US5154922A
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US
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Compositions for transdermal delivery of estradiol
Assignee: Merck Sharp & Dohme LLC
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Filing: 1989-11-29
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Granted: 1992-10-13
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Expires: 2009-11-29
Abstract
Abstract PCT No. PCT/US89/05288 Sec. 371 Date May 7, 1991 Sec. 102(e) Date May 7, 1991 PCT Filed Nov. 29, 1989.Solvent systems comprising oleic acid, linear alcohol lactate and either dipropylene glycol or N-methyl-2-pyrrolidine useful for preparing adhesive matrix and reservoir-type transdermal delivery devices for estradiol are disclosed.
Inventors
- 👤 Sharad K. Govil
- 👤 Dale Sterner
- 👤 Stephen Jones
- 👤 Geraldine Kennedy
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 17:42
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K9/7038; A61K9/7046; A61K9/7053; A61K31/00; A61K31/56; A61K31/565; A61K47/00; A61K47/06; A61K47/08; A61K47/14; A61K9/0012; A61K9/0014
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
39 words
A pharmaceutical composition for use in an adhesive-matrix of reservoir transdermal device for transdermal delivery of estradiol or a pharmaceutically acceptable ester thereof comprising oleic acid, D 12 -C 15 linear alcohol lactate and either dipropylene glycol or N-methyl-2-pyrrolidone.
Claim 2
Dependent Claim
39 words
A pharmaceutical composition for use in an adhesive-matrix of reservoir transdermal device for transdermal delivery of estradiol or a pharmaceutically acceptable ester thereof comprising oleic acid, D 12 -C 15 linear alcohol lactate and either dipropylene glycol or N-methyl-2-pyrrolidone.
Claim 3
Dependent Claim
23 words
A pharmaceutical composition of claim 1 for use in an adhesive-matrix further comprising a pharmaceutically acceptable pressure sensitive polymeric adhesive or adhesive mixture.
Claim 4
Dependent Claim
31 words
A pharmaceutical composition of claim 2 wherein the adhesive is selected from the group consisting of vinyl acetate, acrylic, silicone, synthetic or natural rubber latex pressure sensitive adhesives and mixtures thereof.
Claim 5
Dependent Claim
49 words
A pharmaceutical composition as defined in claim 2 comprising about 1 to about 10% estradiol or a pharmaceutically acceptable ester thereof, about 2.5 to about 5% oleic acid, about 2.5 to about 5% C 12 -C 15 linear alcohol lactate, about 5 to about 10% dipropylene glycol or N-methyl-2-pyrrolidone.
Claim 6
Dependent Claim
21 words
A pharmaceutical composition of claim 4 further comprising about 0.1 to about 0.5% crosslinker and about 1 to about 2% thickener.
Claim 7
Dependent Claim
65 words
A polymer mixture suitable for preparing a pharmaceutical composition of claim 2 comprising about 0.5 to about 5% estradiol or a pharmaceutically acceptable ester thereof, about 1 to about 20% oleic acid, about 1 to about 10% C 12 -C 15 linear alcohol lactate, about 1 to about 20% dipropylene glycol or N-methyl-2-pyrrolidone, and about 60 to about 80% pressure sensitive adhesive or adhesive mixture.
Claim 8
Dependent Claim
47 words
A polymer mixture of claim 6 comprising about 2 to about 5% oleic acid, about 1 to about 10% C 12 -C 15 linear alcohol lactate, about 1 to about 20% dipropylene glycol or N-methyl-2-pyrrolidone, and about 60 to about 80% pressure sensitive adhesive or adhesive mixture.
Claim 9
Dependent Claim
36 words
A polymer mixture as defined in claim 6 further comprising about 0.1 to about 0.5% crosslinking agent, about 0.5 to about 1.5% thickener, about 5 to about 10% water, and about 2 to about 10% ethanol.
Claim 10
Dependent Claim
40 words
A polymer mixture of claim 8 comprising 72.9% pressure sensitive adhesive; 1.1% estradiol; 2.7 % C 12 -C 15 linear alcohol lactate; 2.7% oleic acid; 0.3% crosslinking agent; 1.0% thickener; 8.7% water; 5.3% ethanol; and 5.3% dipropylene glycol or N-methyl-2-pyrrolidone.
Claim 11
Dependent Claim
20 words
A polymer mixture of claim 9 wherein the pressure sensitive adhesive is a vinyl acetate adhesive or an acrylic adhesive.
Claim 12
Dependent Claim
55 words
A pharmaceutical composition of claim 1 for use in a reservoir transdermal device comprising about 20 to about 60% dipropylene glycol or N-methyl-2-pyrrolidone; about 10 to about 40% oleic acid; about 10 to about 40% C 12 -C 15 linear alcohol lactate; and about 5 to about 20% estradiol or a pharmaceutically acceptable ester thereof.
Claim 13
Dependent Claim
15 words
A pharmaceutical composition of claim 11 further comprising about 0.1 to about 2% gelling agent.
Claim 14
Dependent Claim
117 words
A process for preparing an adhesive matrix transdermal device for administering estradiol or a pharmaceutically acceptable ester thereof, said process comprising applying a polymer mixture to a backing member and curing the polymer mixture, wherein said polymer mixture comprises about 0.5 to about 5% estradiol or a pharmaceutically acceptable ester thereof, about 1 to about 20% oleic, about 1 to about 10% C 12 -C 15 linear alcohol lactate, about 1 to about 20% dipropylene glycol or N-methyl-2-pyrrolidone, about 60 to about 80% pharmaceutically acceptable pressure sensitive adhesive or adhesive mixture, about 0.1 to about 0.5% crosslinking agent, about 0.5 to about 1.5% thickener, about 5 to about 10% water, and about 2 to about 10% ethanol.
Claim 15
Dependent Claim
117 words
A process for preparing an adhesive matrix transdermal device for administering estradiol or a pharmaceutically acceptable ester thereof, said process comprising applying a polymer mixture to a backing member and curing the polymer mixture, wherein said polymer mixture comprises about 0.5 to about 5% estradiol or a pharmaceutically acceptable ester thereof, about 1 to about 20% oleic, about 1 to about 10% C 12 -C 15 linear alcohol lactate, about 1 to about 20% dipropylene glycol or N-methyl-2-pyrrolidone, about 60 to about 80% pharmaceutically acceptable pressure sensitive adhesive or adhesive mixture, about 0.1 to about 0.5% crosslinking agent, about 0.5 to about 1.5% thickener, about 5 to about 10% water, and about 2 to about 10% ethanol.
References Cited (Backward Citations)
GB1470355A
Cited
US4291014A
Cited
US4305936A
Cited
GB2093694A
Cited
US4559222A
Cited
FR2547502A1
Cited
US4557934A
Cited
US4710383A
Cited
DE3333240A1
Cited
EP0147146A2
Cited
US4685911A
Cited
US4695465A
Cited
GB2158355A
Cited
US4704282A
Cited
US4624665A
Cited
US4568343A
Cited
WO1986002584A1
Cited
US4668232A
Cited
US4666441A
Cited
GB2185187A
Cited
WO1987007138A1
Cited
EP0250125A2
Cited
US4746515A
Cited
US4788062A
Cited
US4842864A
Cited
US4764379A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1995-10-13 | 1996-04-13 | 1996-10-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-10-13 | 2000-04-13 | 2000-10-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-10-13 | 2004-04-13 | 2004-10-13 | $7700.00 | Window Closed / Lapsed |