Abuse deterrent transdermal formulations of opiate agonists and agonist-antagonists
First Claim
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1. An abuse-resistant patch for transdermally delivering an opioid to a subject, comprising:
- (a) a backing layer;
(b) a first layer underlying the backing layer, the first layer comprising;
an opioid antagonist or opioid antagonist prodrug which is not transdermally delivered at therapeutic levels when the patch is used for transdermally administering the opioid to the subject;
wherein the backing layer is substantially impermeable to the opioid antagonist or opioid antagonist prodrug of the first layer;
(c) a second layer underlying the first layer, the second layer comprising;
(i) an opioid selected from the group consisting of;
an opioid agonist, an opioid agonist prodrug, an opioid agonist-antagonist and an opioid agonist-antagonist prodrug;
(ii) a pressure sensitive adhesive;
wherein the second layer is adapted to be in diffusional communication with the skin of the subject to transdermally administer a therapeutically effective amount of the opioid to the subject; and
(d) a barrier layer located between the first and second layer, the barrier layer comprising;
a water-insoluble polymeric material and a water-soluble polymer;
wherein the release ratio is between about 1;
60 and about 60;
1 after the patch has been placed in ethanol, water or a phosphate buffer having a pH of about 6.5 for greater than about 30 seconds.
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Abstract
Described herein are abuse-resistant multi-layer transdermal patches comprising opioids and opioid prodrugs having a barrier layer located between the layer containing opioid or opioid prodrug and a layer containing an opioid antagonist or opioid antagonist prodrug.
28 Citations
30 Claims
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1. An abuse-resistant patch for transdermally delivering an opioid to a subject, comprising:
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(a) a backing layer; (b) a first layer underlying the backing layer, the first layer comprising;
an opioid antagonist or opioid antagonist prodrug which is not transdermally delivered at therapeutic levels when the patch is used for transdermally administering the opioid to the subject;
wherein the backing layer is substantially impermeable to the opioid antagonist or opioid antagonist prodrug of the first layer;(c) a second layer underlying the first layer, the second layer comprising; (i) an opioid selected from the group consisting of;
an opioid agonist, an opioid agonist prodrug, an opioid agonist-antagonist and an opioid agonist-antagonist prodrug;(ii) a pressure sensitive adhesive;
wherein the second layer is adapted to be in diffusional communication with the skin of the subject to transdermally administer a therapeutically effective amount of the opioid to the subject; and(d) a barrier layer located between the first and second layer, the barrier layer comprising;
a water-insoluble polymeric material and a water-soluble polymer;wherein the release ratio is between about 1;
60 and about 60;
1 after the patch has been placed in ethanol, water or a phosphate buffer having a pH of about 6.5 for greater than about 30 seconds. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26)
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27. A method of making an abuse-resistant transdermal patch for delivering an opioid to a subject comprising the steps of:
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(a) applying a first layer to a substrate comprising a backing layer, the layer comprising;
an opioid antagonist or opioid antagonist prodrug which is not transdermally delivered at therapeutic levels when the patch is used for transdermally administering the opioid;(b) applying a barrier layer to the first layer, the barrier layer comprising;
a water-insoluble polymeric material and a water-soluble polymer; and(c) applying a second layer to the barrier layer, the second layer comprising; (i) an opioid selected from the group consisting of;
an opioid agonist, a prodrug of an opioid agonist, an opioid agonist-antagonist and a prodrug of an opioid agonist-antagonist; and(ii) a pressure sensitive adhesive;
wherein the second layer is adapted to be in diffusional communication with the skin of the subject to transdermally administer a therapeutically effective amount of the opioid to the subject;wherein the release ratio is between about 1;
60 and about 60;
1 after the patch has been placed in ethanol, water or a phosphate buffer having a pH of about 6.5 for greater than about 30 seconds. - View Dependent Claims (28, 29, 30)
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Specification