US5227157A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Delivery of therapeutic agents
Assignee: The University of Texas System
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Filing: 1989-07-31
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Granted: 1993-07-13
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Expires: 2009-07-31
Abstract
Abstract The present invention relates to a composition of matter for the time-dependent liberation of therapeutic agents. This composition of matter comprises a polymeric slab and a homogeneously dispersed enzyme which degrades the polymeric slab in the presence of moisture. The therapeutic agent is physically entrapped in the polymeric slab by inclusion during polymerization to form the polymeric slab or by mixture of the therapeutic agent with a liquid form of the polymeric slab and conversion of the liquid to a solid form. The therapeutic agent is not chemically bound to the polymer, and thus release of the agent is immediately effected upon the specific moisture-activated enzymatic degradation of the polymer slab. Moisture for enzymatic activation is provided by the biological surface on which the slab is emplaced, such as the dermal surface. The composition comprises a polymer such as poly (DL-lactide) and an enzyme such as proteinase K together with chlorpheniramine maleate as the therapeutic agent.
Inventors
- 👤 James W. McGinity
- 👤 Susan L. Ashley
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 12:31
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2031; A61K9/204; A61K9/2068; A61K9/70; A61K9/7023
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
69 words
A pharmacologically acceptable composition of matter comprising: a biodegradable polymeric slab; a moisture activated enzyme included within the polymeric slab in a therapeutic agent releasing concentration which enzymatically degrades said slab; a non-polymer bound therapeutic agent incorporated into said slab, wherein enzymatic degradation of the biodegradable polymeric slab releases the incorporated therapeutic agent at a rate which is a function of the concentration of the enzyme in the slab.
Claim 2
Dependent Claim
69 words
A pharmacologically acceptable composition of matter comprising: a biodegradable polymeric slab; a moisture activated enzyme included within the polymeric slab in a therapeutic agent releasing concentration which enzymatically degrades said slab; a non-polymer bound therapeutic agent incorporated into said slab, wherein enzymatic degradation of the biodegradable polymeric slab releases the incorporated therapeutic agent at a rate which is a function of the concentration of the enzyme in the slab.
Claim 3
Dependent Claim
85 words
A pharmacologically acceptable composition of matter for the time dependent liberation of a therapeutic agent in vivo, the composition consisting essentially of: a biologically degradable polymeric slab; a non-polymer bound, homogeneously dispersed therapeutic agent physically entrapped in said polymeric slab; and an enzyme included at a concentration within the polymeric slab which degrades said slab in the presence of moisture to facilitate the controlled release of entrapped therapeutic agent at a rate which is a function of the concentration of the enzyme in the slab.
Claim 4
Dependent Claim
85 words
A pharmacologically acceptable composition of matter for the time dependent liberation of a therapeutic agent in vivo, the composition consisting essentially of: a biologically degradable polymeric slab; a non-polymer bound, homogeneously dispersed therapeutic agent physically entrapped in said polymeric slab; and an enzyme included at a concentration within the polymeric slab which degrades said slab in the presence of moisture to facilitate the controlled release of entrapped therapeutic agent at a rate which is a function of the concentration of the enzyme in the slab.
Claim 5
Dependent Claim
91 words
A deliver device for the transdermal administration of a therapeutic agent, said device comprising: a polymeric slab having a side for dermal contact; a non-polymer bound, homogeneously dispersed therapeutic agent physically entrapped in said polymeric slab; at least one moisture activated enzyme included within the slab at a concentration which provides for the controlled release of the therapeutic agent; and a means for holding the device in dermal contact, wherein the therapeutic agent is released at a rate which is a function of the concentration of the enzyme within the slab.
Claim 6
Dependent Claim
91 words
A deliver device for the transdermal administration of a therapeutic agent, said device comprising: a polymeric slab having a side for dermal contact; a non-polymer bound, homogeneously dispersed therapeutic agent physically entrapped in said polymeric slab; at least one moisture activated enzyme included within the slab at a concentration which provides for the controlled release of the therapeutic agent; and a means for holding the device in dermal contact, wherein the therapeutic agent is released at a rate which is a function of the concentration of the enzyme within the slab.
Claim 7
Dependent Claim
40 words
The composition of claim 1 or 2 or delivery device of claim 3 wherein the polymeric slab comprises a polymer selected from the group consisting of: polyesters, polyamides, polypeptides, polysaccharides, cellulose, dextran, elastin, fibrin, gelatin, polyethylene, pectin, and polygalacturonic acid.
Claim 8
Dependent Claim
21 words
The composition of claim 1 or 2 or delivery device of claim 3 wherein the polymeric slab comprises a biodegradable polyester.
Claim 9
Dependent Claim
39 words
The composition of claim 1 or 2 delivery device of claim 3 wherein the polymeric slab comprises a polyester of biologically metabolizable monomeric units selected from the group consisting of lactic acid, glycolic acid, hydroxypropionic acid, and hydroxybutyric acid.
Claim 10
Dependent Claim
31 words
The composition of claim 1 or 2 or delivery device of claim 3 wherein the polymeric slab comprises a polyester of biologically metabolizable monomeric units of lactic acid or glycolic acid.
Claim 11
Dependent Claim
20 words
The composition of claim 1 or 2 or delivery device of claim 3 wherein the polymeric slab comprises a polyamide.
Claim 12
Dependent Claim
20 words
A composition of claim 1 or 2 or delivery device of claim 3 wherein the polymeric slab comprises a polypeptide.
Claim 13
Dependent Claim
26 words
The composition of claim 1 or 2 or delivery device of claim 3 wherein the enzyme hydrolyses ester bonds and comprises a hydrolase or a protease.
Claim 14
Dependent Claim
45 words
The composition of claim 1 or 2 or delivery device of claim 3 wherein the enzyme is selected from the group consisting of: proteinase K, bromelain, pronase E, cellulase, dextranase, elastase, plasmid, streptokinase, trypsin, chymotrypsin, papain, chymopapain, collagenase, subtilisin, ficin, carboxypeptidase A, pectinase, and pectinesterase.
Claim 15
Dependent Claim
23 words
The composition of claims 1 or 2 or delivery device of claim 3 wherein the enzyme is proteinase K, bromelain or pronase E.
Claim 16
Dependent Claim
19 words
The compositions of claim 1 or 2 or delivery device of claim 3 wherein the enzyme is proteinase K.
Claim 17
Dependent Claim
31 words
The compositions of claim 1 or 2 or delivery device of claim 3 wherein the enzyme is proteinase K at a concentration of about 0.5% by weight of the polymeric slab.
Claim 18
Dependent Claim
23 words
The device of claim 3 wherein the enzyme is dispersed on the side of the polymeric slab for contact with the dermal surface.
Claim 19
Dependent Claim
27 words
The delivery device of claim 3 wherein the means for holding the device in contact with a dermal surface is an adhesive, elastic band or bandaging tape.
Claim 20
Dependent Claim
20 words
The compositions of claim 1 or 2 or delivery device of claim 3 wherein the therapeutic agent comprises chlorpheniramine maleate.
Claim 21
Dependent Claim
106 words
A delivery device for the transdermal administration of a therapeutic agent, said device comprising: a poly(DL-lactide) polymeric slab having a side for dermal contact; a non-polymer bound, homogeneously dispersed therapeutic agent physically entrapped in said poly(DL-lactide) polymeric slab; proteinase K included with the slab, which degrades the polymeric slab in the presence of moisture to release the therapeutic agent; and a means for holding the device in dermal contact selected from the group consisting of: an adhesive; an elastic band; and a bandaging tape, wherein the therapeutic agent is released at a rate which is a function of the concentration of the enzyme within the slab.
Claim 22
Dependent Claim
106 words
A delivery device for the transdermal administration of a therapeutic agent, said device comprising: a poly(DL-lactide) polymeric slab having a side for dermal contact; a non-polymer bound, homogeneously dispersed therapeutic agent physically entrapped in said poly(DL-lactide) polymeric slab; proteinase K included with the slab, which degrades the polymeric slab in the presence of moisture to release the therapeutic agent; and a means for holding the device in dermal contact selected from the group consisting of: an adhesive; an elastic band; and a bandaging tape, wherein the therapeutic agent is released at a rate which is a function of the concentration of the enzyme within the slab.
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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) | 1996-07-12 | 1997-01-11 | 1997-07-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-07-12 | 2001-01-11 | 2001-07-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-07-12 | 2005-01-11 | 2005-07-13 | $7700.00 | Window Closed / Lapsed |