Tanabe Seiyaku Company, Limited

Masakazu Mizobe

Hiroyuki Yoshino

Takashi Ishibashi

Keigo Nagao

Kengo Ikegami

Yoshihiro Hashimoto

Takahiro Ito

Hiroshi Narita

Yasuo Sekine

Harumi Hatano

Eiji Kawanishi

Hiroaki Kubo

The present invention is to provide a sustained release preparation comprising a drug-containing core substance and a multilayered coating layer covering the core substance, wherein all adjacent layers in the multilayered coating layer contain mutually different hydrophobic organic compound-water-soluble polymer mixtures; and, a method of producing a sustained release preparation, having a multilayered coating layer in which adjacent layers contain different hydrophobic organic compound-water-soluble polymer mixtures, which comprises spray-coating a solution containing a hydrophobic organic compound-water-soluble polymer mixture onto a drug-containing core substance, continuing to spray-coat a solution containing a different hydrophobic organic compound-water-soluble polymer mixture onto the resulting coating layer, and repeating this step.

Sustained-release preparation and process for producing the same

The present invention discloses an efficient preparation method of spherical fine particles containing a drug for an easily-swallowed, controlled-release preparation comprising the production of drug-containing spherical fine particles (mean particle size: 60-200 &mgr;m) by adding a binder solution to a mixture containing an excipient powder having the property of retaining solvent (and preferably having a mean length of the long axis of 40 &mgr;m or less) and a drug powder (preferably having a mean length of the long axis of 50 &mgr;m or less), followed by high-speed mixing granulation.

Preparation method of drug-containing spherical fine particles

The present invention discloses sustained release particles having a mean particle size of 300 &mgr;m, or less, comprising a drug-containing core substance coated with a mixed coating of a hydrophobic organic compound-water-insoluble polymer, which prevents sticking during compression molding when producing oral sustained release tablets, a preparation method of those sustained release particles, and a preparation method of tablets using those sustained release particles.

Sustained-release particles

A preparation capable of releasing a medicinal substance at a targeted site in the intestine, wherein the preparation dose not releases medicinal substance in endogastri at all, but can quickly release a medicinal substance when it reaches the desired site in the intestine after a certain period of time from discharge of the preparation from the stomach, and wherein a core material containing a medicinal substance is coated with a mixed film of a hydrophobic organic compound&mdash;an enteric polymer. The preparation is useful for a local therapy of inflammatory disease in the intestine such as ulcerative colitis or Crohn's disease, or an oral administrative therapy with a medicinal substance of a peptide which is apt to be decomposed chemically or enzymatically in any site except for a specific site in the intestine such as the large intestine, or with a medicinal substance whose absorption site in the intestine is limited, or the like, because a medicinal substance can be delivered selectively to a specific site in the intestine.

Preparation capable of releasing drug at target site in intestine

A pharmaceutical preparation in the form of a coated capsule which can release contents of a capsule at a lower part of the digestive tract comprising (a) a hard capsule containing at least an acidic substance, (b) a polymer film soluble at low pH which is formed on a surface of said hard capsule, and (c) an enteric coating film which is formed on a surface of said polymer film soluble at low pH. According to the pharmaceutical preparation of the present invention, any kind of a medicament can be delivered to any desired site between the upper part of the small intestine and the lower part of the large intestine in the digestive tract by controlling the amount of polymer(s) used for the polymer film soluble at low pH and/or by selecting the kind of the polymer film soluble at low pH and/or the acidic substance without any complicated requirements for each medicament.

Pharmaceutical preparation in form of coated capsule releasable at lower part of digestive tract

An imidazopyridine derivative of the formula �I!: ##STR1## wherein R.sup.1 is a lower alkyl group, R.sup.2 is a lower alkanoyl group, and R.sup.3 and R.sup.4 are each lower alkyl groups, or both combine at the end thereof to form an alkylene group having 3 to 6 carbon atoms, and a pharmaceutically acceptable salt thereof, said imidazopyridine derivatives have an excellent angiotensin II antagonistic activity and are useful for the prophylaxis or treatment of hypertension.

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Takatsuki, Japan

Masakazu Mizobe