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EP0267051A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Transdermal administration of amines

Assignee: Purepac Inc
•
Filing: 1987-11-06
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Granted: —
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Expires: 2007-11-06
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Abstract

Abstract Transdermal or percutaneous administration of systemic dosages of physiologically active amines to humans is accomplished at an increased rate by diluting the amine or a salt of said amine by dissolving it in a nonpolar nonvolatile solvent before bringing it into contact with the skin. The dilution may be applied to the skin from a supply absorbed in a polymeric matrix or sponge.

Inventors

  • 👤 Larry R. Brown
  • 👤 John F. Cline
  • 👤 S. James Davidson

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-02 12:45
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/08; A61K47/12; A61K47/14; A61K9/00; A61K9/0012; A61K9/0014; A61K9/70; A61K9/7023; A61P; A61P43/00

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 42 words
A composition adapted to be maintained in contact with human skin to provide systemic administration of a physiologically active non-­irratating amine in said human, said composition comprising a dilution comprising said amine dissolved in an effective amount of a nonpolar nonvolatile solvent.
Claim 2
Dependent Claim 42 words
A composition adapted to be maintained in contact with human skin to provide systemic administration of a physiologically active non-­irratating amine in said human, said composition comprising a dilution comprising said amine dissolved in an effective amount of a nonpolar nonvolatile solvent.
Claim 3
Dependent Claim 54 words
A composition adapted to be maintained in contact with human skin to provide systemic administration of a physiologically active amine in said human, said composition comprising a dilution comprising a salt of said amine with a fatty acid having 8 to 20 carbon atoms dissolved in an effective amount of a nonpolar nonvolatile solvent.
Claim 4
Dependent Claim 54 words
A composition adapted to be maintained in contact with human skin to provide systemic administration of a physiologically active amine in said human, said composition comprising a dilution comprising a salt of said amine with a fatty acid having 8 to 20 carbon atoms dissolved in an effective amount of a nonpolar nonvolatile solvent.
Claim 5
Dependent Claim 27 words
A composition as claimed in claim 1 or claim 2 in which said solvent has a dielectic constant less than 4 and a boiling point above 150°C.
Claim 6
Dependent Claim 19 words
A composition as claimed in any one of claims 1 to 3 in which said amine is an antihistamine.
Claim 7
Dependent Claim 45 words
An article adapted to be maintained in contact with human skin to provide systemic administration of a physiologically active amine in said human, said article comprising a composition as claimed in any one of claims 1 to 4 absorbed in a solid porous water-insoluble carrier.
Claim 8
Dependent Claim 15 words
An article as claimed in claim 5 in which said carrier comprises a polymeric matrix.
Claim 9
Dependent Claim 15 words
An article as claimed in claim 6 in which said polymeric matrix comprises cellulose triacetate.
Claim 10
Dependent Claim 87 words
The use of a physiologically active non-­irritating amine, e.g., an antihistamine, in preparing a medicament for administration systemically to a human by providing a dilution comprising said amine dissolved in an effective amount of a nonpolar nonvolatile solvent, or by providing a dilution of a salt of said amine with a fatty acid having 8 to 20 carbon atoms dissolved in an effective amount of a nonpolar nonvolatile solvent, and in either case maintaining said dilution in a form adapted to contact the skin of said human.
Claim 11
Dependent Claim 87 words
The use of a physiologically active non-­irritating amine, e.g., an antihistamine, in preparing a medicament for administration systemically to a human by providing a dilution comprising said amine dissolved in an effective amount of a nonpolar nonvolatile solvent, or by providing a dilution of a salt of said amine with a fatty acid having 8 to 20 carbon atoms dissolved in an effective amount of a nonpolar nonvolatile solvent, and in either case maintaining said dilution in a form adapted to contact the skin of said human.
Claim 12
Dependent Claim 26 words
The use claimed in claim 8 in which said dilution is absorbed into a solid porous water-­insoluble carrier designed to contact the skin of said human
Claim 13
Dependent Claim 14 words
The use claimed in claim 9 in which said carrier comprises a polymeric matrix.
Claim 14
Dependent Claim 14 words
The use claimed in claim 10 in which said polymeric matrix comprises cellulose triacetate.
Claim 15
Dependent Claim 30 words
The use claimed in any one of claims 8 to 11 in which said dilution includes an excess of said acid above the stoichiometric amount required to form said salt.
Claim 16
Dependent Claim 28 words
The use claimed in any one of claims 8 to 12 in which said solvent has a dielectric constant less than 4 and a boiling point above 150°C.
Claim 17
Dependent Claim 23 words
The use of a nonpolar nonvolatile solvent in diluting a physiologically active amine or salt thereof in preparation for transdermal or percutaneous delivery.
Claim 18
Dependent Claim 23 words
The use of a nonpolar nonvolatile solvent in diluting a physiologically active amine or salt thereof in preparation for transdermal or percutaneous delivery.

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