regulation de ph
WO2001080858A1 (fr) * 2000-04-24 2001-11-01 Daiichi Pharmaceutical Co., Ltd. Preparation liquide stable

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
"Edited by Japan Pharmaceutical Excipients Council, Iyakuhin Tenkabutsu Jiten, First edition", YAKUJI NIPPO LTD, 14 January 1994 (1994-01-14), pages 130, XP002986761 *
DATABASE CAPLUS [online] XP002977886, accession no. STN Database accession no. 2002:149098 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1757598A4 (fr) * 2004-05-13 2010-07-21 Daiichi Seiyaku Co Dérivé de pyrrolidine substituée
US7977327B2 (en) 2004-05-13 2011-07-12 Daiichi Sankyo Company, Limited Substituted pyrrolidine derivative
US8455482B2 (en) 2004-05-13 2013-06-04 Daiichi Sankyo Company, Limited Substituted pyrrolidine derivative
US12036219B2 (en) 2013-03-15 2024-07-16 Melinta Subsidiary Corp. Methods of treating infections in overweight and obese patients using antibiotics

Also Published As

Publication number Publication date
TW200507845A (en) 2005-03-01
JP2006151808A (ja) 2006-06-15
AU2003289478A1 (en) 2004-07-22

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