[The pharmacokinetics and pharmacodynamics of recombinant hirudin-2 nasal spray].
OBJECTIVE
To investigate the pharmacokinetics and the anticoagulation action of recombinant hirudin-2 (rHV2) nasal spray after administration of the preparation.


METHODS
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.


RESULTS
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.


CONCLUSIONS
rHV2 spray could be an effective nasal preparation of rHV2.
Zhang
Yu-jie
YJ
Department of Chinese Pharmacy, Beijing University of Chinese Medicine. zhyj227@126.com
Zhang
Qiang
Q
Hou
Jun-ling
JL
Wang
Xiao-liang
XL
Chen
Ming-xia
MX
D000281:Administration, Intranasal; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D004211:Disseminated Intravascular Coagulation / Q000503:physiopathology; D006629:Hirudins / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology*; D008297:Male; D010314:Partial Thromboplastin Time; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D011994:Recombinant Proteins / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D013918:Thrombin Time
D006629:Hirudins; D011994:Recombinant Proteins; C072299:hirudin HV2