Patent EP0246653A2 successfully refreshed from Google Patents.
EP0246653A2
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EP
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Delayed/sustained release of macromolecules
Assignee: Syntex USA LLC
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Filing: 1987-05-21
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Granted: —
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Expires: 2007-05-21
Abstract
Abstract This invention concerns novel, delayed/sustained release devices including methods of their manufacture and use. The devices comprise macromolecules, particularly polypeptide pharmaceuticals, and an initially partially-hydrated, non-biodegradable, hydrogel rate-limiting membrane.
Inventors
- 👤 Lynda Mary Sanders
- 👤 Abraham Jacob Domb
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-24 21:34
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0087; A61K9/0092; A61K9/0012; A61K9/0048; A61K9/0051
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
91 words
A device for the delayed/sustained release of a compound, said device comprising: (a) a macromolecular compound having a molecular weight greater than about 1,000; (b) a carrier having said macromolecular compound mixed therewith; and (c) an initially partially-hydrated, non-biodegradable, hydrogel rate-limiting membrane, wherein said membrane: (i) comprises a homopolymer or a copolymer material encompassing said carrier and said macromolecular compound, (ii) is substantially non-permeable to said macromolecular compound when in said initially partially-hydrated state, and (iii) is hydratable, when placed in a delivery environment, to become permeable to said macromolecular compound.
Claim 2
Independent Claim
91 words
A device for the delayed/sustained release of a compound, said device comprising: (a) a macromolecular compound having a molecular weight greater than about 1,000; (b) a carrier having said macromolecular compound mixed therewith; and (c) an initially partially-hydrated, non-biodegradable, hydrogel rate-limiting membrane, wherein said membrane: (i) comprises a homopolymer or a copolymer material encompassing said carrier and said macromolecular compound, (ii) is substantially non-permeable to said macromolecular compound when in said initially partially-hydrated state, and (iii) is hydratable, when placed in a delivery environment, to become permeable to said macromolecular compound.
Claim 3
Dependent Claim
21 words
The device of Claim 1 wherein said macromolecular compound is a pharmaceutical compound and said carrier is a pharmaceutically acceptable carrier.
Claim 4
Dependent Claim
48 words
The device of Claim 2 wherein said carrier is selected from the group: (a) aqueous systems; (b) solvents; (c) solid substrates; (d) unpolymerized monomers or comonomers; (e) xerogels; (f) partially hydrated hydrogels; and (g) fully hydrated hydrogels, preferably wherein said carrier is silicone oil or alginic acid gel.
Claim 5
Independent Claim
39 words
The device of any one of Claims 1 to 3 wherein said membrane is selected from the group of crosslinked and non-crosslinked homopolymers or copolymers consisting of: HEMA, GMA, HEMA/GMA, HEMA/MMA, GMA/MMA, and HEMA/GMA/MMA, preferably a crosslinked HEMA homopolymer.
Claim 6
Independent Claim
48 words
The device of any one of Claims 2 to 4 wherein said macromolecular drug is selected from hormonally active polypeptides, mammalian growth hormones, mammalian growth hormone-releasing hormones, and polypeptides having thymosin-like activity, preferably wherein said hormonally active polypeptides comprise luteinizing hormone-releasing hormone analogs or pharmaceutically acceptable salts thereof.
Claim 7
Dependent Claim
35 words
The device of Claim 5 wherein said luteinizing hormone-releasing hormone analog is (pyro)Glu-His-Trp-Ser-Tyr-3-(naphthyl)-D-alanyl-Leu-Arg-Pro-Gly-NH₂ or a pharmaceutically acceptable salt thereof, preferably nafarelin acetate, or is (pyro)Glu-His-Trp-Ser-Tyr-3-(naphthyl)-D-alanyl-Leu-Arg-Pro-aza-Gly-NH₂ or a pharmaceutically acceptable salt thereof, preferably aza-Gly¹⁰ nafarelin acetate.
Claim 8
Independent Claim
14 words
The device of any one of Claims 2 to 6, which is a reservoir.
Claim 9
Independent Claim
45 words
The device of any one of Claims 2 to 6 which is a monolithic device, wherein said carrier serves as said rate-limiting membrane, preferably wherein said carrier comprises a comonomer or a copolymer of HEMA and MMA, and which is useful as an ocular insert.
Claim 10
Independent Claim
81 words
A method for delivering a macromolecular compound, comprising placing into a delivery environment a delayed/sustained release device, said device comprising: (a) a carrier; (b) a macromolecular compound having a molecular weight greater than about 1,000 mixed with said carrier; and (c) an initially partially-hydrated, non-biodegradable, hydrogel rate-limiting membrane, wherein said membrane: (i) comprises a homopolymer or a copolymer material encompassing said carrier and drug, and (ii) has an initial water content such that it is substantially non-permeable to said macromolecular drug.
Claim 11
Independent Claim
81 words
A method for delivering a macromolecular compound, comprising placing into a delivery environment a delayed/sustained release device, said device comprising: (a) a carrier; (b) a macromolecular compound having a molecular weight greater than about 1,000 mixed with said carrier; and (c) an initially partially-hydrated, non-biodegradable, hydrogel rate-limiting membrane, wherein said membrane: (i) comprises a homopolymer or a copolymer material encompassing said carrier and drug, and (ii) has an initial water content such that it is substantially non-permeable to said macromolecular drug.
Claim 12
Dependent Claim
119 words
A process for making a delayed/sustained release device which comprises a carrier, a macromolecular compound having a molecular weight greater than about 1,000 mixed with said carrier, and a non-biodegradable, hydrogel rate-limiting membrane comprising a homopolymer or a copolymer material encompassing said carrier and said compound, which process comprises either (a) partially hydrating said membrane to an initial water content such that it is: (i) structurally manipulable, and (ii) substantially non-permeable to said macromolecular drug, or (b) where said carrier serves as said rate limiting membrane, forming a monolithic device by allowing a mixture of said carrier and said macromolecular compound to cure, after having initially molded, or subsequently cutting or molding into the desired shape suitable for implantation.
Claim 13
Dependent Claim
119 words
A process for making a delayed/sustained release device which comprises a carrier, a macromolecular compound having a molecular weight greater than about 1,000 mixed with said carrier, and a non-biodegradable, hydrogel rate-limiting membrane comprising a homopolymer or a copolymer material encompassing said carrier and said compound, which process comprises either (a) partially hydrating said membrane to an initial water content such that it is: (i) structurally manipulable, and (ii) substantially non-permeable to said macromolecular drug, or (b) where said carrier serves as said rate limiting membrane, forming a monolithic device by allowing a mixture of said carrier and said macromolecular compound to cure, after having initially molded, or subsequently cutting or molding into the desired shape suitable for implantation.
References Cited (Backward Citations)
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