FUNDAMENTAL AND CLINICAL STUDIES ON TA-058 IN SURGERY

Abstract

The laboratory and clinical studies on TA-058 were carried out. TA-058 has antibacterial activity against Staphylococci, S. faecalis, E. coli, K. pneumoniae, E. cloacae, P. aeruginosa.
As for the results, TA-058 was equal to CBPC, SBPC, TIPC, PIPC against coagulase positive Staphylococci, inferior to PCG, ABPC. Antibacterial activity against coagulase negative Staphylococci was equal to CBPC, SBPC and it was superior by one grade to TIPC, inferior to another PCs.
The activity against S. faecalis was superior to CBPC, SBPC, TIPC by 2-3 grade, but inferior to ABPC, PCG, PIPC.
TA-058 was active as PIPC, ABPC against E. coli and was more active than CBPC and SBPC. Against K. pneumoniae it was equal to ABPC and against E. cloacae it was inferior by 3-4 grade to PIPC. TA-058 had same activity to CBPC against P. aeruginosa, but was inferior to SBPC, TIPC and PIPC.
Bile levels of TA-058, PIPC and CEZ in the rat were measured after intramuscular administration (20mg/kg).
Bile levels of TA-058 as follows were found: 15 min. 92, 30 min. 391, 1 hr. 340, 2 hr. 70μg/ml in average and bile levels of CEZ were as follows were found: 15 min. 93, 30min. 142, 1 hr. 90, 2 hr. 12μg/ml and concentration of PIPC were 2, 650, 3, 000, 1, 630, and 534μg/ml.
Bile levels of TA-058 after intraperitoneal administration were higher than those of intramuscular administration by double times.
TA-058 was administered to 14 cases of infections (respiratory tract infections 3, peritonitis 3, biliary tract infections 2, wound infection 1).
Results obtained were good in 11 cases, failure in 3 cases.
No marked side effects were observed throughout the clinical trials.