The pharmacokinetics and pharmacodynamics of recombinant hirudin-2 nasal spray / 药学学报

ABSTRACT

<p><b>AIM</b>To investigate the pharmacokinetics and the anticoagulation action of recombinant hirudin-2 (rHV2) nasal spray after administration of the preparation.</p><p><b>METHODS</b>rHV2 concentration in plasma was determined by chromogenic substrate method and the relative bioavailability was calculated. The anticoagulation action of rHV2 spray after intranasal administration in normal rats and DIC model rabbits after intranasal administration of rHV2 spary were studied.</p><p><b>RESULTS</b>The in vivo course of rHV2 in rats fitted to the one-compartment model after intranasal administration of rHV2 spray and the relative bioavailability was 28.53%. Coagulating times of APTT and TT were significantly prolonged in normal rats, and APTT in DIC model rabbits was significantly shortened and was close to the normal values after administration of rHV2 nasal spray.</p><p><b>CONCLUSION</b>rHV2 spray could be an effective nasal preparation of rHV2.</p>