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EP0165696A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Improved transdermal dosage form

Assignee: Wyeth LLC
•
Filing: 1985-05-09
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Granted: —
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Expires: 2005-05-09
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Abstract

Abstract ine invention concerns an improves pnarmaceuticar composition and dosage form for the transdermal delivery of a therapeutic agent dispersed in a solvent system comprising a mixture of propylene glycol and glycerine in the ratio of about 1:1 to about 1:5 by weight of each other and if required such other pharmaceutically acceptable solvent or solvents necessary to achieve a solubility of at least 0.5 milligrams millilitre of the therapeutic agent in the solvent system, the amount of propylene glycol and glycerine being such as to enhance the transdermal penetration of the therapeutic agent.

Inventors

  • 👤 Pramod Purushottam Sarpotdar
  • 👤 James Lawrence Gaskill
  • 👤 Robert Peter Giannini

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-04 23:55
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K9/7084; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/12

Claims Analysis

Total Claims: 22
Claim 1
Independent Claim 91 words
A pharmaceutical composition for the transdermal delivery of a therapeutic agent dispersed in a solvent system characterised in that the solvent system comprises a mixture of propylene glycol and glycerine in the ratio of about 1:1 to about 1:5 by weight of each other and if required such other pharmaceutically acceptable solvent or solvents necessary to achieve a solubility of at least 0.5 milligrams/millilitre of the therapeutic agent in the solvent system, the amount of propylene glycol and glycerine being such as to enhance the transdermal penetration of the therapeutic agent.
Claim 2
Dependent Claim 91 words
A pharmaceutical composition for the transdermal delivery of a therapeutic agent dispersed in a solvent system characterised in that the solvent system comprises a mixture of propylene glycol and glycerine in the ratio of about 1:1 to about 1:5 by weight of each other and if required such other pharmaceutically acceptable solvent or solvents necessary to achieve a solubility of at least 0.5 milligrams/millilitre of the therapeutic agent in the solvent system, the amount of propylene glycol and glycerine being such as to enhance the transdermal penetration of the therapeutic agent.
Claim 3
Dependent Claim 24 words
A composition as claimed in Claim 1 in which the propylene glycol-glycerine mixture comprises 10 to 93 per cent by weight of the composition.
Claim 4
Dependent Claim 22 words
A composition as claimed in Claim 1 or Claim 2 in which the propylene glycol:glycerine ratio is about 1:1 to about 1:4.
Claim 5
Dependent Claim 18 words
A composition as claimed in any one of Claims 1 to 3 further comprising an additional penetration enhancer.
Claim 6
Dependent Claim 34 words
A composition as claimed in any one of Claims 1 to 4 wherein the therapeutic agent is soluble in the solvent system in an amount of at least 3 milligrams per millilitre of solvent.
Claim 7
Dependent Claim 25 words
A composition as claimed in any one of Claims 1 to 5 wherein the therapeutic agent comprises 1 to 50 per cent of the composition.
Claim 8
Dependent Claim 23 words
A pharmaceutical transdermal dosage form comprising a matrix having dispersed therein a composition as claimed in any one of Claims 1 to 6.
Claim 9
Dependent Claim 16 words
A dosage form as claimed in Claim 7 in which the matrix is a non-polymeric gel.
Claim 10
Dependent Claim 21 words
A dosage form as claimed in Claim 8 in which the non-polymeric gel comprises a metal salt of a fatty acid.
Claim 11
Dependent Claim 87 words
A pharmaceutical dosage form for transdermal administration of an active ingredient comprising a thin flexible non-polymeric matrix in planar form further comprising: a) about 3 to 50 per cent by weight of solid non-polymeric gel; b) about 10 to 93 per cent by weight of a solvent medium dispersed in said gel comprising propylene glycol and glycerine in a ratio of about 35:65 by weight of each other; and c) from 1 to 50 per cent by weight of a therapeutic agent dispersed in said solvent medium.
Claim 12
Dependent Claim 87 words
A pharmaceutical dosage form for transdermal administration of an active ingredient comprising a thin flexible non-polymeric matrix in planar form further comprising: a) about 3 to 50 per cent by weight of solid non-polymeric gel; b) about 10 to 93 per cent by weight of a solvent medium dispersed in said gel comprising propylene glycol and glycerine in a ratio of about 35:65 by weight of each other; and c) from 1 to 50 per cent by weight of a therapeutic agent dispersed in said solvent medium.
Claim 13
Dependent Claim 47 words
A dosage form as claimed in Claim 9 or Claim 10 in which the non-polymeric matrix comprises a gelling agent selected from sodium stearate, sodium caprylate, sodium laurate, sodium myristate, sodium palmilate, sodium oleate, potassium caprylate, potassium laurate, potassium myristate, potassium palmitate, potassium oleate and potassium stearate.
Claim 14
Dependent Claim 28 words
A dosage form as claimed in any one of Claims 7 to 11 in which the matrix comprises about 6 per cent by weight of the dosage form.
Claim 15
Dependent Claim 40 words
A drug delivery system suitable for the transdermal administration of a therapeutic agent comprising a dosage form as claimed in any one of claims 7 to 12 and an impervious backing member adapted to attach said system to the skin.
Claim 16
Dependent Claim 40 words
A dosage form or composition as claimed in any one of Claims 1 to 14 in which the therapeutic agent is guanabenz, 17-beta-estradiol, indo- methacin, propanolol, phenobarbital, novacaine, benzocaine, xylocaine, gentamycin, amphotericim, clonidine, dezocine, ethinyl estradiol, levo- norgestrel or verapamil.
Claim 17
Dependent Claim 87 words
A process for preparing a transdermal pharmaceutical composition which comprises bringing into association a transdermally effective therapeutic agent, propylene glycol, glycerine and if required such other solvent or solvents to achieve a solubility of at least about 0.5 milligrams per millilitre of the therapeutic agent in the mixture of solvents, the ratio of propylene glycol to glycerine being from about 1:1 to 1:5 by weight of each other and the amount of propylene glycol - glycerine mixture being such as to enhance the penetration of the drug.
Claim 18
Dependent Claim 87 words
A process for preparing a transdermal pharmaceutical composition which comprises bringing into association a transdermally effective therapeutic agent, propylene glycol, glycerine and if required such other solvent or solvents to achieve a solubility of at least about 0.5 milligrams per millilitre of the therapeutic agent in the mixture of solvents, the ratio of propylene glycol to glycerine being from about 1:1 to 1:5 by weight of each other and the amount of propylene glycol - glycerine mixture being such as to enhance the penetration of the drug.
Claim 19
Dependent Claim 102 words
A process for preparing a pharmaceutical dosage form which comprises bringing into association a matrix or matrix forming agent, a transdermally effective therapeutic agent, propylene glycol, other solvent or solvents to achieve a solubility of at least 0.5 milligrams per millilitre of the therapeutic agent in the mixture of solvents; the ratio of propylene glycol to glycerine being from about 1:1 to 1:5 by weight of each other and the amount of propylene glycol - glycerine mixture being such as to enhance the penetration of the drug, and if required forming the matrix from the matrix forming agent at any suitable stage.
Claim 20
Dependent Claim 102 words
A process for preparing a pharmaceutical dosage form which comprises bringing into association a matrix or matrix forming agent, a transdermally effective therapeutic agent, propylene glycol, other solvent or solvents to achieve a solubility of at least 0.5 milligrams per millilitre of the therapeutic agent in the mixture of solvents; the ratio of propylene glycol to glycerine being from about 1:1 to 1:5 by weight of each other and the amount of propylene glycol - glycerine mixture being such as to enhance the penetration of the drug, and if required forming the matrix from the matrix forming agent at any suitable stage.
Claim 21
Dependent Claim 16 words
A process as claimed in Claim 16 in which the matrix comprises a non polymeric gel.
Claim 22
Dependent Claim 20 words
A process as claimed in Claim 17 in which the , matrix comprises a metal salt of a fatty acid.

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