Metabolism of [3H]pentosan polysulfate sodium (PPS) in healthy human volunteers

Simon M, McClanahan RH, Shah JF, Repko T, Modi NB · Xenobiotica

Where an oral dose actually goes: 84% left in the faeces as intact PPS and about 6% appeared in the urine, largely as low-molecular-weight and desulfated fragments. Oral PPS is very poorly absorbed, and the fraction that reaches the bladder does so as urinary excretion product.

Population

Two groups of eight healthy female volunteers

Intervention

A single oral dose of tritium-labelled PPS with 300 mg or 450 mg unlabelled PPS

Comparator

None (mass-balance study)

Limitations

Radiolabel mass balance in 16 healthy women after a single dose; total radioactivity does not distinguish parent drug from metabolites everywhere it is measured, and no injected comparison arm was run.