Preparation of dextran-bound recombinant hirudin and its pharmacokinetic behaviour

Markwardt, F.; Richter, M.; Walsmann, P.; Riesener, G.; Paintz, M.

Biomedica Biochimica Acta 49(10): 1103-1108


ISSN/ISBN: 0232-766X
PMID: 1706917
Document Number: 366926
Recombinant desulphatohirudin was bound via lysine residues to oxidized dextrans. The hirudin-dextran conjugates inhibit thrombin like free hirudin. The Ki-values are in the same range. in rabbits and rats the pharmacokinetic behavior following i.v. administration of these conjugates was examined in comparison to that of hirudin. The hirudin-dextran conjugates were more slowly eliminated than hirudin, the distribution volumes in steady-state were significantly reduced, and, in comparison to hirudin, 5 to 15 times larger areas under the plasma concentration-time-curves were obtained.

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