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Claims for Patent: 4,588,580

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Claims for Patent: 4,588,580

Title: Transdermal administration of fentanyl and device therefor
Abstract:Transdermal delivery systems for delivery of fentanyl and its analgetically effective derivatives for extended periods of time are disclosed which deliver the base form of the drug at a rate of from 0.5 to 10 .mu.g/cm.sup.2 /hr for a substantial portion of their useful life. The systems can be from 5-100 cm.sup.2 in releasing surface and preferably employ an in-line amine resistant adhesive. Preferred rate controlled systems utilize an aqueous ethanolic gel to minimize drug content.
Inventor(s): Gale; Robert M. (Los Altos, CA), Goetz; Victor (Palo Alto, CA), Lee; Eun S. (Redwood City, CA), Taskovich; Lina T. (Palo Alto, CA), Yum; Su I. (Los Altos, CA)
Assignee: Alza Corporation (Palo Alto, CA)
Application Number:06/633,762
Patent Claims: 1. A process for inducing and maintaining analgesia which comprises administering through an area of intact skin, a skin permeable form of a material selected from the group consisting of fentanyl and its analgetically effective derivatives at an analgetically effective rate and continuing the administration of said material at said rate for an extended period of time at least sufficient to induce analgesia.

2. The process for claim 1 further comprising the coadministration with said material of a skin permeation enhancer for said material.

3. The process of claim 1 wherein said extended period of time is in the range of from 12 hours to 7 days.

4. The process of claim 1 wherein the steady state administration rate of said material is maintained within the range of about 10 to 300 .mu.g/hr for a substantial portion of said extended period of time.

5. The process of claim 1 wherein said area of intact skin is within the range of about 5 to 100 cm.sup.2 and said material is delivered through the skin at a rate within the range of about 0.5 to 10 .mu.g/cm.sup.2 /hr.

6. The process of claim 5 in which said area is in the range of from about 10 to 50 cm.sup.2 and said rate is in the range of about 1 to 5 .mu.g/cm.sup.2 /hr.

7. The process of claim 4 wherein the steady state

8. The process of claim 2 wherein said permeation enhancer is ethanol.

9. The process of claim 1 wherein said material is the base form of a material selected from the group consisting of fentanyl, sufentanyl, carfentanyl, lofentanyl, and alfentanyl.

10. The process of claim 2 wherein the material is fentanyl base.

11. The process of claim 3 wherein the material is fentanyl base.

12. The process of claim 4 wherein the material is fentanyl base.

13. The process of claim 5 wherein the material is fentanyl base.

14. The process of claim 6 wherein the material is fentanyl base.

15. The process of claim 7 wherein the material is fentanyl base.

16. A process for the transdermal administration of a material selected from the group consisting of fentanyl and its analgetically effective derivatives which comprises:

(a) contacting a predetermined area of intact skin with a source of skin permeable form of said materia1;

(b) maintaining said source in material transmitting relationship to said area of intact skin for an administration period of at least 12 hours; and

(c) delivering said material into the skin at a rate within the range of about 0.1-10 .mu.g/cm.sup.2 /hour for at least about 12 hours.

17. The process of claim 16 further comprising maintaining said source at unit activity throughout said administration period.

18. The process of claim 17 wherein said predetermined area of intact skin is in the range of 5 to 100 cm.sup.2.

19. The process of claim 16 wherein said material is the base form of a material selected from the group consisting of fentanyl, sufentanyl, carfentanyl, lofentanyl and alfentanyl.

20. The process of claim 18 further comprising coadministering a permeation enhancer for said material during said administration period.

21. The process of claim 16 wherein the material is fentanyl base.

22. A medical device for the transdermal administration of a material selected from the group consisting of fentanyl and its analgetically effective derivatives at an analgetically effective rate for an extended period of time of at least four hours which comprises:

(a) reservoir means containing a skin permeable form of said material in an amount sufficient to deliver said material at said analgetically effective rate for said extended period of time and,

(b) means for maintaining a said reservoir means in material transmitting relationship to intact skin.

23. The medical device of claim 22 wherein said system delivers the base form of the material through intact skin at a rate in the range of from about 10 to 300 .mu.g/hr for a substantial portion of said period of time.

24. The medical device of claim 22 wherein said reservoir means contains a skin permeation enhancer for said material.

25. The medical device of claim 22 wherein said predetermined area is in the range of about 5-100 cm.sup.2 and the rate of delivery of said material is in the range of about 0.5-10 .mu.g/cm.sup.2 /hr.

26. The medical device of claim 25 wherein said area is in the range of about 10-50 cm.sup.2 and said delivery rate is in the range of about 1-5 .mu.g/cm.sup.2 /hr.

27. The medical device of claim 25 wherein said material is fentanyl base.

28. A medical device for continuous transdermal administration of a material selected from the group consisting of fentanyl and its analgetically effective, derivates comprising, in combination:

(a) a reservoir for said material having a skin proximal, material releasing surface area in the range of about 5-100 cm.sup.2, said reservoir containing between 0.1 and 50% by weight of a skin permeable form of said material in amounts and at a concentration adequate to permit delivery of said material through intact human skin at a rate within the range of from 0.5 to 10 .mu.g/cm.sup.2 /hr for at least about 12 hours and

(b) means for maintaining said reservoir in material transmitting relationship to the skin.

29. The medical device of claim 28 wherein said means for maintaining said reservoir in material transmitting relationship to the skin is an amine resistant adhesive disposed in the flow path of the material from the reservoir to the skin.

30. The medical device of claim 28 further comprising release rate controlling means disposed in the flow path of said material to the skin which means limit the flux of material from said system to a level less than the flux of material through the skin to which it is applied.

31. The medical device of claim 17 wherein said material is the base form of a material selected from the group consisting of fentanyl, sufentanyl, carfentanyl, lofentanyl and alfentanyl.

32. The medical device of claim 17 wherein said reservoir contains an aqueous gel comprising up to about 47% of 95% ethanol, 1-10% gelling agent, 0.1-10% of said material, and release rate controlling means disposed between said reservoir and the skin, said release rate controlling means being more permeable to said material than ethanol.

33. The medical device of claim 31 wherein said material is fentanyl base.

34. The medical device of claim 30 further comprising permeation enhancer means for increasing the permeability to said material of the skin to which said device is applied.

35. The medical device of claim 34 wherein said permeation enhancer means is admixed in said reservoir means.

36. The medical device system of claim 35 wherein said release rate controlling means restricts the flux of said material from said system substantially more than the flux of said permeation enhancer from said device.

37. The medical device of claim 30 wherein said reservoir is an aqueous gel comprising approximately from 0-47% of 95% ethanol., 1-10% gelling agent, 0.1-10% of said material.

38. The medical device of claim 37 wherein said aqueous gel comprises from approximately 20-35% of said ethanol, 1-5% gelling agent and 0.1-2% of said material.

39. The medical device of claim 38 wherein said release rate controlling means is substantially more permeable to ethanol than to said material.

40. The medical device of claim 39 wherein said material is initially contained in said reservoir at equilibrated levels no greater than 0.5 .mu.g/cm.sup.2.

41. The medical device of claim 39 wherein said means for maintaining said system on the skin is an amine resistant adhesive disposed on said release rate controlling means and said material is fentanyl.

42. The medical device of claim 41 wherein said surface area is in the range of from about 10-50 cm.sup.2.

43. The medical device of claim 28 wherein said reservoir is an polymeric matrix having said material contained therein in an amount from about 5-50% by weight.

44. The medical device of claim 43 wherein said means for maintaining said device in material transmitting relationship to the skin comprises an amine resistant adhesive disposed in the flow path of material from the reservoir to the skin.

45. The medical device of claim 43 wherein said matrix is selected from the group consisting of polyisobutylene and silicone polymers.

46. The medical device of claim 45 wherein said device further comprises release rate controlling means disposed in the flow path of said material to the skin which limits the flux of said material from said device to a level less than the flux of material through the skin to which it is applied.

47. The medical device of claim 46 in which said means for maintaining said device in material transmitting relationship to the skin is an amine resistant adhesive disposed on said release controlling means.

48. The medical device of claim 47 wherein said material is fentanyl base.

49. The medical device of claim 28 wherein said release rate is in the range of from about 1-5 g/cm.sup.2 /hr and said material is fentanyl.

50. The medical device of claim 30 wherein said release rate is in the range of from about 1-5 .mu.g/cm.sup.2 /hr and said material is fentanyl.

51. The medical device of claim 35 wherein said release rate is in the range of from about 1-5 .mu.g/cm.sup.2 /hr and said material is fentanyl base.

52. The medical device of claim 36 wherein said release rate is in the range of from about 1-5 .mu.g/cm.sup.2 /hr and said material is fentanyl.

53. The medical device of claim 38 wherein said release rate is in the range of from about 1-5 .mu.g/cm.sup.2 /hr and said material is fentanyl.

54. The medical device of claim 40 wherein said release rate is in the range of from about 1-5 .mu.g/cm.sup.2 /hr and said material is fentanyl.

55. The medical device of claim 43 wherein said release rate is in the range of from about 1-5 .mu.g/cm.sup.2 /hr and said material is fentanyl.

56. The medical device of claim 44 wherein said release rate is in the range of from about 1-5 .mu.g/cm.sup.2 /hr and said material is fentanyl.

57. The medical device of claim 45 wherein said release rate is in the range of from about 1-5 .mu.g/cm.sup.2 /hr and said material is fentanyl.

58. The medical device of claim 47 wherein said release rate is in the range of from about 1-5 .mu.g/cm.sup.2 /hr and said material is fentanyl.
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