US4774074A
Expired / Lapsed
US
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Erodible matrix for sustained release bioactive composition
Assignee: Actavis Laboratories UT Inc
•
Filing: 1986-10-14
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Granted: 1988-09-27
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Expires: 2006-10-14
Abstract
Abstract A sustained release composition for releasing a biologically active compound into an aqueous liquid environment comprises said biologically active compound dispersed in a bioerodible matrix, the matrix comprising a mixture of a. 5% to 99.5% by weight of a solid water-dispersible polyether diol having a molecular weight from about 1000 to about 20,000, and b. 95 to 0.5% by weight of an erosion rate modifier which is an amphiphilic compound insoluble in the aqueous liquid. Dosage forms comprising the erodible matrix are prepared by molding, particularly by injection molding.
Inventors
- 👤 Wallace C. Snipes
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 11:25
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2031; A61K9/2013; B; B29; B29K; B29K2105/00; B29K2105/0005; B29K2105/0035; Y; Y10; Y10T; Y10T428/00; Y10T428/29; Y10T428/2913; Y10T428/2933; Y10T428/294; Y10T428/298; Y10T428/2982; Y10T428/2989
Claims Analysis
Total Claims: 88
Claim 1
Independent Claim
66 words
A composition erodible by an aqueous liquid comprising 5 to 99.5 % by weight of a polyethylene glycol having a molecular weight of from about 1000 to about 20,000, and 95 to 0.5 % by weight of an erosion rate modifier which is an amphiphilic compound insoluble in said aqueous liquid, the molecular structure of said amphiphilic compound having a lipophilic portion and a hydrophilic portion.
Claim 2
Dependent Claim
66 words
A composition erodible by an aqueous liquid comprising 5 to 99.5 % by weight of a polyethylene glycol having a molecular weight of from about 1000 to about 20,000, and 95 to 0.5 % by weight of an erosion rate modifier which is an amphiphilic compound insoluble in said aqueous liquid, the molecular structure of said amphiphilic compound having a lipophilic portion and a hydrophilic portion.
Claim 3
Dependent Claim
16 words
The composition of claim 1 wherein said polyethylene glycol has a molecular weight of about 8000.
Claim 4
Dependent Claim
18 words
The composition of claim 1 wherein said erosion rate modifier is a C 12 -C 20 fatty acid.
Claim 5
Dependent Claim
21 words
The composition of claim 3 wherein said fatty acid is selected from the group consisting of myristic acid and stearic acid.
Claim 6
Dependent Claim
22 words
The composition of claim 1 additionally comprising a substance which increases the compatibility of the polyethylene glycol and the erosion rate modifier.
Claim 7
Dependent Claim
41 words
The composition of claim 5 wherein said substance is a polyethylene glycol having a molecular weight from about 200 to about 10000 and having at least one of its terminal OH groups esterified with a C 12 -C 20 fatty acid.
Claim 8
Dependent Claim
13 words
The composition of claim 6 wherein said polyethylene glycol is polyethylene glycol 400.
Claim 9
Dependent Claim
25 words
The composition of claim 7 wherein said substance is polyethylene glycol 400 having at least one of its terminal OH groups esterified with stearic acid.
Claim 10
Dependent Claim
9 words
The composition of claim 1 additionally comprising a disintegrant.
Claim 11
Dependent Claim
10 words
The composition of claim 9 wherein said disintegrant is starch.
Claim 12
Dependent Claim
10 words
The composition of claim 1 additionally comprising a molding adjuvant.
Claim 13
Dependent Claim
20 words
The composition of claim 11 wherein said molding adjuvant is polyethylene oxide having a molecular weight of 100,000 to 5,000,000.
Claim 14
Dependent Claim
95 words
A sustained release composition for releasing a biologically active compound into its surrounding environment comprising said biologically active compound dispersed in a matrix which, when contacted with an aqueous liquid, erodes progressively, said matrix comprising a mixture of 5 to 99.5 % by weight of a polyethylene glycol having a molecular weight of from about 1000 to about 20,000, and 95to 0.5 % by weight of an erosion rate modifier which is an amphiphilic compound insoluble in said aqueous liquid, the molecular structure of said amphiphilic compound having a lipophilic portion and a hydrophilic portion.
Claim 15
Dependent Claim
95 words
A sustained release composition for releasing a biologically active compound into its surrounding environment comprising said biologically active compound dispersed in a matrix which, when contacted with an aqueous liquid, erodes progressively, said matrix comprising a mixture of 5 to 99.5 % by weight of a polyethylene glycol having a molecular weight of from about 1000 to about 20,000, and 95to 0.5 % by weight of an erosion rate modifier which is an amphiphilic compound insoluble in said aqueous liquid, the molecular structure of said amphiphilic compound having a lipophilic portion and a hydrophilic portion.
Claim 16
Dependent Claim
16 words
The composition of claim 13 wherein said polyethylene glycol has a molecular weight of about 8000.
Claim 17
Dependent Claim
18 words
The composition of claim 13 wherein said erosion rate modifier is a C 12 -C 20 fatty acid.
Claim 18
Dependent Claim
21 words
The composition of claim 15 wherein said fatty acid is selected from the group consisting of myristic acid and stearic acid.
Claim 19
Dependent Claim
22 words
The composition of claim 13 additionally comprising a substance which increases the compatibility of the polyethylene glycol and the erosion rate modifier.
Claim 20
Dependent Claim
41 words
The composition of claim 17 wherein said substance is a polyethylene glycol having a molecular weight from about 200 to about 10000 and having at least one of its terminal OH groups esterified with a C 12 -C 20 fatty acid.
Claim 21
Dependent Claim
13 words
The composition of claim 18 wherein said polyethylene glycol is polyethylene glycol 400.
Claim 22
Dependent Claim
25 words
The composition of claim 19 wherein said substance is polyethylene glycol 400 having at least one of its terminal OH groups esterified with stearic acid.
Claim 23
Dependent Claim
9 words
The composition of claim 13 additionally comprising a disintegrant.
Claim 24
Dependent Claim
10 words
The composition of claim 21 wherein said disintegrant is starch.
Claim 25
Dependent Claim
10 words
The composition of claim 13 additionally comprising a molding adjuvant.
Claim 26
Dependent Claim
20 words
The composition of claim 23 wherein said molding adjuvant is polyethylene oxide having a molecular weight of 100,000 to 5,000,000.
Claim 27
Dependent Claim
105 words
A sustained release composition for releasing a biologically active compound into its surrounding environment comprising a pharmaceutically active compound or non-toxic pharmaceutically acceptable salt of said pharmaceutically active compound dispersed in a matrix which, when contacted with an aqueous liquid, erodes progressively, said matrix comprising a mixture of 5to 99.5 % by weight of a polyethylene glycol having a molecular weight of from about 1000 to about 20,000, and 95 to 0.5 % by weight of an erosion rate modifier which is an amphiphilic compound insoluble in said aqueous liquid, the molecular structure of said amphiphilic compound having a lipophilic portion and a hydrophilic portion.
Claim 28
Dependent Claim
105 words
A sustained release composition for releasing a biologically active compound into its surrounding environment comprising a pharmaceutically active compound or non-toxic pharmaceutically acceptable salt of said pharmaceutically active compound dispersed in a matrix which, when contacted with an aqueous liquid, erodes progressively, said matrix comprising a mixture of 5to 99.5 % by weight of a polyethylene glycol having a molecular weight of from about 1000 to about 20,000, and 95 to 0.5 % by weight of an erosion rate modifier which is an amphiphilic compound insoluble in said aqueous liquid, the molecular structure of said amphiphilic compound having a lipophilic portion and a hydrophilic portion.
Claim 29
Dependent Claim
10 words
The composition of claim 25 wherein said compound is clonidine.
Claim 30
Dependent Claim
10 words
The composition of claim 25 wherein said compound is dipyridamole.
Claim 31
Dependent Claim
10 words
The composition of claim 25 wherein said compound is hydrochlorothiazide.
Claim 32
Dependent Claim
10 words
The composition of claim 25 wherein said compound is furosemide.
Claim 33
Dependent Claim
10 words
The composition of claim 25 wherein said compound is indomethacin.
Claim 34
Dependent Claim
10 words
The composition of claim 25 wherein said compound is scopolamine.
Claim 35
Dependent Claim
11 words
The composition of claim 25 wherein said compound is a bronchodilator.
Claim 36
Dependent Claim
10 words
The composition of claim 32 wherein said bronchodilator is theophylline.
Claim 37
Dependent Claim
10 words
The composition of claim 25 wherein said compound is quinidine.
Claim 38
Dependent Claim
10 words
The composition of claim 25 wherein said compound is naproxen.
Claim 39
Dependent Claim
10 words
The composition of claim 25 wherein said compound is propranolol.
Claim 40
Dependent Claim
11 words
The composition of claim 25 wherein said compound is a salicylate.
Claim 41
Dependent Claim
10 words
The composition of claim 37 wherein said salicylate is aspirin.
Claim 42
Dependent Claim
10 words
The composition of claim 25 wherein said compound is nitroglycerin.
Claim 43
Dependent Claim
11 words
The composition of claim 25 wherein said compound is isosorbide dinitrate.
Claim 44
Dependent Claim
95 words
A sustained release composition for releasing an ecologically active compound into its surrounding environment comprising said ecologically active compound dispersed in a matrix which, when contacted with an aqueous liquid, erodes progressively, said matrix comprising a mixture of 5to 99.5 % by weight of a polyethylene glycol having a molecular weight of from about 1000 to about 20,000, and 95 to 0.5 % by weight of an erosion rate modifier which is an amphiphilic compound insoluble in said aqueous liquid, the molecular structure of said amphiphilic compound having a lipophilic portion and a hydrophilic portion.
Claim 45
Dependent Claim
95 words
A sustained release composition for releasing an ecologically active compound into its surrounding environment comprising said ecologically active compound dispersed in a matrix which, when contacted with an aqueous liquid, erodes progressively, said matrix comprising a mixture of 5to 99.5 % by weight of a polyethylene glycol having a molecular weight of from about 1000 to about 20,000, and 95 to 0.5 % by weight of an erosion rate modifier which is an amphiphilic compound insoluble in said aqueous liquid, the molecular structure of said amphiphilic compound having a lipophilic portion and a hydrophilic portion.
Claim 46
Dependent Claim
13 words
The composition of claim 41 wherein said ecologically active compound is a fertilizer.
Claim 47
Dependent Claim
13 words
The composition of claim 41 wherein said ecologically active compound is a pesticide.
Claim 48
Dependent Claim
13 words
The composition of claim 41 wherein said ecologically active compound is an insecticide.
Claim 49
Dependent Claim
13 words
The composition of claim 41 wherein said ecologically active compound is an herbicide.
Claim 50
Dependent Claim
92 words
A sustained release dosage form for releasing a biologically active compound into an aqueous liquid environment comprising a non-porous solid erodible matrix having dispersed therein a biologically active compound, said matrix comprising a mixture of 5 to 99.5 % by weight of a polyethylene glycol having a molecular weight of from about 1000 to about 20,000, and 95to 0.5 % by weight of an erosion rate modifier which is an amphiphilic compound insoluble in said aqueous liquid, the molecular structure of said amphiphilic compound having a lipophilic portion and a hydrophilic portion.
Claim 51
Dependent Claim
92 words
A sustained release dosage form for releasing a biologically active compound into an aqueous liquid environment comprising a non-porous solid erodible matrix having dispersed therein a biologically active compound, said matrix comprising a mixture of 5 to 99.5 % by weight of a polyethylene glycol having a molecular weight of from about 1000 to about 20,000, and 95to 0.5 % by weight of an erosion rate modifier which is an amphiphilic compound insoluble in said aqueous liquid, the molecular structure of said amphiphilic compound having a lipophilic portion and a hydrophilic portion.
Claim 52
Dependent Claim
17 words
The dosage form of claim 46 wherein said polyethylene glycol has a molecular weight of about 8000.
Claim 53
Dependent Claim
19 words
The dosage form of claim 46 wherein said erosion rate modifier is a C 12 -C 20 fatty acid.
Claim 54
Dependent Claim
22 words
The dosage form of claim 48 wherein said fatty acid is selected from the group consisting of myristic acid and stearic acid.
Claim 55
Dependent Claim
23 words
The dosage form of claim 46 additionally comprising a substance which increases the compatibility of the polyethylene glycol and the erosion rate modifier.
Claim 56
Dependent Claim
42 words
The dosage form of claim 50 wherein said substance is a polyethylene glycol having a molecular weight from about 200 to about 10000 and having at least one of its terminal OH groups esterified with a C 12 -C 20 fatty acid.
Claim 57
Dependent Claim
14 words
The dosage form of claim 51 wherein said polyethylene glycol is polyethylene glycol 400.
Claim 58
Dependent Claim
26 words
The dosage form of claim 52 wherein said substance is polyethylene glycol 400 having at least one of its terminal OH groups esterified with stearic acid.
Claim 59
Dependent Claim
10 words
The dosage form of claim 46 additionally comprising a disintegrant.
Claim 60
Dependent Claim
11 words
The dosage form of claim 54 wherein said disintegrant is starch.
Claim 61
Dependent Claim
11 words
The dosage form of claim 46 additionally comprising a molding adjuvant.
Claim 62
Dependent Claim
21 words
The dosage form of claim 56 wherein said molding adjuvant is polyethylene oxide having a molecular weight of 100,000 to 5,000,000.
Claim 63
Dependent Claim
38 words
The dosage form of claim 46 wherein said biologically active compound is a pharmaceutically active compound or non-toxic pharmaceutically acceptable salt of said compound and said dosage form contains an effective amount of said compound or said salt.
Claim 64
Dependent Claim
11 words
The dosage form of claim 58 wherein said compound is clonidine.
Claim 65
Dependent Claim
11 words
The dosage form of claim 58 wherein said compound is dipyridamole.
Claim 66
Dependent Claim
11 words
The dosage form of claim 58 wherein said compound is hydrochlorothiazide.
Claim 67
Dependent Claim
11 words
The dosage form of claim 58 wherein said compound is furosemide.
Claim 68
Dependent Claim
11 words
The dosage form of claim 58 wherein said compound is indomethacin.
Claim 69
Dependent Claim
11 words
The dosage form of claim 58 wherein said compound is scopolamine.
Claim 70
Dependent Claim
12 words
The dosage form of claim 58 wherein said compound is a bronchodilator.
Claim 71
Dependent Claim
11 words
The dosage form of claim 65 wherein said bronchodilator is theophylline.
Claim 72
Dependent Claim
11 words
The dosage form of claim 58 wherein said compound is quinidine.
Claim 73
Dependent Claim
11 words
The dosage form of claim 58 wherein said compound is naproxen.
Claim 74
Dependent Claim
11 words
The dosage form of claim 58 wherein said compound is propranolol.
Claim 75
Dependent Claim
12 words
The dosage form of claim 58 wherein said compound is a salicylate.
Claim 76
Dependent Claim
10 words
The composition of claim 70 wherein said salicylate is aspirin.
Claim 77
Dependent Claim
11 words
The dosage form of claim 58 wherein said compound is nitroglycerin.
Claim 78
Dependent Claim
12 words
The dosage form of claim 58 wherein said compound is isosorbide dinitrate.
Claim 79
Dependent Claim
16 words
The dosage form of claim 46 wherein said dosage form has the shape of a cylinder.
Claim 80
Dependent Claim
20 words
The dosage form of claim 74 wherein said cylinder has a diameter from about 3 mm to about 8 mm.
Claim 81
Dependent Claim
16 words
The dosage form of claim 75 wherein said cylinder has a diameter of about 6 mm.
Claim 82
Dependent Claim
20 words
The dosage form of claim 74 wherein said cylinder has a length from about 5 mm to about 20 mm.
Claim 83
Dependent Claim
16 words
The dosage form of claim 77 wherein said cylinder has a length of about 10 mm.
Claim 84
Dependent Claim
19 words
The dosage form of claim 74 additionally comprising at least a partial coating of a liquid impermeable non-self-supporting coating.
Claim 85
Dependent Claim
18 words
The dosage form of claim 79 wherein said coating comprises a solid C 12 -C 20 fatty acid.
Claim 86
Dependent Claim
12 words
The dosage form of claim 80 wherein said coating comprises myristic acid.
Claim 87
Dependent Claim
12 words
The dosage form of claim 80 wherein said coating comprises palmitic acid.
Claim 88
Dependent Claim
27 words
The dosage form of claim 79 wherein said dosage form has a cylindrical shape and is coated on its peripheral cylindrical surface with a liquid-impervious non-self-supporting coating.
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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) | 1991-09-27 | 1992-03-28 | 1992-09-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-09-27 | 1996-03-28 | 1996-09-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-09-27 | 2000-03-28 | 2000-09-27 | $7700.00 | Window Closed / Lapsed |