The apparent absorption kinetics of Ro 15-5458, a schistosomicidal drug.
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 microM). 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.
Eshete
F
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Department of Pharmacology and Toxicology, Michigan State University, East Lansing 48824.
Bennett
J L
JL
D000166:Acridines / Q000493:pharmacokinetics*; D000818:Animals; D005260:Female; D006207:Half-Life; D007408:Intestinal Absorption; D011817:Rabbits; D012556:Schistosomicides / Q000097:blood / Q000493:pharmacokinetics*
D000166:Acridines; D012556:Schistosomicides; C062730:Ro 15-5458