Pharmacokinetics of bismuth and ranitidine following multiple doses of ranitidine bismuth citrate

1The pharmacokinetics of bismuth and ranitidine derived from oral doses of ranitidine bismuth citrate 800 mg given twice daily for 28 days were examined in this double‐blind, placebo‐controlled, parallel‐group study in 27 healthy subjects.

2Bismuth accumulation in plasma reflected its multicompartmental disposition, achieving the majority of predicted steady state within 14–28 days. Bismuth absorption from ranitidine bismuth citrate is limited (<0.5% of the dose), and bismuth elimination is predominantly renal secretion. Peak plasma concentrations did not exceed 19 ng ml⁻¹, remaining well below those associated with bismuth toxicity. Bismuth was measurable at low concentrations in plasma and urine for up to 5 months after the last dose. Plasma bismuth concentration‐time data and urinary excretion data were best described by separate multicompartmental models, with terminal half‐lives averaging 21 days and 45 days, respectively.

3The pharmacokinetics of ranitidine derived from ranitidine bismuth citrate were similar to those of ranitidine administered alone. Ranitidine did not appreciably accumulate in plasma.

4Ranitidine bismuth citrate was well‐tolerated during 28 days of repeated dosing.

DOI: 10.1046/j.1365-2125.1996.39310.x

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