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EP0302582A1
Expired / Lapsed
EP
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Drug delivery system and method of making the same
Assignee: Southern Research Institute
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Filing: 1988-03-31
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Granted: —
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Expires: 2008-03-31
Abstract
Abstract A compatible, biodegradable microcapsule delivery system for active ingredients, including hormonally active peptides, proteins, or other bioactive molecules, and a method of making the same. The ingredients are encapsulated in biodegradable copolymer excipients of varying mole ratios and the blend of the microcapsules are administered to an animal. Delivery of the ingredient occurs over a prolonged period of time at a constant rate as a result of the varying break-down rates of the copolymer excipients.
Inventors
- 👤 Thomas R. Tice
- 👤 Richard M. Gilley
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 22:10
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5084; A61K38/00; A61K38/04; A61K38/08; A61K38/09; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1641; A61K9/1647
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
92 words
A composition capable of delivering an effective amount of constant dose of an active ingredient to an animal over a preselected, prolonged period of time, comprising a blend of effective amounts of an active ingredient encapsulated in at least two biodegradable and biocompatible copolymer excipients to form first and second microcapsules, each excipient capable of a different rate of release of said ingredient therethrough, said composition having a delivery profile wherein the release of said ingredient through said second microcapsule begins as the release of said ingredient through said first microcapsule declines.
Claim 2
Dependent Claim
92 words
A composition capable of delivering an effective amount of constant dose of an active ingredient to an animal over a preselected, prolonged period of time, comprising a blend of effective amounts of an active ingredient encapsulated in at least two biodegradable and biocompatible copolymer excipients to form first and second microcapsules, each excipient capable of a different rate of release of said ingredient therethrough, said composition having a delivery profile wherein the release of said ingredient through said second microcapsule begins as the release of said ingredient through said first microcapsule declines.
Claim 3
Dependent Claim
13 words
A composition as claimed in Claim 1, wherein said copolymer excipients are poly(D,L-lactide-co-glycolide).
Claim 4
Dependent Claim
23 words
A composition as claimed in Claim 2, wherein said copolymer excipients have mole ratios of lactide to glycolide of 40:60 to 100:0, respectively.
Claim 5
Dependent Claim
15 words
A composition as claimed in Claim 1, wherein said active ingredient is a bioactive molecule.
Claim 6
Dependent Claim
14 words
A composition as claimed in Claim 1, wherein said active ingredient is a peptide.
Claim 7
Dependent Claim
13 words
A composition as claimed in Claim 5, wherein said peptide is hormonally active.
Claim 8
Dependent Claim
20 words
A composition as claimed in Claim 5, wherein said peptide is a luteinizing hormone releasing hormone or an analog thereof.
Claim 9
Dependent Claim
16 words
A composition as claimed in Claim 7, wherein said luteinizing hormone releasing hormone is [D-Trp⁶,des-Gly¹⁰]-LHRH ethylamide.
Claim 10
Dependent Claim
14 words
A composition as claimed in Claim 1, wherein said active ingredient is a protein.
Claim 11
Dependent Claim
61 words
A composition as claimed in Claim 1, wherein said blend of microencapsulated peptide is comprised of appropriate amounts of 3% by weight loaded [D-Trp⁶,des-Gly¹⁰]-LHRH ethylamide encapsulated in a copolymer excipient having a mole ratio of 52% lactide to 48% glycolide, and 10% weight loaded [D-Trp⁶,des-Gly¹⁰]-LHRH ethylamide encapsulated in a copolymer excipient having a mole ratio of 68% lactide to 32% glycolide.
Claim 12
Dependent Claim
39 words
A composition as claimed in Claim 10 and further comprising an appropriate amount of 8% by weight loaded [D-Trp⁶,des-Gly¹⁰]-LHRH ethylamide encapsulated in a copolymer excipient having a mole ratio of 85% lactide to 15% glycolide added to said blend.
Claim 13
Dependent Claim
29 words
A composition as claimed in Claim 11, wherein said blend delivers [D-Trp⁶,des-Gly¹⁰]-LHRH ethylamide at a constant rate of about 50 g to 250 g per day for 180 days.
Claim 14
Dependent Claim
19 words
A composition as claimed in Claim 5, wherein said peptide is [D-N-Ac-4-Cl-Phe²,D-Trp⁶,D-Ala¹⁰]-LHRH or an LHRH antagonist of similar structure.
Claim 15
Dependent Claim
33 words
A composition as claimed in Claim 13, wherein said blend delivers [D-N-Ac-4-Cl-Phe²,D-Trp⁶,D-Ala¹⁰]-LHRH or LHRH antagonist of similar structure at a constant rate of about 200 g per day for at least 90 days.
Claim 16
Independent Claim
113 words
A method of preparing a composition for delivering a an effective amount of constant dose of an active ingredient to an animal over a preselected, prolonged period of time, comprising the steps of: (a) encapsulating effective amounts of said ingredient in first and second separate biodegradable and biocompatible copolymer excipients to form first and second microcapsules, each of said microcapsules capable of a different rate of release therefrom of said ingredient; and (b) combining an effective amount of said first and second microcapsules to form said composition having a delivery profile wherein the diffusion of said ingredient through said second microcapsule begins as the release of said ingredient through said first microcapsule declines.
Claim 17
Independent Claim
113 words
A method of preparing a composition for delivering a an effective amount of constant dose of an active ingredient to an animal over a preselected, prolonged period of time, comprising the steps of: (a) encapsulating effective amounts of said ingredient in first and second separate biodegradable and biocompatible copolymer excipients to form first and second microcapsules, each of said microcapsules capable of a different rate of release therefrom of said ingredient; and (b) combining an effective amount of said first and second microcapsules to form said composition having a delivery profile wherein the diffusion of said ingredient through said second microcapsule begins as the release of said ingredient through said first microcapsule declines.
Claim 18
Dependent Claim
18 words
The method as claimed in Claim 15, wherein said first and second copolymer excipients have different monomer ratios.
Claim 19
Dependent Claim
34 words
A method as claimed in Claim 15, wherein said excipient is selected from the group consisting of polyacetal polymers, polyorthoesters, polyesteramides, polycaprolactone and copolymers thereof, polycarbonates, polyhydroxybuterate and copolymers thereof, polymaleamides, copolyaxalates, and polysaccharides.
Claim 20
Dependent Claim
19 words
A method according to Claim 15, wherein the composition is according to any one of Claims 1 to 14.
References Cited (Backward Citations)
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