| Table 3. Day 1 and steady-state (day 5) pharmacokinetic estimates for acetaminophen |
| |
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 tramadol/APAP
1 tablet q6h |
IR OC/APAP
1 tablet q6h |
| Day 1 |
|
|
|
|
|
|
| AUC0-12h, ng•h/mL |
12192 (3331) |
24141 (6436) |
24884 (6656) |
24924 (5667) |
26343 (4721) |
25094 (5085) |
| Cmax, ng/mL |
2631 (815) |
5245 (1473) |
5146 (1553) |
4858 (1066) |
4568 (976) |
4318 (1006) |
| Tmax, ha |
0.55 (0.25-3.0) |
0.75 (0.25-2.0) |
0.50 (0.25-8.0) |
1.0 (0.5-4.0) |
6.75 (0.5-8.2) |
0.53 (0.5-8.0) |
| tlag, ha |
0.0 (0.0-0.25) |
0.0 (0.0-0.25) |
0.0 (0.0-0.0) |
0.0 (0.0-0.0) |
0.0 (0.0-0.3) |
0.0 (0.0-0.0) |
| Day 5 (steady state) |
|
|
|
|
|
|
| AUC0-12hss, ng•h/mL |
15307 (4092) |
28512 (7714) |
28719 (7023) |
28160.40 (5807.09) |
29711.92 (5427.37) |
29284.22 (5477.73) |
| Cavgss, ng/mL |
1276 (341) |
2376 (643) |
2393 (585) |
2346.70 (483.92) |
2475.99 (452.28) |
2440.35 (456.48) |
| Cmaxss, ng/mL |
3117 (840) |
5872 (1932) |
5968 (1639) |
4792.50 (1132.40) |
5078.33 (1189.70) |
4876.67 (1383.08) |
| Cminss, ng/mL |
474.67 (163) |
870.42 (336) |
922.58 (321) |
852.75 (273.25)b,c |
1070.92 (367.35) |
1069.13 (291.83) |
| Degree of fluctuation, % |
212.1 (52.3) |
218.1 (81.1) |
213.8 (50.5) |
169.1 (39.8) |
163.9 (47.2) |
155.3 (38.8) |
| Swing |
6.0 (2.0) |
6.6 (3.6) |
5.9 (2.2) |
5.1 (2.1)b,c |
4.2 (2.1) |
3.8 (1.6) |
| Tmaxss, ha |
0.5 (0.3-3.0) |
0.5 (0.3-3.0) |
0.5 (0.3-8.0) |
1.0 (0.5, 4.0) |
0.9 (0.3, 8.0) |
0.8 (0.3, 8.0) |
| t1/2, h |
5.6 (1.4) |
7.5 (2.9)b |
5.7 (3.0) |
6.9 (1.8)c |
5.3 (1.1) |
6.2 (1.8) |
| Kel, 1/h |
0.1308 (0.0317) |
0.1026 (0.0292)b |
0.1416 (0.0515) |
0.1072 (0.0285)c |
0.1355 (0.0279) |
0.1201 (0.0338) |
aMedian (range); bReached statistical significance vs IR OC/APAP; cReached statistical significance vs IR tramadol/APAP
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 |
