Patent US5160742A successfully refreshed from Google Patents.
US5160742A
Expired / Lapsed
US
⏱️ 0.0 years remaining
System for delivering an active substance for sustained release
Assignee: Abbott Laboratories
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Filing: 1991-12-31
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Granted: 1992-11-03
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Expires: 2011-12-31
Abstract
Abstract A system for delivering an active substance has sustained release of the active substance in the intestinal tract. This delivery system is especially useful for an active substance such as a β-lactam antibiotic which preferably has minimal exposure to the acidic environment of the stomach. Particles comprise an active ingredient disposed in a core which has at least one coating of a prolamine and one coating of an enteric compound thereon. The particles may be very small and suspended in a liquid medium.
Inventors
- 👤 Terrence B. Mazer
- 👤 Glenn A. Meyer
- 👤 Shie-Ming Hwang
- 👤 Edrick L. Candler, Jr.
- 👤 Lonnie R. Drayer
- 👤 Andre Daab-Krzykowski
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 11:42
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5073; A61K9/5005; A61K9/5021; A61K9/5052
Claims Analysis
Total Claims: 45
Claim 1
Independent Claim
114 words
A system for delivery of an active substance for sustained release in the intestinal tract, comprising a particle having a core containing an active substance, said core being encapsulated by at least two layers of coating materials, one of said layers of a coating material consisting essentially of a prolamine and at least one material selected from the group consisting of plasticizers and hydrophobic substances and the other layer a coating material consisting essentially of an enteric compound and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said other layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids.
Claim 2
Independent Claim
114 words
A system for delivery of an active substance for sustained release in the intestinal tract, comprising a particle having a core containing an active substance, said core being encapsulated by at least two layers of coating materials, one of said layers of a coating material consisting essentially of a prolamine and at least one material selected from the group consisting of plasticizers and hydrophobic substances and the other layer a coating material consisting essentially of an enteric compound and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said other layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids.
Claim 3
Dependent Claim
107 words
A system for delivery of an active substance for sustained release in the intestinal tract according to claim 1 wherein the core is encapsulated by a first layer of a coating material, consisting essentially of a prolamine and at least one material selected from the group consisting of plasticizers and hydrophobic substances said first layer is encapsulated by an exterior layer of a coating material consisting essentially of an enteric compound and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said exterior layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids.
Claim 4
Dependent Claim
108 words
A system for delivery of an active substance for sustained release in the intestinal tract according to claim 1 wherein the core is encapsulated by a first layer of a coating material consisting essentially of an enteric compound and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said first layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids, and said first layer is encapsulated by an exterior layer of a coating material consisting essentially of a prolamine and at least one material selected from the group consisting of plasticizers and hydrophobic substances.
Claim 5
Dependent Claim
141 words
A system for delivery of an active substance for sustained release in the intestinal tract according to claim 1 wherein the core is encapsulated by a first layer comprising a coating material consisting essentially of a prolamine and at least one material selected from the group consisting of plasticizers and hydrophobic substances, said first layer is encapsulated by a second layer comprising a coating material consisting essentially of an enteric compound and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said second layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids, and said second layer is encapsulated by an exterior layer comprising a coating material consisting essentially of a prolamine and at least one material selected from the group consisting of plasticizers and hydrophobic substances.
Claim 6
Independent Claim
29 words
A system for delivery of an active substance for sustained release in the intestinal tract according to any one of claims 1 through 4 wherein the prolamine is zein.
Claim 7
Independent Claim
45 words
A system for delivery of an active substance for sustained release in the intestinal tract according to any one of claims 1 through 4 wherein the enteric compound comprises at least one material selected from the group consisting of acids and esters of methacrylic copolymers.
Claim 8
Dependent Claim
40 words
A system for delivery of an active substance for sustained release in the intestinal tract according to claim 5 wherein the enteric compound comprises at least one material selected from the group consisting of acids and esters of methacrylic copolymers.
Claim 9
Independent Claim
60 words
A system for delivery of an active substance for sustained release in the intestinal tract according to any one of claims 1 through 4 comprising a plurality of said particles where in the particles have a size of not greater than about 700 microns, and the system further comprises a liquid medium, said particles being disposed within said liquid medium.
Claim 10
Dependent Claim
26 words
A system for delivery of an active substance for release in the intestinal tract according to claim 8 wherein the liquid medium is an aqueous medium.
Claim 11
Dependent Claim
44 words
A system for delivery of an active substance for release in the intestinal tract according to claim 9 wherein the prolamine is zein and the enteric compound comprises at least one material selected from the group consisting of acids and esters of methacrylic copolymers.
Claim 12
Dependent Claim
26 words
A system for delivery of an active substance for release in the intestinal tract according to claim 10 wherein the active substance is a β-lactam antibiotic.
Claim 13
Independent Claim
46 words
A system for delivery of an active substance for release in the intestinal tract according to claims 1 through 4 wherein the active substance is selected from the group consisting of analgesics, antibiotics, antidepressants, antivirals, antibodies, immuno-modulators, oncolytics, immunogens, hormones, vaccines, enzymes, nutrients and dietary fiber.
Claim 14
Independent Claim
151 words
A system for delivery of an active substance for release in the intestinal tract comprising a particle having a core containing an active substance, said core being encapsulated by a first layer of a coating material consisting essentially of an enteric compound in an amount of about 10% to 70% of the total weight of the core and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said first coating layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids, and said first coating layer being encapsulated by an exterior layer of a coating material consisting essentially zein in the amount of about 20% to 100% by weight of the sum of the weights of the core and the first coating layer and at least one material selected from the group consisting of plasticizers and hydrophobic substances.
Claim 15
Independent Claim
151 words
A system for delivery of an active substance for release in the intestinal tract comprising a particle having a core containing an active substance, said core being encapsulated by a first layer of a coating material consisting essentially of an enteric compound in an amount of about 10% to 70% of the total weight of the core and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said first coating layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids, and said first coating layer being encapsulated by an exterior layer of a coating material consisting essentially zein in the amount of about 20% to 100% by weight of the sum of the weights of the core and the first coating layer and at least one material selected from the group consisting of plasticizers and hydrophobic substances.
Claim 16
Dependent Claim
39 words
A system for delivery of an active substance for release in the intestinal tract according to claim 13 wherein the enteric compound comprises at least one material selected from the group consisting of acids and esters of methacrylic copolymers.
Claim 17
Dependent Claim
33 words
A system for delivery of an active substance for release in the intestinal tract according to claim 14 wherein the zein has an ash content of not greater than about 2% by weight.
Claim 18
Independent Claim
49 words
A system for delivery of an active substance for release in the intestinal tract according to any one of claims 13 through 15 wherein the active substance is selected from the group consisting of analgesics, antibiotics, antidepressants, antivirals, antibodies, immuno-modulators, oncolytics, immunogens, hormones, vaccines, enzymes, nutrients and dietary fiber.
Claim 19
Independent Claim
31 words
A system for delivery of an active substance for release in the intestinal tract according to any one of claims 13 through 15 wherein the active substance is a β-lactam antibiotic.
Claim 20
Independent Claim
147 words
A system for delivery of an active substance for release in the intestinal tract comprising a particle having a core containing an active substance, said core being encapsulated by a first layer of a coating material consisting essentially of zein in the amount of about 10% to 70% of the total weight of the core and at least one material selected from the group consisting of plasticizers and hydrophobic substances, and said first coating layer being encapsulated by a second coating layer consisting essentially of an enteric compound in an amount of about 10% to 70% of the sum of the weights of the core and the first coating layer and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said second coating layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids.
Claim 21
Independent Claim
147 words
A system for delivery of an active substance for release in the intestinal tract comprising a particle having a core containing an active substance, said core being encapsulated by a first layer of a coating material consisting essentially of zein in the amount of about 10% to 70% of the total weight of the core and at least one material selected from the group consisting of plasticizers and hydrophobic substances, and said first coating layer being encapsulated by a second coating layer consisting essentially of an enteric compound in an amount of about 10% to 70% of the sum of the weights of the core and the first coating layer and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said second coating layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids.
Claim 22
Dependent Claim
28 words
A system for delivery of an active substance for release in the intestinal tract according to claim 18 wherein the particle is in the form of a tablet.
Claim 23
Independent Claim
48 words
A system for delivery of an active substance for release in the intestinal tract according to either of claims 18 or 19 wherein the active substance is selected from the group consisting of analgesics, antibiotics, antidepressants, antivirals, antibodies, immuno-modulators, oncolytics, immunogens, hormones, vaccines, enzymes, nutrients and dietary fiber.
Claim 24
Independent Claim
30 words
A system for delivery of an active substance for release in the intestinal tract according to either of claims 18 or 19 wherein the active substance is a β-lactam antibiotic.
Claim 25
Independent Claim
201 words
A system for delivery of an active substance for release in the intestinal tract comprising a particle having a core containing an active substance, said core being encapsulated by a first layer of a coating material consisting essentially of zein in an amount of about 10% to 70% of the total weight of the core and at least one material selected from the group consisting of plasticizers and hydrophobic substances, said first coating layer being encapsulated by a second coating layer consisting essentially of an enteric compound in the amount of about 5% to 70% of the sum of the weights of the core and first coating layer and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids, and said second coating layer being encapsulated by an exterior coating layer of a coating material consisting essentially of zein in an amount of about 20% to 70% of the sum of the weights of the core and the first two coating layers and at least one material selected from the group consisting of plasticizers and hydrophobic substances.
Claim 26
Independent Claim
201 words
A system for delivery of an active substance for release in the intestinal tract comprising a particle having a core containing an active substance, said core being encapsulated by a first layer of a coating material consisting essentially of zein in an amount of about 10% to 70% of the total weight of the core and at least one material selected from the group consisting of plasticizers and hydrophobic substances, said first coating layer being encapsulated by a second coating layer consisting essentially of an enteric compound in the amount of about 5% to 70% of the sum of the weights of the core and first coating layer and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids, and said second coating layer being encapsulated by an exterior coating layer of a coating material consisting essentially of zein in an amount of about 20% to 70% of the sum of the weights of the core and the first two coating layers and at least one material selected from the group consisting of plasticizers and hydrophobic substances.
Claim 27
Dependent Claim
33 words
A system for delivery of an active substance for release in the intestinal tract according to claim 22 wherein the zein has an ash content of not greater than about 2% by weight.
Claim 28
Dependent Claim
39 words
A system for delivery of an active substance for release in the intestinal tract according to claim 22 wherein the enteric compound comprises at least one material selected from the group consisting of acids and esters of methacrylic copolymers.
Claim 29
Dependent Claim
39 words
A system for delivery of an active substance for release in the intestinal tract according to claim 23 wherein the enteric compound comprises at least one material selected from the group consisting of acids and esters of methacrylic copolymers.
Claim 30
Independent Claim
49 words
A system for delivery of an active substance for release in the intestinal tract according to any one of claims 22 through 25 wherein the active substance is selected from the group consisting of analgesics, antibiotics, antidepressants, antivirals, antibodies, immuno-modulators, oncolytics, immunogens, hormones, vaccines, enzymes, nutrients and dietary fiber.
Claim 31
Independent Claim
31 words
A system for delivery of an active substance for release in the intestinal tract according to any one of claims 22 through 25 wherein the active substance is a β-lactam antibiotic.
Claim 32
Independent Claim
133 words
A system for delivery of an active substance for release in the intestinal tract comprising a liquid medium having a plurality of particles disposed therein, said particles comprising a core containing an active substance, said core being encapsulated by at least two layers of coating materials, one of said layers comprising a coating material, consisting essentially of zein and least one material selected from the group consisting of plasticizers and hydrophobic substances and the other layer comprising a coating material consisting essentially of an enteric compound and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said other layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids, said particles having sizes of not greater than about 700 microns.
Claim 33
Independent Claim
133 words
A system for delivery of an active substance for release in the intestinal tract comprising a liquid medium having a plurality of particles disposed therein, said particles comprising a core containing an active substance, said core being encapsulated by at least two layers of coating materials, one of said layers comprising a coating material, consisting essentially of zein and least one material selected from the group consisting of plasticizers and hydrophobic substances and the other layer comprising a coating material consisting essentially of an enteric compound and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said other layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids, said particles having sizes of not greater than about 700 microns.
Claim 34
Dependent Claim
113 words
A system for delivery of an active substance for release in the intestinal tract according to claim 28 wherein said particles have a structure such that the core is encapsulated by a first layer comprising a coating material, consisting essentially of zein and at least one material selected from the group consisting of plasticizers and hydrophobic substances and said first layer is encapsulated by an exterior layer comprising a coating material consisting essentially of an enteric compound and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said second layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids.
Claim 35
Dependent Claim
113 words
A system for delivery of an active substance for release in the intestinal tract according to claim 28 wherein said particles have a structure such that the core is encapsulated by a first layer comprising a coating material, consisting essentially of an enteric compound and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said first layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids, and said first layer is encapsulated by an exterior layer comprising a coating material consisting essentially of zein and at least one material selected from the group consisting of plasticizers and hydrophobic substances.
Claim 36
Dependent Claim
146 words
A system for delivery of an active substance for release in the intestinal tract according to claim 28 wherein said particles have a structure such that the core is encapsulated by a first layer comprising a coating material, consisting essentially of zein and at least one material selected from the group consisting of plasticizers and hydrophobic substances and said first layer is encapsulated by a second layer comprising a coating material, consisting essentially of an enteric compound and at least one material selected from the group consisting of plasticizers and anti-tackiness agents, such that said second layer is generally resistant to disintegration in human gastric juices but will disintegrate in human intestinal fluids, and said second layer is encapsulated by an exterior layer comprising a coating material consisting essentially of zein and at least one material selected from the group consisting of plasticizers and hydrophobic substances.
Claim 37
Dependent Claim
54 words
A system for delivery of an active substance for release in the intestinal tract according to claim 28 wherein the zein has an ash content of not greater than about 2% by weight, and the enteric compound comprises at least one material selected from the group consisting of acids and esters of methacrylic copolymers.
Claim 38
Dependent Claim
54 words
A system for delivery of an active substance for release in the intestinal tract according to claim 29 wherein the zein has an ash content of not greater than about 2% by weight, and the enteric compound comprises at least one material selected from the group consisting of acids and esters of methacrylic copolymers.
Claim 39
Dependent Claim
54 words
A system for delivery of an active substance for release in the intestinal tract according to claim 30 wherein the zein has an ash content of not greater than about 2% by weight and the enteric compound comprises at least one material selected from the group consisting of acids and esters of methacrylic copolymers.
Claim 40
Dependent Claim
54 words
A system for delivery of an active substance for release in the intestinal tract according to claim 31 wherein the zein has an ash content of not greater than about 2% by weight, and the enteric compound comprises at least one material selected from the group consisting of acids and esters of methacrylic copolymers.
Claim 41
Independent Claim
31 words
A system for delivery of an active substance for release in the intestinal tract according to any one of claims 28 through 35 wherein the liquid medium is an aqueous medium.
Claim 42
Independent Claim
49 words
A system for delivery of an active substance for release in the intestinal tract according to any one of claims 28 through 35 wherein the active substance is selected from the group consisting of analgesics, antibiotics, antidepressants, antivirals, antibodies, immuno-modulators, oncolytics, immunogens, hormones, vaccines, enzymes, nutrients and dietary fiber.
Claim 43
Independent Claim
30 words
A system for delivery of an active substance for release in the intestinal tract according to either of claims 28 or 35 wherein the active substance is a β-lactam antibiotic.
Claim 44
Dependent Claim
25 words
A system for delivery of an active substance for release in the intestinal tract according to claim 36 wherein the active substance is an antibiotic.
Claim 45
Dependent Claim
26 words
A system for delivery of an active substance for release in the intestinal tract according to claim 36 wherein the active substance is a β-lactam antibiotic.
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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) | 1995-11-03 | 1996-05-04 | 1996-11-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-11-03 | 2000-05-04 | 2000-11-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-11-03 | 2004-05-04 | 2004-11-03 | $7700.00 | Window Closed / Lapsed |