A study of the relationship between dose and pharmacokinetics of ceftriaxone

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Abstract
In a crossover study healthy volunteers received either 500 or 1500 mg of ceftriaxone. Serial blood and tissue levels of the drug were measured. The purpose of the study was to ascertain if the pharmacokinetics obeyed a linear dose relationship as it had been suggested that a larger dose may decrease serum protein binding which may affect the pharmacokinetics. The serum half-life, total and renal clearances, and volume of distribution were similar after each dose. Dose-corrected initial serum concentrations, blister fluid concentrations and AUCs were also similar. It was considered that in the range of doses studied here, differences in protein binding did not affect the pharmacokinetics.