Table 6.
Pharmacokinetic parameters of cannabidiol and metabolites for the single ascending dose arm of the trial
| Pharmacokinetic parameter (unit) | Cannabidiol, mg | |||
|---|---|---|---|---|
| 1500 (n = 6) | 3000 (n = 6) | 4500 (n = 6) | 6000 (n = 6) | |
| CBD | ||||
| Cmax (ng/mL)a | 292.4 (87.9) | 533.0 (35.1) | 722.1 (52.3) | 782 (83.0) |
| AUCt (ng·h/mL)a | 1517 (78.2) | 2669 (36.4) | 3215 (50.3) | 3696 (79.9) |
| AUC∞ (ng·h/mL)a | 1618 (74.6) | 2802 (35.5) | 3426 (48.3) | 3900 (79.3) |
| tmax (h)b | 4.00 (3.00–5.00) | 5.00 (3.00–5.00) | 5.00 (5.00–5.00) | 5.00 (3.00–5.02) |
| t½,z (h)c | 14.43 (36.1) | 14.39 (14.9) | 16.61 (18.7) | 15.42 (29.0) |
| CL/F (L/h)c | 1111 (67.2) | 1121 (30.5) | 1445 (52.6) | 1909 (77.3) |
| Vz/F (L/h)c | 20,963 (55.3) | 23,357 (32.9) | 36,575 (66.8) | 42,849 (75.5) |
| 6-OH-CBD | ||||
| Cmax (ng/mL)a | 10.7 (65.7) | 14.4 (28.6) | 14.5 (36.5) | 23.5 (68.6) |
| AUCt (ng·h/mL)a | 91.23 (66.7) | 121.1 (14.7) | 127.1 (53.1) | 160.7 (91.4) |
| AUC∞ (ng·h/mL)a | 132.5 (93.7)d | 126.0 (18.2)e | 127.1 (50.3)e | 215.0 (92.0)f |
| tmax (h)b | 4.00 (2.50–4.00) | 4.50 (2.50–5.00) | 5.00 (4.00–5.00) | 5.00 (3.00–5.02) |
| t½,z (h)c | 40.75 (73.6) | 22.78 (81.9)d | 33.92 (55.9) | 28.67 (104.5) |
| 7-OH-CBD | ||||
| Cmax (ng/mL)a | 238.7 (84.0) | 332.2 (30.2) | 404.8 (37.3) | 515.8 (42.3) |
| AUCt (ng·h/mL)a | 1616 (76.9) | 1959 (24.1) | 2810 (40.3) | 3299 (63.5) |
| AUC∞ (ng·h/mL)a | 1826 (74.6) | 2143 (23.2) | 3039 (42.2) | 3531 (63.1) |
| tmax (h)b | 3.50 (2.50–4.00) | 4.50 (3.00–5.00) | 5.00 (4.00–5.00) | 5.00 (3.00–5.02) |
| t½,z (h)c | 18.70 (11.4) | 15.42 (32.5) | 14.89 (22.4) | 14.46 (23.1) |
| 7-COOH-CBD | ||||
| Cmax (ng/mL)a | 3060 (62.4) | 3557 (34.7) | 5120 (19.7) | 4591 (44.3) |
| AUCt (ng·h/mL)a | 60,467 (85.4) | 74,660 (40.2) | 111,025 (39.7) | 107,022 (74.1) |
| AUC∞ (ng·h/mL)a | 75,869 (95.1)e | 90,818 (47.5)d | 132,731 (51.1)d | 113,026 (42.3)e |
| tmax (h)b | 4.00 (4.00–5.00) | 5.00 (4.00–5.00) | 5.00 (4.00–8.00) | 5.01 (4.00–8.00) |
| t½,z (h)c | 25.98 (26.5) | 23.88 (40.5) | 25.18 (25.3) | 30.24 (52.7) |
AUCt area under the plasma concentration-time curve from time zero to time t, AUC∞ area under the concentration-time curve from time zero to infinity, 7-COOH-CBD 7-carboxy–cannabidiol, 6-OH-CBD 6–hydroxy-cannabidiol, 7-OH-CBD 7–hydroxy-cannabidiol, CBD cannabidiol, CL/F oral clearance of drug from plasma, Cmax maximum measured plasma concentration, CV% percentage coefficient of variation, tmax time to maximum plasma concentration, t½,z terminal elimination half-life, Vz/F apparent volume of distribution
aGeometric mean (geometric CV%)
bMedian (range)
cArithmetic mean (arithmetic CV%)
dn = 4
en = 3
fn = 5