Table 3.
Prodrug |
Incubation medium |
|||||||||
HCl buffer (pH 1.2) and stomach homogenates | Phosphate buffer (pH 7.4) and intestinal homogenates |
Colon homogenate |
Fecal matter |
|||||||
K ± SD (min-1)1 | t1/2 (min) | Prodrug hydrolyzed | BBA released | K ± SD (min-1)1 | t1/2 (min) | Prodrug hydrolyzed | BBA released | |||
BH | Stable | Negligible | 0.0013 | 514.1 | 78.10% | 73.60% | 0.0009 | 723.1 | 62.29% | 57.37% |
hydrolysis | ||||||||||
BP | Stable | Negligible | 0.0014 | 488.3 | 75.08% | 71.79% | 0.0010 | 636.7 | 57.38% | 56.67% |
hydrolysis | ||||||||||
BT | Stable | Negligible | 0.0018 | 379.4 | 86.67% | 86.39% | 0.0010 | 662.5 | 69.75% | 72.52% |
hydrolysis | ||||||||||
BTY | Stable | Negligible | 0.0014 | 484.4 | 70.33% | 68.57% | 0.0010 | 677.6 | 55.95% | 55.13% |
hydrolysis |
Average of three readings; follows first-order kinetics.