Patent US5053227A successfully refreshed from Google Patents.
US5053227A
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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 13:22
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).
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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) | 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 |