Table 3.
AACV | SACV | EACV | VACV | IACV | ||||||
---|---|---|---|---|---|---|---|---|---|---|
Rate (k* 103) | Half life (hrs) | Rate (k* 103) | Half life (hrs) | Rate (k* 103) | Half life (hrs) | Rate (k* 103) | Half life (hrs) | Rate (k* 103) | Half life (hrs) | |
Caco2 | 10.1 ± 0.6 | 1.15 ± 0.07 | 2.1 ± 0.6 | 6.1 ± 2.2 | 2.82 ± 0.54 | 4.2 ± 0.7 | 11.9 ± 0.7 | 1.6 ± 0.15 | 1.8 ± 0.6 | 6.9 ± 1.9 |
Plasma | 2.45 ± 0.35 | 4.8 ± 0.7 | 0.06 ± 0.02 | 195 ± 57 | 0.28 ± 0.04 | 42.4 ± 6.1 | 0.05 ± 0.02 | 226 ± 67 | 0.08 ± 0.006 | 139 ± 9.2 |
Intestine | 105 ± 2.7 | 0.11 ± 0.002 | 5.7 ± 0.7 | 2.1 ± 0.2 | 1.42 ± 0.08 | 8.2 ± 0.5 | 18.5 ± 0.7 | 0.6 ± 0.02 | 8.8 ± 0.5 | 1.32 ± 0.07 |
Liver | -- | a | 27 ± 3 | 0.44 ± 0.06 | 0.05 ± 0.002 | 223 ± 8.8 | 163 ± 9 | 0.07 ± 0.004 | 165 ± 0.9 | 0.07 ± 0.004 |
Values are mean ± S.D. (n = 3–6).
min−1.mg protein−1
No intact prodrug detected after 1 min.