US4547358A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Sustained release tablet containing at least 95 percent theophylline
Assignee: Mead Johnson and Co LLC
•
Filing: 1984-06-04
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Granted: 1985-10-15
•
Expires: 2004-06-04
Abstract
Abstract Non-disintegrating theophylline tablets having a pair of opposing substantially planar surfaces and a very thin cross-section have a high bioavailability on ingestion and a relatively steady release rate permitting a 12 hr. dosing interval for maintenance of non-toxic therapeutic blood theophylline concentrations. Excipients or tableting aids are not required, but trace amounts of a tableting lubricant are preferably included to facilitate continuous large scale production.
Inventors
- 👤 Stephen T. David
- 👤 Dana Brooke
- 👤 Claude E. Gallian
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 21:11
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2072; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K31/519; A61K31/52
Claims Analysis
Total Claims: 33
Claim 1
Independent Claim
87 words
A sustained release pharmaceutical tablet comprising 95% to 99.8% by weight of theophylline, and the remainder conventional pharmaceutical tablet ingredients selected to provide a tablet that remains intact during dissolution, said tablet having a pair of substantially planar opposing faces joined by edge walls and a thickness of from 0.08 to 0.12 inches which when administered to a human in a therapeutically effective amount at consecutive 12 hour intervals affords a continuous blood serum concentration of from 10 mcg/ml to 20 mcg/ml of theophylline during said intervals.
Claim 2
Dependent Claim
87 words
A sustained release pharmaceutical tablet comprising 95% to 99.8% by weight of theophylline, and the remainder conventional pharmaceutical tablet ingredients selected to provide a tablet that remains intact during dissolution, said tablet having a pair of substantially planar opposing faces joined by edge walls and a thickness of from 0.08 to 0.12 inches which when administered to a human in a therapeutically effective amount at consecutive 12 hour intervals affords a continuous blood serum concentration of from 10 mcg/ml to 20 mcg/ml of theophylline during said intervals.
Claim 3
Dependent Claim
14 words
The pharmaceutical tablet of claim 1 containng 100 mg to 500 mg of theophylline.
Claim 4
Dependent Claim
14 words
The pharmaceutical tablet of claim 1 having a thickness of 0.09 to 0.11 inches.
Claim 5
Dependent Claim
19 words
The pharmaceutical tablet of claim 1 containing from 0.2% to 0.6% by weight of magnesium stearate as tableting lubricant.
Claim 6
Dependent Claim
18 words
The pharmaceutical tablet of claim 1 containing 0.3% to 0.5% by weight of magnesium stearate as tableting lubricant.
Claim 7
Dependent Claim
21 words
The pharmaceutical tablet of claim 1 consisting essentially of 99.6% by weight of theophylline and 0.4% by weight of magnesium stearate.
Claim 8
Dependent Claim
11 words
The pharmaceutical tablet of claim 6 containing 300 mg of theophylline.
Claim 9
Dependent Claim
92 words
A sustained release pharmaceutical tablet consisting essentially of 99.4% to 99.8% by weight of theophylline and 0.1% to 0.6% by weight of a tableting lubricant selected to provide a tablet that remains intact during dissolution, said tablet having a pair of substantially planar opposing faces joined by edge walls and a thickness of from 0.08 to 0.12 inches which when administered to a human in a therapeutically effective amount at consecutive 12 hour intervals affords a continuous blood serum concentration of from 10 mcg/ml to 20 mcg/ml of theophylline during said intervals.
Claim 10
Dependent Claim
92 words
A sustained release pharmaceutical tablet consisting essentially of 99.4% to 99.8% by weight of theophylline and 0.1% to 0.6% by weight of a tableting lubricant selected to provide a tablet that remains intact during dissolution, said tablet having a pair of substantially planar opposing faces joined by edge walls and a thickness of from 0.08 to 0.12 inches which when administered to a human in a therapeutically effective amount at consecutive 12 hour intervals affords a continuous blood serum concentration of from 10 mcg/ml to 20 mcg/ml of theophylline during said intervals.
Claim 11
Dependent Claim
12 words
The tablet of claim 8 where the tableting lubricant is magnesium stearate.
Claim 12
Dependent Claim
126 words
A pharmaceutically tablet for the maintenance of a therapeutically effective blood concentration of theophylline during a dosage interval of up to 12 hours following ingestion thereof in therapeutically effective amount comprised of at least 95% by weight of theophylline and the remainder conventional pharmaceutical tablet ingredients selected to provide a tablet which dissolves without first disintegrating when contacted with water during a period of about 4 hours to the extent of from 83% to 100% by weight, wherein said tablet has a pair of substantially planar opposing faces joined by edge walls and a thickness of from 0.08 to 0.12 inches and the therapeutically effective theophylline blood serum concentration maintained by said tablet is substantially within the range of from about 10 mcg/ml to 20 mcg/ml.
Claim 13
Dependent Claim
126 words
A pharmaceutically tablet for the maintenance of a therapeutically effective blood concentration of theophylline during a dosage interval of up to 12 hours following ingestion thereof in therapeutically effective amount comprised of at least 95% by weight of theophylline and the remainder conventional pharmaceutical tablet ingredients selected to provide a tablet which dissolves without first disintegrating when contacted with water during a period of about 4 hours to the extent of from 83% to 100% by weight, wherein said tablet has a pair of substantially planar opposing faces joined by edge walls and a thickness of from 0.08 to 0.12 inches and the therapeutically effective theophylline blood serum concentration maintained by said tablet is substantially within the range of from about 10 mcg/ml to 20 mcg/ml.
Claim 14
Dependent Claim
16 words
The pharmaceutical tablet of claim 10 containing from about 100 mg to 500 mg of theophylline.
Claim 15
Dependent Claim
38 words
The pharmaceutical tablet of claim 10 which when administered to a human in bronchodilative effective amount at consecutive intervals of from about 8 to 12 hours maintains a bronchodilative effective blood serum concentration of theophylline during said interval.
Claim 16
Dependent Claim
14 words
The pharmaceutical tablet of claim 10 having a thickness of 0.09 to 0.11 inches.
Claim 17
Dependent Claim
18 words
The pharmaceutical tablet of claim 10 containing at least 99% by weight of theophylline and a tableting lubricant.
Claim 18
Dependent Claim
19 words
The pharmaceutical tablet of claim 14 containing from 0.1% to 0.6% by weight of magnesium stearate as tableting lubricant.
Claim 19
Dependent Claim
19 words
The pharmaceutical tablet of claim 14 containing from 0.3% to 0.5% by weight of magnesium stearate as tableting lubricant.
Claim 20
Dependent Claim
21 words
The pharmaceutical tablet of claim 10 consisting essentially of 99.6% by weight of theophylline and 0.4% by weight of magnesium stearate.
Claim 21
Dependent Claim
11 words
The pharmaceutical tablet of claim 10 containing 300 mg of theophylline.
Claim 22
Dependent Claim
27 words
The pharmaceutical tablet of claim 10 wherein said tablet consists essentially of 99.4% to 99.8% by weight of theophylline and 0.1% to 0.6% weight of magnesium stearate.
Claim 23
Independent Claim
129 words
The method for maintaining a therapeutically effective blood serum concentration of theophylline during an extended treatment period which comprises orally administering a therapeutically effective dose of theophylline to a patient requiring theophylline therapy said dose consisting of one or more pharmaceutical tablets which dissolve without first disintegrating when contacted with water for a period of at least 4 hours said tablets being comprised of at least 95% by weight of theophylline, and the remainder conventional pharmaceutical tablet ingredients selected to provide a tablet that remains intact while dissolving, said tablet having a pair of substantially planar opposing faces joined by edge walls and a thickness of from 0.08 to 0.12 inches wherein said tablet is administered on a repeat dose schedule at dose intervals of up to 12 hours.
Claim 24
Independent Claim
129 words
The method for maintaining a therapeutically effective blood serum concentration of theophylline during an extended treatment period which comprises orally administering a therapeutically effective dose of theophylline to a patient requiring theophylline therapy said dose consisting of one or more pharmaceutical tablets which dissolve without first disintegrating when contacted with water for a period of at least 4 hours said tablets being comprised of at least 95% by weight of theophylline, and the remainder conventional pharmaceutical tablet ingredients selected to provide a tablet that remains intact while dissolving, said tablet having a pair of substantially planar opposing faces joined by edge walls and a thickness of from 0.08 to 0.12 inches wherein said tablet is administered on a repeat dose schedule at dose intervals of up to 12 hours.
Claim 25
Dependent Claim
35 words
The method of claim 20 wherein said therapeutically effective dose is a bronchodilative effective dose and said therapeutically effective blood serum concentration is substantially within the range of from about 10 mcg/ml to 20 mcg/ml.
Claim 26
Dependent Claim
19 words
The method of claim 20 wherein said dosage interval is within the range of about 8 to 12 hours.
Claim 27
Dependent Claim
17 words
The method of claim 20 wherein said tablet contains from 100 mg to 500 mg of theophylline.
Claim 28
Dependent Claim
16 words
The method of claim 20 wherein said tablet has a thickness of 0.09 to 0.11 inches.
Claim 29
Dependent Claim
20 words
The method of claim 20 wherein said tablet contains at least 99% by weight of theophylline and a tableting lubricant.
Claim 30
Dependent Claim
21 words
The method of claim 20 wherein said tablet contains from 0.1% to 0.6% by weight of magnesium stearate as tableting lubricant.
Claim 31
Dependent Claim
21 words
The method of claim 20 wherein said tablet contains from 0.3% to 0.5% by weight of magnesium stearate as tableting lubricant.
Claim 32
Dependent Claim
27 words
The method of claim 20 wherein said tablet consists essentially of 99.4% to 99.8% by weight of theophylline and 0.1% to 0.6% by weight of magnesium stearate.
Claim 33
Dependent Claim
23 words
The method of claim 20 wherein said tablet consists essentially of 99.6% by weight of theophylline and 0.4% by weight of magnesium stearate.
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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) | 1988-10-14 | 1989-04-15 | 1989-10-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-10-14 | 1993-04-15 | 1993-10-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-10-14 | 1997-04-15 | 1997-10-15 | $7700.00 | Window Closed / Lapsed |