TABLE 1

Enzymatic stability of ACV prodrugs in rat plasma and intestinal homogenates

Values are mean ± S.D. (n = 3−6).


Drug

Plasmaa

Intestinal Segmentsb
kobs c
t1/2
kobs c
t1/2
min−1 min min−1 min
VACV 0.002 ± 0.001 346.5 ± 133.3 0.02 ± 0.001 28.8 ± 1.6
GVACV 0.034 ± 0.009 20.9 ± 5.3 0.04 ± 0.009 17.2 ± 6.4
VVACV 0.13 ± 0.009 5.3 ± 0.3 0.03 ± 0.002 24.5 ± 2.3
VYACV 0.53 ± 0.48 2.1 ± 1.2 *
GYACV
*

*

  • a Measured using rat plasma.

  • b Measured using intestinal segments.

  • c First order rate constant.

  • * No intact prodrug detected after 1 min.