The oral bioavailability of pentosan polysulphate sodium in healthy volunteers

Faaij RA, Srivastava N, van Griensven JM, Schoemaker RC, Kluft C, Burggraaf J, Cohen AF · European Journal of Clinical Pharmacology

The pharmacokinetic result that separates the oral and injected drug. Intravenous PPS raised aPTT, anti-Xa activity, hepatic triglyceride lipase and lipoprotein lipase like any injected heparinoid; 1500 mg by mouth — thirty times the intravenous dose — moved none of them. Point estimates for oral bioavailability came out around 0% with narrow confidence intervals.

Population

18 healthy young male volunteers, three-way randomized crossover

Intervention

PPS 50 mg intravenously and PPS 1500 mg orally

Comparator

Oral placebo

Limitations

Bioavailability inferred from pharmacodynamic surrogates because no assay for PPS in plasma existed; 18 healthy young men, single doses, so it says nothing about accumulation on chronic dosing; the effects measured are systemic ones, and a drug excreted intact into urine can still act on the bladder surface.