The Pharmacokinetics of DR-3355 (I) : Absorption, Distribution and Excretion after a Single Oral Administration to Rats

1991 
The absorption, distribution, excretion and accumulation of DR-3355, a new quinolone antimicrobial agent, were investigated in male rats after repeated oral administrations at a daily dose of 20mg/kg for 21 days. 1. Blood levels of radioactivity at 30min after daily administration were within the range from 1.8 to 3.3μg equiv. to DR-3355/ml for the period of dosing, indicating that no accumulation in blood occurred. At 24hr after daily administration, blood levels of radioactivity were not detected. 2. The tissue levels of radioactivity at 30min after each dosing were almost of the same levels during the period of dosing. Autoradiograms showed that radioactivity did not accumulate in tissues after repeated administration. On the 21st day after repeated administration, the radioactivity in the bone decreased more gradually than that of other tissues. 3. The excretion rates of radioactivity in the urine and feces were constant during the period of administration. Most of administered radioactivity was excreted into urine and feces until 120hr after the last dosing. Cumulative excretions of radioactivity in urine and feces were 32.1 and 63.7%, respectively. These results were almost the same as those after single administration. 4. Blood cell binding and serum protein binding were almost constant for the period of dosing, and the extent of binding to blood cell and serum protein were 50 ?? 55 and 16 ?? 22%, respectively.
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