Abstract
Absorption, excretion and tissue distribution of T-1220 were studied in various animals in comparison with carbenicillin and the following results were obtained.
1) When T-1220 (20 mg/kg) was administered intramuscularly or subcutaneously to various animals, the serum levels of T-1220 were higher in order as follows; dog> monkey> rabbit> rat> mouse. In dog, serum level of T-1220 was similar to that of CBPC in cross over test.
2) Total amounts of T-1220 excreted in urine of rat, rabbit and dog administered intramuscularly were 25.2%, 52.8% and 60.2% respectively, while in bile, 54.3%, 27.3% and 10.5% respectively.
3) The distributions of T-1220 in the kidney and liver of mouse and rat were higher than those in other tissues and serum.
4) When T-1220 was intramuscularly administered to healthy adult men at doses of 250, 500 and 1, 000 mg, serum levels attained to maximum at 30 minutes after administration and those levels were 5.0 μg/ml, 12.8 μg/ml and 33.4 μg/ml respectively. Excretion rates of T-1220 in urine were 64.6-66.6% within 6 hours.
5) Excretion rate of T-1220 in goat's milk was 0.015% within 24 hours, which was one sixth of that of CBPC.
6) When T-1220 was administered intrathecally to dogs, cerebrospinal fluid level of T-1220 decreased rapidly.
7) Serum level and excretion in urine and bile of T-1220 in rats pretreated with CCl4 were not remarkably different from those in normal rats.
