A novel transdermal pharmaceutical absorption dosage unit

Claim 2

A transdermal pharmaceutical-containing polymer matrix dosage unit comprising: a) a backing layer which is substantially impervious to the pharmaceutical to be delivered transdermally; b) a polymer matrix disc layer which is adhered to said backing layer and which has microdispersed therein an amount of the pharmaceutical which will provide a dosage amount of the pharmaceutical to be delivered transdermally; and c) an adhesive layer which is adhered to said pharmaceutical-containing polymer matrix disc layer and which has distributed therein an effective amount of one or more skin absorption enhancers which provide substantial skin absorption enhancement for said pharmaceutical; said dosage unit having an Enhancing Factor as herein defined of at least 1.2.

Claim 3

A transdermal pharmaceutical-containing polymer matrix dosage unit as claimed in claim 1 wherein the polymer matrix disc layer is a cross-linked polysiloxane polymer of the following formula: wherein R is alkyl or alkoxy having 1 -7 carbon atoms, vinyl, phenyl or a combination thereof and wherein n is about 100 to about 5,000.

Claim 4

A transdermal pharmaceutical-containing polymer matrix dosage unit as claimed in claim 2 wherein R in the polysiloxane formula is propoxy.

Claim 5

A transdermal pharmaceutical-containing polymer matrix dosage unit as claimed in any of claims 1 to 3 wherein the polymer matrix disc layer has a thickness of from 0.05 to 5mm.

Claim 6

A transdermal pharmaceutical-containing polymer matrix dosage unit as claimed in any of claims 1 to 4 wherein the polymer matrix disc provides microdispersian compartments having a cross sectional dimension of from about 10 to about 200 microns.

Claim 7

A transdermal pharmaceutical-containing polymer matrix dosage unit as claimed in any of claims 1 to 5 wherein the adhesive layer is made from a pressure-sensitive adhesive.

Claim 8

A transdermal pharmaceutical-containing polymer matrix dosage unit as claimed in any of claims 1 to 6 wherein the adhesive layer is made from a silicone polymer adhesive.

Claim 9

A transdermal pharmaceutical-containing polymer matrix dosage unit as claimed in any of claims 1 to 7 wherein the skin absorption enhancer is selected from decyl methyl suphoxide; 1-dodecylazacycloheptan-2-one; a compound of formula: wherein R is H or a lower alkyl group, m is 5-7 and n is 0-17,saturated and unsaturated fatty acids and their alkyl esters,alcohols, monoglycerides, diethanolamides, triethanolamine complexes, and N, N-dimethylamide derivatives, and acetate esters of said alcohol derivatives; propyl myristate; myristyl alcohol; propyl oleate; oleic acid; oleyl alcohol; oleyl acetate; monoolein; myristyl N, N-dimethyl amide; stearic acid; stearyl alcohol; propyl stearate; mono- stearin; mono-myristein; salicylic acid and derivatives; glycylglycine; N,N-diethyl-m-toluamide; crotamiton; and combinations thereof.

Claim 10

A transdermal pharmaceutical-containing polymer matrix dosage unit as claimed in any of claims 1 to 8 wherein the adhesive layer has distributed therein from about 1 to about 30 per cent of one or more skin absorption enhancers based on the weight of the polysiloxane adhesive.

Claim 11

A transdermal pharmaceutical-containing polymer matrix dosage unit as claimed in any of claims 1 to 9 wherein the Enhancing Factor as herein defined is at least about 2.0.

Claim 12

A transdermal pharmaceutical-containing polymer matrix dosage unit as claimed in any of claims 1 to 10 which has a releasable protective layer adhered to the adhesive layer.

Claim 13

A transdermal pharmaceutical-containing polymer matrix dosage unit as claimed in any of claims 1 to 1 wherein the pharmaceutical has anti-anginal, anti-arrhythmic, anti-hypertensive, tranquillizing, diuretic, central nervous system, anti-inflammatory, analgesic or anti-arthritic activity.

Claim 14

A transdermal pharmaceutical-containing polymer matrixdosage unit as claimed in any of claims 1 to 12 wherein the pharmaceutical is a steroid.

Claim 15

1 4. A transdermal pharmaceutical-containing polymer matrix dosage unit as claimed in claim 13, wherein the pharmaceutical comprises testosterone, estradiol, progesterone, hydrocortisone or indomethacin.

Claim 16

A-transdermal pharmaceutical-containing polymer matrix dosage unit as claimed in any of claims 1 to 12 wherein the pharmaceutical is nitroglycerin.

Claim 17

1 6. A method of producing a transdermal pharmaceutical-containing polymer matrix dosage unit having an Enhancing Factor as herein defined of at least 1.2, which method comprises: (a) adhering one side of a polymer matrix disc-layer which has microdispersed therein an amount of the pharmaceutical which will provide a dosage amount of the pharmaceutical to be delivered transdermally to a backing layer which is substantially impervious to said pharmaceutical, and (b) adhering the other side of said polymer matrix disc layer to an adhesive layer which has distributed therein an effective amount of one or more skin absorption enhancers which provide substantial skin absorption enhancement for said pharmaceutical.

Claim 18

1 6. A method of producing a transdermal pharmaceutical-containing polymer matrix dosage unit having an Enhancing Factor as herein defined of at least 1.2, which method comprises: (a) adhering one side of a polymer matrix disc-layer which has microdispersed therein an amount of the pharmaceutical which will provide a dosage amount of the pharmaceutical to be delivered transdermally to a backing layer which is substantially impervious to said pharmaceutical, and (b) adhering the other side of said polymer matrix disc layer to an adhesive layer which has distributed therein an effective amount of one or more skin absorption enhancers which provide substantial skin absorption enhancement for said pharmaceutical.