TABLE 4.
Geometric mean pharmacokinetics parameters (%CV) of naltrexone and naloxone in female and male participants
| Variable (U)a | Naloxone (Treatment B) |
Naloxone (Treatment C) |
Naltexone (Treatment A) |
Naltrexone (Treatment C) |
||||
|---|---|---|---|---|---|---|---|---|
| Female | Male | Female | Male | Female | Male | Female | Male | |
| N | 5 | 6 | 5 | 6 | 6 | 6 | 5 | 6 |
| Cmax (ng/ml) | 4.75 (62.4) | 3.96 (36.6) | 3.41 (42.6) | 3.77 (34.2) | 5.45 (50.8) | 3.80 (109) | 1.71 (43.2) | 1.71 (31.6) |
| Tmax (h) | 0.75 (0.25–0.75) | 0.42 (0.27–0.75) | 0.50 (0.33–0.50) | 0.50 (0.25–0.75) | 0.42 (0.17–1.0) | 0.33 (0.25–0.75) | 1.0 (0.50–2.0) | 0.75 (0.25–1.0) |
| AUC0–inf (ng·h/ml) | 8.90 (46.3) | 7.55 (32.7) | 7.33 (47.9) | 6.74 (17.9) | 11.9 (19.2) | 7.75 (42.6) | 7.07 (29.7)b | 5.20 (12.3) |
| λz (h−1) | 0.412 (30.0) | 0.355 (34.9) | 0.407 (32.6) | 0.317 (51.8) | 0.309 (24.0) | 0.329 (11.6) | 0.314 (14.0)b | 0.327 (8.08) |
| t1/2 (h) | 1.68 (30.0) | 1.95 (34.9) | 1.70 (32.6) | 2.19 (51.8) | 2.25 (24.0) | 2.10 (11.6) | 2.21 (14.0)b | 2.12 (8.08) |
| CL/F (l/min) | 6.13 (46.3) | 7.23 (32.7) | 7.44 (47.9) | 8.10 (17.9) | 2.52 (19.2) | 3.87 (42.6) | 4.25 (29.7)b | 5.76 (12.3) |
AUC0–inf, area under the plasma concentration-time curve from time zero to infinity; CL/F, apparent clearance; t1/2, terminal phase half-life; λz, terminal phase rate constant; Tmax, time to reach Cmax; Treatment A, 2 mg naltrexone, intranasally; Treatment B, 4 mg naloxone, intranasally; Treatment C, 2 mg naltrexone plus 4 mg naloxone, intranasally.
a
Geometric mean (%CV) for all except median (range) for Tmax.
b
N = 4.