US4728513A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Granular delayed-release form of pharmaceutically active substances
Assignee: Haleon CH SARL
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Filing: 1986-07-23
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Granted: 1988-03-01
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Expires: 2006-07-23
Abstract
Abstract A granular delayed-release form of pharmaceutically active substances, which is prepared by coating a granulated or crystalline pharmaceutically active substance, or mixtures thereof, with a coating material mixture consisting essentially of a homogeneous mixture of a poly(H+meth)-acrylic acid-(methyl+ethyl)ester which is insoluble but dispersible in water and an ethyl cellulose which is insoluble but dispersible in water in the weight ratio of 20:1 to 1:5, is presented, which is characterized by the fact that the coated granules are heated for at least 5 minutes at elevated temperatures ranging from between 50 DEG to 120 DEG C.
Inventors
- 👤 Kimon Ventouras
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 09:45
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5036; A61K9/5042; A61K9/5047; A61K9/5026
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
129 words
A process for the manufacture of a granular delayod-release form of a pharmaceutically active substance, or mixtures thereof, wherein a granulated or crystalline pharmaceutically active substance, or mixtures thereof, is coated with a coating material mixture consisting essentially of a homogeneous mixture of a poly(H+meth)-acrylic acid-(methyl+ethyl) eater which is insoluble but dispersible in water and ethyl cellulose which is insoluble but dispersible in water in the weight ratio of 20:1 to 1:5, characterised in that the dry coated granules are then heated for at least 5 minutes at elevated temperature ranging from between 50° to 120° C. whereby the instant heat treated coated granules have improved storage stability, slower release of active substance, and release rate kinetics closer to zero order kinetics than identical granules not so heat treated.
Claim 2
Dependent Claim
129 words
A process for the manufacture of a granular delayod-release form of a pharmaceutically active substance, or mixtures thereof, wherein a granulated or crystalline pharmaceutically active substance, or mixtures thereof, is coated with a coating material mixture consisting essentially of a homogeneous mixture of a poly(H+meth)-acrylic acid-(methyl+ethyl) eater which is insoluble but dispersible in water and ethyl cellulose which is insoluble but dispersible in water in the weight ratio of 20:1 to 1:5, characterised in that the dry coated granules are then heated for at least 5 minutes at elevated temperature ranging from between 50° to 120° C. whereby the instant heat treated coated granules have improved storage stability, slower release of active substance, and release rate kinetics closer to zero order kinetics than identical granules not so heat treated.
Claim 3
Dependent Claim
28 words
Process according to claim 1, characterised in that the coated granules are heated for at least 15 minutes at elevated temperatures ranging from between 60° to 90° C.
Claim 4
Dependent Claim
28 words
Process according to claim 1, characterised in that the coated granules are heated for at least 30 minutes at elevated temperatures ranging from between 65° to 80° C.
Claim 5
Dependent Claim
25 words
Process according to claim 1, characterised in that the weight ratio of the coating materials poly(H+meth)-acrylic acid ester and ethyl cellulose is 20:1 to 1:1.
Claim 6
Dependent Claim
25 words
Process according to claim 1, characterised in that the weight ratio of the coating materials poly(H+meth)-acrylic acid ester and ethyl cellulose is 14:1 to 2:1.
Claim 7
Dependent Claim
25 words
Process according to claim 1, characterised in that the weight ratio of the coating materials poly(H+meth)-acrylic acid ester and ethyl cellulose is 9:1 to 4:1.
Claim 8
Dependent Claim
22 words
Process according to claim 1 characterised in that the coating material mixture in addition is blended with at least one antistatic substance.
Claim 9
Dependent Claim
13 words
Process according to claim 7, characterised in that the antistatic substance is talcum.
Claim 10
Dependent Claim
38 words
Process according to claim 1, characterised in that the coating material mixture in addition is blended with at least one auxiliary, which is able to adjust the release of the pharmaceutically active substance(a) used to a desired rate.
Claim 11
Dependent Claim
13 words
Process according to claim 9, characterised in that the auxiliary is low-substituted hydroxypropylcellulose.
Claim 12
Dependent Claim
26 words
Process according to claim 1, characterised in that the granulated or crystalline pharmaceutically active substance(s) is (are) in the range of size of 0.05-2 mm diameter.
Claim 13
Dependent Claim
26 words
Process according to claim 1, characterised in that the granulated or crystalline pharmaceutically active substance(s) is (are) in the range of size of 0.3-1.2 mm diameter.
Claim 14
Dependent Claim
124 words
A granular delayed-release form of a pharmaceutically active substance, or mixtures thereof, which is prepared by coating a granulated or crystalline pharmaceutically active substance, or mixtures thereof, with a coating material mixture consisting essentially of a homogeneous mixture of a poly(H+meth)-acrylic acid-(methyl+ethyl) ester which is insoluble but dispersible in water and an ethyl cellulose which is insoluble but dispersible in water in the weight ratio of 20:1 to 1:5, characterised in that the coated granules are heated for at least 5 minutes at elevated temperatures ranging from between 50° to 120° C. whereby the instant heat treated coated granules have improved storage stability, slower release of active substance, and release rate kinetics closer to zero order kinetics than identical granules not so heat treated.
Claim 15
Dependent Claim
124 words
A granular delayed-release form of a pharmaceutically active substance, or mixtures thereof, which is prepared by coating a granulated or crystalline pharmaceutically active substance, or mixtures thereof, with a coating material mixture consisting essentially of a homogeneous mixture of a poly(H+meth)-acrylic acid-(methyl+ethyl) ester which is insoluble but dispersible in water and an ethyl cellulose which is insoluble but dispersible in water in the weight ratio of 20:1 to 1:5, characterised in that the coated granules are heated for at least 5 minutes at elevated temperatures ranging from between 50° to 120° C. whereby the instant heat treated coated granules have improved storage stability, slower release of active substance, and release rate kinetics closer to zero order kinetics than identical granules not so heat treated.
Claim 16
Dependent Claim
21 words
A granular delayed-release form of pharmaceutically active substances according to claim 13, characterised in that the active substance is potassium chloride.
Claim 17
Dependent Claim
22 words
A granular delayed-release form of pharmaceutically active substance according to claim 13, characterised in that the active substance is a lithium salt.
Claim 18
Dependent Claim
23 words
A granular delayed-release form of pharmaceutically active substance according to claim 13, characterised in that the active substance is a non-steroidal antiinflammatory drug.
Claim 19
Dependent Claim
21 words
A granular delayed-release form of pharmaceutically active substances according to claim 13, characterised in that the active substance is calcium salt.
Claim 20
Dependent Claim
25 words
A granular delayed-release form of pharmaceutically active substances according to claim 13, characterised in that the active substance(s) is (are) proxyphilline and/or diprophylline and/or theophylline.
Claim 21
Dependent Claim
26 words
A granular delayed-release form of pharmaceutically active substances according to claim 13, characterised in that the active substance is dimethindene or a pharmaceutically acceptable salt thereof.
Claim 22
Dependent Claim
21 words
A granular delayed-release form of pharmaceutically active substance according to claim 13, characterised in that the active substance is sodium fluoride.
Claim 23
Dependent Claim
26 words
A granular delayed-release form of pharmaceutically active substances according to claim 13, characterised in that the active substance is pridinol or a pharmaceutically acceptable salt thereof.
Claim 24
Dependent Claim
24 words
A granular delayed-release form of pharmaceutically active substances according to claim 13, characterised in that the active substance is a mixture of O-β-hydroxyethylated rutine.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-03-01 | 1991-08-31 | 1992-03-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-03-01 | 1995-08-31 | 1996-03-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-03-01 | 1999-08-31 | 2000-03-01 | $7700.00 | Window Closed / Lapsed |