Pharmacokinetics of hepatobiliary imaging agents in rats: concise communication

Abstract

The distribution and elimination kinetics of Tc-99m pyridoxlidene glutamate (Tc-99m PG), of Tc-99m N-(2,6-dimethyl-phenylcarbamoylmethyl) iminodiacetic acid (Tc-99m HIDA), and of I-131 rose bengal in blood were quantitated after i.v. injection in rats. This was performed by use of a unique indwelling catheter that externalizes the systemic circulation, permitting continuous monitoring of blood radioactivity. The blood activity-time curves of Tc-99m PG and Tc-99m HIDA are described by the sum of three exponential functions. Only two exponentials are required in the case of I-131 rose bengal. The rank order for the rates of loss from blood was Tc-99m HIDA less than Tc-99m PG less than I-131 rose bengal. Bile was collected after administration of Tc-99m HIDA and Tc-99m PG. The total excretion of radioactivity over a 70-min period amounted to 95.7% and 42.8% of the dose of Tc-99m HIDA and Tc-99m PG, respectively. A linear compartmental kinetic model was developed to account for the disappearance from blood and the biliary excretion of these radiopharmaceuticals in rats.