| |
Study 1
(n=33) |
Study 2
(n=24) |
| Parameter, mean (SD) |
OC/APAP ER
1 tablet q12h |
OC/APAP ER
2 tablets q12h |
IR OC/APAP
1 tablet q6h |
OC/APAP ER
2 tablets q12h |
IR Oxycodone
1 tablet q6h |
IR OC/APAP
1 tablet q6h |
| Day 1 |
|
|
|
|
|
|
| AUC0-12h, ng•h/mL |
66.9 (15.1) |
135.9 (30.8) |
141.7 (29.8) |
136.1 (23.7) |
242.6 (19.9) |
132.5 (22.8) |
| Cmax, ng/mL |
8.34 (2.37) |
17.05 (3.97) |
21.93 (4.80) |
16.04 (3.64) |
34.78 (8.64) |
19.83 (5.07) |
| Tmax, ha |
3.0 (0.75-7.0) |
3.0 (0.5-5.9) |
7.0 (0.5-8.0) |
3.0 (0.5-8.0) |
7.0 (0.75-10.0) |
8.0 (0.5-10.0) |
| tlag, ha |
0.0 (0.0-0.5) |
0.0 (0.0-0.3) |
0.0 (0.0-0.25) |
0.0 (0.0-0.27) |
0.0 (0.0-0.25) |
0.0 (0.0-0.25) |
| Day 5 (steady state) |
|
|
|
|
|
|
| AUC0-12hss, ng•h/mL |
102.4 (29.3) |
208.6 (59.3) |
208.9 (57.3) |
208.3 (45.3) |
376.9 (83.9) |
191.5 (42.8) |
| Cavgss, ng/mL |
8.53 (2.44) |
17.38 (4.94) |
17.41 (4.78) |
17.36 (3.78) |
31.41 (6.99) |
15.96 (3.57) |
| Cmaxss, ng/mL |
12.67 (3.48)b |
25.67 (7.49)b |
30.50 (8.91) |
24.00 (5.38) |
45.15 (10.54) |
26.32 (6.18) |
| Cminss, ng/mL |
4.06 (1.40) |
8.98 (3.52) |
8.78 (3.17) |
9.31 (2.39) |
19.91 (4.93) |
8.81 (2.40) |
| Degree of fluctuation, % |
101.7 (14.1)b |
97.2 (18.8)b |
126.8 (27.9) |
83.9 (17.6)b |
79.9 (19.8) |
110.9 (33.4) |
| Swing |
2.2 (0.6)b |
2.0 (0.7)b |
2.7 (0.9) |
1.7 (0.6)b |
1.3 (0.5) |
2.1 (0.9) |
| Tmaxss, ha |
2.0 (0.5-10.0)b |
2.0 (0.5-7.0)b |
6.5 (0.5-8.0) |
3.0 (1.0, 5.9)b,c |
3.0 (1.0, 12.0) |
7.3 (0.5, 8.1) |
| t1/2, h |
5.5 (1.2) |
6.1 (1.5)b |
5.5 (1.7) |
5.4 (0.9)b,c |
4.6 (0.6) |
4.7 (0.6) |
| Kel, 1/h |
0.1326 (0.0269) |
0.1199 (0.0291)b |
(0.0418)
|
0.1318 (0.0223)b,c |
0.1525 (0.0206) |
0.1517 (0.0205) |
aMedian (range); bReached statistical significance vs IR OC/APAP; c Reached statistical significance vs IR oxycodone
APAP, acetaminophen; AUC0-12hss, area under the plasma concentration-time curve from time 0 to 12 h at steady state; Cavgss, average observed plasma concentration during
the dosing interval at steady state; Cmaxss, maximum observed plasma concentration at steady state; Cminss, plasma concentration obtained at predose during steady state;
ER, extended release; IR, immediate release; Kel, apparent terminal elimination rate constant; OC, oxycodone; Tmaxss, time to Cmax at steady state; t1/2, terminal elimination
half-life |
