Sustained release formulations of nalbuphine
Sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof; methods for making the sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof; and methods for using the sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof to treat patients suffering from pain are provided.
1. A sustained release oral solid dosage form comprising a therapeutically effective amount of nalbuphine or a pharmaceutically acceptable salt thereof in a sustained release delivery system, wherein the dosage form provides a mean Tmax at 1.77 (±1.539) to 8.01 (±2.196) hours after oral administration to human subjects and maintains a plateau of a relatively constant blood serum level of nalbuphine which does not consistently increase or decrease from time point to time point.
2. The dosage form of claim 1 , wherein the plateau has a duration of about 1 hours to about 12 hours.
3. The dosage form of claim 1 , wherein the plateau has a duration of about 2 to about 10 hours.
4. The dosage form of claim 1 , wherein the plateau has a duration of about 6 hours to about 9 hours.
5. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of about 7 to about 16 ng/ml.
6. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 8.58 ng/ml (±4.217) based on a 60 mg single dose.
7. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 7.17 ng/ml (±3.175) based on a 60 mg single dose.
8. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 7.920 ng/ml (±1.4722) based on a 60 mg single dose.
9. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 7.750 ng/ml (±6.034) based on a 60 mg single dose.
10. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 12.87 ng/ml (±4.031) based on a 120 mg single dose.
11. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 14.1 ng/ml (±6.23) based on a 120 mg single dose.
12. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 11.3 ng/ml (±7.17) based on a 120 mg single dose.
13. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 13.4 ng/ml (±8.81) based on a 120 mg single dose.
14. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 14.2 ng/ml (±8.87) based on a 120 mg single dose.
15. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 12.5 ng/ml (±8.02) based on a 120 mg single dose.
16. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 15.574 ng/ml (±8.4070) based on a 120 mg single dose.
17. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 12.498 ng/ml (±7.1308) based on a 120 mg single dose.
18. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 12.903 ng/ml (±5.4062) based on a 120 mg single dose.
19. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 12.700 ng/ml (±5.7697) based on a 120 mg single dose.
20. The dosage form of claim 1 , wherein the dosage form provides a mean Cmax of 13.265 ng/ml (±6.458) based on a 120 mg single dose.
21. The dosage form of claim 1 , wherein the dosage form provides a mean Tmax at about 1.77 to about 8.01 hours after oral administration to human subjects.