TABLE 2.
Summary of the ORIN1001 pharmacokinetic parameters calculated using the non-compartmental analysis (NCA).
| Dose (mg) | AUC0-t a , b (ng·h/mL) | AUC0-inf a (ng·h/mL) | Cmax a (ng/mL) | Tmax c (h) | t1/2 a (h) | Vz/F a (L) | CL/F a (L/h) | |
|---|---|---|---|---|---|---|---|---|
| Single-dose | 100 (n = 3) | 68788.93 (11862.47) | 75962.73 (13066.34) | 3820 (663.67) | 2 (2,2) | 33.26 (6.66) | 64.02 (14.63) | 1.34 (0.22) |
| 200 (n = 3) | 131728.83 (7053.45) | 145145.68 (10518.25) | 5590 (1,092.34) | 7.33 (4,12) | 32.01 (1.36) | 63.74 (2.71) | 1.38 (0.10) | |
| 300 (n = 4) | 228262.75 (40115.46) | 255482.73 (43998.63) | 9360 (1947.67) | 4 (2,6) | 32.03 (2.65) | 56.10 (14.76) | 1.20 (0.22) | |
| 400 (n = 3) | 368183.33 (134885.27) | 429240.23 (187717.63) | 13446.67 (3589.78) | 4 (4,4) | 33.68 (8.52) | 48.56 (14.41) | 1.05 (0.43) | |
| 500 (n = 3) | 378935.33 (11038.56) | 423552.73 (9794.66) | 14866.67 (2182.51) | 4.33 (1,6) | 33.46 (5.25) | 57.01 (9.18) | 1.18 (0.03) | |
| 650 (n = 5) | 522604.40 (160299.01) | 577313.57 (191065.33) | 18300 (1826.20) | 5.60 (2,12) | 29.74 (4.81) | 51.51 (14.21) | 1.24 (0.43) | |
| 900 (n = 4) | 1043135 (389883.52) | 1188790.39 (477250.87) | 31225 (9468.32) | 11.50 (6,24) | 33.90 (3.82) | 43.46 (23.54) | 0.90 (0.48) | |
| Multiple- dose | 100 (n = 3) | 66065 (7377.35) | 4846.67 (226.79) | 3.33 (2,4) | 16.05 (5.98) | 20.85 (1.68) | 0.99 (0.35) | |
| 200 (n = 3) | 171946.67 (33840.18) | 10633.33 (650.64) | 4.67 (2,8) | 20.19 (4.41) | 18.65 (2.44) | 0.67 (0.23) | ||
| 300 (n = 3) | 239481.67 (52023.15) | 14700 (3459.77) | 4 (2,6) | 21.25 (2.61) | 20.64 (3.97) | 0.68 (0.19) | ||
| 400 (n = 3) | 371281.67 (95066.09) | 21466.67 (4781.56) | 4 (2,6) | 25.53 (8.60) | 18.76 (4.12) | 0.55 (0.23) | ||
| 500 (n = 3) | 579450 (201502.75) | 33533.33 (10802.93) | 4.33 (1,8) | 31.04 (9.63) | 16.37 (4.96) | 0.40 (0.19) | ||
| 650 (n = 2) | 661975 | 39400 | 2 (2,2) | 18.91 | 16.29 | 0.59 | ||
| 900 (n = 2) | 1022700 | 58650 | 5 (4,6) | 17.81 | 14.73 | 0.57 |
a
These data are displayed as mean (SD).
b
t means the time points at 100 h after single-dose and 24 h after multiple-dose on day 21.
c
Tmax is displayed as median (minimum, maximum).