US4746509A
Expired / Lapsed
US
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Transdermal medicament
Assignee: Rhone Poulenc Sante SA
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Filing: 1987-02-03
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Granted: 1988-05-24
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Expires: 2007-02-03
Abstract
Abstract New transdermal medicaments comprise the active ingredient dispersed in a heat-reversible, non-crosslinked, film-forming, homogeneous polymer optionally with a non-ionic emulsifier and, if appropriate, a hydrophobic, water-insoluble copolymer.
Inventors
- 👤 Johnny Haggiage
- 👤 Christian Pusineri
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 18:32
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K9/7084; A61K31/00; A61K31/33; A61K31/335; A61K31/34
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
131 words
A transdermal medicament comprising 10 to 20% of a transdermally active ingredient selected from the group consisting of antianginal agents, antiemetic agents, anticholinergic agents, non-steroid anti-inflammatory agents, steroid anti-inflammatory agents, antihypertensive agents, beta-blockers, vasodilators, neuroleptic agents, tranquillizers, bronchodilators, antispasmodic agents and hormones and 10 to 20% of a non-ionic emulsifying agent selected from the group consisting of polycondensates of ethylene oxide with a fatty acid or fatty alcohol, sorbitan esters, triglycerides with free hydroxyl group, polypropylene glycol monoglycerides and polyglycerol esters, the said active ingredient being dispersed in crystalline or solubilized form in a non-crosslinked, film-forming homogeneous, thermoplastic, elastomeric, water-insoluble polymer selected from the group consisting of polyurethanes based on a polyether or polyester, polyamides, polyesters, polyethers, and polyolefins, the said percentages being by weight based on the said film-forming polymer.
Claim 2
Dependent Claim
131 words
A transdermal medicament comprising 10 to 20% of a transdermally active ingredient selected from the group consisting of antianginal agents, antiemetic agents, anticholinergic agents, non-steroid anti-inflammatory agents, steroid anti-inflammatory agents, antihypertensive agents, beta-blockers, vasodilators, neuroleptic agents, tranquillizers, bronchodilators, antispasmodic agents and hormones and 10 to 20% of a non-ionic emulsifying agent selected from the group consisting of polycondensates of ethylene oxide with a fatty acid or fatty alcohol, sorbitan esters, triglycerides with free hydroxyl group, polypropylene glycol monoglycerides and polyglycerol esters, the said active ingredient being dispersed in crystalline or solubilized form in a non-crosslinked, film-forming homogeneous, thermoplastic, elastomeric, water-insoluble polymer selected from the group consisting of polyurethanes based on a polyether or polyester, polyamides, polyesters, polyethers, and polyolefins, the said percentages being by weight based on the said film-forming polymer.
Claim 3
Dependent Claim
167 words
A transdermal medicament comprising 5 to 20% of a transdermally active ingredient selected from the group consisting of antianginal agents, antiemetic agents, anticholinergic agents, non-steroid anti-inflammatory agents, steroid anti-inflammatory agents, antihypertensive agents, beta-blockers, vasodilators, neuroleptic agents, tranquillizers, bronchodilators, antispasmodic agents and hormones, 5 to 30% of a non-ionic emulisfying agent selected from the group consisting of polycondensates of ethylene oxide with a fatty acid or fatty alcohol, sorbitan esters, triglycerides with free hydroxyl groups, polypropylene glycol monoglycerides and polyglycerol esters, and 1 to 30% of a copolymer containing a hydrophobic sequence which migrates to the surface of the said medicament to form a homogeneous membrane which provides complementary control of the release of the transdermally active ingredient, the said active ingredient being dispersed in crystalline or solubilized form in a non-crosslinked, film-forming homogeneous, thermoplastic, elastomeric, water-insoluble polymer selected from the group consisting of polyurthanes based on a polyether or polyester, polyamides, polyesters, polyethers, and polyolefines, the said percentages being by weight based on the said film-forming polymer.
Claim 4
Dependent Claim
167 words
A transdermal medicament comprising 5 to 20% of a transdermally active ingredient selected from the group consisting of antianginal agents, antiemetic agents, anticholinergic agents, non-steroid anti-inflammatory agents, steroid anti-inflammatory agents, antihypertensive agents, beta-blockers, vasodilators, neuroleptic agents, tranquillizers, bronchodilators, antispasmodic agents and hormones, 5 to 30% of a non-ionic emulisfying agent selected from the group consisting of polycondensates of ethylene oxide with a fatty acid or fatty alcohol, sorbitan esters, triglycerides with free hydroxyl groups, polypropylene glycol monoglycerides and polyglycerol esters, and 1 to 30% of a copolymer containing a hydrophobic sequence which migrates to the surface of the said medicament to form a homogeneous membrane which provides complementary control of the release of the transdermally active ingredient, the said active ingredient being dispersed in crystalline or solubilized form in a non-crosslinked, film-forming homogeneous, thermoplastic, elastomeric, water-insoluble polymer selected from the group consisting of polyurthanes based on a polyether or polyester, polyamides, polyesters, polyethers, and polyolefines, the said percentages being by weight based on the said film-forming polymer.
Claim 5
Dependent Claim
28 words
A medicament according to claim 1 in which the homogeneous thermoplastic polymer is a polyurethane/polyoxyethylene glcyol/polyoxypropylene glycol copolymer or a polyurethane based on polytetramethylene glycol, polycaprolactone or polyadipate.
Claim 6
Dependent Claim
33 words
A medicament according to claim 1, in which the non-ionic emulsifier is polyglycerol palmitostearate, polyglycerol isostearate, sucrose monopalmitate, polyoxymethylene oleyl glyceride, diethylene glycol monoethyl ether, or a polyoxymethyleneated C 8 -C 10 -glyceride.
Claim 7
Dependent Claim
18 words
A medicament according to clalim 2, in which the said hydrophobic copolymer is a polydimethylsiloxane polyoxyethylene glycol copolymer.
Claim 8
Dependent Claim
18 words
A medicament according to clalim 2, in which the said hydrophobic copolymer is a polydimethylsiloxane polyoxyethylene glycol copolymer.
Claim 9
Dependent Claim
12 words
A medicament according to claim 1, which is covered by an adhesive.
Claim 10
Dependent Claim
40 words
A medicament according to claim 1, in which the transdermally active ingredient is isosorbide dinitrate, isosorbide monoitrate, trinitrin, metopimazine, dimenhydrinate, scopolamine, ketoprofen, prednisolone, dexamethazone, clonidine, acebutolol, nicergoline, a neuroleptic phenothiazine, a tranquilling benzodiazepine, suriclone, suproclone, phenylpropanolamine, butylhyoscine bromide, or estradiol.
Claim 11
Dependent Claim
12 words
A transdermal medicament according to claim 1 packaged in a unit dose.
Claim 12
Dependent Claim
45 words
Method of administering a medicament to a patient which comprises applying to the skin of the said patient a transdermal medicament as claimed in claim 1 whereby an effective amount of the transdermally active ingredient in the said medicament is absorbed by the said patient.
Claim 13
Dependent Claim
31 words
A medicament according to claim 1 in which the active ingredient is isosorbide dinitrate, the non-ionic emulsifier is polyglycerol palmitostearate, and the thermoplastic elastomeric polymer is a polyurethane/polyoxyethylene glycol/polyoxypropylene glycol copolymer.
Claim 14
Dependent Claim
28 words
A medicament according to claim 2 in which the homogeneous thermoplastic polymer is a polyurethane/polyoxyethylene glycol/polyoxypropylene glycol copolymer, or a polyurethane based on polytetramethylene glycol, polycaprolactone or polyadipate.
Claim 15
Dependent Claim
32 words
A medicament according to claim 2, in which the non-ionic emulsifier is polyglycerol palmitostearate, plyglycerol isostearate, sucrose monopalmitate, polyoxymethylene oleyl glyceride, diethylene glycol monoethyl ether or a C 8 -C 10 -glyceride.
Claim 16
Dependent Claim
12 words
A medicament according to claim 2, which is covered by an adhesive.
Claim 17
Dependent Claim
40 words
A medicament according to claim 2, in which the transdermally active ingredient is isosorbide dinitrate, isosorbide monoitrate, trinitrin, metopimazine, dimenhydrinate, scopolamine, ketoprofen, predinsolone, dexamethazone, clonidine acebutolol, nicergoline, a neuroleptic phenothiazine, a tranquillising benzodiazepine, suriclone, suproclone, phenylpropanolamine, butylhyoscine bromide, or estradiol.
Claim 18
Dependent Claim
12 words
A transdermal medicament according to claim 2 packaged in a unit does.
Claim 19
Dependent Claim
31 words
A medicament according to claim 2 in which the active ingredient is isosorbide dinitrate, the non-ionic emulsifier is polyglycerol palmitostearate, and the thermoplastic elastomeric polymer is a polyurethane/polyoxyethylene glycol/polyoxypropylene glycol copolymer.
Claim 20
Dependent Claim
45 words
Method of administering a medicament to a patient which comprises applying to the skin of the said patient a transdermal medicament as claimed in claim 2 whereby an effective amount of the transdermally active ingredient in the said medicament is absorbed by the said patient.
Claim 21
Dependent Claim
40 words
A transdermal medicament according to claim 2 in which the transdermally active ingredient is isosorbide dinitrate, the non-ionic emulsifier is polyglycerol palmitostearate, the hydrophobic copolymer is polydimethylsiloxane/polyoxyethylene glycol copolymer, and the thermoplastic elastomeric polymer is a polyurethane/polyoxyethylene glycol/polyoxypropylene glycol copolymer.
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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) | 1991-05-24 | 1991-11-23 | 1992-05-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-05-24 | 1995-11-23 | 1996-05-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-05-24 | 1999-11-23 | 2000-05-24 | $7700.00 | Window Closed / Lapsed |