Recoveries of the radioactive doses after single 15-μmol/kg iv and po doses of [14C] I and po doses of the mono-, di-, and triester prodrugs to rats
| I (Acid) | I (Acid) | II(Monoester) | III (Diester) | IV (Triester) | |
|---|---|---|---|---|---|
| Route | Intravenous | Oral | Oral | Oral | Oral |
| Dose (μmol/kg) | 15 | 15 | 15 | 15 | 15 |
| Recovery (% of radioactive dose) | |||||
| JVC rats1-a | |||||
| Urine | 18.8 ± 1.0 | 2.2 ± 1.0 | |||
| Feces | 72.8 ± 1.2 | 96.5 ± 3.7 | |||
| Total | 91.7 ± 1.7 | 98.8 ± 2.7 | |||
| BDC rats1-b | |||||
| Bile | 41.3 ± 0.8 | 0.6 ± 0.1 | 3.2 ± 1.0 | 43.6 ± 7.2 | 29.0 ± 2.2 |
| Urine | 14.1 ± 0.7 | 0.5 ± 0.1 | 0.2 ± 0.0 | 33.4 ± 6.5 | 12.5 ± 1.0 |
| Feces | NS1-c | NS | NS | NS | 3.0 ± 2.6 |
| Liver | 31.3 ± 0.4 | 0.9 ± 0.3 | 2.6 ± 0.5 | 1.6 ± 0.5 | 2.4 ± 1.6 |
| Gastrointestinal tract | 0.7 ± 0.1 | 99.9 ± 0.7 | 87.4 ± 2.8 | 14.1 ± 0.9 | 48.1 ± 2.6 |
| Carcass | 7.7 ± 0.5 | 0.9 ± 0.8 | 5.2 ± 2.41-d | 1.3 ± 0.7 | 1.0 ± 0.4 |
| Total | 95.1 ± 1.7 | 102.8 ± 0.2 | 97.5 ± 1.0 | 94.0 ± 0.4 | 96.2 ± 0.5 |
| Absorption (%)1-e | 2.9 ± 0.5 | 6.0 ± 1.51-f | 79.9 ± 1.2 | 45.2 ± 4.9 |
Values are mean ± SE (N = 3).
↵1-a Study duration, 96 hr. JVC, jugular vein-cannulated.
↵1-b Study duration, 12 hr.
↵1-c NS, not significant.
↵1-d The carcasses of two rats were contaminated by gastrointestinal tract contents. These values were excluded from the estimation of absorption.
↵1-e Estimated as the sum of radioactivity recovered in all samples minus the radioactivity in feces and the gastrointestinal tract.
↵1-f Estimated as the sum of radioactivity recovered in bile, urine, and liver.