Tamper resistant transdermal dosage form
View Patent ↗The invention comprises a transdermal dosage form comprising an active agent component comprising an active agent and an adverse agent component comprising an adverse agent, wherein the active agent component defines at least one channel extending substantially there through.
1. A transdermal dosage form comprising:
an active agent component having a proximal, skin contacting surface and a distal surface and comprising an opioid agonist;
an adverse agent component having a proximal surface and a distal surface and comprising an opioid antagonist;
a backing;
a barrier having a proximal surface and a distal surface that is interposed between the active agent component and the adverse agent component, wherein one or more channels extend completely from the proximal surface of the active agent component to the distal surface of the barrier and terminate prior to the proximal surface of the adverse agent component;
wherein air is disposed in one or more channels;
and wherein the barrier is permeable to a solvent selected from the group consisting of water, ethanol, ether, and mixtures thereof, and wherein the barrier is impermeable to diffusion of opioid agonist and opioid antagonist in the absence of said solvent.
2. A transdermal dosage form of claim 1 , wherein the active agent component further comprises a polymeric material and the opioid agonist is dispersed in the polymeric material.
3. A transdermal dosage form according to claim 2 , wherein the opioid agonist is homogeneously dispersed in the polymeric material.
4. A transdermal dosage form according to claim 1 , further comprising an adhesive component connecting the adverse agent component and the barrier.
5. A transdermal dosage form according to claim 1 , wherein the adverse agent component is interposed between the barrier and a portion of the backing.
6. A transdermal dosage form according to claim 5 , wherein the backing is a continuous, polymeric film.
7. A transdermal dosage form according to claim 5 , wherein the backing is an overlay backing.
8. A transdermal dosage form according to claim 1 , wherein the adverse agent component comprises a pressure-sensitive adhesive and the opioid antagonist is dispersed in the pressure-sensitive adhesive.
9. A transdermal dosage form according to claim 8 , wherein the pressure-sensitive adhesive comprises an acrylate pressure-sensitive adhesive.
10. A transdermal dosage form according to claim 1 , wherein the opioid agonist is selected from the group consisting of alfentanil, allylprodine, alphaprodine, anileridine, benzylmorphine, bezitramide, buprenorphine, butorphanol, clonitazene, codeine, desomorphine, dextromoramide, dezocine, diampromide, diamorphone, dihydrocodeine, dihydromorphine, dimenoxadol, dimepheptanol, dimethylthiambutene, dioxaphetyl butyrate, dipipanone, eptazocine, ethoheptazine, ethylmethylthiambutene, ethylmorphine, etonitazene, etorphine, dihydroetorphine, fentanyl, hydrocodone, hydromorphone, hydromorphodone, hydroxypethidine, isomethadone, ketobemidone, levorphanol, levophenacylmorphan, lofentanil, meperidine, meptazinol, metazocine, methadone, metopon, morphine, myrophine, narceine, nicomorphine, norlevorphanol, normethadone, nalorphine, nalbuphene, normorphine, norpipanone, opium, oxycodone, oxymorphone, pantopon, papavereturn, paregoric, pentazocine, phenadoxone, phendimetrazine, phendimetrazone, phenomorphan, phenazocine, phenoperidine, piminodine, piritramide, propheptazine, promedol, properidine, propoxyphene, propylhexedrine, sufentanil, tilidine, tramadol, a pharmaceutically acceptable salt thereof, and mixtures of two or more of the foregoing.
11. A transdermal dosage form according to claim 1 , wherein the opioid antagonist is selected from the group consisting of naloxone, naltrexone, nalmefene, nalbuphine, nalorphine, cyclazacine, cyclazocine, levallorphan, a pharmaceutically acceptable salt thereof, and mixtures of two or more of the foregoing.
12. A transdermal dosage form according to claim 1 , wherein the opioid agonist is fentanyl or a pharmaceutically acceptable salt thereof.
13. A transdermal dosage form according to claim 1 , wherein the opioid antagonist is naltrexone or a pharmaceutically acceptable salt thereof.
14. A transdermal dosage form according to claim 13 , wherein the opioid agonist is fentanyl or a pharmaceutically acceptable salt thereof.
15. A method of transdermal delivery of an active agent from a tamper-resistant dosage form comprising: (a) providing a transdermal dosage form according to claim 1 ; and (b) applying the dosage form to a portion of the skin or mucosa of a patient for a period sufficient to achieve the desired therapeutic result.
16. A transdermal dosage form according to claim 1 , wherein said transdermal dosage form can deliver, when tampered with, a ratio of opioid antagonist to opioid agonist of about 1 to about 10 to a ratio of about 1 to about 1.
17. A transdermal dosage form according to claim 16 , wherein said opioid agonist is fentanyl and said opioid antagonist is naltrexone.
18. A transdermal dosage form according to claim 2 , wherein the opioid antagonist is an antagonist to the opioid agonist.
19. A transdermal dosage form according to claim 1 , wherein the barrier is at least partially soluble in a solvent selected from the group consisting of water, ethanol, ether, and mixtures thereof.
20. A transdermal dosage form according to claim 1 , wherein the barrier is permeable to water, ethanol, and mixtures thereof.