Hepatic Disposition of Tilorone Hydrochloride in the Rat

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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.