Abstract
Studies have been made on the absorption, excretion and distribution of aminocyclohexyl penicillin (AC-PC) in the human and animal body, as well as on its anti-bacterial activity. Some clinical trialshave also been made.
(1) The blood level of AC-PC reached its peak (14.4mcg/ml on average) 30minutes after singleoral dose of 500mg in adult humans. The peak level of AC-PC was much higher and came earlierthan that of aminobenzyl penicillin (AB-PC)(5.2mcg/ml on average; 2 hours after administration).
(2) Percent recovery of AC-PC from urine in human adults was larger than that of AB-PC;i. e. 71% of AC-PC and 42% of AB-PC in 6 hours on average.
(3) AC-PC was excreted into bire in a lower concentration than AC-PC or carbenicillin. Percent recoveryof AC-PC from bile was similar to that of PC-G.
(4) Concentration of AC-PC in organs of rats after oral administration was found to be several times higher than that of AB-PC. The order of organs according to their concentration of AC-PC was kidney>liver>lung>spleen>blood (brain, muscle≅0), while that of AB-PC was liver>kidney>lung>blood>spleen (brain, muscle≅0).
(5) Forty-nine strains of Staphylococcus aureus isolated from patients were tested for their sensitivityto AC-PC. The MIC of AC-PC was generally higher than that of AB-PC; while MIC of some strainswere lower than those of PC-G.
All of 24 strains of Eschericia coli isolated from patients were resistant against AC-PC (>100mcg/ml); while the MIC of AB-PC was lower than 25 mcg/ml in 14 strains.
(6) Thirteen patients with various infections (1 acute bronchitis, 2 chronic bronchitis, 3 cholecystitis, 1 cystits, 5 pyelonephritis, and 1 salpingitis) have been treated with AC-PC. The daily dose was 1.5g orally in most cases. The total dosages varied from 6 to 94g (21g on average). Twelve patients out of the thirteen showed fair response to the therapy.
