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US4954487A Expired / Lapsed US ⏱️ 0.0 years remaining

Penetrating topical pharmaceutical compositions

Assignee: Procter and Gamble Co
•
Filing: 1989-02-15
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Granted: 1990-09-04
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Expires: 2009-02-15
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Abstract

Abstract A large group of lipophilic, pharmacologically active compounds can be effectively delivered across intact skin by applying them topically in a binary, penetration-enhancing vehicle containing (1) a C3-C4 diol, diol ester, or diol ether and (2) a cell envelope-disordering compound. This vehicle provides surprising enhancement of skin penetration for the pharmacological active, compared to either component alone.

Inventors

  • 👤 Eugene R. Cooper
  • 👤 Maurice E. Loomans
  • 👤 Richard R. Wickett

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-05 23:24
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0014; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/14

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 123 words
A composition of matter for topical administration, said composition comprising (a) from about 0.5% to about 35% by weight of a nonsteroidal anti-inflammatory agent selected from the group consisting of salicylic acid, ibuprofen, sulindac, naproxen, ketoprofen, ethofenamate, and indomethacin, and the pharmaceutically-acceptable salts and esters thereof; (b) from 0% to about 70% by weight ethanol or 2-propanol; and (c) a penetration-enhancing carrier consisting essentially of (i) from about 10% to about 98% by weight of the composition of propylene glycol; and (ii) from about 1% to about 5% by weight of the composition of a cell envelope-disordering compound selected from the group consisting of methyl myristate, methyl laurate, methyl caprate, ethyl myristate, ethyl laurate, ethyl caprate, myristyl acetate, lauryl acetate and capric acetate.
Claim 2
Dependent Claim 123 words
A composition of matter for topical administration, said composition comprising (a) from about 0.5% to about 35% by weight of a nonsteroidal anti-inflammatory agent selected from the group consisting of salicylic acid, ibuprofen, sulindac, naproxen, ketoprofen, ethofenamate, and indomethacin, and the pharmaceutically-acceptable salts and esters thereof; (b) from 0% to about 70% by weight ethanol or 2-propanol; and (c) a penetration-enhancing carrier consisting essentially of (i) from about 10% to about 98% by weight of the composition of propylene glycol; and (ii) from about 1% to about 5% by weight of the composition of a cell envelope-disordering compound selected from the group consisting of methyl myristate, methyl laurate, methyl caprate, ethyl myristate, ethyl laurate, ethyl caprate, myristyl acetate, lauryl acetate and capric acetate.
Claim 3
Dependent Claim 30 words
The composition of claim 1 wherein the cell-envelope disordering compound is selected from the group consisting of methyl myristate, methyl laurate, ethyl myristate, ethyl laurate, myristyl acetate and lauryl acetate.
Claim 4
Dependent Claim 12 words
The composition of claim 1 wherein the nonsteroidal anti-inflammatory agent is ibuprofen.
Claim 5
Dependent Claim 12 words
The composition of claim 1 wherein the nonsteroidal anti-inflammatory agent is naproxen.
Claim 6
Dependent Claim 12 words
The composition of claim 1 wherein the nonsteroidal anti-inflammatory agent is ketoprofen.
Claim 7
Dependent Claim 13 words
The composition of claim 1 wherein the cell-envelope disordering compound is methyl laurate.
Claim 8
Dependent Claim 24 words
The composition of any of claim 1-6 wherein the concentration of the nonsteroidal anti-inflammatory agent is from about 1% to saturation in the composition.
Claim 9
Independent Claim 45 words
A method for treating and preventing pain or inflammation in a human or lower animal, which method comprises applying topically to a human or lower animal in need of such treatment a safe and effective amount of a composition according to any of claims 1-6.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1993-09-03 1994-03-05 1994-09-04 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1997-09-03 1998-03-05 1998-09-04 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2001-09-03 2002-03-05 2002-09-04 $7700.00 Window Closed / Lapsed

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