Hepatic disposition of tilorone hydrochloride in the rat.

Abstract

1. The hepatic disposition of tilorone HCl, an antiviral and antitumour agent, was studied in male Wistar rats after intraduodenal administration. 2. A concentrative transfer into the liver occurred, the liver/portal blood concentration ratio being 120 or higher. The relationship between dose and hepatic concentration was linear. 3. Biliary excretion of tilorone was low and dose-related; whole blood concentration was also dose-related. 4. Neither hepatic concentration nor biliary excretion exhibited saturation over the dosage studied (6--174 mg/kg). The hepatic 'depot' of tilorone lacked the characteristics of a true 'first-pass' effect.