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US4863970A Expired / Lapsed US ⏱️ 0.0 years remaining

Penetration enhancement with binary system of oleic acid, oleins, and oleyl alcohol with lower alcohols

Assignee: Actavis Laboratories UT Inc
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Filing: 1988-07-13
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Granted: 1989-09-05
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Expires: 2008-07-13
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Abstract

Abstract Penetration-enhancing pharmaceutical compositions for topical transepidermal and percutaneous application are disclosed which are non-irritating to the skin. These compositions are made up of a safe and effective amount of an active pharmaceutical permeant, including hydrophilic salt forms, contained in a novel penetration-enhancing vehicle comprising, (i) 1-95% w. of a cell-envelope disordering compound selected from the group consisting of oleic acid, oleyl alcohol, glycerol monoleate, glycerol dioleate, glycerol trioleate and mixtures thereof, (ii) 5-75% w., and preferably 5-49% w., of a lower alkanol selected from the group consisting of ethanol, propanol and isopropanol and mixtures thereof and (iii) 0-45% w., and preferably 1-45% w., of an inert diluent which, according to properties of the permeant used, may range from hydrophilic to hydrophobic. Water, polyethylene or polypropylene glycols and mineral oil are exemplary diluents.

Inventors

  • 👤 Dinesh C. Patel
  • 👤 Yunik Chang

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-26 23:08
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/08; A61K47/14; A61K47/10; A61K47/12; A61K9/00; A61K9/0012; A61K9/0014

Claims Analysis

Total Claims: 41
Claim 1
Independent Claim 97 words
A pharmaceutical composition for topical application having penetration-enhancing properties consisting essentially of: (a) a safe and effective amount of an active pharmaceutical agent contained in, (b) a penetration-enhancing vehicle exclusive of diols and N-cyclic solvents consisting essentially of: (i) 1-95% by weight of one or more cell-envelope disordering compounds selected from the group consisting of oleic acid, oleyl alcohol, glycerol esters of oleic acid and mixtures thereof; (ii) 5-75% by weight of a lower alkanol selected from the group consisting of ethanol, propanol and isopropanol and mixtures thereof; and (iii) 0-45% by weight of an inert diluent.
Claim 2
Dependent Claim 97 words
A pharmaceutical composition for topical application having penetration-enhancing properties consisting essentially of: (a) a safe and effective amount of an active pharmaceutical agent contained in, (b) a penetration-enhancing vehicle exclusive of diols and N-cyclic solvents consisting essentially of: (i) 1-95% by weight of one or more cell-envelope disordering compounds selected from the group consisting of oleic acid, oleyl alcohol, glycerol esters of oleic acid and mixtures thereof; (ii) 5-75% by weight of a lower alkanol selected from the group consisting of ethanol, propanol and isopropanol and mixtures thereof; and (iii) 0-45% by weight of an inert diluent.
Claim 3
Dependent Claim 21 words
A composition according to claim 1 wherein the lower alkanol is present in amounts of between 5 and 49% by weight.
Claim 4
Dependent Claim 38 words
A composition according to claim 2 wherein the active pharmaceutical agent is present in amount ranging from about 0.01 to 50% by weight and the penetration enhancing vehicle is present in amounts ranging from about 50-99.99% by weight.
Claim 5
Dependent Claim 78 words
A composition according to claim 3 wherein the cell-envelope disordering compounds are members selected from the following groupings: (1) oleic acid and oleyl alcohol or mixtures thereof; (2) one or more glycerol esters of oleic acid; (3) oleic acid and one or more glycerol esters of oleic acid; (4) oleyl alcohol and one or more glycerols ester of oleic acid; and (5) mixtures of oleic acid and oleyl alcohol and one or more glycerol esters of oleic acid.
Claim 6
Dependent Claim 40 words
A composition according to claim 4 wherein the active pharmaceutical agent is present in amounts ranging from about 0.01 to 30% by weight and the penetration enhancing vehicle is present in amounts ranging from about 70 to 99.99% by weight.
Claim 7
Dependent Claim 28 words
A composition according to claim 5 wherein the cell-envelope disordering compound is a member selected from the group consisting of oleic acid and oleyl alcohol and mixtures thereof.
Claim 8
Dependent Claim 14 words
A composition according to claim 5 wherein the cell-envelope disordering compound is oleic acid.
Claim 9
Dependent Claim 14 words
A composition according to claim 6 wherein the cell-envelope disordering compound is oleyl alcohol.
Claim 10
Dependent Claim 29 words
A composition according to claim 5 wherein the cell-envelope disordering compound is a member selected from the group consisting of a one or more glycerol esters of oleic acid.
Claim 11
Dependent Claim 14 words
A composition according to claim 9 wherein the cell-envelope disordering compound is glycerol monooleate.
Claim 12
Dependent Claim 14 words
A composition according to claim 8 wherein the cell-envelope disordering compound is glycerol dioleate.
Claim 13
Dependent Claim 14 words
A composition according to claim 7 wherein the cell-envelope disordering compound is glycerol trioleate.
Claim 14
Dependent Claim 33 words
A composition according to claim 5 wherein the cell-envelope disordering compound is oleic acid admixed with a member selected from the group consisting of a one or more glycerol esters of oleic acid.
Claim 15
Dependent Claim 14 words
A composition according to claim 13 wherein the cell-envelope disordering compound is glycerol monooleate.
Claim 16
Dependent Claim 14 words
A composition according to claim 13 wherein the cell-envelope disordering compound is glycerol dioleate.
Claim 17
Dependent Claim 14 words
A composition according to claim 13 wherein the cell-envelope disordering compound is glycerol trioleate.
Claim 18
Dependent Claim 33 words
A composition according to claim 5 wherein the cell-envelope disordering compound is oleyl alcohol admixed with a member selected from the group consisting of a one or more glycerol esters of oleic acid.
Claim 19
Dependent Claim 14 words
A composition according to claim 17 wherein the cell-envelope disordering compound is glycerol monooleate.
Claim 20
Dependent Claim 14 words
A composition according to claim 17 wherein the cell-envelope disordering compound is glycerol dioleate.
Claim 21
Dependent Claim 14 words
A composition according to claim 17 wherein the cell-envelope disordering compound is glycerol trioleate.
Claim 22
Dependent Claim 26 words
A composition according to claim 5 wherein the alcohol is present in the penetration enhancer vehicle in amounts of between about 20 and 49% by weight.
Claim 23
Dependent Claim 26 words
A composition according to claim 4 wherein the inert diluent is present in the penetration enhancer vehicle in amounts ranging from 1 to 45% by weight.
Claim 24
Dependent Claim 39 words
A composition according to claim 22 wherein the active pharmaceutical agent is present in amounts ranging from about 0.01 to 30% by weight and the penetration enhancing is present in amounts ranging from about 70 to 99.99% by weight.
Claim 25
Dependent Claim 28 words
A composition according to claim 23 wherein the cell-envelope disordering compound is a member selected from the group consisting of oleic acid and oleyl alcohol and mixtures thereof.
Claim 26
Dependent Claim 14 words
A composition according to claim 24 wherein the cell-envelope disordering compound is oleic acid.
Claim 27
Dependent Claim 14 words
A composition according to claim 24 wherein the cell-envelope disordering compound is oleyl alcohol.
Claim 28
Dependent Claim 29 words
A method according to claim 23 wherein the cell-envelope disordering compound is a member selected from the group consisting of a one or more glycerol esters of oleic acid.
Claim 29
Dependent Claim 14 words
A composition according to claim 27 wherein the cell-envelope disordering compound is glycerol monooleate.
Claim 30
Dependent Claim 14 words
A composition according to claim 27 wherein the cell-envelope disordering compound is glycerol dioleate.
Claim 31
Dependent Claim 14 words
A composition according to claim 27 wherein the cell-envelope disordering compound is glycerol trioleate.
Claim 32
Dependent Claim 33 words
A composition according to claim 23 wherein the cell-envelope disordering compound is oleic acid admixed with a member selected from the group consisting of a one or more glycerol esters of oleic acid.
Claim 33
Dependent Claim 14 words
A composition according to claim 31 wherein the cell-envelope disordering compound is glycerol monooleate.
Claim 34
Dependent Claim 14 words
A composition according to claim 31 wherein the cell-envelope disordering compound is glycerol dioleate.
Claim 35
Dependent Claim 14 words
A composition according to claim 31 wherein the cell-envelope disordering compound is glycerol trioleate.
Claim 36
Dependent Claim 33 words
A composition according to claim 23 wherein the cell-envelope disordering compound is oleyl alcohol admixed with a member selected from the group consisting of a one or more glycerol esters of oleic acid.
Claim 37
Dependent Claim 14 words
A composition according to claim 35 wherein the cell-envelope disordering compound is glycerol monooleate.
Claim 38
Dependent Claim 14 words
A composition according to claim 35 wherein the cell-envelope disordering compound is glycerol dioleate.
Claim 39
Dependent Claim 14 words
A composition according to claim 35 wherein the cell-envelope disordering compound is glycerol trioleate.
Claim 40
Dependent Claim 45 words
A composition according to claim 23 wherein the inert diluent is a member selected from the group consisting of water, polypropylene glycol, polyethylene glycol, polyvinyl alcohols, polyvinylpyrrolidone, mineral oil, silicone oil, ethylene-vinyl acteate polymers or other suitable water or oil soluble low molecular weight polymers.
Claim 41
Dependent Claim 25 words
A composition according to claim 23 wherein the alcohol is present in the penetration enhancer combination in amounts between about 20 and 49% by weight.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1992-09-04 1993-03-06 1993-09-05 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1996-09-04 1997-03-06 1997-09-05 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2000-09-04 2001-03-06 2001-09-05 $7700.00 Window Closed / Lapsed

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