Abstract

Lipid solubility and a basic pKa are the necessary requirements for the secretion of antibacterial agents into the prostatic fluid in dogs in concentrations exceeding the simultaneous serum concentrations. Protein binding appears to be of less importance. This was demonstrated in constant infusion experiments in dogs. Ampicillin concentrations in prostatic fluid in a patient with urinary diversion were found to be much higher following oral administration of the lipid-soluble hetacillin ester than following administration of ampicillin. This had also previously been found to be true in prostatic fluid and tissue of dogs. The prostatic tissue ampicillin concentrations in humans were not found to be increased following hetacillin ester administration, possibly because the drug was washed out of the tissue during surgery. The importance of the basic pKa is shown in constant infusion experiments in dogs with trimethoprim, erythromycin and rosamicin, all 3 lipid-soluble antibiotics having a high pKa and all being found to concentrate in prostatic fluid and tissue of dogs.

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