US2013004550A1PendingUtilityA1

Sustained-release solid preparation for oral use

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Assignee: DAIICHI SANKYO CO LTDPriority: Feb 22, 2010Filed: Aug 22, 2012Published: Jan 3, 2013
Est. expiryFeb 22, 2030(~3.6 yrs left)· nominal 20-yr term from priority
Inventors:Taro KanamaruShinichiro TajiriSachiko FukuiKazuhiro Yoshida
A61K 9/2054A61K 31/4745A61K 9/2018A61K 9/2027A61K 9/5047A61K 31/437A61K 9/7007A61K 31/403A61K 9/2077A61K 31/522A61P 7/02A61P 43/00
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Claims

Abstract

It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release matrix preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release preparation obtained by mixing of (A) a pharmacologically active drug, (B) hydroxypropyl methylcellulose acetate succinate having a median size (D 50 ) of 40 μm or smaller, (C) a cellulose derivative, and (D) a saccharide or a nonionic water-soluble polymer followed by molding.

Claims

exact text as granted — not AI-modified
1 . A sustained-release preparation obtained by mixing of
 (A) a pharmacologically active drug,   (B) hydroxypropyl methylcellulose acetate succinate having a median size (D 50 ) of 40 μm or smaller,   (C) a cellulose derivative, and   (D) a saccharide or a nonionic water-soluble polymer followed by molding.   
     
     
         2 . The preparation according to  claim 1 , wherein the component (B) has a median size (D 50 ) of 20 μm or smaller. 
     
     
         3 . The preparation according to  claim 1 , wherein the component (B) has a median size (D 50 ) of 10 μm or smaller. 
     
     
         4 . The preparation according to  claim 1 , wherein the component (B) has a median size (D 50 ) of 10 μm or smaller and D 90  of 20 μm or smaller. 
     
     
         5 . The preparation according to  claim 1 , wherein the content of the component (B) in the preparation is 15 to 80% by weight. 
     
     
         6 . The preparation according to  claim 1 , wherein the content of the component (B) in the preparation is 20 to 50% by weight. 
     
     
         7 . The preparation according to  claim 1 , wherein the content of the component (B) in the preparation is 25 to 45% by weight. 
     
     
         8 . The preparation according to  claim 1 , wherein the content of the component (A) in the preparation is 2 to 35% by weight. 
     
     
         9 . The preparation according to  claim 1 , wherein the cellulose derivative as the component (C) in the preparation is hydroxypropyl cellulose. 
     
     
         10 . The preparation according to  claim 9 , wherein the hydroxypropyl cellulose is hydroxypropyl cellulose having a 100-mesh sieve passing rate of 99%. 
     
     
         11 . The preparation according to  claim 9 , wherein the hydroxypropyl cellulose is hydroxypropyl cellulose having a viscosity of 150 to 400 mPa·s or 1000 to 4000 mPa·s. 
     
     
         12 . The preparation according to  claim 1 , wherein the content of the component (C) in the preparation is 5 to 35% by weight. 
     
     
         13 . The preparation according to  claim 1 , wherein the component (D) in the preparation is a saccharide. 
     
     
         14 . The preparation according to  claim 13 , wherein the saccharide is lactose or a sugar alcohol. 
     
     
         15 . The preparation according to  claim 14 , wherein the sugar alcohol is mannitol, xylitol, or erythritol. 
     
     
         16 . The preparation according to  claim 1 , wherein the component (D) in the preparation is a nonionic water-soluble polymer. 
     
     
         17 . The preparation according to  claim 16 , wherein the nonionic water-soluble polymer is povidone. 
     
     
         18 . The preparation according to  claim 1 , further containing an organic acid. 
     
     
         19 . The preparation according to  claim 18 , wherein the organic acid is fumaric acid or alginic acid. 
     
     
         20 . The preparation according to  claim 18 , wherein the organic acid is fumaric acid. 
     
     
         21 . The preparation according to  claim 1 , wherein the component (A) is a basic drug. 
     
     
         22 . The preparation according to  claim 1 , wherein the component (A) is a compound selected from the group consisting of
 (±)-1-(carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol,   N 1 -(5-chloropyridin-2-yl)-N 2 -((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide, and   N 1 -(5-chloropyridin-2-yl)-N 2 -[(1S,2R,4S)-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}-4-([1,3,4]oxadiazol-2-yl)cyclohexyl]ethanediamide   
       or a pharmacologically acceptable salt thereof, or a hydrate thereof. 
     
     
         23 . The preparation according to  claim 1 , wherein the dosage form of the preparation is a tablet.

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