US2003203025A1PendingUtilityA1
Sustained release oral formulations
Priority: Oct 1, 1998Filed: Mar 31, 2003Published: Oct 30, 2003
Est. expiryOct 1, 2018(expired)· nominal 20-yr term from priority
A61P 25/28A61K 9/2077A61K 9/5084A61K 9/2866A61K 9/2886A61K 9/5078A61K 31/27A61K 9/20
49
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Claims
Abstract
Pharmaceutical composition capable of releasing a therapeutically effective dose of active agent, e.g., rivastigamine, in a time-controlled manner.
Claims
exact text as granted — not AI-modified1 . A pharmaceutical composition comprising
a first component comprising a first active agent dose wherein on contact with water 70 to 95% of said dose is released within 3 to 4 hours, and a second component comprising a second active agent dose, a water soluble osmosis inducing agent and a water swellable excipient, said second component having a water permeable coating which, in use on contact with water, ruptures after a delay, and releases the active agent.
2 . A pharmaceutical composition according to claim 1 , wherein the coating in the second component is a semi-permeable membrane.
3 . A pharmaceutical composition according to claim 1 or 2 wherein the second component releases an effective dose of the active agent 6 to 12 hours after ingestion.
4 . A pharmaceutical composition according to any one of claims 1 to 3 wherein the first component comprises a cellulose derivative coating.
5 . A pharmaceutical composition according to claim 4 wherein the cellulose derivative coating comprises ethyl cellulose and hydroxypropyl methylcellulose.
6 . A pharmaceutical composition according to any one of claims 1 to 3 wherein the first component comprises the active agent in a matrix.
7 . A pharmaceutical composition according to claim 6 wherein in the first component the active agent is in a hydrophilic gel forming substance.
8 . A pharmaceutical composition according to claim 7 wherein the hydrophilic gel forming substance is present in a ratio of 10 to 50% by weight of the first component.
9 . A pharmaceutical composition according to claim 7 or 8 wherein the hydrophilic gel forming substance comprises hydroxypropylmethylcellulose having a viscosity of 100,000 mPa-s.
10 . A pharmaceutical composition according to any one of claims 1 to 9 wherein the second component has the following release characteristics in water:
time (minutes)
amount (percentage)
0
0-1
120
0-1
180
0-1
240
0-75
300
0-95
360
>99
11 . A pharmaceutical composition according to any one of claims 1 to 10 wherein the active agent is rivastigmine.
12 . A pharmaceutical composition according to any one of claims 1 to 11 comprising from 0.5 to 25% by weight of rivastigmine as active agent of the total composition.
13 . A pharmaceutical composition according to any one of claims 1 to 12 wherein the second component comprises a second coating.
14 . A pharmaceutical composition comprising rivastigmine adapted so that in use on oral administration a therapeutically effective dose of rivastigmine is released only after 6 hours.
15 . A pharmaceutical composition capable of releasing on administration twice a therapeutically effective dose of rivastigmine at different intervals upon oral administration.
16 . A pharmaceutical oral controlled release tablet composition comprising rivastigmine.
17 . A pharmaceutical composition comprising Rivastigmine having the following release characteristics in water:
time (minutes)
amount (percentage)
30
1-40
60
10-60
120
40-80
180
60-90
240
65-95
300
70-99
360
75-99
420
>80
18 . A controlled release, oral pharmaceutical composition containing rivastigmine having the following release characteristic in water or artificial stomach juices:
time (minutes)
amount (percentage)
30
1-8
60
15-25
120
45-70
180
75-90
240
92-95
300
95-98
360
97-99
420
>99
19 . A controlled release, oral pharmaceutical composition containing rivastigmine having the following release characteristic in water or artificial stomach juices:
time (minutes)
amount (percentage)
30
5-25
60
25-45
120
50-70
180
65-80
240
70-90
300
75-95
360
80-90
420
85-95
480
85-95
20 . A controlled release, oral pharmaceutical composition containing rivastigmine having the following release characteristic in water or artificial stomach juices:
time (minutes)
amount (percentage)
30
25-40
60
45-65
120
65-85
180
75-95
240
75-96
300
85-97
360
87-98
420
90-98
480
90-99
21 . A controlled release, oral pharmaceutical composition containing rivastigmine wherein in use 50 to 80% of said rivastigmine is released in artificial stomach juices within 3 hours.
22 . A composition according to any one of claims 16 to 21 comprising coated particles.
23 . A composition according to any one of claims 16 to 22 comprising coated pellets.
24 . A composition according to Claim 22 or 23 wherein the coating comprises a cellulose derivative.
25 . A composition according to claim 24 wherein the cellulose derivative comprises ethyl cellulose and hydroxypropyl methylcellulose.
26 . A pharmaceutical composition according to claim 16 or 17 wherein rivastigmine is in a hydrophilic swellable substance.
27 . A pharmaceutical composition according to claim 26 wherein the hydrophilic swellable substance comprises hydroxypropylmethylcellulose 100,000 cps.
28 . A pharmaceutical oral controlled release tablet composition comprising rivastigmine having the following release characteristic in water or artificial stomach juices:
time (minutes)
amount (percentage)
30
28-35
60
40-55
120
58-75
180
70-90
240
80-95
300
88-98
360
>92
29 . A pharmaceutical oral controlled release tablet composition comprising rivastigmine wherein in use 60 to 90% of said rivastigmine is released in artificial stomach juices within 3 hours.
30 . Use of rivastigmine and excipients as defined in any one of claims 1 to 29 in the manufacture of a medicament for the treatment of patients with mild to moderately severe Dementia of the Alzheimer's type by oral administration.
31 . A pharmaceutical composition comprising a core coated with two films, the first Inner film being a semi-permeable to water or body fluids film applied directly on said core and comprising cellulose acetate, the second outer film being a permeable to water or body fluids film comprising ethylcellulose.Cited by (0)
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