US5053227A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Skin permeation enhancer compositions, and methods and transdermal systems associated therewith
Assignee: Janssen Pharmaceuticals Inc
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Filing: 1990-06-12
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Granted: 1991-10-01
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Expires: 2010-06-12
Abstract
Abstract Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The composition contains diethylene glycol monoethyl or monomethyl ether in addition to an ester component such as propylene glycol monolaurate, methyl laurate or the like. The compositions are particularly useful in conjunction with the transdermal administration of steroid drugs such as progestogens and estrogens. Methods and drug delivery systems for using the enhancer compositions are provided as well.
Inventors
- 👤 Chia-Ming Chiang
- 👤 Gary W. Cleary
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 04:42
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K9/7038; A61K9/7046; A61K9/7069; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/14; A61K9/0012; A61K9/0014; A61M; A61M37/00; A61M2037/0007
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
159 words
A transdermal delivery system for administering at least one pharmacologically active agent to a patient, comprising: (a) a source of the at least one pharmacologically active agent to be administered; (b) a source of a permeation enhancer composition comprising an ether component selected from the group consisting of diethylene glycol monoethyl ether, diethylene glycol monomethyl ether, and mixtures thereof, and an ester component given by the formula [CH 3 (CH 2 ) m COO] n R, in which m is an integer in the range of 8 to 16, n is 1 or 2, and R is a lower alkyl (C 1 -C 3 ) residue that is either unsubstituted or substituted with one or two hydroxyl groups, wherein the ratio of ether to ester in the enhancer composition is in the range of about 90:10 to 40:60 (v/v); and (c) a means for maintaining the transdermal delivery system in agent and enhancer composition transmitting relationship to the skin.
Claim 2
Dependent Claim
159 words
A transdermal delivery system for administering at least one pharmacologically active agent to a patient, comprising: (a) a source of the at least one pharmacologically active agent to be administered; (b) a source of a permeation enhancer composition comprising an ether component selected from the group consisting of diethylene glycol monoethyl ether, diethylene glycol monomethyl ether, and mixtures thereof, and an ester component given by the formula [CH 3 (CH 2 ) m COO] n R, in which m is an integer in the range of 8 to 16, n is 1 or 2, and R is a lower alkyl (C 1 -C 3 ) residue that is either unsubstituted or substituted with one or two hydroxyl groups, wherein the ratio of ether to ester in the enhancer composition is in the range of about 90:10 to 40:60 (v/v); and (c) a means for maintaining the transdermal delivery system in agent and enhancer composition transmitting relationship to the skin.
Claim 3
Dependent Claim
9 words
The system of claim 1, wherein n is 10.
Claim 4
Dependent Claim
14 words
The system of claim 1, wherein the ether component is diethylene glycol monoethyl ether.
Claim 5
Dependent Claim
32 words
The system of claim 1, wherein the ether component is diethylene glycol monoethyl ether and the ester component is propylene glycol monolaurate or propylene glycol monolaurate in combination with propylene glycol dilaurate.
Claim 6
Dependent Claim
19 words
The system of claim 1, wherein the ester component is a lower alkyl (C 1 -C 3 ) laurate.
Claim 7
Dependent Claim
16 words
The system of claim 2, wherein the at least one pharmacologically active agent is a steroid.
Claim 8
Dependent Claim
22 words
The composition of claim 4, wherein the at least one pharmacologically active agent comprises a progestogen, an estrogen, or a mixture thereof.
Claim 9
Dependent Claim
18 words
The composition of claim 4, wherein the progestogen is norethindrone or norethindrone acetate, and the estrogen is estradiol.
Claim 10
Dependent Claim
149 words
A transdermal delivery system for administering at least one pharmacologically active agent to a patient, comprising: a drug reservoir comprising a polymeric adhesive matrix; a backing layer laminated thereto, comprising a flexible polymer film; and contained with the reservoir, a selected pharmacologically active agent, and an enhancer composition comprising an ether component selected from the group consisting of diethylene glycol monoethyl ether, diethylene glycol monomethyl ether, and mixtures thereof, and an ester component given by the formula [CH 3 (CH 2 ) m COO] n R, in which m is an integer in the range of 8 to 16, n is 1 or 2, and R is a lower alkyl (C 1 -C 3 ) residue that is ether unsubstituted or substituted with one or two hydroxyl groups, wherein the ratio of ether to ester in the enhancer composition is in the range of about 90:10 to 40:60 (v/v).
Claim 11
Dependent Claim
149 words
A transdermal delivery system for administering at least one pharmacologically active agent to a patient, comprising: a drug reservoir comprising a polymeric adhesive matrix; a backing layer laminated thereto, comprising a flexible polymer film; and contained with the reservoir, a selected pharmacologically active agent, and an enhancer composition comprising an ether component selected from the group consisting of diethylene glycol monoethyl ether, diethylene glycol monomethyl ether, and mixtures thereof, and an ester component given by the formula [CH 3 (CH 2 ) m COO] n R, in which m is an integer in the range of 8 to 16, n is 1 or 2, and R is a lower alkyl (C 1 -C 3 ) residue that is ether unsubstituted or substituted with one or two hydroxyl groups, wherein the ratio of ether to ester in the enhancer composition is in the range of about 90:10 to 40:60 (v/v).
References Cited (Backward Citations)
US3551554A
Cited
US3472931A
Cited
US3598122B1
Cited
US3598123A
Cited
US3598122A
Cited
US3797494A
Cited
US3854480A
Cited
US3964482A
Cited
US3731683A
Cited
US3742951A
Cited
US3742951B1
Cited
US3923989A
Cited
US4006218A
Cited
US3926188A
Cited
US4316893A
Cited
US3989816A
Cited
US4405616A
Cited
US4460372A
Cited
US4379454A
Cited
US4440771A
Cited
US4435180A
Cited
US4746509A
Cited
US4559222A
Cited
US4537776A
Cited
US4552872A
Cited
US4557934A
Cited
US4704282A
Cited
US4568343A
Cited
US4717568A
Cited
EP0235090A1
Cited
EP0261429A1
Cited
WO1988001496A1
Cited
EP0272987A2
Cited
EP0275716A1
Cited
US4746515A
Cited
EP0279982A1
Cited
US4788062A
Cited
EP0285563A1
Cited
US4783450A
Cited
US4764379A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1994-09-30 | 1995-04-01 | 1995-10-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-09-30 | 1999-04-01 | 1999-10-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-09-30 | 2003-04-01 | 2003-10-01 | $7700.00 | Window Closed / Lapsed |