Table 2.
Summary of the PK Parameters of Caffeine and Paraxanthine Following Administration of Caffeine + Placebo (Day 1) and of Caffeine + CBD (Day 26) — PK Analysis Set
| Primary Analysis | Sensitivity Analysis | ||
|---|---|---|---|
| Parameter | Caffeine + Placebo (Day 1) n = 16 | Caffeine + CBD (Day 26) n = 9 | Caffeine + CBD (Day 26) n = 6 |
| Caffeine | |||
| AUC0‐t (ng∙h/mL) | 45 600 (55.5) | 82 800 (35.4) | 89 600 (33.5) |
| AUC0‐∞ (ng∙h/mL) | 46 900 (57.4) | 89 200 (38.2) | 97 900 (36.1) |
| Cmax (ng/mL) | 4710 (22.1) | 5270 (20.8) | 5520 (18.7) |
| tmax a (h) | 1.51 (0.50‐3.00) | 3.00 (0.50‐5.00) | 3.00 (0.50‐4.13) |
| tlast a (h) | 35.99 (18.00‐47.92) | 48.00 (35.92‐48.00) | 48.00 (35.92‐48.00) |
| t1/2 (h) | 5.40 (42.5) | 10.9 (32.5) | 11.7 (35.1) |
| tlag a (h) | 0.00 (0.00‐0.00) | 0.00 (0.00‐0.00) | 0.00 (0.00‐0.00) |
| CL/F (L/h) | 5.55 (50.2) | 2.57 (39.4) | 2.30 (37.9) |
| Paraxanthine | |||
| Parameter | Caffeine + Placebo (Day 1) n = 16 |
Caffeine + CBD (Day 26) n = 7 |
Caffeine + CBD (Day 26) n = 6 |
| Caffeine | 22 200 (26.1) | 24 100 (13.0) | 24 100 (14.2) |
| AUC0‐∞ (ng∙h/mL) | 23 900 (29.9) | 28 300 (18.4) | 28 600 (19.8) |
| Cmax (ng/mL) | 1250 (19.9) | 895 (16.4) | 905 (17.5) |
| tmax a (h) | 7.99 (4.00‐18.02) | 14.00 (5.97‐18.00) | 14.00 (10.00‐18.00) |
| tlast a (h) | 36.00 (24.00‐47.92) | 48.00 (35.92‐48.00) | 48.00 (35.92‐48.00) |
| t1/2 (h) | 7.15 (55.3) | 13.7 (30.4) | 13.8 (33.0) |
| tlag a (h) | 0.00 (0.00‐0.52) | 0.00 (0.00‐0.50) | 0.00 (0.00‐0.50) |
| MRAUC0‐t | 0.603 (27.0) | 0.323 (26.1) | 0.311 (27.2) |
| MRAUC0‐∞ | 0.627 (25.5) | 0.349 (23.6) | 0.336 (24.6) |
| MRCmax | 0.299 (28.5) | 0.186 (18.4) | 0.180 (18.2) |
AUC0‐t, area under the plasma concentration‐time curve up to time t, where t is the last point with a concentration above the lower limit of quantification; AUC0‐∞, area under the plasma concentration‐time curve from time 0 to infinity; CBD, cannabidiol; Cmax, maximum (peak) concentration of drug in blood plasma; CV%, coefficient of variation; FU, follow‐up; max, maximum; min, minimum; MRAUC0‐t, ratio of metabolite AUC0‐t to parent AUC0‐t; MRAUC0‐∞, ratio of metabolite AUC0‐∞ to parent AUC0‐∞; MRCmax, ratio of metabolite Cmax to parent Cmax; PK, pharmacokinetic; t1/2, terminal‐phase half‐life; tlag, time to the observation prior to the first observation with a quantifiable plasma concentration; tlast, time of Ĉlast (the estimated last plasma concentration); tmax, (observed) time after drug administration at which peak plasma concentration occurs.
Note: For the treatment of caffeine + placebo, the primary analysis and sensitivity analysis are equal.
Note: Arithmetic mean (%CV) is presented unless otherwise noted.
Median (min‐max).