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US4849418A Expired / Lapsed US ⏱️ 0.0 years remaining

Transdermally absorbable water-containing preparations of arylpropionic acid derivatives and process for preparing same

Assignee: Dolorgiet Beteiligungs GmbH
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Filing: 1987-11-16
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Granted: 1989-07-18
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Expires: 2007-11-16
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Abstract

Abstract Transdermally absorbable water-containing preparations of therapeutically active arylpropionic acid derivatives comprises 1 to 15% by weight of such active ingredient, from 10 to 40% by weight of polyoxyethylene polyoxypropylene copolymers, from 10 to 50% by weight of one or more physiologically acceptable organic solvents, optionally up to 1% by weight of preservatives, colorants and/or perfumes, and at least 10% by weight of water. From polyoxyethylene polyoxypropylene copolymers having a relative molecular weight of more than 6,000 there may also be prepared gels, if certain ratios of amounts are chosen.

Inventors

  • 👤 Manfred Lohner
  • 👤 Hans H. Wagener

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 19:00
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0014; A61K31/00; A61K31/185; A61K31/19; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/20; A61K47/26; A61P; A61P25/00; A61P25/04; A61P29/00

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 66 words
A transdermally absorbable water-containing analgesic, antirheumatic, antiinflammatory, gel preparation comprising from 5 to 10% of ibuprofen, from 10 to 40% by weight of polyoxyethylene polyoxypropylene copolymers, from 10 to 50% by weight of one or more physiologically acceptable organic solvents, optionally up to 1% by weight of preservatives, colorants and/or perfumes, and at least 10% by weight of water, said gel being free of neutralizing bases.
Claim 2
Dependent Claim 66 words
A transdermally absorbable water-containing analgesic, antirheumatic, antiinflammatory, gel preparation comprising from 5 to 10% of ibuprofen, from 10 to 40% by weight of polyoxyethylene polyoxypropylene copolymers, from 10 to 50% by weight of one or more physiologically acceptable organic solvents, optionally up to 1% by weight of preservatives, colorants and/or perfumes, and at least 10% by weight of water, said gel being free of neutralizing bases.
Claim 3
Dependent Claim 33 words
A preparation according to claim 1, which comprises from 15 to 32% by weight of polyoxyethylene polyoxypropylene copolymers, and from 17 to 44% by weight of one or more physiologically acceptable organic solvents.
Claim 4
Dependent Claim 20 words
A preparation according to claim 1, wherein the polyoxyethylene polyoxypropylene copolymers have relative molecular weights of from 1,000 to 13,000.
Claim 5
Dependent Claim 22 words
A preparation according to claim 1, characterized in that the polyoxyethylene polyoxypropylene copolymers have relative molecular weights of from 6,000 to 13,000.
Claim 6
Dependent Claim 59 words
A preparation according to claim 1, characterized in that as the physiologically acceptable organic solvents there are used dimethyl sulfoxide or mono-, di- or tri-hydroxy straight-chain, branched or cyclic alcohols having from 2 to 6 carbon atoms in the carbon backbone into which 0 to 2 oxygen atoms have been inserted, or polyoxyalkylene fatty alcohol ethers or mixtures thereof.
Claim 7
Dependent Claim 27 words
A preparation according to claim 5, characterized in that there are used as solvents ethanol, isopropanol, 1,2-propanediol, glycerol, isosorbide, dimethylisosorbide, polyoxyethylene-(4)-lauryl ether, polyoxypropylene-(15)-stearyl ether or mixtures thereof.
Claim 8
Dependent Claim 35 words
A preparation according to claim 1, characterized in that it further comprises up to 2% by weight of a blood circulation-promoting or rubefacient substance selected from the group consisting of benzyl nicotinate and a salicylate.
Claim 9
Dependent Claim 18 words
A preparation according to claim 7, characterized in that the blood circulation-promoting or rubefacient substance is benzyl nicotinate.
Claim 10
Dependent Claim 18 words
A preparation according to claim 7, characterized in that the blood circulation-promoting or rubefacient substance is a salicylate.
Claim 11
Dependent Claim 92 words
A process for making a transdermally absorbable water-containing antirheumatic, anti-inflammatory, analgesic gel characterized in that a mixture comprising from 5 to 10% by weight of ibuprofen as an active ingredient, from 10 to 40% by weight of polyoxyethylene polyoxypropylene copolymers, from 10 to 50% by weight of one or more physiologically acceptable organic solvents, optionally up to 1% by weight of preservatives, colorants and/or perfumes, and at least 10% by weight of water are heated with stirring at from 40° C. to 90° C. in the absence of neutralizing bases then cooled.
Claim 12
Dependent Claim 92 words
A process for making a transdermally absorbable water-containing antirheumatic, anti-inflammatory, analgesic gel characterized in that a mixture comprising from 5 to 10% by weight of ibuprofen as an active ingredient, from 10 to 40% by weight of polyoxyethylene polyoxypropylene copolymers, from 10 to 50% by weight of one or more physiologically acceptable organic solvents, optionally up to 1% by weight of preservatives, colorants and/or perfumes, and at least 10% by weight of water are heated with stirring at from 40° C. to 90° C. in the absence of neutralizing bases then cooled.
Claim 13
Dependent Claim 56 words
The process for making a gel according to claim 10, characterized in that from 15 to 32% by weight of polyoxyethylene polyoxypropylene copolymers and from 17 to 44% by weight of one or more physiologically acceptable organic solvents are heated at from 80° C. to 90° C. in the absence of neutralizing bases and then cooled.
Claim 14
Dependent Claim 55 words
The process according to claim 10, characterized in that, as the physiologically acceptable organic solvents there are used dimethyl sulfoxide or mono-, di- or trihydroxy straight-chain, branched or cyclic alcohols having from 2 to 6 carbon atoms and 0 to 2 oxygen atoms in the carbon backbone or polyoxyalkylene fatty alcohol ethers or mixtures thereof.
Claim 15
Dependent Claim 27 words
The process according to claim 12, characterized in that there are used as solvents ethanol, isopropanol, 1,2-propanediol, glycerol, isosorbide, dimethylisosorbide, polyoxyethylene-(4)-lauryl ether, polyoxypropylene-(15)-stearyl ether or mixtures thereof.
Claim 16
Dependent Claim 37 words
The process according to claim 10, characterized in that the mixture further comprises up to 2% by weight of a blood circulation-promoting or rubefacient substance selected from the group consisting of a benzyl nicotinate and a salicylate.
Claim 17
Dependent Claim 18 words
The process according to claim 14, characterized in that the blood circulation-promoting or rubefacient substance is benzyl nicotinate.
Claim 18
Dependent Claim 18 words
The process according to claim 14, characterized in that the blood circulation-promoting or rubefacient substance is a salicylate.

References Cited (Backward Citations)

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DE2708152A1 Cited
EP0072462A2 Cited
US4555524A Cited
US4533546A Cited
US4511563A Cited
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EP0178436A1 Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1992-07-17 1993-01-16 1993-07-18 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1996-07-17 1997-01-16 1997-07-18 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2000-07-17 2001-01-16 2001-07-18 $7700.00 Window Closed / Lapsed

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