Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2002-06-24
2004-03-16
Weddington, Kevin E. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
Reexamination Certificate
active
06706733
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a quinolinone derivative formulation having superior stability and bioabsorption, and its production method.
The present specification is based on a Japanese patent application filed in Japan (Japanese Patent Application No. Hei 10-62907), and the described contents of said Japanese patent application are incorporated as a portion of the present specification.
BACKGROUND ART
The inventors of the present invention reported in Japanese Unexamined Patent Application, First Publication No. Hei 9-255659 that a novel quinolinone derivative represented with chemical formula (I) has low toxicity, is effective against both immediate and delayed allergies, and is extremely useful as an antiallergic.
In addition, the inventors of the present invention also reported at the 12
th
Annual Convention of the Japan Pharmaceutical Society (Ohmiya, 1997) that the quinolinone derivative represented with chemical formula (I) demonstrates crystal polymorphism consisting of four crystal types of the &agr;, &bgr;, &ggr; and &dgr; forms, and that each form exhibits different absorption in the body. However, the stability of these four crystal forms along with the preferable forms as pharmaceutical formulations were not clarified.
DISCLOSURE OF THE INVENTION
An object of the present invention is to provide a quinolinone derivative, having for its active ingredient the &bgr;-form crystal and/or &ggr;-form crystal of a quinolinone derivative represented with chemical formula (I) that is useful as a pharmaceutical, and particularly as an antiallergic, and having superior bioabsorption and stability, along with its production method.
As a result of eager research to achieve the above object, the inventors of the present invention found that, although each crystal form of the quinolinone derivative represented with chemical formula (I) is converted to an amorphous form resulting in improved bioabsorption as a result of crushing, the &bgr;, &ggr; and &dgr; crystal forms demonstrate superior bioabsorption as compared With the &agr; crystal form, and the &agr;, &bgr; and &ggr; crystal forms demonstrate superior stability as compared with the &dgr; crystal form. Thus, the inventors found that a pharmaceutical formulation having for its active ingredient the &bgr; crystal form and/or &ggr; crystal form demonstrates the most superior bioabsorption and stability. Moreover, the inventors found that a pharmaceutical formulation has even more superior stability by adding antioxidant and/or lubricant to a pharmaceutical formulation having for its active ingredient the &bgr; crystal form and/or &ggr; crystal form. Thereby, the inventors are led to completion of the present invention.
Namely, the present invention provides the following:
(1) a quinolinone derivative formulation including for its active ingredient a &bgr; crystal form and/or a &ggr; crystal form of a quinolinone derivative represented with chemical formula (I):
(2) a quinolinone derivative formulation including for its active ingredient a &bgr; crystal form and/or a &ggr; crystal form of a quinolinone derivative represented with chemical formula (I):
and including an antioxidant and/or a lubricant;
(3) a quinolinone derivative formulation according to (1) or (2), wherein the &bgr; crystal form and/or the &ggr; crystal form is obtained by recrystallizing from ethanol;
(4) a quinolinone derivative formulation according to any of (1) through (3), wherein a formulation form of the quinolinone formulation is selected from capsules, coated granules, coated tablets, or sugar-coated tablets, which can block lights;
(5) a production method of a quinolinone derivative formulation comprising: producing a formulation in a formulation form selected from capsules, coated granules, coated tablets, or sugar-coated tablets, which can block lights, by using a &bgr; crystal form and/or a &ggr; crystal form of the quinolinone derivative represented with chemical formula (I):
(6) a production method of a quinolinone derivative formulation comprising: producing a formulation in a formulation form selected from capsules, coated granules, coated tablets or sugar-coated tablets, which can block lights, by using a &bgr; crystal form and/or a &ggr; crystal form of the quinolinone derivative represented with chemical formula (I):
and an antioxidant and/or a lubricant; and
(7) a production method of a quinolinone derivative formulation according to (5) or (6), wherein the &bgr; crystal form and/or &ggr; crystal form is obtained by recrystallizing from ethanol.
REFERENCES:
patent: 5179203 (1993-01-01), Ao et al.
patent: 5942521 (1999-08-01), Takagaki et al.
patent: 6114352 (2000-09-01), Takagaki et al.
patent: 6136822 (2000-10-01), Takagaki et al.
patent: 6271416 (2001-08-01), Takagaki et al.
patent: 0 785 190 (1997-07-01), None
patent: 0 927 718 (1999-07-01), None
patent: 0 933 378 (1999-08-01), None
patent: 9-255659 (1997-09-01), None
patent: 11-255649 (1999-09-01), None
Proceedings of the 12th Annual Convention of the Japan Pharmaceutical Society published on Mar. 14, 1997 (Ohmiya).*
Proceedings of the 12thAnnual Convention of the Japan Pharmaceutical Society published on Mar. 14, 1997.
Fukui Hiroyuki
Kimura Nobuyuki
Muratake Nahoko
Takagaki Hidetsugu
Armstrong Kratz Quintos Hanson & Brooks, LLP
Dainippon Ink and Chemicals Inc.
Weddington Kevin E.
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