Fentanyl suspension-based silicone adhesive formulations and devices for transdermal delivery of fentanyl
View Patent ↗Silicone adhesive formulations are provided, in which fentanyl particles are suspended in one or more solvated silicone adhesives. The formulations can be used for manufacturing improved, matrix-type transdermal devices for administering fentanyl.
1. A monolithic suspension-blend transdermal patch comprising:
(a) a backing layer having inner and outer surfaces and being substantially impervious to fentanyl;
(b) a first adhesive layer having a first surface covering at least a portion of said inner surface of said backing layer, said adhesive layer comprising a uniform suspension of a therapeutically-effective amount of fentanyl particles suspended in a silicone adhesive, said fentanyl particles consisting essentially of non-recrystallized fentanyl; and
(c) a removable release liner in contact with a second surface of said adhesive layer.
2. A patch as defined in claim 1 , wherein said silicone adhesive comprises heptane solvent fully-solvated silicone adhesive from which the heptane solvent is substantially removed.
3. A patch as defined in claim 1 , wherein said adhesive comprises a pressure sensitive adhesive.
4. A patch as defined in claim 1 , wherein said adhesive layer comprises about 1% to about 15% w/w fentanyl.
5. A patch as defined in claim 1 , wherein said adhesive layer further comprises up to about 25% w/w silicone fluid.
6. A patch as defined in claim 5 , wherein said silicone fluid comprises polydimethylsiloxane.
7. A patch as defined in claim 1 , further comprising a second adhesive layer which is between and in contact with said backing layer and said first adhesive layer; said second adhesive layer extending at least partially beyond said first adhesive layer.
8. A patch as defined in claim 1 , wherein said adhesive layer further comprises a flux enhancer.
9. A patch as defined in claim 1 , wherein when said patch is administered to a subject in need thereof, said adhesive layer delivers from about 10 μg/hr to about 100 μg/br of said fentanyl to said subject for a period of from 24 to 168 hours.
10. A patch as defined in claim 1 , wherein when said patch is administered to a subject in need thereof, said adhesive layer delivers from about 10 μg/hr to about 100 μg/k of said fentanyl to said subject for a period of from 72 to 168 hours.
11. A patch as defined in claim 1 , wherein when said patch is administered to a subject in need thereof, said adhesive layer delivers about 25 μg/hr of said fentanyl to said subject for a period of from 24 to 168 hours.
12. A patch as defined in claim 1 , wherein when said patch is administered to a subject in need thereof, said adhesive layer delivers about 25 μg/hr of said fentanyl to said subject for a period of from 72 to 168 hours.
13. A patch as defined in claim 1 , wherein when said patch is administered to a subject in need thereof, said adhesive layer delivers about 50 μg/hr of said fentanyl to said subject for a period of from 24 to 168 hours.
14. A patch as defined in claim 1 , wherein when said patch is administered to a subject in need thereof, said adhesive layer delivers about 50 μg/hr of said fentanyl to said subject for a period of from 72 to 168 hours.
15. A patch as defined in claim 1 , wherein when said patch is administered to a subject in need thereof, said adhesive layer delivers about 75 μg/hr of said fentanyl to said subject for a period of from 24 to 168 hours.
16. A patch as defined in claim 1 , wherein when said patch is administered to a subject in need thereof, said adhesive layer delivers about 75 μg/hr of said fentanyl to said subject for a period of from 72 to 168 hours.
17. A patch as defined in claim 1 , wherein when said patch is administered to a subject in need thereof, said adhesive layer delivers about 100 μg/hr of said fentanyl to said subject for a period of from 24 to 168 hours.
18. A patch as defined in claim 1 , wherein when said patch is administered to a subject in need thereof, said adhesive layer delivers about 100 μg/hr of said fentanyl to said subject for a period of from 72 to 168 hours.
19. A monolithic suspension-blend transdermal patch comprising:
(a) a backing layer having inner and outer surfaces and being substantially impervious to fentanyl;
(b) a first adhesive layer having a first surface covering at least a portion of said inner surface of said backing layer, said adhesive layer comprising a uniform suspension of a 72 to 168 hour period therapeutically-effective amount of fentanyl particles suspended in a silicone adhesive, said fentanyl particles consisting essentially of non-recrystallized fentanyl, said silicone adhesive comprising heptane solvent fully-solvated silicone adhesive from which the heptane solvent is substantially removed, said heptane solvated adhesive being incapable of dissolving greater than about 1% w/w of said fentanyl particles; and
(c) a removable release liner in contact with a second surface of said adhesive layer; wherein the fentanyl load of said suspension-based patch ranges from about 1 to about 15% w/w (dry weight) based upon the weight of said fentanyl silicone adhesive suspension; whereby when said suspension-blend patch is administered to a subject in need thereof, said adhesive layer delivers from about 5 μg/hr to about 250 μg/hr of said fentanyl to said subject for said period.