Opioid formulations

• US 20070014820A1
• Filed: 06/27/2006
• Published: 01/18/2007
• Est. Priority Date: 01/23/2003
• Status: Abandoned Application

• Current Assignee: Barbara Laidlaw, Dana Litmanovitz
• Original Assignee: Barbara Laidlaw, Dana Litmanovitz
• Inventors: Laidlaw, Barbara, Litmanovitz, Dana
• Application Number:
  US11/477,140
• Publication Number:
  US 20070014820A1
• Time in Patent Office: Days
• US Class Current: 424/400
• CPC Class Codes: A61K 31/4468 having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
• CPC Class Codes: A61K 31/4535 containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen

Abstract

The present invention provides high-concentration formulations of opioids such as fentanyl or fentanyl congeners. The formulation of the invention comprises fentanyl or a fentanyl congener in concentrations significantly in excess of conventional formulations, e.g., on the order about 2-fold to about 10,000-fold greater than conventional formulations, e.g., currently commercially available formulations. These formulations are particularly useful for long-term delivery to a subject suffering from pain. The invention further provides drug delivery devices comprising the high-concentration opioid formulations, and further provides methods of alleviating pain in a subject, comprising administering the high-concentration formulations to a subject in need thereof.

Claims

1. A pharmaceutical formulation comprising fentanyl or a fentanyl congener and a non-aqueous carrier, wherein the fentanyl or fentanyl congener is present in the formulation at a concentration of at least about 500 μ

g/mL.

2. The pharmaceutical formulation according to claim 1, wherein the non-aqueous carrier is a lower molecular weight alcohol comprising an aromatic moiety.

3. The pharmaceutical formulation according to claim 2, wherein the alcohol is benzyl alcohol.

4. The pharmaceutical formulation according to claim 1, wherein the non-aqueous carrier comprises a non-ionic surfactant and an alcohol ester.

5. The pharmaceutical formulation according to claim 4, wherein the non-ionic surfactant is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 80, and sorbitan trioleate.

6. The pharmaceutical formulation according to claim 4, wherein the alcohol is benzyl alcohol.

18. A dosage form comprising a formulation according to claims 1, 7 or 12.

19. A method of treating pain in a subject suffering from pain, comprising administering to a subject suffering from pain a formulation according to claims 1, 7 or 12 in an amount effective to alleviate pain in the subject.

7. A pharmaceutical formulation comprising fentanyl or a fentanyl congener in a concentration of from about 0.5 mg/mL to about 500 mg/mL in a lower molecular weight alcohol which comprises an aromatic moiety.

8. The pharmaceutical formulation of claim 7, comprising fentanyl or fentanyl congener in a concentration of from about 50 mg/mL to about 400 mg/mL.

9. The pharmaceutical formulation of claim 7, wherein the fentanyl congener is sufentanil.

10. The pharmaceutical formulation of claim 7, wherein the lower molecular weight alcohol is benzyl alcohol.

11. The pharmaceutical formulation of claim 7, wherein the fentanyl or a fentanyl congener is present in the formulation as a fentanyl base or a fentanyl congener base.

12. A pharmaceutical formulation comprising fentanyl or a fentanyl congener in a concentration from about 0.5 mg/mL to about 500 mg/mL, and a nonionic surfactant in a concentration of from about 50 mg/mL to about 200 mg/mL, in an alcohol ester which comprises an aromatic moiety.

13. The pharmaceutical formulation of claim 12, comprising fentanyl or fentanyl congener in a concentration of from about 50 mg/mL to about 250 mg/mL.

14. The pharmaceutical formulation of claim 12, wherein the fentanyl congener is sufentanil.

15. The pharmaceutical formulation of claim 12, wherein the nonionic surfactant is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 80, and sorbitan trioleate.

16. The pharmaceutical formulation of claim 12, wherein the alcohol ester is benzyl benzoate.

17. The pharmaceutical formulation of claim 12, wherein the fentanyl or fentanyl congener is present in the formulation as a fentanyl base or a fentanyl congener base.

20. A pharmaceutical formulation comprising sufentanil and a non-aqueous diluent, wherein sulfentanil is present in the formulation in a concentration greater than about 500 μ

g/mL.

21. The pharmaceutical formulation of claim 20, wherein the formulation comprises a lower molecular weight alcohol comprising an aromatic moiety.

22. The pharmaceutical formulation of claim 21, wherein the lower molecular weight alcohol is benzyl alcohol.

23. The pharmaceutical formulation of claim 20, wherein the formulation comprises a nonionic surfactant in a concentration of from about 50 mg/mL to about 200 mg/mL, and an alcohol ester which comprises an aromatic moiety.

24. The pharmaceutical formulation of claim 23, wherein the alcohol ester is benzyl benzoate and wherein the nonionic surfactant is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 80, and sorbitan trioleate.

25. A drug dosage form comprising a formulation according claim 20.

26. A method of treating pain in a subject suffering from pain, comprising administering to a subject suffering from pain a formulation according to claim 20, thereby alleviating pain in the subject.