Takeda Pharmaceutical Company Limited

Takeda Chemical Industries, Inc.

Toshihiro Shimizu

Tetsuro Tabata

Shuji Morimoto

Masae Sugaya

Yoshinori Nakano

Junichi Kikuta

Hikaru Fukuyama

Hiroshi Fukada

Etsuji Nakamura

Norio Kameoka

An orally disintegrable tablet, of the present invention, which comprises (i) fine granules having an average particle diameter of 400 &#x3bc;m or less, which fine granules comprise a composition coated by an enteric coating layer, said composition having 10 weight % or more of an acid-labile physiologically active substance and (ii) an additive, has superior disintegrability or dissolution in the oral cavity so that it can be used for treatment or prevention of various diseases, as an orally disintegrable tablet capable of being administered to the aged or children and easily administered without water. Also, because the tablet of the present invention contains fine granules having the average particle diameter such that it will not impart roughness in mouth, it can be administered easily without discomfort at the administration.

Orally disintegrable tablets

It is intended to provide preparations such as capsules containing an acid-unstable medicament (in particular, a benzimidazole compound having an antiulcer effect, etc.) at a high concentration which are prepared by using about 12% by weight or more (based on the total granules) of the acid-unstable chemical and blending a basic inorganic salt therewith to give granules of about 600 &#x3bc;m or more in the average particle size.

Granules containing acid-unstable chemical in large amount

An orally disintegrable tablet of the present invention, which comprises (i) fine granules having an average particle diameter of 400 &#x3bc;m or less, which fine granules comprise a composition coated by an enteric coating layer, said composition having 10 weight % or more of an acid-labile physiologically active substance and (ii) an additive, has superior disintegrability or dissolution in the oral cavity so that it can be used for treatment or prevention of various diseases, as an orally disintegrable tablet capable of being administered to the aged or children and easily administered without water. Also, because the tablet of the present invention contains fine granules having the average particle diameter such that it will not impart roughness in mouth, it can be administered easily without discomfort at the administration.

A rapidly disintegrable solid preparation which comprises (i) a pharmacologically active ingredient, (ii) a sugar and (iii) a low-substituted hydroxypropylcellulose having 5% by weight or more to less than 7% by weight of hydroxypropoxyl group. The rapidly disintegrable solid preparation has fast disintegrability, suitable strength and no roughness.

Rapidly Disintegrable solid preparation

Rapidly disintegrable solid preparation

The punch coated with Cr-Dop&eacute;-N is advantageous as a punch for preparing tablets containing an acidic substance or an adhesive substance and is excellent in corrosion resistance and releasing property.

Compressing mallet with coating treatment

A solid preparation which comprises (i) a pharmaceutically active ingredient, (ii) one or more water-soluble sugar alcohol selected from the group consisting of sorbitol, maltitol, reduced starch saccharide, xylitol, reduced palatinose and erythritol, and (iii) low-substituted hydroxypropylcellulose having hydroxypropoxyl group contents of 7.0 to 9.9 percent by weight; which exhibits excellent buccal disintegration and dissolution and also appropriate strength.

Solid preparation

An orally disintegrable tablet, of the present invention, which comprises (i) fine granules having an average particle diameter of 400 &mgr;m or less, which fine granules comprise a composition coated by an enteric coating layer, said composition having 10 weight % or more of an acid-labile physiologically active substance and (ii) an additive, has superior disintegrability or dissolution in the oral cavity so that it can be used for treatment or prevention of various diseases, as an orally disintegrable tablet capable of being administered to the aged or children and easily administered without water. Also, because the tablet of the present invention contains fine granules having the average particle diameter such that it will not impart roughness in mouth, it can be administered easily without discomfort at the administration.

A solid preparation which comprises (i) a pharmaceutically active ingredient, (ii) one or more water-soluble sugar alcohols selected from the group consisting of sorbitol, maltitol, reduced starch saccharide, xylitol, reduced palatinose and erythritol, and (iii) low-substituted hydroxypropylcellulose having hydroxypropoxyl group contents of 7.0 to 9.9 percent by weight; which exhibits excellent buccal disintegration and dissolution and also appropriate strength.

Solid pharmaceutical preparation

An effervescent composition comprising a core-shell powder consisting of a fine granular core spray-coated with a liquid mixture containing a water-soluble polymer such as hydroxypropylcellulose or hydroxypropylmethylcellulose, and at least one physiologically active substance, especially an acid-sensitive drugs, and enteric coating film, an effervescing component and an auxiliary effervescing agent which provides for controlled release of the physiologically active substance and in useful for preparing uniform solution or suspension having a refreshing sensation on ingestion.

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Itami, Japan

Toshihiro Shimizu