Pharmacokinetic study of rifaximin after oral administration in healthy volunteers

Eighteen healthy male volunteers, with a mean age of 24 yrs (range 18-40), underwent an open pharmacokinetics study, aimed at detecting rifaximin concentration in blood and urine after a single oral administration of 400 mg of the antibiotic. Administration took place after a 9 hours' fast and was followed by a breakfast after 2 hours and a lunch after 5 hours. Blood samples were collected before rifaximin administration and 1, 2, 4, 8, 12, 24 and 48 hours after dosing. Urine samples were collected immediately before dosing (reference sample) and then at the end of the following intervals of time: 0-6 h, 6-12 h, 12-24 h, 24-48 h. During the whole study period, the local and general tolerance to rifaximin administration was checked. Rifaximin concentration was assessed by reversed phase high performance liquid chromatography with electrochemical detection. In almost every plasma sample, rifaximin concentration was undetectable (lower than the detection limit of the analytical method, i.e. 2 ng/ml). In urine, very small amounts of the unchanged molecule (< 0.01% of the administered dose) were found in the period 0-48 hours. These results confirm the negligible absorption by the intestinal tract of a single oral dose of rifaximin (400 mg). Local and general tolerance of the administered drug was very good.