Takeda Chemical Industries, Inc.

Takeda Pharmaceutical Company Limited

Yohko Akiyama

Naoki Nagahara

Masafumi Nakao

Takashi Kurasawa

Minoru Yoshioka

Shin-Ichiro Hirai

Hiroto Bando

Susumu Iwasa

Hidetoshi Horibe

Keiji Kamiyama

Shigetoshi Tsubotani

Shigeo Yanai

Nobuyuki Kitamori

Katsuichi Sudo

Ken-ichiro Miyagawa

Motoo Izawa

Yasuko Watanabe

Keiko Miyamoto

Megumi Kitano

Yoshitaka Nakano

Yuji Nishikimi

Eiji Nara

Kenji Nakamura

The present invention provides an orally-disintegrating solid preparation comprising fine granules showing controlled release of a pharmaceutically active ingredient, wherein the outermost layer of the fine granules is coated with a coating layer comprising hydroxypropylmethylcellulose and low-substituted hydroxypropylcellulose and breakage of the fine granules during tableting is suppressed.

Orally disintegrating solid preparation

The present invention provides a controlled release composition showing release of an active ingredient (proton pump inhibitor) controlled in two or more steps at different release rates, which contains 1) a release-controlled part A capable of controlling release of the active ingredient to occur at a predetermined rate, 2) a release-controlled part B capable of controlling release of the active ingredient to occur at a predetermined rate lower than the release rate of the release-controlled part A, and where necessary, 3) a release-controlled part C capable of controlling release of the active ingredient to occur at a predetermined rate faster than the release rate of the release-controlled part B, wherein the release of the active ingredient from the release-controlled part B precedes the release of the active ingredient from the release-controlled part A (when release-controlled part C is contained, the release of the active ingredient from the release-controlled part C precedes the release of the active ingredient from the release-controlled part B).

Controlled release composition

A controlled release preparation wherein the release of active ingredient is controlled, which releases an active ingredient for an extended period of time by staying or slowly migrating in the gastrointestinal tract, is provided by means such as capsulating a tablet, granule or fine granule wherein the release of active ingredient is controlled and a gel-forming polymer. Said tablet, granule or fine granule has a release-controlled coating-layer formed on a core particle containing an active ingredient.

Controlled release preparation

In order to provide a composition having a long gastroduodenal residence time and exhibiting an improved efficacy, is provided a gastrointestinal mucosa-adherent composition comprising an active ingredient and a material which swells a viscogenic agent capable of being viscous with water a (e.g. curdlan and/or a low-substituted hydroxypropylcellulose etc.).

Gastrointestinal mucosa-adherent pharmaceutical composition

Polyol-amino acid compounds having anti-helicobacter pylori activity

A solid matrix composition which is solid at ambient temperature, which comprises a viscogenic agent, such as an acrylic acid polymer, capable of developing viscosity on contact with water, as dispersed at least in the neighborhood of the surface layer of a matrix particle containing a polyglycerol fatty acid ester or a lipid and an active ingredient. The matrix may be such that a matrix particle containing a polyglycerol fatty acid ester or a lipid and an active ingredient has been coated with a coating composition containing at least one viscogenic agent. Such composition can adhere to the digestive tract and remain there for a prolonged period of time, thereby increasing the bioavailability of the active ingredient. Solid preparations, such as fine granules and granules, contain the above matrix composition.

Gastrointestinal mucosa-adherent matrixes pharmaceutical preparations and a coating composition

The present invention includes a formulation which comprises an antibacterial substance and an antiulcer substance, wherein at least either of them is formulated into a gastrointestinal mucosa-adherent solid preparation. The formulation of the present invention shows long retention time in the gastrointestinal tract because of adhesion to the gastrointestinal tract mucosa, synergetically enhances the pharmaceutical effects of an antibacterial substance, specially antibiotic against,(HP) and an antiulcer substance, with very low doses of active ingredients, particularly the anti-HP antibiotic with low prevalence of side effects. The present agent is useful as an antiulcer agent, showing potent anti-HP activity.

Formulation comprising antibacterial substance and antiulcer substance

A controlled-release composition comprising a drug-containing core coated with a coating composition containing a water-insoluble substance and a swellable polymer having no basic groups which is capable of maintaining an almost constant drug concentration in plasma over an extended period of time to ensure sustained drug action in the body.

Controlled-release composition

The present invention includes a formulation which comprises an antibacterial substance and an antiulcer substance, wherein at least either of them is formulated into a gastrointestinal mucosa-adherent solid preparation. The formulation of the present invention shows long retention time in the gastrointestinal tract because of adhesion to the gastrointestinal tract mucosa, synergetically enhances the pharmaceutical effects of an antibacterial substance, specially antibiotic against Helicobacter pylori (HP) and an antiulcer substance, with very low doses of active ingredients, particularly the anti-HP antibiotic with low prevalence of side effects. The present agent is useful as an anti ulcer agent, showing potent anti-HP activity.

The present invention relates to a pharmaceutical composition for oral administration in which a fumagillol derivative is stabilized and exhibits remarkable antiangiogenesis activity in oral administration.

Oral composition of fumagillol derivative

Gastrointestinal mucosa-adherent granules, pharmaceutical preparations

There is provided a matrix preparation produced by dispersing a pharmaceutically active ingredient into a matrix which is solid at ambient temperature and comprised of a fatty acid ester of a polyglycerol. The preparation has stable release-controlling ability, can be processed to fine granules, granules, capsules, tablets etc., and contributes to reduce the administration times of the active ingredient and side effects of the ingredient.

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Osaka, Japan

Yohko Akiyama