TABLE 2.
Plasma pharmacokinetic parameters of filociclovir by dose level on days 1 and 7
| Parameter | Value by group and daya
|
|||||
|---|---|---|---|---|---|---|
| Day 1 |
Day 7 |
|||||
| 100 mg (N = 6) | 350 mg (N = 6) | 750 mg (N = 6) | 100 mg (N = 6) | 350 mg (N = 6) | 750 mg (N = 5) | |
| Mean AUC0–24, ng·h/ml (%CV) | 2,281.0 (29.7) | 4,832.2 (55.9) | 11,343.0 (153.5) | 2,170.8 (37.5) | 4,211.3 (33.1) | 3,962.8 (33.0) |
| Mean Cmax, ng/ml (%CV) | 547.8 (26.1) | 1,086.0 (41.9) | 2,084.0 (119.1) | 588.5 (25.3) | 855.5 (49.0) | 882.0 (60.1) |
| Mean Tmax, h (Min, max) | 1.835 (1.00, 3.65) | 2.050 (1.43, 3.97) | 2.500 (1.43, 3.87) | 1.618 (0.95, 1.98) | 2.552 (1.98, 3.80) | 1.882 (1.43, 2.07) |
| Mean t1/2, h (%CV) | 3.2080 (10.3) | 3.3532 (15.5) | 3.5905 (21.4) | 3.6220 (17.2) | 3.2635 (9.4) | 3.8974 (12.3) |
| Mean CL/F, liters/h (%CV) | 47.198 (32.3) | 96.750 (63.4) | 195.658 (91.7) | 52.618 (42.4) | 91.268 (33.1) | 210.970 (40.3) |
| Mean CLr, liters/h (%CV) | 15.359 (29.9) | 15.517 (47.1) | 15.602 (36.1) | 16.090 (31.8) | 17.005 (17.2) | 16.978 (17.0) |
| Mean Pctrec, % (%CV) | 34.25 (30.3) | 22.18 (65.7) | 13.82 (76.3) | 32.46 (30.3) | 19.67 (20.9) | 9.07 (40.7) |
| Mean V/F, liters (%CV) | 220.95 (35.8) | 502.08 (83.2) | 1015.37 (105.8) | 286.53 (53.6) | 430.92 (34.1) | 1,205.16 (49.6) |
a
N, number of subjects in the PK population; AUC, area under the curve; Cmax, maximum observed concentration; Tmax, time to maximum concentration; t1/2, elimination half-life; CL/F, dose/AUC; CLr, Ae/AUC, where Ae is the amount recovered in urine during the dosing interval; Pctrec, 100 × (Ae/dose); V/F, dose/(AUC × ke), where ke is the elimination rate constant.