Table 5.
Comparative bioavailability of apomorphine sublingual film and subcutaneous apomorphine formulations
| PK parameter | APL (n = 8) | SC-APO (n = 6) | SC-APO-GO (n = 7) |
|---|---|---|---|
| Cmax/dose, ng/ml/mg | |||
| LS meana (90% CI) | 0.28 (0.19–0.41) | 2.29 (1.46–3.59) | 2.74 (1.82–4.13) |
| GMRb (90% CI) vs. SC-APO | 12.3 (7.5–20.3) | – | – |
| GMR (90% CI) vs. SC-APO-GO | 10.3 (6.5–16.3) | 83.4 (50.5–137.6) | – |
| AUC0–24/dose, h·ng/ml/mg | |||
| LS mean (90% CI) | 0.52 (0.36–0.76) | 2.97 (2.01–4.39) | 3.04 (2.08–4.45) |
| GMR (90% CI) vs. SC-APO | 17.6 (13.7–22.5) | – | – |
| GMR (90% CI) vs. SC-APO-GO | 17.2 (13.7–21.6) | 97.8 (76.6–124.8) | – |
| AUClast/dose, h·ng/ml/mg | |||
| LS mean (90% CI) | 0.50 (0.34–0.73) | 2.91 (1.97–4.30) | 3.00 (2.05–4.39) |
| GMR (90% CI) vs. SC-APO | 17.2 (13.1–22.5) | – | – |
| GMR (90% CI) vs. SC-APO-GO | 16.7 (13.0–21.3) | 96.9 (74.2–126.4) | – |
| AUC∞/dose, h·ng/ml/mg | |||
| LS mean (90% CI) | 0.52 (0.36–0.76) | 2.97 (2.02–4.39) | 3.04 (2.08–4.45) |
| GMR (90% CI) vs. SC-APO | 17.6 (13.7–22.5) | – | – |
| GMR (90% CI) vs. SC-APO-GO | 17.2 (13.7–21.6) | 97.8 (76.6–124.8) | – |
APL apomorphine sublingual film, AUC area under the concentration-time curve, AUC0–24 AUC from time 0 to 24 h, AUC∞ AUC from time 0 extrapolated to infinity, AUClast AUC from time 0 to the last measurable plasma concentration, CI confidence interval, Cmax maximum observed plasma concentration, GMR geometric mean ratio, LS least squares, PK pharmacokinetics, SC-APO subcutaneous apomorphine injection, SC-APO-GO subcutaneous apomorphine prefilled injection pen
aLS mean and 90% CI for LS mean have been exponentiated
bEstimates of the mean and CI limits for the natural log values were exponentiated and multiplied by 100