Patent US4226849A successfully refreshed from Google Patents.
US4226849A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Sustained release therapeutic compositions
Assignee: Forest Laboratories LLC
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Filing: 1979-06-14
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Granted: 1980-10-07
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Expires: 1999-06-14
Abstract
Abstract Shaped pharmaceutical tablets, lozenges, suppositories and other solid dosage unit forms which have a prolonged and regular release pattern of a therapeutically active medicament incorporated therein, wherein the shaped dosage unit comprises a carrier base material of hydroxypropylmethylcellulose or a mixture thereof with up to 30% ethylcellulose and/or up to 30% sodium carboxymethylcellulose and wherein the carrier base material is subjected to hydrolysis and oxidation so as to generate thereon a desired minimum concentration of carbonyl and carboxyl groups, and then admixed and shaped with a therapeutically active medicament.
Inventors
- 👤 Joseph M. Schor
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 07:46
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/205; A61K9/2054
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
219 words
A shaped and compressed sustained release therapeutic composition comprising a therapeutically active medicament and a carrier base material, characterized by a long-lasting slow and regular incremental release of the medicament upon administration, wherein the carrier base material is hydroxypropylmethylcellulose or a mixture of hydroxypropylmethylcellulose and either up to 30% ethylcellulose or 30% sodium carboxymethylcellulose or both, and wherein the hydroxypropylmethylcellulose or the mixtures thereof have been subjected to hydrolysis and oxidation and have a carbonyl content which ranges from 0.2 to 3.0 grams/100 grams and a carboxyl content which ranges from 0.37 to 2.6 grams/100 grams, the oxidation having been carried out at about 30° to 50° C. in the presence of oxygen or a stream of air for a period of time sufficient to obtain the desired carbonyl and carboxyl values and the composition having incorporated therein 0.1-1.0%, based on the weight of the carrier material, of a reducing stabilizing agent which prevents undesired further oxidation and the hydrolysis having been carried out either (a) by humidification in a chamber at ambient or elevated temperature until the humidity of the chamber reaches at least 85% and the humidity is maintained for at least 12 hours or (b) by mixing the carrier base material with water and heating to a temperature of 30°-100° C. for at least 12 hours.
Claim 2
Dependent Claim
219 words
A shaped and compressed sustained release therapeutic composition comprising a therapeutically active medicament and a carrier base material, characterized by a long-lasting slow and regular incremental release of the medicament upon administration, wherein the carrier base material is hydroxypropylmethylcellulose or a mixture of hydroxypropylmethylcellulose and either up to 30% ethylcellulose or 30% sodium carboxymethylcellulose or both, and wherein the hydroxypropylmethylcellulose or the mixtures thereof have been subjected to hydrolysis and oxidation and have a carbonyl content which ranges from 0.2 to 3.0 grams/100 grams and a carboxyl content which ranges from 0.37 to 2.6 grams/100 grams, the oxidation having been carried out at about 30° to 50° C. in the presence of oxygen or a stream of air for a period of time sufficient to obtain the desired carbonyl and carboxyl values and the composition having incorporated therein 0.1-1.0%, based on the weight of the carrier material, of a reducing stabilizing agent which prevents undesired further oxidation and the hydrolysis having been carried out either (a) by humidification in a chamber at ambient or elevated temperature until the humidity of the chamber reaches at least 85% and the humidity is maintained for at least 12 hours or (b) by mixing the carrier base material with water and heating to a temperature of 30°-100° C. for at least 12 hours.
Claim 3
Dependent Claim
18 words
A composition according to claim 1 wherein the carbonyl content is in the range of 0.2-3.0 grams/100 grams.
Claim 4
Dependent Claim
18 words
A composition according to claim 1 wherein the carboxyl content is in the range of 0.37-2.6 grams/100 grams.
Claim 5
Dependent Claim
30 words
A composition according to claim 1 wherein the carbonyl content is in the range of 0.2-2.0 grams/100 grams and the carboxyl content is in the range of 0.37-2.6 grams/100 grams.
Claim 6
Dependent Claim
22 words
A composition according to claim 1 wherein the subjection of the carrier base material to hydrolysis and oxidation is successive or concurrent.
Claim 7
Dependent Claim
36 words
A composition according to claim 4 wherein hydrolysis and oxidation are carried out concurrently by the treatment of the carrier base material with air or oxygen containing a sufficient amount of water at an elevated temperature.
Claim 8
Dependent Claim
15 words
A composition according to claim 1 wherein the shaped composition is in unit dosage form.
Claim 9
Dependent Claim
13 words
A composition according to claim 1 wherein the carrier base material is hydroxypropylmethylcellulose.
Claim 10
Dependent Claim
19 words
A composition according to claim 1 in which the stabilizing agent is ascorbyl stearate or palmitate or sodium metabisulfite.
References Cited (Backward Citations)
US2726982A
Cited
US3034964A
Cited
US2949401A
Cited
US2980589A
Cited
US3065143A
Cited
US3251824A
Cited
US3424842A
Cited
GB1171691A
Cited
US3870790A
Cited
US3852421A
Cited
US3950508A
Cited
US3965256A
Cited
CA1018456A
Cited
US4136145A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-10-07 | 1984-04-07 | 1984-10-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-10-07 | 1988-04-07 | 1988-10-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-10-07 | 1992-04-07 | 1992-10-07 | $7700.00 | Window Closed / Lapsed |