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Journal of Antimicrobial Chemotherapy (1990) 25, 255-261
© 1990 The British Society for Antimicrobial Chemotherapy

research-article

The apparent absorption kinetics of Ro 15-5458, a schistosomicidal drug

Feleke Esbete and James L. Bennett*

Department of Pharmacology and Toxicology, Michigan State University East Lansing, Michigan 48824, USA

Received 10 July 1989; accepted 27 September 1989

*Corresponding author

The absorption kinetics of Ro 15-5458, a new antischistosomal drug, was studied in rabbits following the administration of a single 50 mg/kg oral dose as an aqueous suspension in 25% glycerol-1% cremophor EL. Ro 15-5458 was absorbed from the gastrointestinal tract rapidly with a lag time of about 6 min and declined without a plateau with a half-life of about 6 h. There was variable extent of drug appearance in plasma after oral administration. Maximum plasma levels ranged from 500 to 1200 ng/ml (1·3–3·1 µM). The plasma concentration-time profile of Ro 15-5458 after a single oral dose appears to follow a one-compartment pharmacokinetic model with zero-order absorption, first-order elimination.


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