Table 2.
Pharmacokinetics of Buprenorphine Formulations
| Formulations | Doses (mg) | Single Dose |
Steady State |
|||
|---|---|---|---|---|---|---|
| Cmax (ng/mL) | AUC0-inf (h*ng/mL) | Cmin (ng/mL) | Cavg (ng/mL) | Cmax (ng/mL) | ||
| Buprenorphine/Naloxone Tablet | ||||||
| Brand namea | 2/0.5 and 2 | -- | -- | -- | -- | -- |
| 8/2 and 8 | 3.00 | 20.22b | 0.65 | 1.19 | 4.74 | |
| 12 | -- | -- | 0.81 | 1.71 | 5.35 | |
| 24 | -- | -- | 1.54 | 2.91 | 8.27 | |
| Generic group 1c | 2/0.5 | 0.95 | 8.65 | -- | -- | -- |
| 8/2 | 3.37 | 30.45 | -- | -- | -- | |
| Generic group 2d | 2/0.5 | 0.78 | 7.65 | -- | -- | -- |
| 8/2 | 2.58 | 25.31 | -- | -- | -- | |
| Generic group 3e | 2/0.5 | 1.25 | 10.93 | -- | -- | -- |
| 8/2 | 2.88 | 28.39 | -- | -- | -- | |
| 16/4 | 4.70 | 47.09 | -- | -- | -- | |
| Buprenorphine/Naloxone Film | 2/0.5 | 1.07 | 8.43 | -- | -- | -- |
| 4/1 | 1.66 | 14.62 | -- | -- | -- | |
| 8/2 | 3.55 | 30.66 | -- | -- | -- | |
| 12/3 | 4.80 | 41.74 | -- | -- | -- | |
| Buprenorphine/Naloxone Tablet (Zubsolv®) | 0.7/0.18 | -- | -- | -- | -- | -- |
| 1.4/0.36 | 0.81 | 7.01 | -- | -- | -- | |
| 2.9/0.71 | -- | -- | -- | -- | -- | |
| 5.7/1.4 | 2.66 | 23.51 | -- | -- | -- | |
| 8.6/2.12 | 3.68 | 32.27 | -- | -- | -- | |
| 11.4/2.9 | 4.58 | 41.51 | -- | -- | -- | |
| Buprenorphine/Naloxone Film (Bunavail®) | 2.1/0.3 | -- | -- | -- | -- | -- |
| 4.2/0.7 | 3.41 | 27.17 | -- | -- | -- | |
| 6.3/1.04 | 4.90 | 38.47 | -- | -- | -- | |
| Buprenorphine Implant (Probuphine®) | 320 | ~2.6f | 19.6g | ~0.6f | ~0.82 | ~2.6f |
| Monthly Buprenorphine Depot (Sublocade®) | 100 | 1.54 | 1557.40 | 2.48 | 3.21 | 4.88 |
| 300 | 5.37 | -- | 5.01 | 6.54 | 10.12 | |
| Buprenorphine Depot (CAM2038) | ||||||
| Weekly | 16 | 3.08 | 335 | 0.84 | 2.09 | 4.30 |
| 24 | 3.64 | -- | -- | -- | -- | |
| 32 | 5.27 | 638 | 2.63 | 4.17 | 6.87 | |
| Monthly | 64 | 3.81 | 1360 | -- | -- | -- |
| 96 | 5.47 | 1830 | -- | -- | -- | |
| 128 | 6.59 | 2550 | 2.09 | 3.89 | 11.1 | |
| 160 | -- | -- | 2.66 | 5.27 | 15.4 | |
Unless otherwise noted, data are taken from product package inserts and Center on Drug Evaluation Research Clinical Biopharmaceutical Review Packages
The brand name product is no longer marketed. The generic products are bioequivalent; thus, pharmacokinetic parameters are similar for all buprenorphine/naloxone tablets.
AUC0–48, not 0-inf
Manufacturers using these pharmacokinetic data in their package inserts are Amneal Pharmaceuticals, LLC and Ethypharm SA
Manufacturers using these pharmacokinetic data in their package inserts are Kremers Urban Pharmaceuticals and SpecGx LLC.
Manufacturers using these pharmacokinetic data in their package inserts are: Actavis Pharma Inc.; Sun Pharmaceutical Industries Limited; Teva Pharmaceuticals USA, Inc.; and West-Ward Pharmaceuticals Corp.
Estimated based on graph from Beebe et al. (2009) poster: Safety, Efficacy, and Pharmacokinetics of Probuphine®, a 6-Month Implantable Sustained-Release Formulation of Buprenorphine, for the Treatment of Opioid Addiction
AUC0–24, not 0-inf