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Last Updated: December 22, 2024

Claims for Patent: 5,035,899


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Summary for Patent: 5,035,899
Title: Peroral preparation of acid-unstable compound
Abstract:A peroral preparation of an acid-unstable compound comprises (1) a core containing the acid-unstable compound, (2) a first layer, coated on the core, comprising a hardly water-soluble, film-forming material and fine particles of a hardly water-soluble substance, suspended in the material, and (3) a second layer, coated on the first layer, of enteric film. The acid-unstable compound is a benzimidazole compound.
Inventor(s): Saeki; Yasuharu (Tsukuba, JP), Koyama; Noritoshi (Ibaraki, JP), Watanabe; Sumio (Aichi, JP), Aoki; Shigeru (Gifu, JP)
Assignee: Eisai Co., Ltd. (Tokyo, JP)
Application Number:07/332,731
Patent Claims: 1. A peroral preparation of a benzimidazole compound, which consists essentially of:

(1) a core containing a pharmacologically effective amount of a pharmacologically effective, acid-unstable benzimidazole compound,

(2) a slightly water-soluble first coating layer, coated on the core, comprising

a slightly water-soluble, film-forming material selected from the group consisting of ethyl cellulose and polyvinyl acetate and

fine particles of a slightly water-soluble substance selected from the group consisting of magnesium oxide, silicic anhydride, calcium silicate, magnesium hydroxide, magnesium carbonate, aluminum hydroxide, calcium stearate, magnesium stearate and sucrose fatty acid esters suspended in the first layer, and

(3) a second coating layer, coated on the first layer, of an enteric polymer film.

2. A peroral preparation as claimed in claim 1 or 2, in which the acid-unstable compound is a benzimidazole compound.

3. A peroral preparation as claimed in claim 1, in which the acid-unstable compound is sodium salt of 2(4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methylsulfinyl)-1H-benzimidazo l.

4. A peroral preparation as claimed in claim 1 or 3, in which a weight ratio to the substance to the material is not less than 5 percent.

5. A peroral preparation as claimed in claim 1 or 3, in which the enteric film is selected from the group consisting of hydroxypropylmethylcellulose phthalate, cellulose acetate phthalate, a copolymer of methacrylic acid and methyl methacrylate, and polyvinyl acetate phthalate.

6. A peroral preparation as claimed in claim 1 or 3, in which the second coating layer also contains a plasticizer.

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