[A phase I study on intravenous drip infusion of astromicin]

A phase I study on intravenous drip infusion of astromicin (ASTM, KW-1070), an aminoglycoside antibiotic, was performed on 9 healthy adult male volunteers to investigate the safety and pharmacokinetics of this drug. ASTM 200 mg was dissolved in 250 ml of saline and given to each of 6 volunteers by drip infusion in 1 hour. For comparison, 200 mg of ASTM in 1 ml of saline was injected intramuscularly. No subjective and objective reactions were found, and laboratory test value did not show any change possibly caused by ASTM. In a single administration study, Cmax was 10.8 micrograms/ml by intramuscular injection and 12.0 micrograms/ml by intravenous drip infusion. The areas under the time-serum concentration curve were 35.6 micrograms X hr/ml and 34.9 micrograms X hr/ml, respectively; that is, the serum levels of ASTM after one-hour intravenous drip infusion changed almost identically to those after intramuscular injection. In a multiple administration study, the change in serum levels of ASTM after the ninth administration was approximately the same as that after the first one. This means that no accumulation of ASTM in serum occurred. Recovery rates of ASTM in urine up to 8 hours after a single intramuscular injection and a single intravenous drip infusion were 85.4% and 87.5%, respectively. These results also support the conclusion that there is no accumulation of ASTM in the body by repeated administrations.