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Last Updated: November 22, 2024

Claims for Patent: 8,318,201


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Summary for Patent: 8,318,201
Title:Method of stabilizing diarylvinylene compound
Abstract: ##STR00001## (wherein Y.sup.1 and Y.sup.2 may be the same or different and each represents a hydrogen atom, halogen or lower alkyl; and Z and A may be the same or different and each represents substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl) The present invention provides, for example, a method for stabilization of a diarylvinylene compound such as a compound represented by the above formula (I) or the like, or a pharmaceutically acceptable salt thereof in a solid formulation containing the diarylvinylene compound or the pharmaceutically acceptable salt thereof, which comprises allowing an inorganic substance and/or a colorant to exist in the solid formulation, and the like.
Inventor(s): Uchida; Akihiro (Sunto-gun, JP), Ishikawa; Yasuhiro (Sunto-gun, JP), Ueno; Yasuhiko (Mishima, JP), Kaji; Kiichiro (Machida, JP), Aimoto; Masaharu (Sunto-gun, JP), Kaneko; Naoki (Sunto-gun, JP)
Assignee: Kyowa Hakko Kirin Co., Ltd. (Tokyo, JP)
Application Number:10/528,451
Patent Claims: 1. A method for suppressing formation of impurities due to dimerization of a (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-puri- ne-2,6-dione represented by the compound of formula (IB) ##STR00025## or a pharmaceutically acceptable salt thereof, in a pharmaceutical composition wherein said pharmaceutical composition is a solid formulation containing the formula (IB) compound or the pharmaceutically acceptable salt thereof, which comprises the step of providing iron oxide in the solid formulation, wherein formation of impurities due to dimerization of the formula (IB) compound or the pharmaceutically acceptable salt thereof is suppressed.

2. The method according to claim 1, wherein the solid formulation consists of: a core consisting of the formula (IB) compound or the pharmaceutically acceptable salt thereof and optionally one or more members selected from the group consisting of a diluent, a binder, a disintegrator, a lubricant, a surfactant, a plasticizer and an inorganic substance; and a coated layer containing the iron oxide, wherein said core bears said coated layer.

3. The method according to claim 2, wherein the coated layer further contains at least one inorganic substance selected from the group consisting of titanium oxide, zinc oxide, magnesium oxide, talc, magnesium silicate, synthetic aluminum silicate, magnesium carbonate, calcium sulfate, aluminum sulfate and barium sulfate.

4. The method according to claim 2, wherein the coated layer contains 0.01 to 70 parts by weight iron oxide per 100 parts by weight of the coated layer.

5. The method according to claim 3, wherein the coated layer contains 0.01 to 70 part(s) by weight of the iron oxide per 100 parts by weight of the coated layer, and wherein the total amount of the inorganic substance and iron oxide is 0.01 to 90 part(s) by weight per 100 parts by weight of the coated layer.

6. The method according to any one of claims 1 and 2-5, wherein the solid formulation comprises 0.001 to 10,000 parts by weight of iron oxide per 100 parts by weight of the formula (IB) compound or the pharmaceutically acceptable salt thereof.

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