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.