US2006159768A1PendingUtilityA1

Quetiapine granules

Assignee: ASTRAZENECA ABPriority: Sep 21, 1999Filed: Jan 10, 2006Published: Jul 20, 2006
Est. expirySep 21, 2019(expired)· nominal 20-yr term from priority
A61P 25/00A61P 25/18A61K 9/1635A61K 31/553A61K 9/0095A61K 31/554A61K 9/1623A61K 9/1652
49
PatentIndex Score
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Claims

Abstract

Granule formulation of quetiapine and pharmaceutically acceptable salt thereof are described, as are their preparation and their use in treating diseases of the central nervous system such as psychotic disease conditions including schizophrenia.

Claims

exact text as granted — not AI-modified
1 - 17 . (canceled)  
   
   
       18 . A granule formulation comprising 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine or a pharmaceutically acceptable salt thereof and a freely or very water-soluble binder, wherein the granules have a bulk density range of 0.15 g/cc to 0.60 g/cc and a tap density range of 0.20 g/cc to 0.70 g/cc and 80% of the granules are in the size range of 75 to 850 microns and wherein the granules have a moisture level in the range of 1.5% to 15%.  
   
   
       19 . A formulation according to  claim 18  wherein 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine is in the form of a fumarate salt.  
   
   
       20 . A formulation according to  claim 18  wherein the freely or very water-soluble binder comprises maltodextrin, mannitol, xylitol, pre-gelatinised starch, sucrose or poly[1-(2-oxo-1-pyrrolidinyl)ethylene].  
   
   
       21 . A formulation according to  claim 19  wherein the freely or very water-soluble binder comprises maltodextrin, mannitol, xylitol, pre-gelatinised starch, sucrose or poly[1-(2-oxo-1-pyrrolidinyl)ethylene].  
   
   
       22 . A formulation according to  claim 20  wherein the binder is maltodextrin.  
   
   
       23 . A formulation according to  claim 21  wherein the binder is maltodextrin.  
   
   
       24 . A formulation according to  claim 18  which further comprises a sweetener.  
   
   
       25 . A formulation according to  claim 19  which further comprises a sweetener.  
   
   
       26 . A formulation according to  claim 20  which further comprises a sweetener.  
   
   
       27 . A formulation according to  claim 21  which further comprises a sweetener.  
   
   
       28 . A formulation according to  claim 22  which further comprises a sweetener.  
   
   
       29 . A formulation according to  claim 23  which further comprises a sweetener.  
   
   
       30 . A formulation according to  claim 18  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       31 . A formulation according to  claim 19  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       32 . A formulation according to  claim 20  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       33 . A formulation according to  claim 21  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       34 . A formulation according to  claim 22  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       35 . A formulation according to  claim 23  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       36 . A formulation according to  claim 24  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       37 . A formulation according to  claim 25  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       38 . A formulation according to  claim 26  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       39 . A formulation according to  claim 27  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       40 . A formulation according to  claim 28  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       41 . A formulation according to  claim 29  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       42 . A granule formulation consisting of 11-[4-[2-(2-hydroxyethoxy)ethyl-1-piperazinyl]dibenzol[b,f][1,4]thiazepine or a pharmaceutically acceptable salt thereof, a freely or very water-soluble binder, and a sweetener wherein the granules have a bulk density range of 0.15 g/cc to 0.60 glcc and a tap density range of 0.20 g/cc to 0.70 g/cc and 80% of the granules are in the size range of 75 to 850 microns and wherein the granules have a moisture level in the range of 1.5% to 15%.  
   
   
       43 . A formulation according to  claim 42  wherein 11-[4-[2-(2-hydroxyethoxy)ethyl-1-piperazinyl]dibenzol[b,f][1,4]thiazepine is in the form of a fumarate salt.  
   
   
       44 . A formulation according to  claim 42  wherein the freely or very water-soluble binder comprises maltodextrin, mannitol, xylitol, pre-gelatinised starch, sucrose or poly[1-(2-oxo-1-pyrrolidinyl)ethylene].  
   
   
       45 . A formulation according to  claim 43  wherein the freely or very water-soluble binder comprises maltodextrin, mannitol, xylitol, pre-gelatinised starch, sucrose or poly[1-(2-oxo-1-pyrrolidinyl)ethylene].  
   
   
       46 . A formulation according to  claim 44  wherein the binder is maltodextrin.  
   
   
       47 . A formulation according to  claim 45  wherein the binder is maltodextrin.  
   
   
       48 . A formulation according to  claim 43  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       49 . A formulation according to  claim 44  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       50 . A formulation according to  claim 45  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       51 . A formulation according to  claim 46  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       52 . A formulation according to  claim 47  wherein the bulk density range is 0.26 g/cc to 0.400 g/cc and the tap density range is 0.342 g/cc to 0.500 g/cc.  
   
   
       53 . A formulation according to  claim 18  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       54 . A formulation according to  claim 19  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       55 . A formulation according to  claim 20  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       56 . A formulation according to  claim 21  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       57 . A formulation according to  claim 22  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       58 . A formulation according to  claim 23  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       59 . A formulation according to  claim 24  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       60 . A formulation according to  claim 25  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       61 . A formulation according to  claim 26  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       62 . A formulation according to  claim 27  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       63 . A formulation according to  claim 28  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       64 . A formulation according to  claim 29  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       65 . A formulation according to  claim 30  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       66 . A formulation according to  claim 31  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       67 . A formulation according to  claim 32  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       68 . A formulation according to  claim 33  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       69 . A formulation according to  claim 34  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       70 . A formulation according to  claim 35  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       71 . A formulation according to  claim 36  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       72 . A formulation according to  claim 37  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       73 . A formulation according to  claim 38  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       74 . A formulation according to  claim 39  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       75 . A formulation according to  claim 40  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       76 . A formulation according to  claim 41  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       77 . A formulation according to  claim 42  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       78 . A formulation according to  claim 43  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       79 . A formulation according to  claim 44  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       80 . A formulation according to  claim 45  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       81 . A formulation according to  claim 46  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       82 . A formulation according to  claim 47  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       83 . A formulation according to  claim 48  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       84 . A formulation according to  claim 49  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       85 . A formulation according to  claim 50  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       86 . A formulation according to  claim 51  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       87 . A formulation according to  claim 52  wherein the granules have a moisture level in the range of from 4% to 8%.  
   
   
       88 . A formulation according to  claim 18  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       89 . A formulation according to  claim 19  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       90 . A formulation according to  claim 20  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       91 . A formulation according to  claim 21  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       92 . A formulation according to  claim 22  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       93 . A formulation according to  claim 23  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       94 . A formulation according to  claim 24  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       95 . A formulation according to  claim 25  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       96 . A formulation according to  claim 26  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       97 . A formulation according to  claim 27  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       98 . A formulation according to  claim 28  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       99 . A formulation according to  claim 29  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       100 . A formulation according to  claim 30  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       101 . A formulation according to  claim 31  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       102 . A formulation according to  claim 32  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       103 . A formulation according to  claim 33  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       104 . A formulation according to  claim 34  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       105 . A formulation according to  claim 35  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       106 . A formulation according to  claim 36  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       107 . A formulation according to  claim 37  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       108 . A formulation according to  claim 38  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       109 . A formulation according to  claim 39  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       110 . A formulation according to  claim 40  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       111 . A formulation according to  claim 41  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       112 . A formulation according to  claim 42  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       113 . A formulation according to  claim 43  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       114 . A formulation according to  claim 44  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       115 . A formulation according to  claim 45  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       116 . A formulation according to  claim 46  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       117 . A formulation according to  claim 47  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       118 . A formulation according to  claim 48  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       119 . A formulation according to  claim 49  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       120 . A formulation according to  claim 50  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       121 . A formulation according to  claim 51  wherein the granules have a moisture level in the range of from 3% to 10%.  
   
   
       122 . A formulation according to  claim 52  wherein the granules have a moisture level in the range of from 3% to 10%.

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