Cefsulodin kinetics in healthy subjects after intramuscular and intravenous injection

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Abstract
Cefsulodin kinetics were evaluated in normal subjects after 250-, 500- and 1000-mg i.m. injections and 500-, 1000- and 2000-mg 3-min i.v. infusions. Twelve plasma and 4 urine samples were collected in the 1st 12 and 24 h. Plasma samples were analyzed by a new, highly precise high-performance liquid chromatographic procedure and urine samples were analyzed microbiologically, using Pseudomonas aeruginosa as the test organism. Mean calculated peak plasma levels from the 250, 500- and 1000-mg i.m. doses were 5.46, 11.81 and 19.40 .mu.g/ml. After 500-, 1000- and 2000-mg i.v. infusions, peak levels were 32.7, 65.7 and 190.1 .mu.g/ml. Data from the i.m. doses were fitted to a 1-compartment open kinetic model, yielding a mean elimination half-life (t1/2) of 1.9 h. Data from i.v. infusions were fitted to a 2-compartment open model, with a mean beta-phase t1/2 of 1.6 h. Mean 0-24-h urinary recoveries after the 3 i.m. doses were 50.0, 54.5 and 51.2% of total dose; after the 3 i.v. doses they were 60.4%, 52.4% and 54.0%. Cefsulodin kinetics were consistent and orderly.