COMPOSITION FOR THE TRANSDERMAL DELIVERY OF FENTANYL
A transdermal drug delivery composition comprises an acrylate copolymer and from about 8% to about 30% by weight fentanyl. A transdermal fentanyl delivery composition comprising methyl laurate or tetraglycol as a permeation enhancer is also provided. The transdermal drug delivery compositions can be used to make a transdermal drug delivery device for the delivery of fentanyl.
1 - 33 . (canceled)
34 . A transdermal patch for administering fentanyl through the skin comprising: (a) a backing layer; (b) a reservoir disposed on the backing layer, at least the skin contacting surface of said reservoir being adhesive; said reservoir comprising a single phase polymeric composition free of undissolved components containing an amount of fentanyl sufficient to induce and maintain analgesia in a human for at least three days.
35 . The patch of claim 34 which is bioequivalent to DURAGESIC® transdermal fentanyl system.
36 . The patch of claim 34 wherein said reservoir is formed from an adhesive.
37 . The patch of claim 34 or 36 wherein said patch exhibits a normalized C max of about 16.8 to 18.7 ng/mL-mg/hr.
38 . The patch of claim 34 or 36 wherein said patch exhibits a standardized C max of about 0.14 to about 0.17 ng/mL/cm 2 .
39 . The patch of claim 36 wherein the patch exhibits a steady state drug flux of about 8.2 to 8.9 μg/cm 2 /hr.
40 . The patch of claim 34 wherein said reservoir comprises an amount of dissolved fentanyl sufficient to induce and maintain analgesia for about 4-14 days.
41 . The patch of claim 34 wherein said reservoir comprises an amount of dissolved fentanyl sufficient to induce and maintain analgesia for about 6-8 days.
42 . The patch of claim 34 wherein fentanyl has a solubility of about 8-30% by weight.
43 . The patch of claim 34 wherein fentanyl has a solubility of about 12-24% by weight.
44 . The patch of claim 40 wherein the reservoir comprises about 0.84 to 3.56 mg/cm 2 of fentanyl base.
45 . The patch of claim 44 wherein the reservoir comprises about 0.84 to 1.72 mg/cm 2 of fentanyl base.
46 . The patch of claim 40 wherein the reservoir has a dry coating weight of about 10 to 12 mg/cm 2 .
47 . The patch of claim 36 wherein said adhesive is a polyacrylate adhesive.
48 . The patch of claim 47 wherein said polyacrylate adhesive has a T g less than −10° C.
49 . The patch of claim 47 wherein the reservoir comprises about 0.84 to 3.56 mg/cm 2 of fentanyl base.
50 . The patch of claim 49 wherein the reservoir comprises about 0.84 to 1.72 mg/cm 2 of fentanyl base.
51 . The patch of claim 47 wherein the reservoir has a dry coating weight of about 10 to 12 mg/cm 2 .
52 . The patch of claim 40 or claim 47 wherein the reservoir further comprises an enhancer.
53 . The patch of any one of claims 34 , 40 or 47 , wherein the backing layer comprises a polymer selected from the group consisting of polyethylene, polyethylene terephthalate, ethylene-vinyl acetate copolymer, and polyurethane.
54 . The patch of claim 53 , wherein the backing layer comprises low density polyethylene or high density polyethylene.
55 . The patch of claim 54 , wherein the backing layer comprises low density polyethylene.
56 . The patch of claim 53 wherein the backing layer has a thickness of about 0.05 mm.
57 . A transdermal patch for administering fentanyl, comprising an adhesive fentanyl reservoir on a backing layer; said reservoir comprising a single phase polymeric composition free of undissolved components containing a polyacrylate adhesive having sufficient solubility for fentanyl to contain dissolved fentanyl in an amount sufficient to induce and maintain analgesia in a human for at least three days, said patch exhibiting a normalized C max of about 16.8 to 18.7 ng/mL-mg/hr.
58 . A transdermal patch for administering fentanyl, comprising an adhesive fentanyl reservoir on a backing layer; said reservoir comprising a single phase polymeric composition free of undissolved components containing a polyacrylate adhesive having sufficient solubility for fentanyl to contain dissolved fentanyl in an amount sufficient to induce and maintain analgesia in a human for at least three days, said patch exhibiting a standardized C max of about 0.14 to about 0.17 ng/mL/cm 2 .
59 . The patch of claim 57 or 58 wherein the patch exhibits a steady state drug flux of about 8.2 to 8.9 μg/cm 2 /hr.
60 . The patch of claim 57 or 58 wherein said reservoir comprises an amount of dissolved fentanyl sufficient to induce and maintain analgesia for about 4-14 days.
61 . The patch of claim 57 or 58 wherein said reservoir comprises an amount of dissolved fentanyl sufficient to induce and maintain analgesia for about 6-8 days.
62 . The patch of claim 60 wherein said adhesive is a polyacrylate adhesive having a T g less than −10° C.; and fentanyl has a solubility of about 8% by weight.
63 . The patch of claim 62 wherein the reservoir has a dry coating weight of about 10 to 12 mg/cm 2 .
64 . The patch of claim 63 wherein the reservoir comprises about 0.84 to 3.56 mg/cm 2 of fentanyl base.
65 . The patch of claim 64 wherein the reservoir comprises about 0.84 to 1.72 mg/cm 2 of fentanyl base.
66 . A monolithic transdermal patch for administering fentanyl, comprising an adhesive fentanyl reservoir on a backing layer, said reservoir comprising a single phase polymeric composition free of undissolved components containing a polyacrylate adhesive having sufficient solubility for fentanyl to contain dissolved fentanyl in an amount sufficient to induce and maintain analgesia in a human for at least three days, said patch being completely free from a rate controlling membrane, said patch exhibiting a normalized C max of about 16.8 to 18.7 ng/mL-mg/hr.
67 . A monolithic transdermal patch for administering fentanyl, comprising an adhesive fentanyl reservoir on a backing layer, said reservoir comprising a single phase polymeric composition free of undissolved components containing a polyacrylate adhesive having sufficient solubility for fentanyl to contain dissolved fentanyl in an amount sufficient to induce and maintain analgesia in a human for at least three days, said patch being completely free from a rate controlling membrane, said patch exhibiting a standardized C max of about 0.14 to about 0.17 ng/mL/cm 2 .
68 . The patch of claim 66 or 67 wherein said reservoir comprises an amount of dissolved fentanyl sufficient to induce and maintain analgesia for about 6-8 days wherein fentanyl has a solubility of about 8% by weight in said reservoir; the reservoir has a drying coating weight of about 10-12 mg/cm 2 ; and said patch exhibits a steady state drug flux of about 8.2 to 8.9 μg/cm 2 /hr.
69 . The patch of claim 66 or 67 wherein the reservoir comprises about 0.84 to 3.56 mg/cm 2 of fentanyl base.
70 . The patch of claim 34 which is pharmacologically equivalent to DURAGESIC® transdermal fentanyl system.