The oral bioavailability of pentosan polysulphate sodium in healthy volunteers

Objective: Pentosan polysulphate sodium (PPS), a heparin-like drug, is supp osed to be orally applicable. The objective of the present study was to ass ess the oral bioavailability of PPS. However, since specific assays for PPS do not exist, this was done by using primary and secondary effect paramete rs. Methods: The study was carried out using a three-way randomized crossover d esign with 18 healthy :young male volunteers. The subjects received three t reatments: PPS i.v. (50 mg), PPS orally (1500 mg) and placebo (orally). Blo od sampling was done for activated partial thromboplastin time (APTT), anti -Xa activity, hepatic triglyceride lipase, lipoprotein lipase, tissue plasm inogen activator (t-PA) activity, fibrin plate lysis, total triglyceride, t otal cholesterol, HDL and LDL. Results: Intravenously administered PPS significantly increased APTT, anti- Xa activity, hepatic triglyceride lipase and lipoprotein lipase compared wi th placebo in a magnitude comparable to other i.v. heparin-like compounds. Orally administered PPS did not significantly influence any of the paramete rs when compared with placebo. Point estimates for the oral bioavailability of PPS were in the range of 0% with small confidence intervals (CIs). Conclusion: The oral bioavailability of PPS is negligible in young healthy males.