Enhancement of transdermal drug delivery

Claim 2

A topical composition for the transdermal delivery of physiologically active agents to mammals comprising an effective amount of a systemically active water soluble or solubilizable drug, a percutaneous transfer enhancing amount of menthol and a pharmaceutically acceptable vehicle comprising at least one pharmaceutically acceptable solvent or solubilizer for said menthol.

Claim 3

A product for topical use containing an effective amount of a systemically active, water soluble or solubilizable drug useful in medicinal therapy, a percutaneous transfer enhancing amount of menthol and a pharmaceutically acceptable vehicle comprising at least one pharmaceutically acceptable solvent or solubilizer for said menthol, as a combined preparation for sequential in any order or simultaneous use in said therapy.

Claim 4

A product for topical use containing an effective amount of a systemically active, water soluble or solubilizable drug useful in medicinal therapy, a percutaneous transfer enhancing amount of menthol and a pharmaceutically acceptable vehicle comprising at least one pharmaceutically acceptable solvent or solubilizer for said menthol, as a combined preparation for sequential in any order or simultaneous use in said therapy.

Claim 5

A composition or product as claimed in Claim 1 or Claim 2 wherein said menthol comprises by weight about 4% to about 16% of the composition or combination.

Claim 6

A composition or product as claimed in any one of Claims 1,2 or 3 in which the pharmaceutically acceptable vehicle further comprises at least one pharmaceutically acceptable solvent for the drug.

Claim 7

A composition or product as claimed in Claim 4 in which the solvent for each of the drug and menthol are in the amounts employed at least partially miscible with each other.

Claim 8

A composition or product as claimed in any one of Claims 1 to 3 in which the solvents for each of the drug and menthol are in the amounts employed wholly soluble or miscible with each other.

Claim 9

A composition or product as claimed in any one of Claims 1 to 6 in which the pharmaceutically acceptable vehicle is selected from one or more of the following glycerin, propylene glycol, isopropanol, ethanol, polyethylene glycol, block copolymer of ethylene glycol and propylene glycol, acetylated monoglyceride, lanolin, mineral oil, water and aqueous buffer.

Claim 10

A composition as claimed in any one of Claims 1 to 7 which is in the form of a cream, lotion, gel, ointment, suppository, spray or aerosol.

Claim 11

A unit transdermal dosage form for transdermal delivery of physiologically active agents to mammals comprising an effective amount of a systemically active water soluble or solubilizable drug comprised within at least one drug reservoir means; a percutaneous transfer enhancing amount of menthol comprised within menthol delivery means selected from the group consisting of any drug reservoir means, distinct menthol reservoir means, menthol matrix means and adhesive means; menthol solubilizing means and securing means for attaching the dosage form to a mammal.

Claim 12

A unit transdermal dosage form for transdermal delivery of physiologically active agents to mammals comprising an effective amount of a systemically active water soluble or solubilizable drug comprised within at least one drug reservoir means; a percutaneous transfer enhancing amount of menthol comprised within menthol delivery means selected from the group consisting of any drug reservoir means, distinct menthol reservoir means, menthol matrix means and adhesive means; menthol solubilizing means and securing means for attaching the dosage form to a mammal.

Claim 13

A unit transdermal dosage form as claimed in Claim 9 wherein the drug reservoir means comprises a pad or sponge impregnated with drug, a gel formulation of the drug,a composition or solution of the drug within a walled container permeable to the drug and available to the skin or membrane of the mammal, a multiplicity of distinct microreservoir compartments containing the drug or drug composition within or homogeneously throughout each reservoir.

Claim 14

A unit transdermal dosage form as claimed in Claim 9 wherein the menthol delivery means is selected from any of the drug reservoir means of Claim 10.

Claim 17

The method of Claim 12 wherein said drug and said percutaneous transfer amount of menthol are supplied to said mammal sequentially,

Claim 18

The method of Claim 12 wherein said drug and said percutaneous transfer amount of menthol are supplied to said mammal simultaneously.

Claim 19

The method of Claim 12, 13 or 14 wherein the menthol is soluble in said vehicle.

Claim 20

The method of Claim 12, 13 or 14 wherein the menthol is soluble in said vehicle and the drug is at least partially soluble in said vehicle.

Claim 21

The method of Claim 12 wherein each of the drug and the menthol are comprised in separate solubilizing compositions therefor and each of said compositions are substantially miscible with the other of said compositions and wherein at least one of said compositions contains said pharmaceutically acceptable vehicle.

Claim 22

CLAIMS FOR AUSTRIA 1. A process for preparing a topical composition for the transdermal delivery of physiologically active agents to mammals which comprises bringing an effective amount of a systemically active water soluble or solubilizable drug, a percutaneous transfer enhancing amount of menthol and a pharmaceutically acceptable vehicle comprising at least one pharmaceutically acceptable solvent or solubilizer for said menthol into a form suitable for therapeutic administration.

Claim 23

A process for preparing a product for topical use containing an effective amount of a systemically active, water soluble or solubilizable drug useful in medicinal therapy, a percutaneous transfer enhancing amount of menthol and a pharmaceutically acceptable vehicle comprising at least one pharmaceutically acceptable solvent or solubilizer for said menthol, which comprises formulating said product as a combined preparation for sequential in any order or simultaneous use in said therapy.

Claim 24

A process for preparing a product for topical use containing an effective amount of a systemically active, water soluble or solubilizable drug useful in medicinal therapy, a percutaneous transfer enhancing amount of menthol and a pharmaceutically acceptable vehicle comprising at least one pharmaceutically acceptable solvent or solubilizer for said menthol, which comprises formulating said product as a combined preparation for sequential in any order or simultaneous use in said therapy.

Claim 25

A process for preparing a composition or product as claimed in Claim 1 or Claim 2 wherein said menthol comprises by weight about 4% to about 16% of the composition or combination.

Claim 26

A process for preparing a composition or product as claimed in any one of Claims 1, 2 or 3 in which the pharmaceutically acceptable vehicle further i comprises at least one pharmaceutically acceptable solvent for the drug.

Claim 27

A process for preparing a composition or product as claimed in Claim 4 in which the solvent for each of the drug and menthol are in the amounts employed at least partially miscible with each other.

Claim 28

A process for preparing a composition or product as claimed in any one of Claims 1 to 3 in which the solvents for each of the drug and menthol are in the amounts employed wholly soluble or miscible with each other. 2

Claim 29

A process for preparing a composition or product as claimed in any one of Claims 1 to 6 in which the pharmaceutically acceptable vehicle is selected from one or more of the following glycerin, propylene glycol, isopropanol, ethanol, polyethylene glycol, block copolymer of ethylene glycol and propylene glycol, acetylated monoglyceride, lanolin, mineral oil, water and aqueous buffer.

Claim 30

A process for preparing a composition as claimed in any one of Claims 1 to 7 which is in the form of a cream, lotion, gel, ointment, suppository, spray or aerosol.

Claim 31

A process for preparing unit transdermal dosage form for transdermal delivery of physiologically active agents to mammals which comprises bringing an effective amount of a systemically active water soluble or solubilizable drug comprised within at least one drug reservoir means; a percutaneous transfer enhancing amount of menthol comprised within menthol delivery means selected from the group consisting of any drug reservoir means, distinct menthol reservoir means, menthol matrix means and adhesive means; menthol solubilising means and securing means for attaching the dosage form to a mammal into a form suitable for therapeutic administration.

Claim 32

A process for preparing unit transdermal dosage form for transdermal delivery of physiologically active agents to mammals which comprises bringing an effective amount of a systemically active water soluble or solubilizable drug comprised within at least one drug reservoir means; a percutaneous transfer enhancing amount of menthol comprised within menthol delivery means selected from the group consisting of any drug reservoir means, distinct menthol reservoir means, menthol matrix means and adhesive means; menthol solubilising means and securing means for attaching the dosage form to a mammal into a form suitable for therapeutic administration.

Claim 33

A process for preparing a unit transdermal dosage form as claimed in Claim 9 wherein the drug reservoir means comprises a pad or sponge impregnated with drug, a gel formulation of the drug, a composition or solution of the drug within a walled container permeable to the drug and available to the skin or membrane of the mammal, a multiplicity of distinct microreservoir compartments containing the drug or drug composition within or homogeneously throughout each reservoir.

Claim 34

A process for preparing a unit transdermal dosage form as claimed in Claim 9 wherein the menthol delivery means is selected from any of the drug reservoir means of Claim 10.