Table 2.
Pharmacokinetic parameters of rivaroxaban after administration of single doses in healthy Chinese subjects (values presented as geometric means with geometric % coefficients of variation and 95% confidence intervals)
| Rivaroxaban dose | |||||
|---|---|---|---|---|---|
| 2.5 mg | 5 mg | 10 mg | 20 mg | 40 mg | |
| (n= 8) | (n= 8) | (n= 8) | (n= 8) | (n= 8) | |
| AUCτ (µg h−1 l−1) | 251.7 (0.57) | 410.6 (0.29) | 1022 (0.13) | 1 354 (0.10) | 1 402 (0.09) |
| [167.8, 335.5] | [352.5, 468.7] | [796.8, 1248] | [1 029, 1 678] | [1 161, 1 643] | |
| AUCτ(norm) (g h−1 l−1) | 6242 (0.02) | 5372 (0.02) | 5950 (0.02) | 3 987 (0.04) | 2 194 (0.06) |
| [4361, 8122] | [4244, 6500] | [4383, 7516] | [2 869, 5 106] | [1 800, 2 587] | |
| AUC/D (h l−1) | 0.1007 (1430) | 0.08212 (1462) | 0.1022 (1256) | 0.06768 (2 000) | 0.03505 (3 524) |
| [0.06709, 0.1342] | [0.07050, 0.09374] | [0.07968, 0.1248] | [0.05146, 0.08390] | [0.02902, 0.04108] | |
| Cmax (µg l−1) | 51.27 (3.40) | 67.21 (1.90) | 143.2 (0.91) | 204.4 (0.57) | 176.1 (0.70) |
| [25.41, 77.13] | [53.21, 81.21] | [110.6, 175.8] | [179.4, 229.3] | [142.9, 209.2] | |
| Cmax,norm (g l−1) | 1270 (0.14) | 879.5 (0.14) | 833.4 (0.16) | 601.9 (0.21) | 275.6 (0.46) |
| [671.6, 1868] | [719.7, 1039] | [619.2, 1047] | [500.4, 703.4] | [215.9, 335.3] | |
| Cmax/D (1 l−1) | 0.02051 (8504) | 0.01344 (9481) | 0.01432 (9131) | 0.01022 (11 419) | 0.00440 (28 156) |
| [0.01016, 0.03086] | [0.01064, 0.01624] | [0.01106, 0.01758] | [0.008972, 0.01146] | [0.003574, 0.005232] | |
| tmax* (h) | 2.00 (0.50–6.00) | 2.00 (1.00–4.00) | 2.25 (1.00–4.00) | 2.00 (0.50–3.00) | 1.25 (0.50–3.00) |
| [0.54, 3.46] | [1.00, 3.00] | [1.23, 3.27] | [1.19, 2.81] | [0.63, 1.87] | |
| t1/2 (h) | 3.38 (46.37) | 7.92 (18.11) | 7.57 (18.45) | 5.62 (24.62) | 7.03 (25.65) |
| [1.85, 4.92] | [5.33, 10.51] | [5.31, 9.82] | [4.06, 7.18] | [2.13, 11.92] | |
| CL/f (l h−1) | 9.93 (14.49) | 12.18 (9.86) | 9.78 (13.13) | 14.78 (9.16) | 28.53 (4.33) |
| [6.50, 13.37] | [10.14, 14.22] | [7.77, 11.79] | [10.44, 19.11] | [23.26, 33.80] | |
| Vz/F (l kg−1) | 0.78 (200.1) | 2.13 (75.54) | 1.84 (77.16) | 2.04 (70.85) | 4.62 (36.10) |
| [0.44, 1.13] | [1.25, 3.00] | [1.34, 2.33] | [1.36, 2.71] | [1.88, 7.35] | |
| Aeur (%) | 27.2 (5.94) | 23.6 (9.42) | 26.7 (5.25) | 19.6 (5.23) | 11.0 (3.26) |
| [22.2, 32.2] | [15.7, 31.5] | [22.3, 31.1] | [15.2, 24.0] | [8.27, 13.7] | |
Median (range). AUCτ, area under the concentration–time curve during the dosage interval τ; AUCτ(norm), AUCτ divided by dose (mg) per kg body weight; AUC/D, AUC divided by dose; Cmax, maximal drug concentration in plasma; Cmax,norm, Cmax divided by dose (mg) per kg body weight; Cmax/D, Cmax divided by dose; tmax, time to reach maximum drug concentration in plasma; t1/2, half-life; CL/f, total body clearance of drug from plasma calculated after oral administration; Vz/F, apparent volume of distribution during terminal phase; Aeur, amount of drug excreted via the urine.