Aqueous kinetics of sisomicin sulphate.

Abstract

Sisomicin sulphate is a new-generation aminoglycoside with a broad spectrum of antimicrobial activity that includes Pseudomonas aeruginosa. It is superior to gentamicin against indole-negative Proteus and some resistant strains of Pseudomonas. The ocular pharmacokinetics of sisomicin have not been explored. We used the agar diffusion technique of microbial assay to determine the aqueous penetration and bioavailability of a subconjunctivally placed standard dose of 20 mg/0.4 ml of sisomicin sulphate in 20 human volunteers undergoing elective cataract surgery. A peak concentration of 16.4 mg/l was found in the aqueous humour 78 minutes after injection, which is 65 times the minimum inhibitory concentration for Pseudomonas. The antibiotic was bioavailable up to 1203 minutes after injection in a concentration of 0.9 mg/l, which easily covers the minimum inhibitory concentration of Staphylococcus aureus and Pseudomonas. The antibiotic disappears from the aqueous humour at the 1434 minute interval (approximately 24 hours). The elimination half-life (t1/2 of sisomicin was determined to be 5.16 hours (K = 0.134/hour) and the aqueous clearance was 2.87 microliters/min.