The oral bioavailability of pentosan polysulphate sodium in healthy volunteers |
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Authors: | R A Faaij N Srivastava J M T van Griensven R C Schoemaker C Kluft J Burggraaf A F Cohen |
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Institution: | (1) Centre for Human Drug Research, Zernikedreef 10, 2333 CL Leiden, The Netherlands e-mail: rf@chdr.nl Tel.: +31-71-5246421, Fax: +31-71-5246499, NL;(2) Gaubius Laboratory, TNO-PG, Leiden, The Netherlands, NL |
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Abstract: | Objective: Pentosan polysulphate sodium (PPS), a heparin-like drug, is supposed to be orally applicable. The objective of the present
study was to assess the oral bioavailability of PPS. However, since specific assays for PPS do not exist, this was done by
using primary and secondary effect parameters.
Methods: The study was carried out using a three-way randomized crossover design with 18 healthy young male volunteers. The subjects
received three treatments: PPS i.v. (50 mg), PPS orally (1500 mg) and placebo (orally). Blood sampling was done for activated
partial thromboplastin time (APTT), anti-Xa activity, hepatic triglyceride lipase, lipoprotein lipase, tissue plasminogen
activator (t-PA) activity, fibrin plate lysis, total triglyceride, total cholesterol, HDL and LDL.
Results: Intravenously administered PPS significantly increased APTT, anti-Xa activity, hepatic triglyceride lipase and lipoprotein
lipase compared with placebo in a magnitude comparable to other i.v. heparin-like compounds. Orally administered PPS did not
significantly influence any of the parameters 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.
Received: 8 June 1998 / Accepted in revised form: 19 October 1998 |
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Keywords: | Pentosan polysulphate sodium Human volunteer study Oral bioavailability |
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