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Compositions controlling pH range of release and/or release rate

a technology of compositions and ph ranges, applied in the direction of drug compositions, biocide, anti-inflammatory agents, etc., can solve the problems of poor soluble compound, poor soluble compound, and difficulty in achieving high-dose doses

Inactive Publication Date: 2009-01-08
SAGARA KAZUYOSHI +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0009]The present inventors have conducted intensive studies in an attempt to develop a solid preparation that can be administered orally, by improving the dissolution property of the compound of the formula (I) in the neutral area in the gastrointestinal tract lumen and controlling the release rate. As a result, the present inventors have found that the dissolution property of the present compound in the neutral area can be improved and the release rate of a drug can be designedly controlled by dispersing the present compound in polymer(s), which resulted in the completion of a composition capable of maximally eliciting a therapeutic effect on the inflammatory bowel diseases.

Problems solved by technology

However, the present compound is a poorly soluble compound, which shows markedly low solubility particularly in the neutral area, and an extremely high dose is problematically necessary for eliciting the effect of the present compound in a conventional oral preparation.
While WO98 / 11111 discloses, as a preparation for oral administration of the present compound, a composition comprising a mixture of the present compound and additives such as sucrose, lactose, crystalline cellulose, methylcellulose, a synthetic or semi synthetic polymer, and the like, a preparation that achieves the above-mentioned objects cannot be obtained by merely admixing the present compound with such additives, because the present compound is poorly soluble.

Method used

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  • Compositions controlling pH range of release and/or release rate
  • Compositions controlling pH range of release and/or release rate
  • Compositions controlling pH range of release and/or release rate

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0057]Compound A (1.074 g, 1 g by conversion to anhydride) and polyvinylpyrrolidone (1 g or 5 g, product name, Kolidon; manufactured by BASF) were dissolved in ethanol and the organic solvent was evaporated under reduced pressure using a rotary evaporator. The obtained solid was pulverized to give fine granules (a) or (b).

[0058](a)—compound A:polyvinylpyrrolidone=1:1

[0059](b)—compound A:polyvinylpyrrolidone=1:5

example 2

[0060]Compound A (1.074 g, 1 g by conversion to anhydride) and polyoxyethylene hydrogenated castor oil (5 g, product name, HCO-60; manufactured by Nihon Surfactant Kogyo K.K.) were dissolved in ethanol and the mixture was adsorbed to special calcium silicate (1 g, product name, FLORITE RE; manufactured by Eisai Co., Ltd.) to give a powder.

example 3

[0061]Compound A (1.074 g, 1 g by conversion to anhydride) was dissolved in ethanol and the mixture was adsorbed to special calcium silicate (1 g, product name, FLORITE RE; manufactured by Eisai Co., Ltd.) to give a powder.

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Abstract

The present invention provides a composition controlling a pH range of release and / or a release rate, which contains (i) a thienotriazolodiazepine compound of the formula (I)and (ii) at least one kind of ingredient selected from the group consisting of a water-soluble polymer, an enteric polymer, a water-insoluble polymer and a porous polymer and / or a surfactant, as well as a production method thereof.

Description

[0001]This is a continuation in part of PCT / JP01 / 05151 filed on Jun. 15, 2001.TECHNICAL FIELD OF THE INVENTION[0002]The present invention relates to a composition that controls a pH range of release and / or a release rate and maximally elicits a therapeutic effect on inflammatory bowel diseases such as ulcerative colitis, Crohn's disease and the like.BACKGROUND OF THE INVENTION[0003]A compound of the formula (I)wherein X is a halogen, R1 is C1-C4 alkyl, R2 is C1-C4 alkyl, a is an integer of 1-4, R3 is C1-C4 alkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, phenyl optionally having substituent(s) or heteroaryl optionally having substituent(s) (hereinafter sometimes to be also referred to as the present compound) is useful as a therapeutic agent for ulcerative colitis and Crohn's disease (WO98 / 11111).[0004]Inflammatory bowel disease is an intractable bowel disease that is developed in a neutral area of from the upper small intestine to large intestine. Particularly, Crohn's disease is observed ...

Claims

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Application Information

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IPC IPC(8): A61K31/551A61P29/00A61K9/14A61K9/16A61K9/20A61K31/5517A61P1/04
CPCA61K9/143A61K9/146A61K9/1635A61K9/1641A61K9/1652A61K9/1676A61K31/551A61K9/204A61K9/2054A61K9/2059A61K31/5517A61K47/38A61K9/2018A61P1/00A61P1/04A61P29/00
Inventor SAGARA, KAZUYOSHIOMURA, TOMOYUKISAMEMOTO, HIROFUMIKOMATSU, HIROTSUGU
Owner SAGARA KAZUYOSHI
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