Granted Patent B2

US 8,475,832 · App. 12/537,571 · Granted Jul 2, 2013

Abstract

Claims (29)

1. A film dosage composition comprising:

a. A polymeric carrier matrix;

b. A therapeutically effective amount of buprenorphine or a pharmaceutically acceptable salt thereof;

c. A therapeutically effective amount of naloxone or a pharmaceutically acceptable salt thereof; and

d. A buffer in an amount to provide a local pH for said composition of a value sufficient to optimize absorption of said buprenorphine, wherein said local pH is from about 3 to about 3.5 in the presence of saliva.

2. The composition of claim 1 , wherein said film dosage composition provides a bioequivalent absorption of buprenorphine to that of a tablet having an equivalent amount of buprenorphine or a pharmaceutically acceptable salt thereof.

3. The composition of claim 1 , wherein said polymeric carrier matrix comprises at least one polymer in an amount of at least 25% by weight of said composition.

4. The composition of claim 1 , wherein said buffer is present in an amount of from about 2:1 to about 1:5 by weight of buffer to buprenorphine.

5. The composition of claim 1 , wherein said polymeric carrier matrix comprises at least one self-supporting film forming polymer.

6. The film dosage composition of claim 1 , wherein said buprenorphine is present in an amount of from about 2 mg to about 16 mg per dosage.

7. The film dosage composition of claim 1 , wherein said buffer comprises sodium citrate, citric acid, and combinations thereof.

8. The film dosage composition of claim 1 , wherein said buffer comprises acetic acid, sodium acetate, and combinations thereof.

9. A method of treating narcotic dependence of a user, comprising the steps of:

a. providing a composition comprising:

i. A polymeric carrier matrix;

ii. A therapeutically effective amount of buprenorphine or a pharmaceutically acceptable salt thereof;

iii. A therapeutically effective amount of naloxone or a pharmaceutically acceptable salt thereof; and

iv. A buffer in an amount to provide a local pH of about 3 to about 3.5 for said composition of a value sufficient to optimize absorption of said buprenorphine and also sufficient to inhibit absorption of said naloxone; and

b. administering said composition to the oral cavity of a user.

10. The composition of claim 9 , wherein said method provides a bioequivalent absorption of buprenorphine to that of a tablet having an equivalent amount of buprenorphine or a pharmaceutically acceptable salt thereof.

11. The method of claim 9 , wherein said film dosage composition is administered to the user through buccal administration, sublingual administration, and combinations thereof.

12. The method of claim 9 , wherein said film dosage composition remains in the oral cavity of the user for a period of at least 1 minute.

13. The method of claim 9 , wherein said film dosage composition remains in the oral cavity of the user for a period of between about 1 and 1.5 minutes.

14. The method of claim 9 , wherein said film dosage composition remains in the oral cavity of the user for a period of up to 3 minutes.

15. An orally dissolving film formulation comprising buprenorphine and naloxone, wherein said formulation provides an in vivo plasma profile having a Cmax of between about 0.624 ng/ml and about 5.638 ng/ml for buprenorphine and an in vivo plasma profile having a Cmax of between about 41.04 pg/ml to about 323.75 pg/ml for naloxone.

16. The formulation of claim 15 , wherein said formulation provides a mean AUC of between about 5.431 hr·ng/ml to about 56.238 hr·ng/ml for buprenorphine.

17. The formulation of claim 15 , wherein said formulation provides a mean AUC of between about 102.88 hr·pg/ml to about 812.00 hr·pg/ml for naloxone.

18. The formulation of claim 15 , wherein said formulation comprises about 2 to about 16 mg of buprenorphine or a salt thereof.

19. The formulation of claim 15 , wherein said formulation comprises about 0.5 to about 4 mg of naloxone or a salt thereof.

Assignments (11)