US5073539A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Transdermal administration of zwitterionic drugs
Assignee: Novartis Corp
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Filing: 1990-01-22
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Granted: 1991-12-17
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Expires: 2010-01-22
Abstract
Abstract Compositions of zwitterionic drugs for transdermal administration and methods of administering zwitterions transdermally are disclosed. The compositions comprise a zwitterionic drug in a salt form and a solvent therefor.
Inventors
- 👤 Gerard C. Mazzenga
- 👤 Bret Berner
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 18:54
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K9/7084; A61K9/7092; A61P; A61P25/00; A61P25/02; A61P43/00
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
79 words
A transdermal device for the administration of a pharmaceutically acceptable zwitterionic active agent to an animal in need thereof comprising a resevoir for said active agent, said active agent in salt form in a transdermally effective amount, and a pharmaceutically acceptable carrier for said active agent, wherein said pharmaceutically acceptable zwitterionic active agent is selected from the group consisting of amino acids, baclofen, and ACE Inhibitors, said pharmaceutically acceptable zwitterionic active agent and said carrier being in said reservoir.
Claim 2
Dependent Claim
79 words
A transdermal device for the administration of a pharmaceutically acceptable zwitterionic active agent to an animal in need thereof comprising a resevoir for said active agent, said active agent in salt form in a transdermally effective amount, and a pharmaceutically acceptable carrier for said active agent, wherein said pharmaceutically acceptable zwitterionic active agent is selected from the group consisting of amino acids, baclofen, and ACE Inhibitors, said pharmaceutically acceptable zwitterionic active agent and said carrier being in said reservoir.
Claim 3
Dependent Claim
33 words
The transdermal device of claim 1 wherein the salt form of said zwitterionic active agent is selected from the group consisting of hydrohalide, lower alkyl sulfonate, lower alkyl dicarboxylate, and alkali metal salt.
Claim 4
Dependent Claim
27 words
The trandermal device of claim 1 wherein said carrier is selected from the group consisting of water, C 1 -C 10 alkanols, and other hydrogen bonding solvents.
Claim 5
Dependent Claim
34 words
The transdermal device of claim 1 further comprising at least one of an additional flux enhancer for the zwitterionic active agent, a pharmaceutically and transdermally acceptable buffer, a thickener, a preservative and a filler.
Claim 6
Dependent Claim
26 words
The transdermal device of claim 1 wherein the pH is maintained at least one pH unit away from the isoelectric point of said zwitterionic active agent.
Claim 7
Dependent Claim
29 words
A method of administering a zwitterionic active agent to an animal in need of such administration comprising applying to said animals skin a transdermal device according to claim 1.
Claim 8
Dependent Claim
11 words
The composition of claim 1 wherein said active agent is benazeprilat.
Claim 9
Dependent Claim
21 words
The composition of claim 1 wherein the melting point of the zwitterionic salt is below that of the parent free zwitterion.
Claim 10
Dependent Claim
26 words
The composition of claim 1 wherein the solubility in a hydrogen bonding solvent of the zwitterionic salt is greater than that of the parent free zwitterion.
Claim 11
Dependent Claim
25 words
The composition of claim 1 wherein the solubility in octanol or chloroform of the zwitterionic salt is greater than that of the parent free zwitterion.
Claim 12
Dependent Claim
25 words
The composition of claim 9 wherein the solubility in octanol or chloroform of the zwitterionic salt is greater than that of the parent free zwitterion.
Claim 13
Dependent Claim
26 words
The composition of claim 8 wherein the solubility in a hydrogen bonding solvent of the zwitterionic salt is greater than that of the parent free zwitterion.
Claim 14
Dependent Claim
25 words
The composition of claim 8 wherein the solubility in octanol or chloroform of the zwitterionic salt is greater than that of the parent free zwitterion.
Claim 15
Dependent Claim
25 words
The composition of claim 12 wherein the solubility in octanol or chloroform of the zwitterionic salt is greater than that of the parent free zwitterion.
References Cited (Backward Citations)
US4575503A
Cited
US4866160A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1994-12-16 | 1995-06-17 | 1995-12-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-12-16 | 1999-06-17 | 1999-12-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-12-16 | 2003-06-17 | 2003-12-17 | $7700.00 | Window Closed / Lapsed |