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

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 com

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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