US4938967A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Pharmaceutical formulations
Assignee: London School of Pharmacy Innovations Ltd
•
Filing: 1987-09-17
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Granted: 1990-07-03
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Expires: 2007-09-17
Abstract
Abstract The residence time in the human stomach of pharmaceutical, gastric controlled release, solid units can be increased significantly if the units have a density that is much higher than normal. A preferred oral dosage form according to the invention comprises a capsule or other dosage form having a dimension above 2 mm and that contains one or more of the said units. The density of each unit is preferably at least 2.5 and usually at least 2.7 g/ml and can conveniently be achieved by including at least 50% by weight of a weighting agent such as barium sulphate.
Inventors
- 👤 John M. Newton
- 👤 Jane E. Devereux
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 18:40
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/14; A61K9/16; A61K9/1605; A61K9/1611
Claims Analysis
Total Claims: 25
Claim 1
Independent Claim
93 words
An oral, solid, pharmaceutical dosage form that is a capsule or disintegratable tablet and that has a minimum dimension of at least 2 mm and that is suitable for oral administration to humans and that comprises a plurality of controlled release units each comprising a pharmaceutically active ingredient and a pharmaceutically acceptable carrier that includes gastric controlled release binder that will permit controlled release of the active ingredient from the controlled release unit while in the stomach, and in which each said controlled release unit has a density of at least 2.5 g/ml.
Claim 2
Dependent Claim
93 words
An oral, solid, pharmaceutical dosage form that is a capsule or disintegratable tablet and that has a minimum dimension of at least 2 mm and that is suitable for oral administration to humans and that comprises a plurality of controlled release units each comprising a pharmaceutically active ingredient and a pharmaceutically acceptable carrier that includes gastric controlled release binder that will permit controlled release of the active ingredient from the controlled release unit while in the stomach, and in which each said controlled release unit has a density of at least 2.5 g/ml.
Claim 3
Dependent Claim
17 words
A dosage form according to claim 1 in which the said density is at least 2.7 g/ml.
Claim 4
Dependent Claim
16 words
A dosage form according to claim 1 in which the said density is below 6 g/ml.
Claim 5
Dependent Claim
26 words
A dosage form according to claim 1 in which the or each said controlled release unit has a mean dimension of at least about 1 mm.
Claim 6
Dependent Claim
23 words
A dosage form according to claim 1 in which each said unit has a mean dimension of about 1 to about 2 mm.
Claim 7
Dependent Claim
26 words
A dosage form according to claim 1 in which each said unit is spheronized pellets having a mean diameter of about 1 to about 2 mm.
Claim 8
Dependent Claim
27 words
A dosage form according to claim 1 having a maximum dimension of about 5 to about 25 mm and a minimum dimension of below about 10 mm.
Claim 9
Dependent Claim
46 words
A dosage form according to claim 1 in which the said carrier of each said controlled release unit includes also about 50% to about 95% by weight of the said unit of a pharmaceutically acceptable weighting agent having a density of at least about 3.0 g/ml.
Claim 10
Dependent Claim
44 words
A dosage form according to claim 1 in which the said carrier of each said controlled release unit includes also about 50% to about 95% by weight of the said unit of a pharmaceutically acceptable weighting agent which comprises barium sulphate or ferrous oxide.
Claim 11
Dependent Claim
24 words
A dosage form according to claim 1 in which the controlled release binder comprises a controlled release coating around each said controlled release unit.
Claim 12
Dependent Claim
36 words
A dosage form according to claim 1 in which the active ingredient is selected from alimentary tract and metabolic products, cardiovascular products, blood and clotting products, neurological products, H 1 antagonists, and products having antiviral activity.
Claim 13
Dependent Claim
15 words
A dosage form according to claim 1 in which the active ingredient is a prostaglandin.
Claim 14
Independent Claim
123 words
A method of prolonging the release of an active ingredient within the human stomach when administering orally a solid pharmaceutical dosage form that is a capsule or disintegratable tablet and that has a minimum dimension of at least 2 mm and that comprises a plurality of controlled release units each comprising the said ingredient and a pharmaceutically acceptable carrier that includes a gastric controlled release binder that will permit controlled release of the active ingredient from the unit while in the stomach, the method comprising incorporating into each said controlled release unit at least 50% by weight of a weighting aid having a density of at least about 3 g/ml and thereby increasing the density of each said unit to above 2.5 g/ml.
Claim 15
Independent Claim
123 words
A method of prolonging the release of an active ingredient within the human stomach when administering orally a solid pharmaceutical dosage form that is a capsule or disintegratable tablet and that has a minimum dimension of at least 2 mm and that comprises a plurality of controlled release units each comprising the said ingredient and a pharmaceutically acceptable carrier that includes a gastric controlled release binder that will permit controlled release of the active ingredient from the unit while in the stomach, the method comprising incorporating into each said controlled release unit at least 50% by weight of a weighting aid having a density of at least about 3 g/ml and thereby increasing the density of each said unit to above 2.5 g/ml.
Claim 16
Dependent Claim
111 words
In a method of releasing an active ingredient within the human stomach by administering orally a solid pharmaceutical dosage form that is a capsule or distingratable tablet and that has a minimum dimension of at least 2 mm and that comprises a plurality of controlled release units each comprising a pharmaceutically active ingredient and a pharmaceutically acceptable carrier that includes gastric controlled release binder that will control release of the active ingredient from the controlled release unit while in the stomach, the improvement which comprises prolonging the release of the active ingredient within the stomach by using, as each controlled release unit, a unit have a density greater than 2.5 g/ml.
Claim 17
Dependent Claim
111 words
In a method of releasing an active ingredient within the human stomach by administering orally a solid pharmaceutical dosage form that is a capsule or distingratable tablet and that has a minimum dimension of at least 2 mm and that comprises a plurality of controlled release units each comprising a pharmaceutically active ingredient and a pharmaceutically acceptable carrier that includes gastric controlled release binder that will control release of the active ingredient from the controlled release unit while in the stomach, the improvement which comprises prolonging the release of the active ingredient within the stomach by using, as each controlled release unit, a unit have a density greater than 2.5 g/ml.
Claim 18
Dependent Claim
24 words
The method according to claim 14, in which each controlled release unit has and a mean dimension of not more than about 2 mm.
Claim 19
Dependent Claim
98 words
In an oral solid pharmaceutical dosage form that is a capsule or disintegratable tablet and that has a minimum dimension of at least 2 mm and that is suitable for oral administration of humans and that comprises a pharmaceutically active ingredient and a pharmaceutically acceptable carrier that includes gastric controlled release binder that will permit controlled release of the active ingredient from the controlled release unit while in the stomach, the improvement which comprises each said controlled release unit having a density of at least 2.5 g/ml, whereby retention in the stomach of all the units is prolonged.
Claim 20
Dependent Claim
98 words
In an oral solid pharmaceutical dosage form that is a capsule or disintegratable tablet and that has a minimum dimension of at least 2 mm and that is suitable for oral administration of humans and that comprises a pharmaceutically active ingredient and a pharmaceutically acceptable carrier that includes gastric controlled release binder that will permit controlled release of the active ingredient from the controlled release unit while in the stomach, the improvement which comprises each said controlled release unit having a density of at least 2.5 g/ml, whereby retention in the stomach of all the units is prolonged.
Claim 21
Dependent Claim
25 words
The oral dosage form of claim 1 in which each controlled release unit has and a mean diameter of not more than about 2 mm.
Claim 22
Dependent Claim
19 words
The oral dosage form of claim 16 in which the density of each controlled release unit is the same.
Claim 23
Dependent Claim
19 words
A dosage form according to claim 1 in which the density of each controlled release unit is the same.
Claim 24
Dependent Claim
19 words
A method according to claim 13 in which the density of each resulting controlled release unit is the same.
Claim 25
Dependent Claim
18 words
A method according to claim 14 in which the density of each controlled release unit is the same.
References Cited (Backward Citations)
GB866924A
Cited
GB936386A
Cited
GB1428426A
Cited
GB1590573A
Cited
GB1590574A
Cited
US4193985A
Cited
GB2015875A
Cited
US4339463A
Cited
EP0025699A1
Cited
GB2100602A
Cited
EP0097651A1
Cited
GB2123690A
Cited
GB2123693A
Cited
EP0119480A2
Cited
GB2155335A
Cited
EP0173210A2
Cited
AU4657085A
Cited
GB2174300A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1993-07-02 | 1994-01-01 | 1994-07-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-07-02 | 1998-01-01 | 1998-07-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-07-02 | 2002-01-01 | 2002-07-03 | $7700.00 | Window Closed / Lapsed |