TABLE 3.
Pharmacokinetic parameters of three major metabolites of artemisone (M1, M2, and M3) in plasma following 3-day courses of artemisone in healthy subjects
| Parameter | Valuea
|
|||
|---|---|---|---|---|
| 40 mg daily for 3 days (n = 8)
|
80 mg daily for 3 days (n = 7)
|
|||
| Day 1 | Day 3 | Day 1 | Day 3 | |
| M1 | ||||
| Cmax (ng/ml) | 51.7/16.2 (39.5-73.1) | 47.8/23.7 (31.3-89.8) | 112.6/16.4 (69.7-140.0) | 85.3/25.9 (45.6-136.0) |
| AUC (ng · h/ml) | 112.6/19.8 (83.6-171.0) | 112.3/17.6 (84.2-175.3) | 296.0/21.2 (173.8-404.5) | 255.2/31.9 (133.2-438.0) |
| Tmax (h) | 1.75 (1.0-2.5) | 1.75 (0.75-2.5) | 2.0 (1.0-3.0) | 1.5 (1.0-3.0) |
| t1/2 (h) | 1.90/19.7 (1.28-3.08) | 1.54/14.9 (1.20-2.12) | 2.13/34.7 (1.11-3.36) | 1.63/22.5 (1.01-2.42) |
| M2 | ||||
| Cmax (ng/ml) | 40.6/23.4 (25.4-60.3) | 36.4/20.5 (23.3-58.2) | 87.2/18.6 (51.2-111.0) | 66.5/22.8 (38.8-101.0) |
| AUC (ng · h/ml) | 117.3/23.5 (70.5-179.2) | 115.1/15.4 (88.6-164.5) | 302.4/20.9 (180.5-416.8) | 263.0/26.8 (145.4-409.5) |
| Tmax (h) | 1.75 (1.0-3.0) | 2.0 (0.75-2.5) | 2.0 (1.5-3.0) | 2.5 (1.5-3.0) |
| t1/2 (h) | 1.31/16.4 (1.02-1.99) | 1.28/15.6 (0.92-1.92) | 1.59/14.0 (1.22-2.18) | 1.44/10.0 (1.21-1.72) |
| M3 | ||||
| Cmax (ng/ml) | 27.8/18.2 (18.8-37.1) | 22.5/18.4 (15.8-34.7) | 51.9/22.9 (26.7-71.7) | 38.2/29.6 (17.6-60.4) |
| AUC (ng · h/ml) | 95.9/18.0 (74.0-146.1) | 84.9/17.1 (62.7-124.7) | 213.1/24.2 (113.1-296.1) | 165.1/31.2 (72.8-266.3) |
| Tmax (h) | 2.0 (1.0-3.0) | 2.5 (1.5-3.0) | 2.0 (1.5-3.0) | 2.5 (2.0-4.0) |
| t1/2 (h) | 1.52/16.4 (1.05-1.94) | 1.69/17.8 (1.13-2.17) | 1.83/7.0 (1.63-2.17) | 1.86/10.6 (1.45-2.25) |
a
Values are presented as geometric mean/geometric %CV (range); median and range are listed for Tmax. Doses were as follows: 40 mg, two 20-mg immediate-release tablets; 80 mg, four 20-mg tablets.