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Title:
STABILIZED PHARMACEUTICAL COMPOSITION
Document Type and Number:
WIPO Patent Application WO/2007/097386
Kind Code:
A1
Abstract:
It is intended to provide a pharmaceutical composition containing an azole compound which is stable and useful as an antifungal drug. According to the invention, the object could be achieved by adding a basic compound such as magnesium carbonate hydroxide, triethylamine or arginine to the azole compound which is unstable to acid. The pharmaceutical composition is stable without causing degradation of the compound even if a condition such as temperature or humidity is changed during production or storage. Further, it is useful as a therapeutic agent for deep mycosis because systemic administration thereof can be achieved by applying it to an oral agent or an injectable agent.

Inventors:
ISHIMOTO HAYATO (JP)
HARADA TSUTOMU (JP)
OMAE HIROSHI (JP)
Application Number:
PCT/JP2007/053246
Publication Date:
August 30, 2007
Filing Date:
February 22, 2007
Export Citation:
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Assignee:
EISAI R&D MAN CO LTD (JP)
ISHIMOTO HAYATO (JP)
HARADA TSUTOMU (JP)
OMAE HIROSHI (JP)
International Classes:
A61K31/4196; A61K9/20; A61K31/4439; A61K31/675; A61K47/02; A61K47/04; A61K47/12; A61K47/18; A61K47/22; A61K47/32; A61K47/38; A61P31/10
Domestic Patent References:
WO2006118351A12006-11-09
WO2006118351A12006-11-09
Foreign References:
JP2005015474A2005-01-20
JPH03258717A1991-11-19
JPH04198106A1992-07-17
JP2004518640A2004-06-24
JP2003520235A2003-07-02
JP2003520235A2003-07-02
JPH10512599A1998-12-02
JPH11228548A1999-08-24
JP2000169372A2000-06-20
US6812238B12004-11-02
JP2004518640A2004-06-24
JP2005015474A2005-01-20
Other References:
OHWADA J. ET AL.: "Design, synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 13, no. 2, 2003, pages 191 - 196, XP003024541
ICHIKAWA T. ET AL.: "Optically active antifungal azoles. XII. Synthesis and antifungal activity of the water-soluble prodrugs of 1-[(1R,2R)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4,-triazol-1-yl)propyl]-3-[4-(1H-1-tetrazolyl)phenyl)-2-imidazolidinone", CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 49, no. 9, 2001, pages 1102 - 1109, XP003024542
JPN., J. MED. MYCOL., vol. 45, 2004, pages 2
Y. UEDA: "BIOORGANIC & MEDICINAL CHEMISTRY LETTERS", vol. 13, PERGAMON, ELSEVIER SCIENCE, pages: 3669 - 3672
Attorney, Agent or Firm:
INABA, Yoshiyuki et al. (Roppongi Hills Mori Tower 6-10-1 Roppongi, Minato-k, Tokyo 23, JP)
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