Table 2.
PK Parameters
| Single-Dose Study | Multiple-Dose Study | |||||
|---|---|---|---|---|---|---|
| Deltoid (n = 16) | Gluteal (n = 17) | GMR (90% CI) | Deltoid/Deltoid (n = 73) | Gluteal/Deltoid (n = 68) | GMR (90% CI) | |
| PK parameters after the first injectiona | ||||||
| Cmax, ng/mL | 170 (58.6) | 136 (70.3) | 1.31 (1.02–1.67) | 135 (57.8) n = 24 | 126 (88.6) n = 22 | 1.20 (0.90–1.60) |
| C28, ng/mL | 103 (49.6) | 86.2 (37.5) | 1.24 (0.94–1.63) | 112 (50.1) n = 51b | 79.0 (37.3) n = 52b | 1.43 (1.22–1.69)† |
| tmax,c days | 7.1 (4.0–63.1) | 24.1 (4.1–70.0)* | N/A | 14.3 (3.8–29.0) n = 24 | 13.9 (3.9–28.0) n = 22 | N/A |
| AUC28, ng•d/mL | 3120 (1150) | 2380 (1410) | 1.42 (1.06–1.91) | 2728 (1277) n = 21 | 2359 (1527) n = 20 | 1.24 (0.91–1.68) |
| AUCt, ng•d/mL | 7360 (2420) | 7340 (2360) | 0.99 (0.80–1.23) | N/A | N/A | N/A |
| AUC∞, ng•d/mL | 7590 (2590) | 7920 (2580) n = 14 | 0.95 (0.75–1.21) | N/A | N/A | N/A |
| t1/2, days | 17.8 (7.45) | 24.0 (7.36) n = 14 | N/A | N/A | N/A | N/A |
| PK parameters after the fifth injection | ||||||
| Combined Deltoid/Deltoid and Gluteal/Deltoid Groups d | ||||||
| Cmax,ss, ng/mL | N/A | 328 (133) n=39 |
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| Cmin,ss, ng/mL | N/A | 239 (133) n=86b |
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| AUCt, ng•d/mL | N/A | 7027 (2689) n=36 |
||||
| tmax,c days | N/A | 3.95 (0.00–27.87) n=39 |
||||
Abbreviations: AUC, area under the concentration-time curve; Cmax, maximum plasma concentration; Cmax,ss, Cmax at steady state; Cmin,ss, minimum plasma concentration at steady state; GMR, geometric mean ratio; N/A, not applicable; PK, pharmacokinetic; t1/2, elimination half-life; tmax, time to maximum (peak) plasma concentration.
*P<0.05; †P=0.0002.
a Unless otherwise noted, PK parameters for the multiple-dose study were assessed following the first and before the second injection of aripiprazole once-monthly 400 mg. Following the first injection, 19 patients were excluded from the PK analysis, because they received oral aripiprazole during the first 2 weeks; 1 patient who had a high baseline aripiprazole concentration and 2 patients who had no baseline PK data were also excluded. Two patients were excluded because of insufficient PK profiles. In addition, AUC28 and C28 were not reported for 11 patients, because the sampling time of their last measurable plasma concentration available before the second injection was not within 28 ± 2 days after the first injection.
b Sample size is larger because of inclusion of data from sparse sampling sites.
c Reported as median (minimum-maximum). All other parameters are reported as mean (SD).
d Following the fifth deltoid injection of aripiprazole once-monthly 400 mg in the deltoid/deltoid group and fourth deltoid injection in the gluteal/deltoid group.