Table 1.
Individual pharmacokinetic variables and summary statistics of RS ketamine following administration of 10 mg as a 30 min i.v. infusion and 25 mg sublingually as a wafer to eight healthy volunteers
| Subject | Cmax,i.v. (ng ml−1) | Cmax,SL (ng ml−1) | tmax,SL (h) | AUC(0,∞)i.v. (ng ml−1 h) | AUC(0,∞)SL (ng ml−1 h) | CL (l h−1) | Vz (l) | t1/2,i.v. (h) | t1/2,SL (h) | F (%) |
|---|---|---|---|---|---|---|---|---|---|---|
| 1 | 226.7 | 88.8 | 0.58 | 282.7 | 202.9 | 35.4 | 126 | 2.5 | 2.9 | 28 |
| 2 | 163.3 | 128.3 | 0.25 | 243.2 | 162.5 | 41.1 | 158 | 2.7 | 1.8 | 27 |
| 3 | 190.3 | 78.7 | 0.75 | 254.6 | 184.3 | 39.3 | 283 | 5.0 | 3.2 | 29 |
| 4 | 124.2 | 60.2 | 1 | 270.0 | 203.5 | 37.0 | 253 | 4.7 | 5.5 | 30 |
| 5 | 120.4 | 50.0 | 0.75 | 289.2 | 171.9 | 34.6 | 300 | 6.0 | 3.5 | 23 |
| 6 | 101.9 | 76.1 | 1 | 299.4 | 211.3 | 33.4 | 164 | 3.4 | 2.3 | 29 |
| 7 | 83.2 | 51.8 | 1 | 261.0 | 186.1 | 38.3 | 385 | 7.0 | 4.6 | 29 |
| 8 | 81.1 | 61.2 | 0.5 | 167.2 | 161.6 | 59.8 | 375 | 4.3 | 5.1 | 38 |
| Gmean* | 128.1 | 71.1 | 0.75 | 255.0 | 184.6 | 39.2 | 237 | 4.5 | 3.4 | 29 |
| Min–max | 81.1–226.7 | 50.0–128.3 | 0.25-1 | 167.2–299.4 | 161.6–211.3 | 33.4–59.8 | 126–385 | 2.5–7.0 | 1.8–5.5 | 23–38 |
| CV (%) | 16 | 14 | 21 | 8 | 4 | 8 | 18 | 16 | 17 | 6 |
| 90% CI† | 27, 31 |
Cmax, peak plasma concentration; tmax, time of Cmax; AUC(0,∞), area under the plasma concentration–time curve from time zero to infinity; CL, clearance following i.v. administration; Vz, apparent volume of distribution following i.v. administration; t1/2, terminal half-life; F, bioavailability; NA, Not applicable; SL, sublingual.
*
Gmean is provided for all variables except for bioavailability, tmax and t1/2 where medians are shown.
†
90% confidence interval (lower, upper).