Abstract
The metabolic fate NC-1300-O-3, a new proton pump inhibitor with potent cytoprotective effect on the gastric mucosa, was investigated after daily oral administration of 14C(Iz)-NC-1300-O-3 (30 mg/kg) for 28 days to male rats. The transfer of radioactivity into fetus and milk was also investigated after a single oral administration (30 mg/kg) to pregnant and lactating rats. 1. The levels of radioactivity in the blood at 24 hr after daily administration rose as number of doses increased, and the concentrations after 28th dose were 9 times higher than those after the first dose. While the levels of radioactivity in the plasma did not change during dosing period. Disappearance of radioactivity from blood following 28th dose was similar to that after a single dose. 2. The distribution of radioactivity in the tissues was measured at 24 hr after the 1st, 7th, 14th, 21st and 28th dose, the radioactivity accumulated throughout the dosing period in most tissues. In the blood, epididymis, spleen and heart after 28th dose, the radioactivity levels rose greatly, and were 11.3-8.0 times higher than those of the first dose, while the radioactivity levels in the other tissues were less than 7 times. 3. The excretion of radioactivity in urine and feces reached near steady state after 2nd dose. Within 168 hr after the 28th dose, urinary and fecal excretion amounted to 60.6 and 39.2% of cumulative dose, respectively. 4. The radioactivity levels in the fetus on day 13 of gestation were less than 40% of the maternal plasma levels at every time point, indicating a low placental transfer. However, on day 18 of gestation, the radioactivity levels in the fetus were nearly equal to those in maternal plasma. 5. The concentrations of radioactivity in the milk were 3-9 times higher than those in plasma at every time point studied.
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