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Last Updated: January 29, 2022

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Claims for Patent: 7,541,363


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Summary for Patent: 7,541,363
Title:Microcrystal
Abstract: Microcrystals of (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,- 6-dione having an average particle size of less than 50 .mu.m; microcrystals of (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,- 6-dione having an average particle size of less than 50 .mu.m and a crystallinity of 20% or more or the like, which possess excellent solubility, stability, bioavailability, dispersing property in a pharmaceutical formulation; and the like are provided. A solid pharmaceutical formulation which is characterized by comprising the same is also provided.
Inventor(s): Kuroda; Kazutoshi (Ichikawa, JP), Aoki; Noboru (Numazu, JP), Ochiai; Toshiro (Sunto-gun, JP), Uchida; Akihiro (Sunto-gun, JP), Ishikawa; Yasuhiro (Sunto-gun, JP), Kigoshi; Makoto (Sunto-gun, JP), Hayakawa; Eiji (Sunto-gun, JP), Asanome; Kazuki (Sunto-gun, JP)
Assignee: Kyowa Hakko Kirin Co., Ltd. (Tokyo, JP)
Application Number:10/554,511
Patent Claims: 1. Microcrystals of (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,- 6-dione represented by the following formula ##STR00002## wherein the average particle size of the microcrystals is less than 50 .mu.m.

2. The microcrystals according to claim 1, wherein the average particle size of the microcrystals is 0.5 to 20 .mu.m.

3. A solid pharmaceutical formulation comprising the microcrystals according to claim 1 or 2, and a pharmaceutically acceptable carrier.

4. The microcrystals according to claim 1 or 2, which are obtained by pulverization using a jet mill of crystals of (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,- 6-dione, said crystals having an average particle size of not less than 50 .mu.m.

5. The solid pharmaceutical formulation according to claim 3, wherein the microcrystals are obtained by pulverization using a jet mill of crystals of (E)-8-(3,4-dimethoxystryl)-1,3 -diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione, said crystals having an average particle size of not less than 50 .mu.m.

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