Monolithic user-activated transdermal therapeutic system

Claim 2

A monolithic therapeutic substance non-releasing drug delivery system having a removable protective layer thereon, said system comprising (a) a monolithic therapeutic substance reservoir containing a therapeutic agent or precursor of said therapeutic agent in a first form which cannot permeate from said therapeutic reservoir through said system to the surface of said system which is or was in contact with said removable protective layer; (b) an activating agent reservoir containing a system activating agent; (c) a burstable seal or membrane between (a) and (b) which is impermeable to said system activating agent and said therapeutic agent or precursor of said therapeutic agent; and (d) an occlusive backing layer; wherein upon bursting of said burstable seal or said burstable membrane, said system activating agent activates said system by contacting and converting said therapeutic agent or precursor of said therapeutic agent from said first form into a therapeutic agent second form which second form migrates from said therapeutic agent or precursor of said therapeutic reservoir to said surface of said system which is or was in contact with said removable protective layer whereby said system becomes a therapeutic substance releasing delivery system.

Claim 3

A drug delivery system of claim 1 wherein said burstable membrane and burstable seal are broken by application of a pressure between about 10 and 50 pounds force.

Claim 4

A drug delivery system of claim 1 wherein said burstable membrane and burstable seal are a membrane and seal which selectively ruptured as compared to other membranes, seals and layers of said system under pressures of about 10 to about 50 pounds force.

Claim 5

A drug delivery system of claim 3 wherein said burstable seal is a heat seal which is no greater than about 1/6 as wide as any other heat seal of the same material in said system.

Claim 6

A drug delivery system of claim 3 wherein said burstable heat seal is from about 0.5 to about 2.0 mm wide.

Claim 7

A drug delivery system of claim 3 wherein said burstable membrane is selectively reinforced with unreinforced areas being no greater than about 20% to about 80% as wide as any other membrane or layer in said system made of the same material.

Claim 8

A drug delivery system of claim 6 where said unreinforced areas of said burstable membrane are no greater than about 10 to about 50 microns thick.

Claim 9

A drug delivery system of claim 3 wherein said burstable membrane is a membrane which would otherwise not be burstable under normal use but which has been selectively weakened.

Claim 10

A drug delivery system of claim 8 wherein said burstable membrane has been made selectively burstable by controlled depth slitting.

Claim 11

A drug delivery system of claim 1 wherein said therapeutic agent is selected from fentanyl, sufentanyl, isoniazid, rifampin, baclofen, terbutaline, theophylline, arecoline, nicotine, progesterone, methyltestosterone, desoxycorticosterone, triprolidine, diphenhydramine, tripelenamine, scopolamine, methscopolamine, nitroglycerine, metoprolol, estradiol, 3-([5-amino-1-carboxy]-pentylmino)-1-carboxy methyl-2,3,4,5-tetrahydro-1H-1-benzazepine-2-one, formoterol, physostigmine, and naloxone.

Claim 12

A monolithic therapeutic substance non-releasing drug delivery system having a removable protective layer thereon, said system comprising (a) a monolithic therapeutic substance reservoir containing a therapeutic agent in a form which cannot permeate from said monolithic substance reservoir through said system to the surface of said system which is or was in contact with said removable protective layer; (b) an activating agent reservoir containing a system activating agent; (c) a burstable membrane or burstable seal between said activating agent reservoir and the portions of said system through which said therapeutic agent must migrate in order to reach said surface which is or was in contact with said removable protective layer but through which said therapeutic agent cannot permeate; and (d) an occlusive backing layer; wherein, upon bursting of said burstable membrane or burstable seal, said activating agent activates said system by contacting said portions through which said therapeutic agent must migrate but cannot migrate to reach the surface of said system which is or was in contact with said removable protection layer and modifying such portions into a form through which said therapeutic agent migrates, whereby said therapeutic agent permeates through said system from said monolithic therapeutic substance reservoir to said surface of said system which is or was in contact with said removable protective layer and said system becomes a therapeutic substance releasing delivery system.

Claim 13

A monolithic therapeutic substance non-releasing drug delivery system having a removable protective layer thereon, said system comprising (a) a monolithic therapeutic substance reservoir containing a therapeutic agent in a form which cannot permeate from said monolithic substance reservoir through said system to the surface of said system which is or was in contact with said removable protective layer; (b) an activating agent reservoir containing a system activating agent; (c) a burstable membrane or burstable seal between said activating agent reservoir and the portions of said system through which said therapeutic agent must migrate in order to reach said surface which is or was in contact with said removable protective layer but through which said therapeutic agent cannot permeate; and (d) an occlusive backing layer; wherein, upon bursting of said burstable membrane or burstable seal, said activating agent activates said system by contacting said portions through which said therapeutic agent must migrate but cannot migrate to reach the surface of said system which is or was in contact with said removable protection layer and modifying such portions into a form through which said therapeutic agent migrates, whereby said therapeutic agent permeates through said system from said monolithic therapeutic substance reservoir to said surface of said system which is or was in contact with said removable protective layer and said system becomes a therapeutic substance releasing delivery system.

Claim 14

A drug delivery system of claim 11 wherein said burstable membrane and burstable seal are broken by application of a pressure between about 10 and 50 pounds force.

Claim 15

A drug delivery system of claim 11 wherein said burstable membrane and burstable seal are a membrane and seal which selectively rupture as compared to other membranes, seals and layers of said system, under pressures of about 10 to about 50 pounds force.

Claim 16

A drug delivery system of claim 13 wherein said burstable seal is a heat seal which is no greater than about 1/6 as wide as any other heat seal of the same material in said system.

Claim 17

A drug delivery system of claim 13 wherein said burstable heat seal is from about 0.5 to about 2.0 mm wide.

Claim 18

A drug delivery system of claim 13 wherein said burstable membrane is selectively reinforced with unreinforced areas being no greater than about 20% to about 80% as wide as any other membrane or layer in said system made of the same material.

Claim 19

A drug delivery system of claim 16 where said unreinforced areas of said burstable membrane are no greater than about 10 to about 50 microns thick.

Claim 20

A drug delivery system of claim 13 wherein said burstable membrane is a membrane which would otherwise not be burstable under normal use but which has been selectively weakened.

Claim 21

A drug delivery system of claim 18 wherein said burstable membrane has been made selectively burstable by controlled depth slitting.

Claim 22

A drug delivery system of claim 11 wherein said therapeutic agent is selected from fentanyl, sufentanyl, isoniazid, rifampin, baclofen, terbutaline, theophylline, arecoline, nicotine, progesterone, methyltestosterone, desoxycorticosterone, triprolidine, diphenhydramine, tripelenamine, scopolamine, methscopolamine, nitroglycerine, metoprolol, estradiol, 3-([5-amino-1-carboxy]-pentylmino)-1-carboxy methyl-2,3,4,5-tetrahydro-1H-1-benzazepine-2-one, formoterol, physostigmine, and naloxone.