TABLE 2.
Parametera | 250 mg IR BID
|
500 mg XR QD
|
500 mg IR BID
|
1,000 mg XR QD
|
||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
Mean | Median | CV (%) | Mean | Median | CV (%) | Mean | Median | CV (%) | Mean | Median | CV (%) | |
V1/F (liters) | 47.4 | 41.7 | 64.5 | 62.7 | 66.8 | 45.6 | 56.4 | 55.4 | 66.8 | 80.9 | 77.5 | 43.3 |
Vp/F (liters) | 203 | 197 | 25.6 | 174 | 166 | 31.8 | 213 | 216 | 33.1 | 198 | 191 | 25.9 |
Vss/F (liters) | 250 | 242 | 21.1 | 237 | 217 | 25.9 | 269 | 277 | 26.6 | 279 | 277 | 18.4 |
CLd/F (liters/h) | 59.8 | 58.5 | 39.5 | 34.6 | 31.1 | 46.8 | 58.0 | 55.0 | 48.6 | 32.7 | 29.7 | 39.2 |
CLt/F (liters/h) | 63.2 | 61.1 | 26.1 | 68.3 | 64.6 | 29.5 | 63.0 | 62.1 | 27.2 | 68.8 | 60.8 | 38.0 |
CLR (liters/h) | 21.5 | 21.5 | 22.9 | 22.9 | 22.2 | 17.7 | 23.2 | 23.8 | 22.4 | 23.8 | 24.1 | 16.4 |
TLag (h) | 0.551 | 0.386 | 172 | 0.379 | 0.380 | 69.5 | 0.708 | 0.471 | 146 | 0.556 | 0.464 | 66.8 |
ka (h−1) | 0.963 | 0.689 | 89.0 | 0.476 | 0.444 | 41.9 | 0.718 | 0.598 | 77.2 | 0.425 | 0.405 | 31.1 |
V1/F, volume of distribution of the central compartment; F, fraction of administered dose systemically available (unidentifiable); Vp/F, volume of distribution of the peripheral compartment; Vss/F, V1/F plus Vp/F; CLd/F, distributional clearance; CLt/F, total clearance; CLR, renal clearance; TLag, lag time before onset of absorption; ka, absorption rate constant.