Cefsulodin kinetics in healthy subjects after intramuscular and intravenous injection

• Published in: Clinical pharmacology and therapeutics Vol. 31; no. 1; p. 95
• Main Authors: Granneman, G R, Sennello, L T, Sonders, R C, Wynne, B, Thomas, E W
• Format: Journal Article
• Language: English
• Published: United States 01.01.1982
• Subjects: Adult; Cefsulodin; Cephalosporins - administration & dosage; Cephalosporins - metabolism; Humans; Infusions, Parenteral; Injections, Intramuscular; Kinetics; Male
• ISSN: 0009-9236
• DOI: 10.1038/clpt.1982.15

We evaluated cefsulodin kinetics in normal subjects after 250-, 500-, and 1,000-mg, intramuscular injections and 500-, 1,000-, and 2,000-mg 30-min intravenous infusions. Twelve plasma and four urine samples were collected in the first 12 and 24 hr. Plasma samples were analyzed by a new, highly precise high-performance liquid chromatographic procedure developed in our laboratory and urine samples were analyzed microbiologically, using Pseudomonas aeruginosa as the test organism. Mean calculated peak plasma levels from the 250-, 500-, and 1,000-mg intramuscular doses were 5.46, 11.81, and 19.40 microgram/ml. After 500-, 1,000-, and 2,000-mg intravenous infusions peak levels were 32.7, 65.7, and 190.1 microgram/ml. Data from the intramuscular doses were fitted to a one-compartment open kinetic model, yielding a mean elimination half-life (t1/2) of 1.9 hr. Data from the intravenous infusions were fitted to a two-compartment open model, with a mean beta-phase t1/2 of 1.6 hr. Mean 0- to 24-hr urinary recoveries after the three intramuscular doses were 50.0%, 54.5%, and 51.2% of total dose; after the three intravenous doses they were 60.4%, 52.4%, and 54.0%. Cefsulodin kinetics were shown to be consistent and orderly.