US2006159768A1PendingUtilityA1
Quetiapine granules
Est. expirySep 21, 2019(expired)· nominal 20-yr term from priority
Inventors:Daniel Boyd Brown
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-modified1 - 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%.Join the waitlist — get patent alerts
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