US4878892A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Electrolytic transdermal delivery of polypeptides
Assignee: Drug Delivery Systems Inc
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Filing: 1987-02-10
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Granted: 1989-11-07
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Expires: 2007-02-10
Abstract
Abstract The invention comprises in combination: a) a polypeptide having from about three to about 20 peptide units in aqueous solution or suspension, and b) an electrolytic device (10) for transdermal transport of the polypeptide to the bloodstream of the patient. It may be useful to enhance the transdermal delivery of the polypeptide by adding an aqueous cosolute/cosolvent with negative Setschenow constants. The electrolytic device preferably comprises a hydrophilic reservoir (24) containing a supply of the aqueous polypeptide solution or suspension, an electric battery (28), two extended contacts (26, 32), and optionally a semipermeable membrane (22) between the reservoir and the patient's skin. Representative polypeptides include oxytocin, angiotensin I, II, and III, substance P, vasopressin, lypressin, desmopressin, leuprolide acetate, antripeptin, and the like.
Inventors
- 👤 Dan Sibalis
- 👤 Sanford Rosen
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 18:55
CPC Classifications
A; A61; A61K; A61K9/00; A61N; A61N1/00; A61N1/02; A61N1/04; A61N1/0404; A61N1/0408; A61N1/0428; A61K9/0002; A61K9/0009
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
96 words
A transdermal patch for delivering at least one drug directly to the bloodstream of the patient comprising in combination: (a) an active ingredient comprising at least one polypeptide having from three to 20 peptide units selected from the group consisting of vasopressin, lypressin, atriopeptin, oxytocin, desmopressin, a dynorphin, leuprolide, an angiotensin, and mixtures thereof contained in a drug reservoir, and (b) electrolytic means for transdermal transport of the polypeptide characterized by a current density from about 0.5 microampere/cm 2 to about 1 milliampere/cm 2 , whereby the skin of the patient is neither irritated nor erythematized.
Claim 2
Dependent Claim
96 words
A transdermal patch for delivering at least one drug directly to the bloodstream of the patient comprising in combination: (a) an active ingredient comprising at least one polypeptide having from three to 20 peptide units selected from the group consisting of vasopressin, lypressin, atriopeptin, oxytocin, desmopressin, a dynorphin, leuprolide, an angiotensin, and mixtures thereof contained in a drug reservoir, and (b) electrolytic means for transdermal transport of the polypeptide characterized by a current density from about 0.5 microampere/cm 2 to about 1 milliampere/cm 2 , whereby the skin of the patient is neither irritated nor erythematized.
Claim 3
Dependent Claim
12 words
A transdermal patch as in claim 1, wherein the polypeptide comprises vasopressin.
Claim 4
Dependent Claim
12 words
A transdermal patch as in claim 1, wherein the polypeptide comprises lypressin.
Claim 5
Dependent Claim
12 words
A transdermal patch as in claim 1, wherein the polypeptide comprises atriopeptin.
Claim 6
Dependent Claim
27 words
A transdermal patch as in claim 1, wherein the electrolytic means comprises a battery, an anode, a cathode, said drug reservoir, and barrier means between the electrodes.
Claim 7
Dependent Claim
15 words
A transdermal patch as in claim 1, further comprising an aqueous solvent for the polypeptide.
Claim 8
Dependent Claim
12 words
A transdermal patch as in claim 6, further comprising a dissociating cosolvent.
Claim 9
Dependent Claim
50 words
A transdermal patch as in claim 7, wherein the dissociating cosolvent is selected from the group consisting of urea, alkylderivatives of urea, guanidine salt, butanol, 2-butanol, water-soluble amides with more than three carbon atoms, sodium and potassium iodide, sodium perchlorate, sodium butyrate, and any other salt with negative Setschenow constants.
Claim 10
Dependent Claim
27 words
A transdermal patch as in claim 1, further comprising at least one compound selected from the group consisting of buffering agents, chelating agents, antioxidants, preservatives, and biocides.
Claim 11
Dependent Claim
20 words
A transdermal patch as in claim 6, further comprising a semipermeable membrane on the skin side of the drug reservoir.
Claim 12
Dependent Claim
18 words
A transdermal patch as in claim 1, wherein at least one polypeptide is LH-RH analog further comprising testosterone.
Claim 13
Dependent Claim
18 words
A transdermal patch as in claim 1, wherein at least one polypeptide is LH-RH analog further comprising Flutamide.
Claim 14
Dependent Claim
30 words
A transdermal patch as in claim 5, further comprising current controlling means whereby the current density of the patch is from 0.5 microamperes/cm 2 to about 10 microamperes/cm 2 .
Claim 15
Dependent Claim
79 words
A transdermal patch for delivering at least one drug directly to the bloodstream of the patient comprising in combination: (a) an active ingredient comprising at least one nonionic polypeptide having from three to 20 peptide units contained in a drug reservoir, and (b) electrolytic means for transdermal transport of the nonionic polypeptide characterized by a current density from about 0.5 microampere/cm 2 to about 1 milliampere/cm 2 , whereby the skin of the patient is neither irritated nor erythematized.
Claim 16
Dependent Claim
79 words
A transdermal patch for delivering at least one drug directly to the bloodstream of the patient comprising in combination: (a) an active ingredient comprising at least one nonionic polypeptide having from three to 20 peptide units contained in a drug reservoir, and (b) electrolytic means for transdermal transport of the nonionic polypeptide characterized by a current density from about 0.5 microampere/cm 2 to about 1 milliampere/cm 2 , whereby the skin of the patient is neither irritated nor erythematized.
Claim 17
Dependent Claim
31 words
A transdermal patch as in claim 14, wherein the nonionic polypeptide is selected from the group consisting of vasopressin, lypressin, atriopeptin, oxytocin, desmopression, leuprolide a dynorphin, an angiotensin, and mixtures thereof.
Claim 18
Dependent Claim
28 words
A transdermal patch as in claim 14, wherein the electrolytic means comprises a battery, an anode, a cathode, a drug reservoir, and a barrier means between the electrodes.
Claim 19
Dependent Claim
15 words
A transdermal patch as in claim 14, comprising an aqueous solvent for the nonionic polypeptide.
Claim 20
Dependent Claim
33 words
A transdermal patch as in claim 14, further comprising at least one compound from the group consisting of buffering agents, chelating agents, antioxidants, preservatives, biocides, and dissociating cosolvents with a negative Setschenow constant.
Claim 21
Dependent Claim
31 words
A transdermal patch as in claim 16, further comprising current controlling means whereby the current density of the patch is from about 0.5 microampere/cm 2 to about 10 microamperes/cm 2 .
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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) | 1992-11-06 | 1993-05-08 | 1993-11-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-11-06 | 1997-05-08 | 1997-11-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-11-06 | 2001-05-08 | 2001-11-07 | $7700.00 | Window Closed / Lapsed |