US4298595A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Pharmaceutical preparations containing a polymeric agent for releasing 5-aminosalicylic acid or its salts into the gastrointestinal tract
Assignee: Dynapol Shareholders Liquidating Trust
•
Filing: 1979-11-29
•
Granted: 1981-11-03
•
Expires: 1999-11-29
Abstract
Abstract An intestinal anti-inflammatory preparation comprising a polymeric agent for releasing 5-aminosalicylic acid or its salts is disclosed. The polymeric agent comprises a nonabsorbable pharmacologically acceptable organic polymer backbone containing aromatic rings to which are covalently bonded via azo bonds a plurality of salicylic acid or salicylate salt groups. The azo bonds attach to the salicylates' 5-position carbon. The polymer's azo bonds undergo bacterial cleavage in the mammalian lower bowel to release 5-aminosalicylic acid and/or its salts.
Inventors
- 👤 Thomas M. Parkinson
- 👤 Joseph P. Brown
- 👤 Robert E. Wingard, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 05:07
CPC Classifications
C; C08; C08G; C08G85/00; C08G85/004; A; A61; A61K; A61K31/00; A61K31/74; A61K31/785; A61K31/795; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58; A61K47/59; A61K47/60; C08F; C08F8/00; C08F8/30; C08F8/34; C08G65/00; C08G65/02; C08G65/32; C08G65/329; C08G65/334; C08G65/34; C08G65/48
Claims Analysis
Total Claims: 50
Claim 1
Independent Claim
101 words
A pharmaceutical formulation for the treatment of the mucosa of the mammalian lower intestinal tract comprising an amount therapeutically effective for such treatment of a polymeric compound which itself comprises a pharmacologically acceptable organic polymer backbone comprising a plurality of aromatic rings and having a molecular size which precludes the backbone's absorption from the intestinal lumen and a plurality of salicyclic acid or pharmaceutically acceptable salicylate salt groups covalently bonded to said backbone via azo groups that are intermediate backbone aromatic carbons and said salicyclic acid or pharmaceutically acceptable salicylate salt 5-position carbons in association with a pharmaceutically acceptable carrier therefor.
Claim 2
Dependent Claim
101 words
A pharmaceutical formulation for the treatment of the mucosa of the mammalian lower intestinal tract comprising an amount therapeutically effective for such treatment of a polymeric compound which itself comprises a pharmacologically acceptable organic polymer backbone comprising a plurality of aromatic rings and having a molecular size which precludes the backbone's absorption from the intestinal lumen and a plurality of salicyclic acid or pharmaceutically acceptable salicylate salt groups covalently bonded to said backbone via azo groups that are intermediate backbone aromatic carbons and said salicyclic acid or pharmaceutically acceptable salicylate salt 5-position carbons in association with a pharmaceutically acceptable carrier therefor.
Claim 3
Dependent Claim
24 words
The formulation of claim 1 wherein in said polymeric compound said backbone has an average molecular weight which is not less than 1000 daltons.
Claim 4
Dependent Claim
33 words
The formulation of claim 2 wherein in said polymeric compound said plurality of aromatic rings is 10 or greater and said plurality of salicylic acid or salicylate salt groups is 5 or greater.
Claim 5
Dependent Claim
27 words
The formulation of claim 3 wherein in said polymeric compound said aromatic rings are pendant from an organic chain which links them together into the polymer backbone.
Claim 6
Dependent Claim
24 words
The formulation of claim 3 wherein in said polymeric compound said aromatic rings are present as integral structural units in the organic backbone chain.
Claim 7
Dependent Claim
25 words
The formulation of claim 3 wherein said polymeric compound has recurring units of the structure ##STR43## wherein M is hydrogen or a pharmaceutically acceptable cation.
Claim 8
Dependent Claim
19 words
The formulation of claim 6 wherein in said polymeric compound M is selected from among hydrogen, potassium and sodium.
Claim 9
Dependent Claim
13 words
The formulation of claim 7 wherein in said polymer compound M is potassium.
Claim 10
Dependent Claim
13 words
The formulation of claim 7 wherein in said polymeric compound M is sodium.
Claim 11
Dependent Claim
34 words
The formulation of claim 3 wherein in said polymeric compound said backbone is poly(vinylamine) and said compound comprises recurring structural units of the formula ##STR44## wherein M is hydrogen or a pharmaceutically acceptable cation.
Claim 12
Dependent Claim
34 words
The formulation of claim 3 wherein said polymeric compound has recurring units of the structure ##STR45## wherein X is an amine group present in poly(ethyleneimine) and M is hydrogen or a pharmaceutically acceptable cation.
Claim 13
Dependent Claim
19 words
The formulation of claim 11 wherein in said polymeric compound M is selected from among hydrogen, sodium and potassium.
Claim 14
Dependent Claim
48 words
A pharmaceutical formulation for the treatment of the mucosa of the mammalian lower intestinal tract comprising an amount therapeutically effective for such treatment of a polymeric compound itself consisting essentially of from about 250 to about 1500 repeating ##STR46## units in association with a pharmaceutically acceptable carrier therefor.
Claim 15
Dependent Claim
48 words
A pharmaceutical formulation for the treatment of the mucosa of the mammalian lower intestinal tract comprising an amount therapeutically effective for such treatment of a polymeric compound itself consisting essentially of from about 250 to about 1500 repeating ##STR46## units in association with a pharmaceutically acceptable carrier therefor.
Claim 16
Dependent Claim
48 words
A pharmaceutical formulation for the treatment of the mucosa of the mammalian lower intestinal tract comprising an amount therapeutically effective for such treatment of a polymeric compound itself consisting esstentially of from about 250 to about 1500 repeating ##STR47## units in association with a pharmaceutically acceptable carrier therefor.
Claim 17
Dependent Claim
48 words
A pharmaceutical formulation for the treatment of the mucosa of the mammalian lower intestinal tract comprising an amount therapeutically effective for such treatment of a polymeric compound itself consisting esstentially of from about 250 to about 1500 repeating ##STR47## units in association with a pharmaceutically acceptable carrier therefor.
Claim 18
Dependent Claim
44 words
A pharmaceutical formulation for the treatment of the mucosa of the mammalian lower intestinal tract comprising an amount therapeutically effective for such treatment of a polymer compount itself consisting essentially of about 1100 repeating ##STR48## units in association with a pharmaceutically acceptable carrier therefor.
Claim 19
Dependent Claim
44 words
A pharmaceutical formulation for the treatment of the mucosa of the mammalian lower intestinal tract comprising an amount therapeutically effective for such treatment of a polymer compount itself consisting essentially of about 1100 repeating ##STR48## units in association with a pharmaceutically acceptable carrier therefor.
Claim 20
Dependent Claim
44 words
A pharmaceutical formulation for the treatment of the mucosa of the mammalian lower intestinal tract comprising an amount therapeutically effective for such treatment of a polymeric component itself consisting essentially of about 1100 repeating ##STR49## units in association with a pharmaceutically acceptable carrier therefor.
Claim 21
Dependent Claim
44 words
A pharmaceutical formulation for the treatment of the mucosa of the mammalian lower intestinal tract comprising an amount therapeutically effective for such treatment of a polymeric component itself consisting essentially of about 1100 repeating ##STR49## units in association with a pharmaceutically acceptable carrier therefor.
Claim 22
Dependent Claim
105 words
A pharmaceutical anti-inflammatory formulation comprising a polymeric compound which itself comprises a pharmacologically acceptable organic polymer backbone comprising a plurality of aromatic rings and having a molecular size which precludes the backbone's absorption from the intestinal lumen and a plurality of salicylic acid or pharmaceutically acceptable salicylate salt groups covalently bonded to said backbone via azo groups that are intermediate backbone aromatic carbons and said salicylic acid or pharmaceutically acceptable salicylate salt 4-position carbons in association with a pharmaceutically acceptable carrier therefor, said polymeric compound being present in an amount effective to release a nontoxic therapeutic anti-inflammatory amount of said salicylic acid or salicylate salts.
Claim 23
Dependent Claim
105 words
A pharmaceutical anti-inflammatory formulation comprising a polymeric compound which itself comprises a pharmacologically acceptable organic polymer backbone comprising a plurality of aromatic rings and having a molecular size which precludes the backbone's absorption from the intestinal lumen and a plurality of salicylic acid or pharmaceutically acceptable salicylate salt groups covalently bonded to said backbone via azo groups that are intermediate backbone aromatic carbons and said salicylic acid or pharmaceutically acceptable salicylate salt 4-position carbons in association with a pharmaceutically acceptable carrier therefor, said polymeric compound being present in an amount effective to release a nontoxic therapeutic anti-inflammatory amount of said salicylic acid or salicylate salts.
Claim 24
Dependent Claim
27 words
The anti-inflammatory formulation of claim 17 wherein said polymeric compound has recurring units of the structure ##STR50## wherein M is selected from among hydrogen, potassium and sodium.
Claim 25
Dependent Claim
45 words
A pharmaceutical anti-inflammatory formulation comprising an effective nontoxic inflammation-treating amount of a polymeric compound itself consisting essentially of from about 250 to about 1500 repeating ##STR51## units wherein M is selected from among sodium, potassium and hydrogen in association with a pharmaceutically acceptable carrier therefor.
Claim 26
Dependent Claim
45 words
A pharmaceutical anti-inflammatory formulation comprising an effective nontoxic inflammation-treating amount of a polymeric compound itself consisting essentially of from about 250 to about 1500 repeating ##STR51## units wherein M is selected from among sodium, potassium and hydrogen in association with a pharmaceutically acceptable carrier therefor.
Claim 27
Dependent Claim
109 words
A pharmaceutical formulation for the treatment of ulcerative colitis comprising a polymeric compound which itself comprises a pharmacologically acceptable organic polymer backbone comprising a plurality of aromatic rings and having a molecular size which precludes the backbone's absorption from the intestinal lumen and a plurality of salicylic acid or pharmaceutically acceptable salicylate salt groups covalently bonded to said backbone via azo groups that are intermediate backbone aromatic carbons and said salicylic acid or pharmaceutically acceptable salicylate salt 5-position carbons in association with a pharmaceutically acceptable carrier therefor, said polymeric compound being present in an amount effective to release an ulcerative colitis-treating amount of said salicylic acid or salicylate salt.
Claim 28
Dependent Claim
109 words
A pharmaceutical formulation for the treatment of ulcerative colitis comprising a polymeric compound which itself comprises a pharmacologically acceptable organic polymer backbone comprising a plurality of aromatic rings and having a molecular size which precludes the backbone's absorption from the intestinal lumen and a plurality of salicylic acid or pharmaceutically acceptable salicylate salt groups covalently bonded to said backbone via azo groups that are intermediate backbone aromatic carbons and said salicylic acid or pharmaceutically acceptable salicylate salt 5-position carbons in association with a pharmaceutically acceptable carrier therefor, said polymeric compound being present in an amount effective to release an ulcerative colitis-treating amount of said salicylic acid or salicylate salt.
Claim 29
Dependent Claim
33 words
The pharmaceutical formulation for the treament of ulcerative colitis of claim 20 wherein said polymeric compound has recurring units of the structure ##STR52## wherein M is selected from among hydrogen, potassium and sodium
Claim 30
Dependent Claim
35 words
A pharmaceutical ulcerative-colitis-treating formulation comprising an effective nontoxic ulcerative-colitis-treating amount of a polymeric compound itself consisting essentially of from about 250 to about 1500 repeating ##STR53## units in association with a pharmaceutically acceptable carrier therefor.
Claim 31
Dependent Claim
35 words
A pharmaceutical ulcerative-colitis-treating formulation comprising an effective nontoxic ulcerative-colitis-treating amount of a polymeric compound itself consisting essentially of from about 250 to about 1500 repeating ##STR53## units in association with a pharmaceutically acceptable carrier therefor.
Claim 32
Dependent Claim
35 words
A pharmaceutical ulcerative-colitis-treating formulation comprising an effective nontoxic ulcerative-colitis-treating amount of a polymeric compound itself consisting essentially of from about 250 to about 1500 repeating ##STR54## units in association with a pharmaceutically acceptable carrier therefor.
Claim 33
Dependent Claim
35 words
A pharmaceutical ulcerative-colitis-treating formulation comprising an effective nontoxic ulcerative-colitis-treating amount of a polymeric compound itself consisting essentially of from about 250 to about 1500 repeating ##STR54## units in association with a pharmaceutically acceptable carrier therefor.
Claim 34
Dependent Claim
16 words
The formulation of claim 1 suited for administration by a route selected from oral and rectal.
Claim 35
Dependent Claim
16 words
The formulation of claim 7 suited for administration by a route selected from oral and rectal.
Claim 36
Dependent Claim
16 words
The formulation of claim 16 suited for administration by a route selected from oral and rectal.
Claim 37
Dependent Claim
16 words
The formulation of claim 19 suited for administration by a route selected from oral and rectal.
Claim 38
Dependent Claim
16 words
The formulation of claim 23 suited for administration by a route selected from oral and rectal.
Claim 39
Dependent Claim
20 words
The formulation of claim 1 in unit dosage form suited for administration by a route selected from oral and rectal.
Claim 40
Dependent Claim
16 words
The formulation of claim 29 in unit dosage form selected from suppositories, pills, tablets, and capsules.
Claim 41
Dependent Claim
20 words
The formulation of claim 14 in unit dosage form suited for administration by a route selected from oral and rectal.
Claim 42
Dependent Claim
20 words
The formulation of claim 19 in unit dosage form suited for administration by a route selected from oral and rectal.
Claim 43
Dependent Claim
13 words
The formulation of claim 23 in unit dosage form suited for oral administration.
Claim 44
Dependent Claim
13 words
The formulation of claim 23 in unit dosage form suited for rectal administration.
Claim 45
Independent Claim
52 words
A method for the treatment of ulcerative colitis in a mammal which comprises the oral administration to the mammal of an effective nontoxic ulcerative-colitis-treatment amount of a pharmaceutical preparation containing a polymeric compound itself consisting essentially of from about 250 to about 1500 repeating ##STR55## units and a pharmaceutically acceptable carrier therefor.
Claim 46
Independent Claim
52 words
A method for the treatment of ulcerative colitis in a mammal which comprises the oral administration to the mammal of an effective nontoxic ulcerative-colitis-treatment amount of a pharmaceutical preparation containing a polymeric compound itself consisting essentially of from about 250 to about 1500 repeating ##STR55## units and a pharmaceutically acceptable carrier therefor.
Claim 47
Independent Claim
51 words
A method for the treatment of ulcerative colitis in a mammal which comprises the rectal administration to the mammal of a nontoxic ulcerative-colitis-treating amount of a pharmaceutical preparation containing a polymeric compound itself consisting essentially of from about 250 to about 1500 repeating ##STR56## units and a pharamaceutically acceptable carrier therefor.
Claim 48
Independent Claim
51 words
A method for the treatment of ulcerative colitis in a mammal which comprises the rectal administration to the mammal of a nontoxic ulcerative-colitis-treating amount of a pharmaceutical preparation containing a polymeric compound itself consisting essentially of from about 250 to about 1500 repeating ##STR56## units and a pharamaceutically acceptable carrier therefor.
Claim 49
Dependent Claim
37 words
A method for delivering to a mammal a therapeutically effective amount of 5-aminosalicylic acid or its pharmacologically acceptable salts which comprises orally or rectally administering to said mammal an effective amount of the formulation of claim 1.
Claim 50
Dependent Claim
38 words
A method for delivering to a mammal a therapeutically effective ulcerative-colitis-treating amount of 5-aminosalicylic acid or its pharmaceutically acceptable salts which comprises orally or rectally administering to said mammal an effective amount of the formulation of claim 23.
References Cited (Backward Citations)
US3862312A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-11-02 | 1985-05-04 | 1985-11-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-11-02 | 1989-05-04 | 1989-11-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-11-02 | 1993-05-04 | 1993-11-03 | $7700.00 | Window Closed / Lapsed |