US5607691A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Compositions and methods for enhanced drug delivery
Assignee: Affymax Technologies NV
•
Filing: 1995-05-24
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Granted: 1997-03-04
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Expires: 2015-05-24
Abstract
Abstract The present invention relates to methods of delivering pharmaceutical agents across membranes, including the skin layer or mucosal membranes of a patient. A pharmaceutical agent is covalently bonded to a chemical modifier, via a physiologically cleavable bond, such that the membrane transport and delivery of the agent is enhanced.
Inventors
- 👤 Ron L. Hale
- 👤 Amy Lu
- 👤 Dennis Solas
- 👤 Harold E. Selick
- 👤 Kevin R. Oldenburg
- 👤 Alejandro C. Zaffaroni
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 21:04
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K31/56; A61K31/565; A61K31/568; A61K47/00; A61K47/50; A61K47/51; A61K47/54; A61K47/541; A61K47/69; A61K47/6957; A61K9/00; A61K9/0002; A61K9/0009; A61K9/10; A61K9/127; A61K9/1271; A61K9/1272
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
184 words
An iontophoretic drug delivery system for administering a pharmaceutical agent to a patient comprising: (a) a pharmaceutical agent-chemical modifier complex comprising: a pharmaceutical agent, suitable for transdermal transport at therapeutically effective doses of less than 50 milligrams per day, having a derivatizable chemical functionality; and a charged, naturally-occurring chemical modifier, conjugated to the agent's derivatizable chemical functionality by a covalent, physiologically cleavable bond, wherein said chemical modifier is selected from the group consisting of taurine, betaine, L carnitine, choline, norcholine, lysine, N-methylated amino acids, trigonelline, stachydrine, betonicine, cytochrome c, squalamine, chonemorphine, and conessine; where said pharmaceutical agent-chemical modifier complex has a charge-to-mass ratio of at least one charge per 1000 daltons, and wherein upon iontophoretic delivery of said composition and cleavage of said covalent bond, said chemical modifier is present at a non-toxic level and said pharmaceutical agent is delivered to said subject at said therapeutically effective dose; and (b) a means for iontophoretically delivering said composition at a selected skin site whereby said chemical modifier is cleaved from the complex by a physiological process and said pharmaceutical agent is released within the patient.
Claim 2
Dependent Claim
184 words
An iontophoretic drug delivery system for administering a pharmaceutical agent to a patient comprising: (a) a pharmaceutical agent-chemical modifier complex comprising: a pharmaceutical agent, suitable for transdermal transport at therapeutically effective doses of less than 50 milligrams per day, having a derivatizable chemical functionality; and a charged, naturally-occurring chemical modifier, conjugated to the agent's derivatizable chemical functionality by a covalent, physiologically cleavable bond, wherein said chemical modifier is selected from the group consisting of taurine, betaine, L carnitine, choline, norcholine, lysine, N-methylated amino acids, trigonelline, stachydrine, betonicine, cytochrome c, squalamine, chonemorphine, and conessine; where said pharmaceutical agent-chemical modifier complex has a charge-to-mass ratio of at least one charge per 1000 daltons, and wherein upon iontophoretic delivery of said composition and cleavage of said covalent bond, said chemical modifier is present at a non-toxic level and said pharmaceutical agent is delivered to said subject at said therapeutically effective dose; and (b) a means for iontophoretically delivering said composition at a selected skin site whereby said chemical modifier is cleaved from the complex by a physiological process and said pharmaceutical agent is released within the patient.
Claim 3
Dependent Claim
41 words
The device of claim 1 wherein the complex is selected from the group consisting of O-(indomethacinyl)norcholine; (indomethacinyl)choline iodide; 3,17β-estradiol-3-choline carbonate, iodide salt; piroxicam-N,O-bis(choline chloride) carbonate ester; digitoxin-4"'-(choline chloride) carbonate ester; 3,17β-estradiol-17β-betaine ester, chloride salt; and indomethacin hydroxymethyl ketone choline iodide carbonate.
Claim 4
Dependent Claim
22 words
The device of claim 1 wherein the transdermal delivery of the complex is enhanced over the transdermal delivery of the agent alone.
Claim 5
Dependent Claim
18 words
The device of claim 1 wherein one or more chemical modifiers are covalently bonded to the pharmaceutical agent.
Claim 6
Dependent Claim
28 words
The device of claim 1 wherein the pharmaceutical is selected from the group consisting of digitalis drugs, steroidal compounds, non-steroidal anti-inflammatories, protein and peptide drugs, and nitrogen heterocycles.
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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) | 2000-03-03 | 2000-09-02 | 2001-03-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2004-03-03 | 2004-09-02 | 2005-03-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2008-03-03 | 2008-09-02 | 2009-03-04 | $7700.00 | Window Closed / Lapsed |