US4962091A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Controlled release of macromolecular polypeptides
Assignee: Syntex USA LLC
•
Filing: 1986-05-23
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Granted: 1990-10-09
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Expires: 2006-05-23
Abstract
Abstract An active agent delivery system for the controlled administration of macromolecular polypeptides which comprises a micro-suspension of water-soluble components in a polylactide matrix.
Inventors
- 👤 Deborah A. Eppstein
- 👤 Brian B. Schryver
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 17:02
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/70; A61K9/7007; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1641; A61K9/1647; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2031; A61K9/204
Claims Analysis
Total Claims: 43
Claim 1
Independent Claim
106 words
A composition for the controlled administration of a biologically active macromolecular polypeptide comprising (a) a polylactide matrix in which is incorporated a micro-suspension of not more than about 30 percent by weight based on weight of the system of (b) particles of at least one biologically active macromolecular polypeptide having a molecular weight not less than about 1000 daltons, wherein substantially all of the particles of polypeptide have a diameter of 10μ or less and are uniformly and discreetly dispersed throughout the matrix, and wherein the polypeptide retains at least about 50 percent of the biological activity which it possessed prior to manufacture of the composition.
Claim 2
Dependent Claim
106 words
A composition for the controlled administration of a biologically active macromolecular polypeptide comprising (a) a polylactide matrix in which is incorporated a micro-suspension of not more than about 30 percent by weight based on weight of the system of (b) particles of at least one biologically active macromolecular polypeptide having a molecular weight not less than about 1000 daltons, wherein substantially all of the particles of polypeptide have a diameter of 10μ or less and are uniformly and discreetly dispersed throughout the matrix, and wherein the polypeptide retains at least about 50 percent of the biological activity which it possessed prior to manufacture of the composition.
Claim 3
Dependent Claim
25 words
The system of claim 1 in which the polypeptide and other water soluble components comprise about 20 percent by weight, or less, of the matrix.
Claim 4
Dependent Claim
17 words
The system of claim 1 in which the polypeptide has a molecular weight greater than about 2,500.
Claim 5
Dependent Claim
17 words
The system of claim 3 in which the polypeptide has a molecular weight greater than about 6,000.
Claim 6
Dependent Claim
17 words
The system of claim 4 in which the polypeptide has a molecular weight greater than about 10,000.
Claim 7
Dependent Claim
21 words
The system of claim 5 in which the polypeptide is selected from the group consisting of cytokines, lymphokines, monokines and interferons.
Claim 8
Dependent Claim
15 words
The system of claim 6 in which the polypeptide is interleukin-2 or an analog thereof.
Claim 9
Dependent Claim
12 words
The system of claim 6 in which the polypeptide is an interferon.
Claim 10
Dependent Claim
14 words
The system of claim 8 which includes a pharmaceutically acceptable stabilizer for the interferon.
Claim 11
Dependent Claim
13 words
The system of claim 9 in which the interferon is a beta interferon.
Claim 12
Dependent Claim
25 words
The system of claim 10 in which the beta interferon and other water-soluble components comprise about 20 percent by weight, or less, of the matrix.
Claim 13
Dependent Claim
25 words
The system of claim 11 in which the beta interferon and other water-soluble components comprise about 10 percent by weight, or less, of the matrix.
Claim 14
Dependent Claim
25 words
The system of claim 12 in which the beta interferon and other water-soluble components comprise about 5 percent by weight, or less, of the matrix.
Claim 15
Dependent Claim
19 words
The system of claim 13 in which the stabilizer comprises either or both of human serum albumin and dextrose.
Claim 16
Dependent Claim
28 words
The system of claim 1 in which the polylactide is a poly(lactide-co-glycolide) copolymer having a molar ratio of lactide to glycolide units of between about 100:0 and 30:70.
Claim 17
Dependent Claim
23 words
The system of claim 15 in which the copolymer has a molar ratio of lactide to glycolide units of between 75:25 and 40:60.
Claim 18
Dependent Claim
21 words
The system of claim 16 in which the copolymer has a molar ratio of lactide to glycolide units of about 50:50.
Claim 19
Dependent Claim
36 words
The system of claim 17 in which the polypeptide is a recombinant human beta interferon, and in which the beta interferon and other water soluble components comprise 10 percent by weight, or less, of the matrix.
Claim 20
Dependent Claim
25 words
The system of claim 18 in which the beta interferon and other water soluble components comprise 5 percent by weight, or less, of the matrix.
Claim 21
Dependent Claim
17 words
The system of claim 1 which is formed from one or more layers of a spray-cast film.
Claim 22
Dependent Claim
12 words
The system of claim 20 which incorporates a biocompatible inert reinforcement material.
Claim 23
Dependent Claim
16 words
The system of claim 1 which contains more than one species of biologically active macromolecular polypeptide.
Claim 24
Dependent Claim
12 words
The system of claim 1 in which the polypeptide is a hormone.
Claim 25
Dependent Claim
15 words
The system of claim 23 in which the hormone is calcitonin or an analog thereof.
Claim 26
Dependent Claim
16 words
The system of claim 23 in which the hormone is parathyroid hormone or an analog thereof.
Claim 27
Dependent Claim
17 words
The system of claim 23 in which the hormone is epidermal growth factor or an analog thereof.
Claim 28
Dependent Claim
12 words
The system of claim 1 in which the polypeptide is an immunomodulator.
Claim 29
Dependent Claim
13 words
The system of claim 27 in which the polypeptide is an immune stimulator.
Claim 30
Dependent Claim
13 words
The system of claim 27 in which the polypeptide is an immune depressant.
Claim 31
Dependent Claim
12 words
The system of claim 1 in which the polypeptide is an enzyme.
Claim 32
Dependent Claim
12 words
The system of claim 30 in which the enzyme is superoxide dismutase.
Claim 33
Dependent Claim
13 words
The system of claim 30 in which the enzyme is a plasminogen activator.
Claim 34
Dependent Claim
13 words
The system of claim 32 in which the enzyme is tissue plasminogen activator.
Claim 35
Dependent Claim
17 words
The system of claim 1 in which the polypeptide is a growth promotant or growth inhibitory factor.
Claim 36
Dependent Claim
13 words
The system of claim 34 in which the polypeptide is transforming growth factor-β.
Claim 37
Dependent Claim
18 words
The system of claim 34 in which the polypeptide is a growth hormone or growth hormone releasing factor.
Claim 38
Dependent Claim
13 words
The system of claim 36 in which the polypeptide is bovine growth hormone.
Claim 39
Dependent Claim
14 words
The system of claim 1 in which the polypeptide is a blood coagulation factor.
Claim 40
Dependent Claim
13 words
The system of claim 1 in which the polypeptide is a vaccine antigen.
Claim 41
Dependent Claim
12 words
The system of claim 1 in which the polypeptide is an antibody.
Claim 42
Dependent Claim
13 words
The system of claim 1 in which the polypeptide is a protease inhibitor.
Claim 43
Dependent Claim
64 words
A composition according to claim 1 further comprising one or more other water soluble, pharmaceutically acceptable components, particles of which have a diameter of about 10μ or less, selected from the group consisting of other active agents, proteins, other polypeptides, stabilizers, carbohydrates, surfactants and plasticizers, wherein the macromolecular agent and other water soluble components together comprise about 30 percent by weight of the system.
References Cited (Backward Citations)
US4419340A
Cited
US3773919A
Cited
US3976071A
Cited
US4225581A
Cited
US4293539A
Cited
US4512972A
Cited
EP0052510B1
Cited
EP0058481A1
Cited
US4613500A
Cited
US4637931A
Cited
US4678809A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1993-10-08 | 1994-04-09 | 1994-10-09 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-10-08 | 1998-04-09 | 1998-10-09 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-10-08 | 2002-04-09 | 2002-10-09 | $7700.00 | Window Closed / Lapsed |