US4743588A
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Compositions and methods of enhancing transdermal and transmembrane penetration systemic agents
Assignee: Allergan Inc
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Filing: 1984-06-13
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Granted: 1988-05-10
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Expires: 2004-06-13
Abstract
Abstract Compositions and methods useful for enhancing the transdermal and transmembrane drug delivery of topical and systemic agents. The compositions and methods comprise the active agent together with an effective amount of certain amides of heterocyclic amines as defined herein as penetration enhancers and topically administering to human or animal skin or other membranes the resulting compositions.
Inventors
- 👤 Dorla Mirejovsky
- 👤 Harun Takruri
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 18:06
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/06; C; C07; C07D; C07D295/00; C07D295/16; C07D295/18; C07D295/182; C07D295/185; A61K47/00; A61K47/06; A61K47/22; A61K9/0012; A61K9/0014
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
83 words
A topical composition for enhancing the transdermal and transmembrane penetration of pharmacologically active substances which are systemically active in the blood stream which comprises an effective amount of said substance and from about 0.1 to 100% of a compound having the structural formula: ##STR11## in which: m is 4 to 9; R 1 is hydrogen or an alkyl group having from 1 to 8 carbon atoms; and R is a straight or branched chain alkyl group having from 1 to 20 carbon atoms.
Claim 2
Dependent Claim
83 words
A topical composition for enhancing the transdermal and transmembrane penetration of pharmacologically active substances which are systemically active in the blood stream which comprises an effective amount of said substance and from about 0.1 to 100% of a compound having the structural formula: ##STR11## in which: m is 4 to 9; R 1 is hydrogen or an alkyl group having from 1 to 8 carbon atoms; and R is a straight or branched chain alkyl group having from 1 to 20 carbon atoms.
Claim 3
Dependent Claim
13 words
The composition of claim 1 in which the active substance is an antibiotic.
Claim 4
Dependent Claim
23 words
The compound of claim 2 in which m is 4 to 6, R 1 is hydrogen, and R is from 1 to 20.
Claim 5
Dependent Claim
22 words
The composition of claim 3 in which m is 6, R 1 is hydrogen, and R is undecyl, the compound being hexamethylenelauramide.
Claim 6
Dependent Claim
19 words
The composition of claim 2 in which the antibiotic is selected from the group consisting of erythromycin and lincomycin.
Claim 7
Dependent Claim
14 words
The composition of claim 1 in which the active substance is an antifungal agent.
Claim 8
Dependent Claim
13 words
The composition of claim 1 in which the active substance is a steroid.
Claim 9
Independent Claim
87 words
A method for enhancing the transdermal and transmembrane penetrations of pharmacologically active systemic substances into the blood stream which comprises topically administering to a human or animal a composition comprising an effective amount of said active substance and a penetrating amount of a compound having the formula: ##STR12## in which: m is 4 to 9; R 1 is hydrogen or an alkyl group having from 1 to 8 carbon atoms; and R is a straight or branched chain alkyl group having from 1 to 20 carbon atoms.
Claim 10
Independent Claim
87 words
A method for enhancing the transdermal and transmembrane penetrations of pharmacologically active systemic substances into the blood stream which comprises topically administering to a human or animal a composition comprising an effective amount of said active substance and a penetrating amount of a compound having the formula: ##STR12## in which: m is 4 to 9; R 1 is hydrogen or an alkyl group having from 1 to 8 carbon atoms; and R is a straight or branched chain alkyl group having from 1 to 20 carbon atoms.
Claim 11
Dependent Claim
13 words
The method of claim 8 in which the active substance is an antibiotic.
Claim 12
Dependent Claim
14 words
The method of claim 8 in which the active substance is an antifungal agent.
Claim 13
Dependent Claim
13 words
The method of claim 8 in which the active substance is a steroid.
Claim 14
Dependent Claim
19 words
The method of claim 8 in which m is 6 and R 1 is undecyl, being the compound hexamethylenelauramide.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-05-10 | 1991-11-09 | 1992-05-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-05-10 | 1995-11-09 | 1996-05-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-05-10 | 1999-11-09 | 2000-05-10 | $7700.00 | Window Closed / Lapsed |