LABORATORY AND CLINICAL STUDIES ON AMINOCYCLOHEXYLPENICILLIN

Abstract

The results of our studies on aminocyclohexylpenicillin (AC-PC) are summarized as follows:
1. The antimicrobial activity against Staphylococcus aureus, Escherichia coli and Pseudotnonas tested by plate-dilution method was poor.
2. The protein binding was very low by cellophane bag dialysis.
3. Urinary and biliary excretions were studied following intravenous administration in a dog. The half-life was 1.05 hour, Cr and Cb 38.4 and 0.37 ml/min, Kr and Kb 0.55 and 0.005, respectively.
4. The tissue distribution was studied following oral administration in rats. The concentrations in the kidneys and the liver were three or four times higher than those in plasma and lungs. The concentrations in the spleen and muscle were low.
5. The mean peak level of serum was 18.7mcg/ml one hour after 500mg oral administration in adults, and the mean urinary recovery was 50.3% of the dose in 6 hours.
6. The immunological cross-reactivity was found by agar diffusion (OUCHTERLONY'S method) and quantitative precipitin reaction.
7. Twenty two cases of infectious diseases were treated with oral administration of 1-1.5g daily. Sixteen cases were cured. The gastrointestinal disturbance was observed in 4 cases.