Table 1.
Summary Statistics of Pharmacokinetic Parameters After Single Dose of NRL‐1
| Arithmetic Mean (CV%) | Geometric Mean (CV%) | |||||
|---|---|---|---|---|---|---|
| Pharmacokinetic Parameter | 5 mg | 10 mg | 20 mg | 5 mg | 10 mg | 20 mg |
| Diazepam | ||||||
| Cmax, ng/mL | 85.6 (67%) | 133.6 (64%) | 235.3 (59%) | 64.2 (106%) | 107 (82%) | 199.6 (65%) |
| tmax, ha | 1.5 (0.3, 8) | 1.5 (0.8, 36) | 1.4 (0.5, 8) | … | … | … |
| AUC0‐t, h•ng/mL | 2232 (51%) | 3803 (52%) | 7946 (52%) | 1910 (68%) | 3303 (62%) | 6864 (63%) |
| AUC0‐∞, h•ng/mL | 2411 (48%) | 4505 (56%) | 9168 (55%) | 2110 (62%) | 3854 (65%) | 7711 (72%) |
| t½, h | 70 (42%) | 71 (44%) | 74 (49%) | 64 (47%) | 65 (48%) | 66 (49%) |
| CL/F, L/h | 2.8 (72%) | 3.1 (69%) | 3.2 (75%) | 2.4 (62%) | 2.6 (65%) | 2.6 (72%) |
| Nordiazepam | ||||||
| Cmax, ng/mL | 11.7 (48%) | 19.3 (61%) | 36.6 (57%) | 10.5 (55%) | 16.1 (71%) | 31.6 (59%) |
| tmax, ha | 96 (8, 240) | 96 (12, 240) | 96 (36, 240) | … | … | … |
| AUC0‐t, h•ng/mL | 1832 (46%) | 3115 (55%) | 6067 (53%) | 1638 (54%) | 2653 (66%) | 5285 (59%) |
| AUC0‐∞, h•ng/mL | 3229 (50%) | 4503 (37%) | 8838 (59%) | 2972 (46%) | 4258 (39%) | 7462 (73%) |
| t½, h | 91 (51%) | 68 (29%) | 85 (32%) | 82 (52%) | 66 (30%) | 82 (28%) |
AUC indicates area under the plasma concentration–time curve; AUC0‐t, AUC from time of dose to last measurement; AUC0–∞, AUC from time of dose extrapolated to infinity; Cmax, peak plasma concentration; CV%, coefficient of variation; tmax, time from dose to Cmax; t½, half‐time of elimination.
a
Values are medians (minimum, maximum). Ranges in subscripts indicate time intervals of measurements.