Lincomycin serum and saliva concentrations after intramuscular injection of high doses

Serum and saliva levels of lincomycin were determined in 15 normal adult male volunteers after a single intramuscular injection of 600, 1000, or 1500 mg lincomycin in a three-way crossover study. The area under the serum concentration-time curve did not increase in proportion to the increase in dose. The increase in concentration of lincomycin in saliva was greater than expected for the increase in dose. There were not significant differences in elimination half-life between doses. These results suggest that the apparent clearance of lincomycin increases with increasing dose possibly because of a decrease in serum protein binding of lincomycin at high serum concentrations.