Sulfobenzylpenicillin (SB-PC), a newly synthesized penicillin derivative, was examined on its antibacterial activity, absorption, excretion and distribution in the body. Some clinical trials were also carried out.
1) Tests on the sensitivity of clinical isolates revealed that the sensitivity of Staphylococcus aureus strains and Pseudomonas aeruginosa strains to SB-PC mostly resembled to that of carbenicillin (CB-PC) among various antibiotics. Clinically isolated E. coli, Klebsiella and Proteus strains were also examined on their sensitivity to SB-PC as well as to other antibiotics.
2) Blood levels of SB-PC in human adults after intramuscular injection were generally higher than those of C13-PC, and their durability, too, was somewhat superior to that of the latter.
3) SB-PC was mainly excreted into the urine at a rate similar to that for CB-PC.
4) Studies on the biliary excretion of SB-PC in rabbits revealed that the antibiotic is excreted into bile at a very high concentration similarl to CB-PC.
5) SB-PC was distributed into kidneys and liver at the highest concentration among organs. The behaviour of SB-PC in the rat's body closely resembled that of CB-PC, while tissue concentrations of SB-PC were somewhat higher than those of CB-PC as well as those of aminobenzylpenicillin.
6) Nine patients with various infections were treated with SB-PC (1 to 4 g daily, intramuscularly). Favourable results were obtained in 4 cases : pyelonephritis, 1 ; pneumonia, 1 ; cholecystitis, 1 ; acute leukemia, 1 (alleviation of fever). None of the patients showed any untoward reactions.
