[Pharmacokinetics of rectal absorption of amodiaquine in rabbits]

Experimental investigations were made in rabbits to examine the rectal absorption of antimalarial amodiaquine [AQ]. To calculate the pharmacokinetic parameters AQ was administered orally (20 mg/kg) and rectally (20 mg/kg) to the animals and the blood concentrations of the drug were controlled during a time interval of 120 hours with help of spectrofluorometric method. The pharmacokinetic analysis was performed by use of two-compartment open model system. Time-concentration curves were fitted to the data in experiments by computer program (MEDUSA) and the kinetic parameters were given in the Tables 1. and 2. It was established that rectally administered AQ resorbed not only from solution but from suppository, too. The bioavailability of the rectal preparations relating to the oral dosage form was 63.35% and 68.70%, respectively. The most appropriate drug delivery system for rectal application had been selected previously.